Paul Workman | Academic Influence

Paul Workman 's AcademicInfluence.com Rankings

Paul Workman

Biology

#3120

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#4814

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Molecular Biology

#286

World Rank

#291

Historical Rank

Genetics

#321

World Rank

#377

Historical Rank

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Biology

Paul Workman 's Degrees

Bachelors Biology University of Oxford

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Why Is Paul Workman Influential?

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According to Wikipedia, Paul Workman is a British scientist noted for his work on the discovery and development of pharmaceutical agents in the field of oncology. He is President and CEO of The Institute of Cancer Research In London.

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Paul Workman 's Published Works

Number of citations in a given year to any of this author's works

Total number of citations to an author for the works they published in a given year. This highlights publication of the most important work(s) by the author

Published Works

Guidelines for the welfare and use of animals in cancer research (2010) (1225)
Patient-derived organoids model treatment response of metastatic gastrointestinal cancers (2018) (981)
Hsp90 Molecular Chaperone Inhibitors: Are We There Yet? (2012) (837)
Combinatorial drug therapy for cancer in the post-genomic era (2012) (822)
Imaging biomarker roadmap for cancer studies (2016) (718)
The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer . (2008) (709)
The promise and peril of chemical probes. (2015) (623)
Targeting the PI3K-AKT-mTOR pathway: progress, pitfalls, and promises. (2008) (537)
HSP90 as a new therapeutic target for cancer therapy: the story unfolds (2002) (527)
The assessment of antiangiogenic and antivascular therapies in early-stage clinical trials using magnetic resonance imaging: issues and recommendations (2005) (520)
Activation of the ATPase activity of hsp90 by the stress-regulated cochaperone aha1. (2002) (507)
Phase I pharmacokinetic and pharmacodynamic study of 17-allylamino, 17-demethoxygeldanamycin in patients with advanced malignancies. (2005) (494)
Discovery of small molecule cancer drugs: Successes, challenges and opportunities (2012) (455)
NVP-AUY922: a novel heat shock protein 90 inhibitor active against xenograft tumor growth, angiogenesis, and metastasis. (2008) (454)
Drugging the Cancer Chaperone HSP90 (2007) (433)
The Hsp90 molecular chaperone: an open and shut case for treatment. (2008) (421)
Challenges to curing primary brain tumours (2019) (414)
4,5-diarylisoxazole Hsp90 chaperone inhibitors: potential therapeutic agents for the treatment of cancer. (2007) (393)
Pharmacologic characterization of a potent inhibitor of class I phosphatidylinositide 3-kinases. (2007) (364)
DT-Diaphorase expression and tumor cell sensitivity to 17-allylamino, 17-demethoxygeldanamycin, an inhibitor of heat shock protein 90. (1999) (357)
New approaches to molecular cancer therapeutics (2006) (351)
Inhibitors of the heat shock response: Biology and pharmacology (2007) (323)
Dual targeting of HSC70 and HSP72 inhibits HSP90 function and induces tumor-specific apoptosis. (2008) (321)
Inhibitors of the HSP90 molecular chaperone: current status. (2006) (318)
Targeting of multiple signalling pathways by heat shock protein 90 molecular chaperone inhibitors. (2006) (295)
Direct measurement of pO2 distribution and bioreductive enzymes in human malignant brain tumors. (1994) (286)
DT-diaphorase and cancer chemotherapy. (1992) (279)
Inhibition of signal transduction by the Hsp90 inhibitor 17-allylamino-17-demethoxygeldanamycin results in cytostasis and apoptosis. (2001) (277)
Biological properties of potent inhibitors of class I phosphatidylinositide 3-kinases: from PI-103 through PI-540, PI-620 to the oral agent GDC-0941 (2009) (270)
Drugging the PI3 kinome: from chemical tools to drugs in the clinic. (2010) (266)
Histone H3.3. mutations drive pediatric glioblastoma through upregulation of MYCN. (2013) (265)
UKCCCR guidelines for the welfare of animals in experimental neoplasia. (1988) (258)
A selective PIKfyve inhibitor blocks PtdIns(3,5)P2 production and disrupts endomembrane transport and retroviral budding (2008) (258)
Envisioning the future of early anticancer drug development (2010) (254)
A phase I trial of the selective oral cyclin-dependent kinase inhibitor seliciclib (CYC202; R-Roscovitine), administered twice daily for 7 days every 21 days (2006) (250)
Combinatorial attack on multistep oncogenesis by inhibiting the Hsp90 molecular chaperone. (2004) (249)
Heat shock protein inhibition is associated with activation of the unfolded protein response pathway in myeloma plasma cells. (2007) (248)
Probing the Probes: Fitness Factors For Small Molecule Tools (2010) (246)
Inhibitors of cyclin‐dependent kinases as cancer therapeutics (2017) (237)
Activated B-RAF is an Hsp90 client protein that is targeted by the anticancer drug 17-allylamino-17-demethoxygeldanamycin. (2005) (235)
Reductase enzyme expression across the National Cancer Institute Tumor cell line panel: correlation with sensitivity to mitomycin C and EO9. (1996) (234)
Personalized Cancer Medicine: Molecular Diagnostics, Predictive biomarkers, and Drug Resistance (2012) (233)
First-in-Human Phase I Study of Pictilisib (GDC-0941), a Potent Pan–Class I Phosphatidylinositol-3-Kinase (PI3K) Inhibitor, in Patients with Advanced Solid Tumors (2014) (225)
Partition coefficient as a guide to the development of radiosensitizers which are less toxic than misonidazole. (1980) (223)
Structure-activity relationships in purine-based inhibitor binding to HSP90 isoforms. (2004) (217)
Isothiazolones as inhibitors of PCAF and p300 histone acetyltransferase activity (2005) (212)
Gene expression profiling of human colon cancer cells following inhibition of signal transduction by 17-allylamino-17-demethoxygeldanamycin, an inhibitor of the hsp90 molecular chaperone (2000) (209)
Altered states: selectively drugging the Hsp90 cancer chaperone. (2004) (208)
Novel, potent small-molecule inhibitors of the molecular chaperone Hsp90 discovered through structure-based design. (2005) (206)
The identification, synthesis, protein crystal structure and in vitro biochemical evaluation of a new 3,4-diarylpyrazole class of Hsp90 inhibitors. (2005) (200)
Anticancer agents targeting signaling molecules and cancer cell environment: challenges for drug development? (1999) (199)
Gene expression microarray analysis in cancer biology, pharmacology, and drug development: progress and potential. (2001) (199)
A Phase I Study of the Heat Shock Protein 90 Inhibitor Alvespimycin (17-DMAG) Given Intravenously to Patients with Advanced Solid Tumors (2011) (192)
Minimally invasive pharmacokinetic and pharmacodynamic technologies in hypothesis-testing clinical trials of innovative therapies. (2006) (190)
Hsp90-Dependent Activation of Protein Kinases Is Regulated by Chaperone-Targeted Dephosphorylation of Cdc37 (2008) (184)
High-throughput screening assay for inhibitors of heat-shock protein 90 ATPase activity. (2004) (183)
Targeting HSP70: The second potentially druggable heat shock protein and molecular chaperone? (2010) (182)
The Cyclin-dependent Kinase Inhibitor CYC202 (R-Roscovitine) Inhibits Retinoblastoma Protein Phosphorylation, Causes Loss of Cyclin D1, and Activates the Mitogen-activated Protein Kinase Pathway (2004) (179)
Drugging PI3K in cancer: refining targets and therapeutic strategies (2015) (176)
Identification of a potent and selective pharmacophore for Cdc25 dual specificity phosphatase inhibitors. (2002) (176)
Sequencing of prostate cancers identifies new cancer genes, routes of progression and drug targets (2018) (169)
Synthesis and biological evaluation of 4-morpholino-2-phenylquinazolines and related derivatives as novel PI3 kinase p110α inhibitors (2006) (167)
To pop or not to pop: p53 as a critical modulator of tumour responsiveness to therapy in vivo? (1995) (164)
Pharmacokinetic-Pharmacodynamic Relationships for the Heat Shock Protein 90 Molecular Chaperone Inhibitor 17-Allylamino, 17-Demethoxygeldanamycin in Human Ovarian Cancer Xenograft Models (2005) (163)
Combining hit identification strategies: fragment-based and in silico approaches to orally active 2-aminothieno[2,3-d]pyrimidine inhibitors of the Hsp90 molecular chaperone. (2009) (156)
MGMT-independent temozolomide resistance in pediatric glioblastoma cells associated with a PI3-kinase-mediated HOX/stem cell gene signature. (2010) (155)
Biomarker-Driven Early Clinical Trials in Oncology: A Paradigm Shift in Drug Development (2009) (154)
Examination by laser scanning confocal fluorescence imaging microscopy of the subcellular localisation of anthracyclines in parent and multidrug resistant cell lines. (1993) (149)
Pharmacodynamic biomarkers for molecular cancer therapeutics. (2007) (144)
A public-private partnership to unlock the untargeted kinome. (2013) (142)
Gene and protein expression profiling of human ovarian cancer cells treated with the heat shock protein 90 inhibitor 17-allylamino-17-demethoxygeldanamycin. (2007) (141)
Maximizing the Therapeutic Potential of HSP90 Inhibitors (2015) (141)
Overview: translating Hsp90 biology into Hsp90 drugs. (2003) (138)
Noninvasive magnetic resonance spectroscopic pharmacodynamic markers of the choline kinase inhibitor MN58b in human carcinoma models. (2006) (136)
Identification of novel small molecule inhibitors of hypoxia-inducible factor-1 that differentially block hypoxia-inducible factor-1 activity and hypoxia-inducible factor-1alpha induction in response to hypoxic stress and growth factors. (2005) (136)
ATP-competitive inhibitors block protein kinase recruitment to the Hsp90-Cdc37 system. (2013) (135)
Choose and Use Your Chemical Probe Wisely to Explore Cancer Biology (2017) (135)
Discovering novel chemotherapeutic drugs for the third millennium. (1999) (132)
Assessment of antiangiogenic and antivascular therapeutics using MRI: recommendations for appropriate methodology for clinical trials. (2003) (132)
Enzyme-directed bioreductive drug development revisited: a commentary on recent progress and future prospects with emphasis on quinone anticancer agents and quinone metabolizing enzymes, particularly DT-diaphorase. (1994) (130)
In vitro and In vivo Pharmacokinetic-Pharmacodynamic Relationships for the Trisubstituted Aminopurine Cyclin-Dependent Kinase Inhibitors Olomoucine, Bohemine and CYC202 (2005) (129)
Silencing of HSP90 cochaperone AHA1 expression decreases client protein activation and increases cellular sensitivity to the HSP90 inhibitor 17-allylamino-17-demethoxygeldanamycin. (2008) (129)
A Phase II trial of 17-allylamino, 17-demethoxygeldanamycin (17-AAG, tanespimycin) in patients with metastatic melanoma (2012) (128)
Selective FLT3 inhibition of FLT3-ITD+ acute myeloid leukaemia resulting in secondary D835Y mutation: a model for emerging clinical resistance patterns (2012) (126)
Discovery and development of pyrazole-scaffold Hsp90 inhibitors. (2006) (125)
Silencing the cochaperone CDC37 destabilises kinase clients and sensitises cancer cells to HSP90 inhibitors (2008) (124)
How much gets there and what does it do?: The need for better pharmacokinetic and pharmacodynamic endpoints in contemporary drug discovery and development. (2003) (122)
Inhibition of the heat shock protein 90 molecular chaperone in vitro and in vivo by novel, synthetic, potent resorcinylic pyrazole/isoxazole amide analogues (2007) (121)
Objective assessment of cancer genes for drug discovery (2012) (118)
Acquired resistance to 17-allylamino-17-demethoxygeldanamycin (17-AAG, tanespimycin) in glioblastoma cells. (2009) (116)
A selective chemical probe for exploring the role of CDK8 and CDK19 in human disease (2015) (115)
Molecular and Phenotypic Characterisation of Paediatric Glioma Cell Lines as Models for Preclinical Drug Development (2009) (115)
Synthesis and biological evaluation of pyrido[3′,2′:4,5]furo[3,2- d ]pyrimidine derivatives as novel PI3 kinase p110α inhibitors (2007) (115)
Effect of p53 status on sensitivity to platinum complexes in a human ovarian cancer cell line. (2000) (114)
Hsp 90 Molecular Chaperone Inhibitors : Are We There Yet ? (2011) (113)
Preclinical antitumor activity and pharmacodynamic studies with the farnesyl protein transferase inhibitor R115777 in human breast cancer. (2001) (112)
Hsp90 inhibitors in the clinic. (2006) (111)
Benzoquinone ansamycin heat shock protein 90 inhibitors modulate multiple functions required for tumor angiogenesis (2006) (110)
Phase I Pharmacokinetic and Pharmacodynamic Study of LAQ824, a Hydroxamate Histone Deacetylase Inhibitor with a Heat Shock Protein-90 Inhibitory Profile, in Patients with Advanced Solid Tumors (2008) (110)
Auditing the pharmacological accounts for Hsp90 molecular chaperone inhibitors: unfolding the relationship between pharmacokinetics and pharmacodynamics. (2003) (107)
Synthesis and biological evaluation of imidazo[1,2-a]pyridine derivatives as novel PI3 kinase p110α inhibitors (2007) (107)
Potentiation of paclitaxel activity by the HSP90 inhibitor 17-allylamino-17-demethoxygeldanamycin in human ovarian carcinoma cell lines with high levels of activated AKT (2006) (107)
The role of NAD(P)H: quinone reductase (EC 1.6.99.2, DT-diaphorase) in the reductive bioactivation of the novel indoloquinone antitumor agent EO9. (1991) (106)
Drug discovery in advanced prostate cancer: translating biology into therapy (2016) (106)
Death by chaperone: HSP90, HSP70 or both? (2009) (106)
Progress in the Preclinical Discovery and Clinical Development of Class I and Dual Class I/IV Phosphoinositide 3-Kinase (PI3K) Inhibitors (2011) (106)
Magnetic resonance spectroscopic pharmacodynamic markers of the heat shock protein 90 inhibitor 17-allylamino,17-demethoxygeldanamycin (17AAG) in human colon cancer models. (2003) (106)
In vitro biological characterization of a novel, synthetic diaryl pyrazole resorcinol class of heat shock protein 90 inhibitors. (2007) (103)
A useful approach to identify novel small-molecule inhibitors of Wnt-dependent transcription. (2010) (100)
HSP90 inhibition: two-pronged exploitation of cancer dependencies. (2012) (99)
Small-molecule targeting of brachyury transcription factor addiction in chordoma (2019) (98)
Synthesis and biological evaluation of sulfonylhydrazone-substituted imidazo[1,2 -a]pyridines as novel PI3 kinase p110α inhibitors (2007) (97)
AHR- and DNA-damage-mediated gene expression responses induced by benzo(a)pyrene in human cell lines. (2007) (96)
Role for amplification and expression of glypican-5 in rhabdomyosarcoma. (2007) (95)
Phospholipid antitumor agents (1995) (95)
Inhibiting the phosphoinositide 3-kinase pathway for cancer treatment. (2004) (94)
The clinical applications of heat shock protein inhibitors in cancer - present and future. (2003) (93)
Exploiting the cancer genome: strategies for the discovery and clinical development of targeted molecular therapeutics. (2012) (92)
Decreased NADPH:cytochrome P-450 reductase activity and impaired drug activation in a mammalian cell line resistant to mitomycin C under aerobic but not hypoxic conditions. (1990) (91)
The Association of PI3 Kinase Signaling and Chemoresistance in Advanced Ovarian Cancer (2012) (91)
Niacin induces PPARgamma expression and transcriptional activation in macrophages via HM74 and HM74a-mediated induction of prostaglandin synthesis pathways. (2006) (91)
Identification of magnetic resonance detectable metabolic changes associated with inhibition of phosphoinositide 3-kinase signaling in human breast cancer cells (2006) (91)
Clinical anticancer drug development: targeting the cyclin-dependent kinases (2004) (90)
Preclinical pharmacokinetics and metabolism of a novel prototype DNA-PK inhibitor NU7026 (2005) (90)
In vivo evaluation of [18F]fluoroetanidazole as a new marker for imaging tumour hypoxia with positron emission tomography (2004) (90)
MIR21 Drives Resistance to Heat Shock Protein 90 Inhibition in Cholangiocarcinoma (2017) (88)
EGFRvIII Deletion Mutations in Pediatric High-Grade Glioma and Response to Targeted Therapy in Pediatric Glioma Cell Lines (2009) (87)
Nitroimidazole bioreductive metabolism. Quantitation and characterisation of mouse tissue benznidazole nitroreductases in vivo and in vitro. (1987) (86)
Gene expression microarray technologies in the development of new therapeutic agents. (2004) (86)
Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19 (2016) (86)
A chemical inhibitor of PPM1D that selectively kills cells overexpressing PPM1D (2008) (86)
Histone modification enzymes: novel targets for cancer drugs. (2004) (85)
Magnetic resonance spectroscopy monitoring of mitogen-activated protein kinase signaling inhibition. (2005) (84)
UKCCCR guidelines for the welfare of animals in experimental neoplasia (1988) (84)
Overexpression of EZH2 in multiple myeloma is associated with poor prognosis and dysregulation of cell cycle control (2017) (83)
Targeting heat shock protein 72 enhances Hsp90 inhibitor-induced apoptosis in myeloma (2010) (81)
Mechanistic Evaluation of the Novel HSP90 Inhibitor NVP-AUY922 in Adult and Pediatric Glioblastoma (2010) (81)
Bioreductive drugs into the next millennium. (1998) (80)
Estimation of the hypoxic cell-sensitiser misonidazole and its O-demethylated metabolite in biological materials by reversed-phase high-performance liquid chromatography. (1978) (80)
Identification of 4-(4-aminopiperidin-1-yl)-7H-pyrrolo[2,3-d]pyrimidines as selective inhibitors of protein kinase B through fragment elaboration. (2008) (80)
Translating basic cancer research into new cancer therapeutics. (2002) (79)
Demonstration of tumor-selective retention of fluorinated nitroimidazole probes by 19F magnetic resonance spectroscopy in vivo. (1989) (78)
Measurement of Tumor Oxygenation: In Vivo Comparison of a Luminescence Fiber-optic Sensor and a Polarographic Electrode in the P22 Tumor (2001) (78)
A structural comparison of inhibitor binding to PKB, PKA and PKA-PKB chimera. (2007) (76)
Molecular pharmacology of phosphatidylinositol 3-kinase inhibition in human glioma (2009) (76)
Can molecular biomarker-based patient selection in Phase I trials accelerate anticancer drug development? (2010) (76)
Unusually marked hypoxic sensitization to indoloquinone E09 and mitomycin C in a human colon‐tumour cell line that lacks DT‐diaphorase activity (2007) (74)
A Phase I study of the angiogenesis inhibitor SU5416 (semaxanib) in solid tumours, incorporating dynamic contrast MR pharmacodynamic end points (2005) (74)
Measuring changes in human tumour vasculature in response to therapy using functional imaging techniques (2001) (74)
Inhibitors of the HSP90 molecular chaperone: attacking the master regulator in cancer. (2006) (74)
4-Amino derivatives of the Hsp90 inhibitor CCT018159. (2006) (73)
The role of cytochrome P450 and cytochrome P450 reductase in the reductive bioactivation of the novel benzotriazine di-N-oxide hypoxic cytotoxin 3-amino-1,2,4-benzotriazine-1,4-dioxide (SR 4233, WIN 59075) by mouse liver. (1992) (73)
AT13148 Is a Novel, Oral Multi-AGC Kinase Inhibitor with Potent Pharmacodynamic and Antitumor Activity (2012) (71)
3-(5-Chloro-2,4-dihydroxyphenyl)-pyrazole-4-carboxamides as inhibitors of the Hsp90 molecular chaperone. (2005) (71)
Molecular enzymology of the reductive bioactivation of hypoxic cell cytotoxins. (1989) (71)
The Aurora Kinase Inhibitor CCT137690 Downregulates MYCN and Sensitizes MYCN-Amplified Neuroblastoma In Vivo (2011) (71)
In vitro selectivity, in vivo biodistribution and tumour uptake of annexin V radiolabelled with a positron emitting radioisotope (2003) (71)
BRAF and NRAS mutations in melanoma: potential relationships to clinical response to HSP90 inhibitors (2008) (70)
Establishment of an isogenic human colon tumor model for NQO1 gene expression: application to investigate the role of DT-diaphorase in bioreductive drug activation in vitro and in vivo. (2000) (70)
Imidazo[4,5-b]pyridine derivatives as inhibitors of Aurora kinases: lead optimization studies toward the identification of an orally bioavailable preclinical development candidate. (2010) (70)
Second-Generation HSP90 Inhibitor Onalespib Blocks mRNA Splicing of Androgen Receptor Variant 7 in Prostate Cancer Cells. (2016) (70)
Hit generation and exploration: imidazo[4,5-b]pyridine derivatives as inhibitors of Aurora kinases. (2007) (69)
How Much Longer Will We Put Up With $100,000 Cancer Drugs? (2017) (69)
Drugging the PI3 kinome (2006) (69)
Normalisation of anti-cancer drug dosage using body weight and surface area: is it worthwhile? (1993) (69)
A fluorescence polarization assay for inhibitors of Hsp90. (2006) (69)
Enzyme-Directed Bioreductive Drug Development (1990) (69)
Establishment and characterisation of cell lines from patients with lung cancer (predominantly small cell carcinoma). (1985) (68)
Keynote address: Bioreductive mechanisms☆ (1992) (67)
Wnt signalling modulates transcribed-ultraconserved regions in hepatobiliary cancers (2016) (67)
The Cyclin-Dependent Kinase Inhibitor Seliciclib (R-roscovitine; CYC202) Decreases the Expression of Mitotic Control Genes and Prevents Entry into Mitosis (2007) (66)
Mechanism-Based Screen for G1/S Checkpoint Activators Identifies a Selective Activator of EIF2AK3/PERK Signalling (2012) (66)
Discovery of Potent, Orally Bioavailable, Small-Molecule Inhibitors of WNT Signaling from a Cell-Based Pathway Screen (2015) (66)
The role of functional and molecular imaging in cancer drug discovery and development. (2003) (66)
Targeting CDC37: An alternative, kinase-directed strategy for disruption of oncogenic chaperoning (2009) (66)
In vivo biological activity of the histone deacetylase inhibitor LAQ824 is detectable with 3'-deoxy-3'-[18F]fluorothymidine positron emission tomography. (2006) (65)
Assessing the mechanism and therapeutic potential of modulators of the human Mediator complex-associated protein kinases (2016) (65)
DT-diaphorase: questionable role in mitomycin C resistance, but a target for novel bioreductive drugs? (1989) (65)
Demonstrating In-Cell Target Engagement Using a Pirin Protein Degradation Probe (CCT367766) (2017) (65)
Enzymology of the reductive bioactivation of SR 4233. A novel benzotriazine di-N-oxide hypoxic cell cytotoxin. (1990) (65)
canSAR: update to the cancer translational research and drug discovery knowledgebase (2018) (64)
Structure-based design of molecular cancer therapeutics. (2009) (64)
The experimental development of bioreductive drugs and their role in cancer therapy (1993) (63)
The phosphoinositide 3-kinase inhibitor PI-103 downregulates choline kinase alpha leading to phosphocholine and total choline decrease detected by magnetic resonance spectroscopy. (2010) (63)
Inhibition of Hsp90 with synthetic macrolactones: synthesis and structural and biological evaluation of ring and conformational analogs of radicicol. (2006) (63)
Retention of activity by selected anthracyclines in a multidrug resistant human large cell lung carcinoma line without P-glycoprotein hyperexpression. (1991) (63)
The application of cassette dosing for pharmacokinetic screening in small-molecule cancer drug discovery (2007) (63)
Challenges of PK/PD measurements in modern drug development. (2002) (63)
The opportunities and challenges of personalized genome-based molecular therapies for cancer: targets, technologies, and molecular chaperones (2003) (61)
Improved cellular accumulation is characteristic of anthracyclines which retain high activity in multidrug resistant cell lines, alone or in combination with verapamil or cyclosporin A. (1989) (61)
Catalytic properties of NAD(P)H:quinone acceptor oxidoreductase: study involving mouse, rat, human, and mouse-rat chimeric enzymes. (1995) (60)
Reduction of 3-amino-1,2,4-benzotriazine-1,4-di-N-oxide (tirapazamine, WIN 59075, SR 4233) to a DNA-damaging species: a direct role for NADPH:cytochrome P450 oxidoreductase. (1994) (60)
Critical parameters in targeted drug development: the pharmacological audit trail. (2016) (59)
Objective, Quantitative, Data-Driven Assessment of Chemical Probes (2017) (59)
The kinase polypharmacology landscape of clinical PARP inhibitors (2020) (59)
A HIF-Regulated VHL-PTP1B-Src Signaling Axis Identifies a Therapeutic Target in Renal Cell Carcinoma (2011) (59)
Expression of Kinase-defective Mutants of c-Src in Human Metastatic Colon Cancer Cells Decreases Bcl-xL and Increases Oxaliplatin- and Fas-induced Apoptosis* (2004) (59)
DT-diaphorase activity correlates with sensitivity to the indoloquinone EO9 in mouse and human colon carcinomas. (1992) (59)
Genome-based cancer therapeutics: targets, kinase drug resistance and future strategies for precision oncology. (2013) (59)
ErbB2 overexpression in an ovarian cancer cell line confers sensitivity to the HSP90 inhibitor geldanamycin. (2002) (58)
Mechanism of action of the Aurora kinase inhibitor CCT129202 and in vivo quantification of biological activity (2007) (58)
Polar fluorescein derivatives as improved substrate probes for flow cytoenzymological assay of cellular esterases. (1988) (58)
An evaluation of the ability of pifithrin-α and -β to inhibit p53 function in two wild-type p53 human tumor cell lines (2005) (57)
Preclinical Pharmacology, Antitumor Activity, and Development of Pharmacodynamic Markers for the Novel, Potent AKT Inhibitor CCT128930 (2010) (57)
Metabolism and pharmacokinetics of the cyclin-dependent kinase inhibitor R-roscovitine in the mouse. (2005) (57)
9-Alkyl, morpholinyl anthracyclines in the circumvention of multidrug resistance. (1990) (56)
Genes and proteins governing the cellular sensitivity to HSP90 inhibitors: a mechanistic perspective. (2003) (56)
The HSP90 Inhibitor NVP-AUY922 Radiosensitizes by Abrogation of Homologous Recombination Resulting in Mitotic Entry with Unresolved DNA Damage (2012) (55)
Optimization of Imidazo[4,5-b]pyridine-Based Kinase Inhibitors: Identification of a Dual FLT3/Aurora Kinase Inhibitor as an Orally Bioavailable Preclinical Development Candidate for the Treatment of Acute Myeloid Leukemia (2012) (55)
DT-diaphorase protects cells from the hypoxic cytotoxicity of indoloquinone EO9. (1994) (55)
Polypharmacology in Precision Oncology: Current Applications and Future  Prospects (2016) (55)
Use of radiolabelled choline as a pharmacodynamic marker for the signal transduction inhibitor geldanamycin (2002) (54)
Structure-based drug design: aiming for a perfect fit (2017) (54)
AT7867 Is a Potent and Oral Inhibitor of AKT and p70 S6 Kinase That Induces Pharmacodynamic Changes and Inhibits Human Tumor Xenograft Growth (2010) (53)
A phase I study of SR-4554 via intravenous administration for noninvasive investigation of tumor hypoxia by magnetic resonance spectroscopy in patients with malignancy. (2003) (53)
Preclinical pharmacokinetics of benznidazole. (1984) (53)
A clinical phase I toxicity study of Ro 03-8799: plasma, urine, tumour and normal brain pharmacokinetics. (1986) (53)
Relative importance of DT-diaphorase and hypoxia in the bioactivation of EO9 by human lung tumor cell lines. (1994) (52)
Synthesis and biological evaluation of 4-morpholino-2-phenylquinazolines and related derivatives as novel PI3 kinase p110alpha inhibitors. (2006) (52)
Aurora Isoform Selectivity: Design and Synthesis of Imidazo[4,5-b]pyridine Derivatives as Highly Selective Inhibitors of Aurora-A Kinase in Cells (2013) (52)
Preclinical evaluation of the fluorinated 2-nitroimidazole N-(2-hydroxy-3,3,3-trifluoropropyl)-2-(2-nitro-1-imidazolyl) acetamide (SR-4554) as a probe for the measurement of tumor hypoxia. (1997) (52)
Synthesis of isothiazol-3-one derivatives as inhibitors of histone acetyltransferases (HATs). (2009) (51)
E3 ubiquitin ligase Cullin-5 modulates multiple molecular and cellular responses to heat shock protein 90 inhibition in human cancer cells (2014) (51)
High-throughput screening for identification of small molecule inhibitors of histone acetyltransferases using scintillating microplates (FlashPlate). (2001) (51)
The pharmacokinetics and tumor and neural tissue penetrating properties of SR-2508 and SR-2555 in the dog--hydrophilic radiosensitizers potentially less toxic than misonidazole. (1980) (50)
Structural basis of the radicicol resistance displayed by a fungal hsp90. (2009) (50)
New Molecular Targets for Cancer Chemotherapy (1994) (50)
Scoring a bull's-eye against cancer genome targets. (2001) (50)
High dose BCNU chemotherapy with autologous bone marrow transplantation and full dose radiotherapy for grade IV astrocytoma. (1988) (49)
Modification of CCNU pharmacokinetics by misonidazole--a major mechanism of chemosensitization in mice. (1983) (49)
Noninvasive imaging of cell proliferation following mitogenic extracellular kinase inhibition by PD0325901 (2008) (49)
Application of meso scale technology for the measurement of phosphoproteins in human tumor xenografts. (2007) (49)
Noninvasive magnetic resonance spectroscopic pharmacodynamic markers of a novel histone deacetylase inhibitor, LAQ824, in human colon carcinoma cells and xenografts. (2008) (49)
Drugging cancer genomes (2013) (48)
Small molecule inhibitors of dual specificity protein phosphatases (2000) (48)
The impact of pharmacokinetically guided dose escalation strategies in phase I clinical trials: critical evaluation and recommendations for future studies. (1992) (47)
Phase I safety, pharmacokinetic, and pharmacogenomic trial of ES-285, a novel marine cytotoxic agent, administered to adult patients with advanced solid tumors (2009) (47)
A phase I study of the hypoxic cell radiosensitizer Ro-03-8799. (1984) (47)
Enzymology of the reduction of the potent benzotriazine-di-N-oxide hypoxic cell cytotoxin SR 4233 (WIN 59075) by NAD(P)H: (quinone acceptor) oxidoreductase (EC 1.6.99.2) purified from Walker 256 rat tumour cells. (1992) (46)
Restricting direct interaction of CDC37 with HSP90 does not compromise chaperoning of client proteins (2013) (45)
New drug targets for genomic cancer therapy: successes, limitations, opportunities and future challenges. (2001) (45)
Chaperoning cell death: a critical dual role for Hsp90 in small-cell lung cancer. (2007) (45)
Assays for the identification and evaluation of histone acetyltransferase inhibitors. (2002) (44)
Genomics and the second golden era of cancer drug development. (2005) (44)
HSF1 Is Essential for Myeloma Cell Survival and A Promising Therapeutic Target (2018) (44)
Discovery of a Chemical Probe Bisamide (CCT251236): An Orally Bioavailable Efficacious Pirin Ligand from a Heat Shock Transcription Factor 1 (HSF1) Phenotypic Screen (2016) (44)
Effects of pretreatment with phenobarbitone and phenytoin on the pharmacokinetics and toxicity of phenytoin on the pharmacokinetics and toxicity of misonidazole in mice. (1979) (44)
Phase I and pharmacokinetic study of tirapazamine (SR 4233) administered every three weeks. (1997) (44)
The role of human and rodent DT-diaphorase in the reductive metabolism of hypoxic cell cytotoxins. (1992) (43)
Pharmacokinetics of hypoxic cell radiosensitizers: a review. (1980) (43)
Disruption of WT1 gene expression and exon 5 splicing following cytotoxic drug treatment: antisense down-regulation of exon 5 alters target gene expression and inhibits cell survival. (2004) (43)
The identification of novel PLC-gamma inhibitors using virtual high throughput screening. (2009) (41)
Inhibitors of HSP90 and other chaperones for the treatment of cancer (2004) (41)
Establishment and characterization of acquired resistance to the farnesyl protein transferase inhibitor R115777 in a human colon cancer cell line. (2002) (41)
Multiparametric analysis of cell membrane permeability by two colour flow cytometry with complementary fluorescent probes. (1990) (40)
The enzymology of doxorubicin quinone reduction in tumour tissue. (1992) (40)
Molecular pharmacology of cancer therapy in human colorectal cancer by gene expression profiling. (2003) (40)
Cassette dosing pharmacokinetics of a library of 2,6,9-trisubstituted purine cyclin-dependent kinase 2 inhibitors prepared by parallel synthesis. (2004) (40)
Pharmacokinetic considerations in testing hypoxic cell radiosensitizers in mouse tumours. (1979) (40)
Hypoxic cell radiosensitizers in the treatment of high grade gliomas: a new direction using combined Ro 03-8799 (pimonidazole) and SR 2508 (etanidazole). (1988) (39)
Gene Expression Profiling after Radiation-Induced DNA Damage Is Strongly Predictive of BRCA1 Mutation Carrier Status (2004) (39)
Inhibition of mTOR-kinase destabilizes MYCN and is a potential therapy for MYCN-dependent tumors (2016) (39)
Distinctive Behaviors of Druggable Proteins in Cellular Networks (2015) (39)
Preclinical development and current status of the fluorinated 2-nitroimidazole hypoxia probe N-(2-hydroxy-3,3,3-trifluoropropyl)-2-(2-nitro-1-imidazolyl) acetamide (SR 4554, CRC 94/17): a non-invasive diagnostic probe for the measurement of tumor hypoxia by magnetic resonance spectroscopy and imagin (1998) (39)
The BRAF Inhibitor Vemurafenib Activates Mitochondrial Metabolism and Inhibits Hyperpolarized Pyruvate–Lactate Exchange in BRAF-Mutant Human Melanoma Cells (2016) (39)
MEK1/2 inhibition decreases lactate in BRAF-driven human cancer cells. (2013) (39)
Combining TRAIL with PI3 Kinase or HSP90 inhibitors enhances apoptosis in colorectal cancer cells via suppression of survival signaling (2013) (39)
Structure-activity relationships for DT-diaphorase reduction of hypoxic cell directed agents: indoloquinones and diaziridinyl benzoquinones. (1992) (38)
Inhibition of Kirsten-ras expression in human colorectal cancer using rationally selected Kirsten-ras antisense oligonucleotides. (2001) (38)
An in vitro and in vivo study of the combination of the heat shock protein inhibitor 17-allylamino-17-demethoxygeldanamycin and carboplatin in human ovarian cancer models (2008) (38)
Pharmacokinetics of the hypoxic cell cytotoxic agent tirapazamine and its major bioreductive metabolites in mice and humans: retrospective analysis of a pharmacokinetically guided dose-escalation strategy in a phase I trial (1997) (38)
Design and development of signal transduction inhibitors for cancer treatment: Experience and challenges with kinase targets (2006) (38)
An evaluation of the ability of pifithrin-alpha and -beta to inhibit p53 function in two wild-type p53 human tumor cell lines. (2005) (37)
Involvement of NADPH: cytochrome P450 reductase in the activation of indoloquinone EO9 to free radical and DNA damaging species. (2001) (37)
2,8-Disubstituted-1,6-Naphthyridines and 4,6-Disubstituted-Isoquinolines with Potent, Selective Affinity for CDK8/19 (2016) (37)
Drugging the cancer kinome: progress and challenges in developing personalized molecular cancer therapeutics. (2005) (37)
Pharmacokinetics, distribution, and metabolism of the novel bioreductive alkylating indoloquinone EO9 in rodents. (1992) (37)
Determinants of response to epidermal growth factor receptor tyrosine kinase inhibition in squamous cell carcinoma of the head and neck (2009) (37)
A phase I study of the nitroimidazole hypoxia marker SR4554 using 19F magnetic resonance spectroscopy (2009) (37)
Phenytoin shortens the half-life of the hypoxic cell radiosensitizer misonidazole in man: implications for possible reduced toxicity. (1980) (36)
Clinical studies with misonidazole. (1978) (36)
Structure-based design of isoquinoline-5-sulfonamide inhibitors of protein kinase B. (2006) (36)
The in vitro effects and cross-resistance patterns of some novel anthracyclines. (1986) (35)
Validation of the fluorinated 2-nitroimidazole SR-4554 as a noninvasive hypoxia marker detected by magnetic resonance spectroscopy. (2002) (35)
Chemical biology approaches to target validation in cancer. (2014) (34)
Clinical pharmacokinetics of oral CCNU (Lomustine) (2004) (34)
Fadraciclib (CYC065), a novel CDK inhibitor, targets key pro-survival and oncogenic pathways in cancer (2020) (34)
From Darkness to Light With Biomarkers in Early Clinical Trials of Cancer Drugs (2009) (34)
Detection of the ATPase Activity of the Molecular Chaperones Hsp90 and Hsp72 Using the Transcreener™ ADP Assay Kit (2010) (33)
Phosphatidylinositide-3-kinase inhibitors: addressing questions of isoform selectivity and pharmacodynamic/predictive biomarkers in early clinical trials. (2012) (33)
The effects of alpha and gamma interferons on human lung cancer cells grown in vitro or as xenografts in nude mice. (1985) (33)
Structure-pharmacokinetic relationships for misonidazole analogues in mice (2004) (32)
Preclinical pharmacokinetics and metabolism of a novel diaryl pyrazole resorcinol series of heat shock protein 90 inhibitors (2006) (32)
Enhancement by electron-affinic agents of the therapeutic effects of cytotoxic agents against the KHT tumor: structure-activity relationships. (1982) (32)
Mode of cell death induced by the HSP90 inhibitor 17-AAG (tanespimycin) is dependent on the expression of pro-apoptotic BAX (2013) (32)
Use of pharmacokinetic/pharmacodynamic biomarkers to support rational cancer drug development. (2007) (32)
Choose and Use Your Chemical Probe Wisely to Explore Cancer Biology (2017) (32)
The expanding proteome of the molecular chaperone HSP90 (2012) (32)
A phase I study of the combination of two hypoxic cell radiosensitizers, Ro 03-8799 and SR-2508: toxicity and pharmacokinetics. (1986) (32)
Drugging the heat shock factor 1 pathway: Exploitation of the critical cancer cell dependence on the guardian of the proteome (2009) (32)
Finding the needle in the haystack: why high-throughput screening is good for your health (2002) (31)
Hsp70 inhibition induces myeloma cell death via the intracellular accumulation of immunoglobulin and the generation of proteotoxic stress☆ (2013) (31)
Initial characterization of the major mouse cytochrome P450 enzymes involved in the reductive metabolism of the hypoxic cytotoxin 3-amino-1,2,4-benzotriazine-1,4-di-N-oxide (tirapazamine, SR 4233, WIN 59075). (1993) (31)
The effect of systemic hyperthermia on melphalan pharmacokinetics in mice. (1985) (31)
A flow cytofluorimetric method for measuring enzyme reaction kinetics in intact cells (1977) (31)
Design, synthesis and biological evaluation of 6-pyridylmethylaminopurines as CDK inhibitors. (2011) (31)
The cell membrane and cell signals: new targets for novel anticancer drugs. (1990) (30)
Pharmacokinetics and bioreductive metabolism of the novel benzotriazine di-N-oxide hypoxic cell cytotoxin tirapazamine (WIN 59075; SR 4233; NSC 130181) in mice. (1993) (30)
The novel fluorinated 2-nitroimidazole hypoxia probe SR-4554: reductive metabolism and semiquantitative localisation in human ovarian cancer multicellular spheroids as measured by electron energy loss spectroscopic analysis. (1995) (30)
Characterization of a human colorectal carcinoma cell line with acquired resistance to flavopiridol. (2001) (30)
Exploiting Protein Conformational Change to Optimize Adenosine-Derived Inhibitors of HSP70 (2016) (30)
Structure/activity relationships for the enhancement by electron-affinic drugs of the anti-tumour effect of CCNU. (1982) (30)
Bioreductive metabolism of the novel fluorinated 2-nitroimidazole hypoxia probe N-(2-hydroxy-3,3,3-trifluoropropyl)-2-(2-nitroimidazolyl) acetamide (SR-4554). (1997) (30)
Reduction of the indoloquinone anticancer drug EO9 by purified DT-diaphorase: a detailed kinetic study and analysis of metabolites. (1998) (30)
A phase I study of the combination of benznidazole and CCNU in man. (1984) (30)
Involvement of DT-diaphorase (EC 1.6.99.2) in the DNA cross-linking and sequence selectivity of the bioreductive anti-tumour agent EO9. (1997) (30)
Geldanamycin-induced cytotoxicity in human colon-cancer cell lines: evidence against the involvement of c-Src or DT-diaphorase (1998) (30)
Targeted therapeutics for cancer treatment: major progress towards personalised molecular medicine. (2008) (30)
The relationship between tumour oxygenation determined by oxygen electrode measurements and magnetic resonance spectroscopy of the fluorinated 2-nitroimidazole SR-4554. (1998) (29)
The efflux of anthracyclines in multidrug-resistant cell lines. (1993) (29)
Orally bioavailable CDK9/2 inhibitor shows mechanism-based therapeutic potential in MYCN-driven neuroblastoma (2020) (29)
Targeting the Hsp90 chaperone: synthesis of novel resorcylic acid macrolactone inhibitors of Hsp90. (2010) (29)
canSAR: update to the cancer translational research and drug discovery knowledgebase (2020) (28)
CHK1 Inhibition Is Synthetically Lethal with Loss of B-Family DNA Polymerase Function in Human Lung and Colorectal Cancer Cells (2020) (28)
Identification of Small-Molecule Inhibitors of Protein Kinase B (PKB/AKT) in an AlphaScreen™ High-Throughput Screen (2006) (28)
Biomarkers In Early Clinical Trials: the Committed and the Skeptics (2008) (28)
Modulation of Biliary Cancer Chemo‐Resistance Through MicroRNA‐Mediated Rewiring of the Expansion of CD133+ Cells (2019) (28)
Identification by High-Throughput Screening of Viridin Analogs as Biochemical and Cell-Based Inhibitors of the Cell Cycle–Regulated Nek2 Kinase (2010) (27)
The contemporary drug development process: advances and challenges in preclinical and clinical development. (2003) (27)
High-throughput screening for the identification of small-molecule inhibitors of retinoblastoma protein phosphorylation in cells. (2003) (27)
Modulation of melanoma cell phospholipid metabolism in response to heat shock protein 90 inhibition (2010) (27)
The role of intracellular free calcium mobilization in the mechanism of action of antitumour ether lipids SRI 62-834 and ET18-OMe. (1993) (26)
Naturally Occurring Mutations in the MPS1 Gene Predispose Cells to Kinase Inhibitor Drug Resistance. (2015) (26)
Monitoring salivary misonidazole in man: a possible alternative to plasma monitoring. (1978) (26)
Pharmacokinetic and tumour-penetration properties of the hypoxic cell radiosensitizer desmethylmisonidazole (Ro 05-9963) in dogs (1980) (26)
Drug metabolism and chemosensitization. Nitroimidazoles as inhibitors of drug metabolism. (1983) (26)
Tyrosine kinase inhibitors. (1992) (26)
Pharmacogenomics in cancer drug discovery and development: inhibitors of the Hsp90 molecular chaperone. (2002) (26)
Histone deacetylase inhibition increases levels of choline kinase α and phosphocholine facilitating noninvasive imaging in human cancers. (2012) (25)
Multiparametric flow cytometry of the modulation of tumor cell membrane permeability by developmental antitumor ether lipid SRI 62-834 in EMT6 mouse mammary tumor and HL-60 human promyelocytic leukemia cells. (1991) (25)
Molecular profiling and combinatorial activity of CCT068127: a potent CDK2 and CDK9 inhibitor (2018) (25)
Cytostasis and Apoptosis 17-Allylamino-17-demethoxygeldanamycin Results in Inhibition of Signal Transduction by the Hsp 90 Inhibitor Updated Version (2001) (24)
Antitumor ether lipids: endocytosis as a determinant of cellular sensitivity. (1991) (24)
Exploiting tumor metabolism for non-invasive imaging of the therapeutic activity of molecularly targeted anticancer agents (2011) (24)
Putting the heat on cancer (2007) (24)
Resisting targeted therapy: fifty ways to leave your EGFR. (2011) (24)
Improved methodology for intracellular enzyme reaction and inhibition kinetics by flow cytometry. (1987) (24)
Lactate and Choline Metabolites Detected In Vitro by Nuclear Magnetic Resonance Spectroscopy Are Potential Metabolic Biomarkers for PI3K Inhibition in Pediatric Glioblastoma (2014) (24)
The Cyclin-dependent Kinase Inhibitor CYC 202 ( R-Roscovitine ) Inhibits Retinoblastoma Protein Phosphorylation , Causes Loss of Cyclin D 1 , and Activates the Mitogen-activated Protein Kinase Pathway (2004) (24)
Synthesis and biological evaluation of sulfonylhydrazone-substituted imidazo[1,2-a]pyridines as novel PI3 kinase p110alpha inhibitors. (2007) (24)
The Pharmacology of Brain Tumour Chemotherapy (1986) (24)
Acute tumour response to the MEK1/2 inhibitor selumetinib (AZD6244, ARRY-142886) evaluated by non-invasive diffusion-weighted MRI (2013) (23)
An investigation of the possibility of chemosensitization by clinically achievable concentrations of misonidazole. (1983) (23)
Assays for HSP90 and inhibitors. (2003) (23)
Dissecting mechanisms of resistance to targeted drug combination therapy in human colorectal cancer (2019) (23)
Misonidazole and CCNU: further evidence for a pharmacokinetic mechanism of chemosensitization and therapeutic gain. (1984) (23)
Strategies for treating cancers caused by multiple genome abnormalities: from concepts to cures? (2003) (22)
Assessment of anti-angiogenic and anti-vascular therapeutics using Magnetic Resonance Imaging: recommendations for appropriate methodology for clinical trials. (2003) (22)
Evaluation of the cassette dosing approach for assessing the pharmacokinetics of geldanamycin analogues in mice (2004) (22)
The pharmacokinetics of misonidazole in the dog. (1979) (22)
Pharmacokinetics and cancer chemotherapy. (1994) (21)
A multiple dose study of the combined radiosensitizers Ro 03-8799 (pimonidazole) and SR 2508 (etanidazole). (1989) (21)
Fused imidazoles as potential chemical scaffolds for inhibition of heat shock protein 70 and induction of apoptosis. Synthesis and biological evaluation of phenanthro[9,10-d]imidazoles and imidazo[4,5-f][1,10]phenanthrolines. (2016) (21)
Novel dynamic flow cytoenzymological determination of intracellular esterase inhibition by BCNU and related isocyanates. (1987) (20)
In vivo pharmacology and anti-tumour evaluation of the tyrphostin tyrosine kinase inhibitor RG13022. (1996) (20)
A fragment-based approach applied to a highly flexible target: Insights and challenges towards the inhibition of HSP70 isoforms (2016) (20)
Targeting the Hsp90 molecular chaperone with novel macrolactams. Synthesis, structural, binding, and cellular studies. (2011) (20)
Nitroimidazoles as modifiers of nitrosourea pharmacokinetics. (1984) (20)
Pharmacokinetic basis for the comparative antitumour activity and toxicity of chlorambucil, phenylacetic acid mustard and β,β-difluorochlorambucil (CB 7103) in mice (2004) (20)
Opportunities and challenges in ovarian cancer research, a perspective from the 11th Ovarian cancer action/HHMT Forum, Lake Como, March 2007. (2008) (20)
Characterisation of molecular events following cisplatin treatment of two curable ovarian cancer models: contrasting role for p53 induction and apoptosis in vivo (2004) (19)
Growth arrest vs direct cytotoxicity and the importance of molecular structure for the in vitro anti-tumour activity of ether lipids. (1995) (19)
Non‐invasive MRS in new anticancer drug development (1992) (19)
Characterisation of molecular events following cisplatin treatment of two curable ovarian cancer models: contrasting role for p53 induction and apoptosis in vivo (2004) (19)
Additivity of radiosensitization by the combination of SR 2508 (etanidazole) and Ro 03-8799 (pimonidazole) in a murine tumor system. (1988) (19)
The combination of cytotoxic and molecularly targeted therapies - can it be done? (2004) (19)
Identification of Inhibitors of the Kinase Activity of Oncogenic V600EBRAF in an Enzyme Cascade High-Throughput Screen (2006) (19)
The discovery of potent ribosomal S6 kinase inhibitors by high-throughput screening and structure-guided drug design (2013) (19)
Synthesis of resorcinylic macrocycles related to radicicol via ring-closing metathesis (2006) (19)
The multi-dose clinical tolerance and pharmacokinetics of the combined radiosensitizers, Ro 03-8799 (pimonidazole) and SR 2508 (etanidazole). (1988) (19)
A phase I study of the combined hypoxic cell radiosensitizers, Ro 03-8799 and SR 2508: a preliminary report of single-dose toxicity, pharmacokinetics and tumour concentrations. (1986) (19)
Effects of localised tumour hyperthermia on pimonidazole (Ro 03-8799) pharmacokinetics in mice. (1989) (19)
Signalling involving MET and FAK supports cell division independent of the activity of the cell cycle-regulating CDK4/6 kinases (2019) (19)
CHAPTER 14 – MECHANISM-BASED HIGH-THROUGHPUT SCREENING FOR NOVEL ANTICANCER DRUG DISCOVERY (2002) (19)
Chemosensitization by lipophilic nitroimidazoles. (1983) (18)
Co-Crystalization and In Vitro Biological Characterization of 5-Aryl-4-(5-Substituted-2-4-Dihydroxyphenyl)-1,2,3-Thiadiazole Hsp90 Inhibitors (2012) (18)
Drug latentiation in cancer chemotherapy. (1978) (18)
Anticancer drug screening and discovery in the 1990s: a European perspective. (1992) (18)
EML4-ALK fusions: propelling cancer but creating exploitable chaperone dependence. (2014) (18)
Solid-phase immunoassays in mechanism-based drug discovery: their application in the development of inhibitors of the molecular chaperone heat-shock protein 90. (2005) (17)
Different esterase activities of exponential and plateau phases of EMT6 cells monitored by flow cytofluorimetry. (1978) (17)
Towards intelligent anticancer drug screening in the post-genome era? (1997) (17)
Synthesis and biological evaluation of pyrido[3',2':4,5]furo[3,2-d]pyrimidine derivatives as novel PI3 kinase p110alpha inhibitors. (2007) (17)
Bioreductive mechanisms. (1992) (17)
Inhibition of Hsp90 with resorcylic acid macrolactones: synthesis and binding studies. (2010) (17)
Synthetic ansamycins prepared by a ring-expanding Claisen rearrangement. Synthesis and biological evaluation of ring and conformational analogues of the Hsp90 molecular chaperone inhibitor geldanamycin. (2007) (17)
Effect of misonidazole or metronidazole pretreatment on the response of the RIF-1 mouse sarcoma to melphalan, cyclophosphamide, chlorambucil and CCNU. (1982) (17)
Benznidazole: nitroreduction and inhibition of cytochrome P-450 in chemosensitization of tumour response to cytotoxic drugs. (1986) (17)
Overview: changing times: developing cancer drugs in genomeland. (2001) (17)
Public resources for chemical probes: the journey so far and the road ahead. (2019) (17)
Preparation and evaluation of trisubstituted pyrimidines as phosphatidylinositol 3-kinase inhibitors. 3-Hydroxyphenol analogues and bioisosteric replacements. (2011) (16)
Cancer genome targets: RAF-ing up tumor cells to overcome oncogene addiction (2002) (16)
The effect of radiosensitizer pretreatment on the response of the RIF-1 mouse sarcoma to cytotoxic drugs. (1982) (16)
Drug interactions with misonidazole: effects of dexamethasone and its derivatives on the pharmacokinetics and toxicity of misonidazole in mice. (1980) (16)
Dose-dependence and related studies on the pharmacokinetics of misonidazole and desmethylmisonidazole in mice (2004) (16)
The discovery of GDC-0941: A potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer (2008) (16)
Transforming cancer drug discovery with Big Data and AI (2019) (16)
Genomic profiling of cancer: what next? (2005) (16)
The pharmacokinetics, bioavailability and biodistribution in mice of a rationally designed 2-nitroimidazole hypoxia probe SR-4554. (1996) (16)
Effects of local hyperthermia on the pharmacokinetics of misonidazole in the anaesthetized mouse. (1980) (16)
Identification of anthracyclines and related agents that retain preferential activity over Adriamycin in multidrug-resistant cell lines, and further resistance modification by verapamil and cyclosporin A (2008) (15)
Oncogenic RAC1 and NRAS drive resistance to endoplasmic reticulum stress through MEK/ERK signalling (2018) (15)
High-Throughput Screening Assay for Identification of Small Molecule Inhibitors of Aurora2/STK15 Kinase (2004) (15)
The use of parallel EEL spectral imaging and elemental mapping in the rapid assessment of anti‐cancer drug localization (1992) (15)
Personalized medicine: patient-predictive panel power. (2012) (15)
Correlation of overall survival with gene expression profiles in a prospective study of resectable esophageal cancer. (2011) (15)
Unveiling the secrets of the ancestral PI3 kinase Vps34. (2010) (15)
A stressful life (or death): Combinatorial proteotoxic approaches to cancer-selective therapeutic vulnerability (2011) (14)
Misonidazole and benznidazole inhibit hydroxylation of CCNU by mouse liver microsomal cytochrome P-450 in vitro. (1987) (14)
Effect of p 53 Status on Sensitivity to Platinum Complexes in a Human Ovarian Cancer Cell Line (2000) (14)
The Association of PI 3 Kinase Signaling and Chemoresistance in Advanced Ovarian Cancer (2012) (14)
Identification of Novel Keratinocyte Differentiation Modulating Compounds by High-Throughput Screening (2006) (14)
An assay for plasma membrane phosphatase activity in populations of individual cells. (1979) (14)
The Cell Membrane and Cell Signals as Targets in Cancer Chemotherapy AACR, EORTC, and BACR Special Conference in Cancer Research (1990) (14)
Pharmacodynamic and Clinical Results from a Phase I/II Study of the HSP90 Inhibitor Onalespib in Combination with Abiraterone Acetate in Prostate Cancer (2019) (14)
The penetration of misonidazole into spontaneous canine tumours. (1979) (14)
Bioreductive prodrugs for cancer therapy. (2004) (14)
Signalling targets for the development of cancer drugs. (1994) (14)
Plasma Metabolomic Changes following PI3K Inhibition as Pharmacodynamic Biomarkers: Preclinical Discovery to Phase I Trial Evaluation (2016) (14)
Innovative cancer drug targets: genomics, transcriptomics and clinomics (2001) (14)
Shock about heat shock in cancer (2012) (13)
Target 2035 – update on the quest for a probe for every protein (2021) (13)
Pharmacology of the mixed-function radio- and chemosensitizers CB 1954 and RSU 1069. (1984) (13)
Reversed-phase high-performance liquid chromatographic method for the simultaneous determination of the 2-nitroimidazole benznidazole and its amine metabolite in biological materials (1986) (13)
Cyclopropamitosenes: novel bioreductive anticancer agents--mechanism of action and enzymic reduction. (1994) (13)
Synthesis and biological evaluation of imidazo[1,2-a]pyridine derivatives as novel PI3 kinase p110alpha inhibitors. (2007) (13)
The antisignaling agent SC-alpha alpha delta 9, 4-(benzyl-(2-[(2,5-diphenyloxazole-4-carbonyl)amino]ethyl)carbamoyl)- 2-decanoylaminobutyric acid, is a structurally unique phospholipid analogue with phospholipase C inhibitory activity. (2002) (13)
Chemical biology: Many faces of a cancer-supporting protein (2011) (13)
The effects of whole body hyperthermia on the pharmacokinetics and toxicity of the basic 2-nitroimidazole radiosensitizer Ro 03-8799 in mice. (1987) (13)
Effects of HSP90 inhibitor 17-allylamino-17-demethoxygeldanamycin (17-AAG) on NEU/HER2 overexpressing mammary tumours in MMTV-NEU-NT mice monitored by Magnetic Resonance Spectroscopy (2012) (13)
A phase II and pharmacokinetic study with oral piritrexim for metastatic breast cancer. (1993) (13)
Pharmacokinetics and early clinical studies of selected new drugs. (1993) (12)
Small-Molecule Inhibitors of the Protein Methyltransferase SET7/9 Identified in a High-Throughput Screen (2012) (12)
The impact of genomic and proteomic technologies on the development of new cancer drugs. (2002) (12)
A duplexed phenotypic screen for the simultaneous detection of inhibitors of the molecular chaperone heat shock protein 90 and modulators of cellular acetylation (2007) (12)
PI(3) kinases: revealing the delta lady. (2010) (12)
Platelet-activating factor (PAF) antagonist WEB 2086 does not modulate the cytotoxicity of PAF or antitumour alkyl lysophospholipids ET-18-O-methyl and SRI 62-834 in HL-60 promyelocytic leukaemia cells. (1991) (12)
Further examination of 9-alkyl- and sugar-modified anthracyclines in the circumvention of multidrug resistance. (1992) (12)
Targeting the cancer chaperone HSP90 (2007) (12)
Enzyme activated anti-tumour agents- II. The role of alkaline phosphatase in the release of p-hydroxyaniline mustard from its phosphate conjugate in cells in culture. (1976) (12)
The Phosphoinositide 3-Kinase Inhibitor PI-103 Downregulates Choline Kinase α Leading to Phosphocholine and Total Choline Decrease Detected by Magnetic Resonance Spectroscopy (2010) (12)
High-performance liquid chromatographic assay for the benzotriazine di-N-oxide (SR 4233) and its reduced metabolites in biological materials. (1988) (12)
The impact of genomic and proteomic technologies on the development of new cancer drugs (2002) (11)
Molecular biology: Choose your protein partners (2012) (11)
Reflections and Outlook on Targeting HSP90, HSP70 and HSF1 in Cancer: A Personal Perspective. (2020) (11)
A New Chemical Probe Challenges the Broad Cancer Essentiality of CK2. (2021) (11)
Histone modification enzymes: novel targets for cancer drugs (2004) (11)
A phase I trial of the HSP90 inhibitor, alvespimycin (17-DMAG) administered weekly, intravenously, to patients with advanced, solid tumours. (2016) (11)
In vitro antitumour activity of the novel imidazoisoquinoline SDZ 62-434. (1993) (11)
Cancer: Drug-tolerant insurgents (2010) (11)
Lipophilicity and the Pharmacokinetics of Nitroimidazoles (1982) (11)
Privileged Structures and Polypharmacology within and between Protein Families (2018) (10)
Blocking the survival of the nastiest by HSP90 inhibition (2016) (10)
Targeted brachyury degradation disrupts a highly specific autoregulatory program controlling chordoma cell identity (2021) (10)
From patent to patient: analysing access to innovative cancer drugs. (2020) (10)
Identification of anthracyclines and related agents that retain preferential activity over Adriamycin in multidrug-resistant cell lines, and further resistance modification by verapamil and cyclosporin A (2004) (10)
Yet more roles for tea in disease prevention (2001) (10)
Pharmacokinetics and cancer: successes, failures and future prospects. (1993) (10)
Heat-stimulated nitroreductive bioactivation of the 2-nitroimidazole benznidazole in vitro. (1987) (10)
Differential intracellular processing of the anthracycline drug ME2303 in doxorubicin‐sensitive (A2780) and ‐resistant (A2780AD) human ovarian cancer cells as studied with confocal laser scanning microscopy and image analysis (1994) (10)
Stimulation by localized tumor hyperthermia of reductive bioactivation of 2-nitroimidazole benznidazole in mice. (1989) (10)
Analysis of tumour gene expression following chemotherapeutic treatment of patients with bowel cancer (1999) (10)
Response of a high-glucuronidase human tumour xenograft to aniline mustard. (1982) (10)
Inhibition of intracellular esterases by antitumour chloroethylnitrosoureas. Measurement by flow cytometry and correlation with molecular carbamoylation activity. (1988) (9)
Is a Potent and Oral Inhibitor of AKT and p 70 S 6 Kinase That Induces Pharmacodynamic Changes and Inhibits Human Tumor Xenograft Growth (2010) (9)
TCNU: a ray of hope for designer nitrosoureas? (1987) (9)
Is body composition an important variable in the pharmacokinetics of anticancer drugs? (2004) (9)
Pediatric and adult glioblastoma radiosensitization induced by PI3K/mTOR inhibition causes early metabolic alterations detected by nuclear magnetic resonance spectroscopy (2017) (9)
Signal transduction inhibitors as novel anticancer drugs: where are we? (1992) (9)
Development and validation of a liquid chromatography/tandem mass spectrometry method for the determination of the novel anticancer agent 17-DMAG in human plasma. (2006) (9)
Inhibiting the molecular evolution of cancer through HSP90 (2012) (9)
Alterations in EGF-dependent proliferative and phosphorylation events in squamous cell carcinoma cell lines by a tyrosine kinase inhibitor. (1994) (9)
Development of synthetic routes to macrocyclic compounds based on the HSP90 inhibitor radicicol (2006) (9)
The reversible N-oxidation of the nitroimidazole radiosensitizer Ro 03-8799. (1985) (9)
Gradient high-performance liquid chromatographic method for simultaneous assay of the radiosensitizers etanidazole (SR 2508) and pimonidazole (Ro 03-8799) in biological materials. (1987) (9)
Effects of the histone deacetylase inhibitor (HDACI) LAQ824 on histone acetylation, Hsp70 and c-Raf in peripheral blood lymphocytes from patients with advanced solid tumours enrolled in a phase I clinical trial (2004) (9)
The pharmacokinetics in mice and dogs of nitroimidazole radiosensitizers and chemosensitizers more lipophilic than misonidazole. (1982) (9)
Paul Workman on the challenges of cancer drug development (2003) (9)
Synthesis and antiproliferative activity of tyrphostins containing heteroaromatic moieties. (1994) (9)
RNAi screen reveals synthetic lethality between cyclin G-associated kinase and FBXW7 by inducing aberrant mitoses (2017) (9)
Modern cancer drug discovery: integrating targets, technologies and treatments (2008) (9)
Estimation of plasma area under the curve for etanidazole (SR 2508) in toxicity prediction and dose adjustment. (1989) (9)
HER3 Is an Actionable Target in Advanced Prostate Cancer (2021) (9)
Enzyme activated anti-tumour agents--III. Hydrolysis of conjugates of p-hydroxyaniline mustard in aqueous solution. (1976) (9)
CB 1954 revisited (2004) (9)
Laboratory and phase I studies of new cancer drugs (1992) (8)
Design of Novel Bioreductive Drugs (1992) (8)
Doxorubicin-3'-NH-oestrone-17-oxime-ethyl-carbonyl, a doxorubicin-oestrone conjugate that does not redox cycle in rat liver microsomes. (1990) (8)
Unpicking the combination lock for mutant BRAF and RAS melanomas. (2013) (8)
A new high-glucuronidase mouse tumor curable by aniline mustard therapy. (1977) (8)
The pharmacological audit trail (PhAT): Use of tumor models to address critical issues in the preclinical development of targeted anticancer drugs (2016) (8)
The role of microsomal enzyme inducers in the reduction of misonidazole neurotoxicity. (1983) (8)
Gradient high-performance liquid chromatographic assay for the determination of the novel indoloquinone antitumour agent E09 in biological specimens. (1990) (8)
Inhibition of human prostatic tumour acid phosphatase by N,N-p-di-2-chloroethylaminophenol, N,N-p-di-2-chloroethylaminophenyl phosphate and other difunctional nitrogen mustards. (1978) (8)
Misonidazole protects mouse tumour and normal tissues from the toxicity of oral CCNU. (1985) (8)
HIGH GRADE GLIOMAS (2012) (8)
Pharmacokinetics and Pharmacodynamics in Drug Development (2008) (7)
HSF1 in Translation. (2013) (7)
Epigenetics: Targeting leukemia on the DOT. (2011) (7)
414A Pharmacological properties and in vitro and in vivo antitumour activity of the potent and selective PI3 kinase inhibitor PI103 (2004) (7)
Analysis of the basic 5-nitroimidazole nimorazole in blood by reversed-phase high-performance liquid chromatography, and its application to pharmacokinetic studies in individual mice. (1979) (7)
Using biomarkers in drug development. (2006) (7)
The Chemical Probes Portal: an expert review-based public resource to empower chemical probe assessment, selection and use (2022) (7)
Stimulation of intracellular free calcium increases by platelet-activating factor in HT29 colon carcinoma cells. Spectrofluorimetric and preliminary spatio-temporal analysis using confocal laser scanning fluorescence imaging microscopy. (1994) (7)
The combination of multiple doses of etanidazole and pimonidazole in 48 patients: a toxicity and pharmacokinetic study. (1991) (7)
Overexpression of EZH 2 in multiple myeloma is associated with poor prognosis and dysregulation of cell cycle control (2017) (7)
Applications of liquid biopsy in the Pharmacological Audit Trail for anticancer drug development (2021) (7)
Development and validation of a solid-phase extraction and high-performance liquid chromatographic assay for a novel fluorinated 2-nitroimidazole hypoxia probe (SR-4554) in Balb/c mouse plasma. (1995) (7)
Enzyme activated anti-tumor agents--IV. Comparative kinetics of N,N-p-di-2-chloroethylaminophenyl phosphate hydrolysis catalysed by phosphatases of normal and neoplastic tissues. (1978) (7)
Lack of enantio-selectivity in the in vitro antitumour cytotoxicity and membrane-damaging activity of ether lipid SRI 62-834: further evidence for a non-receptor-mediated mechanism of action. (1992) (7)
Modulation of Plasma Metabolite Biomarkers of the MAPK Pathway with MEK Inhibitor RO4987655: Pharmacodynamic and Predictive Potential in Metastatic Melanoma (2017) (7)
Synthesis and anti-cancer activity of 2,6-disubstituted N-methylpiperidine derivatives and their N-oxides. (1996) (6)
Pharmacokinetics and metabolism of the mixed-function hypoxic cell sensitizer prototype RSU 1069 in mice (2004) (6)
Synthesis and biological evaluation of a series of tyrphostins containing nitrothiophene moieties as possible epidermal growth factor receptor tyrosine kinase inhibitors. (1996) (6)
Phenytoin sodium-induced alterations in the pharmacokinetics of misonidazole in the dog. (1980) (6)
Tumour concentrations of flavone acetic acid (FAA) in human melanoma: comparison with mouse data. (1992) (6)
Introduction: new anticancer drug design and discovery based on advances in molecular oncology. (1992) (6)
Accelerated elimination of pimonidazole following microsomal enzyme induction in mice: a possible approach to reduced neurotoxicity of the pimonidazole-etanidazole combination. (1989) (6)
The penetration of misonidazole and desmethylmisonidazole into brain tumours and other central nervous system tissues in man. (1983) (6)
ES-285, a novel marine anticancer agent: Investigation of mechanism of action using gene expression microarrays (2005) (6)
Micropharmacokinetics of chemical modifiers. (1989) (6)
SiGNet: A signaling network data simulator to enable signaling network inference (2017) (6)
Biopsy-Derived Biomarkers in Phase I Trials: Building Confidence in Drug Development. (2016) (6)
The promise and peril of chemical probes (vol 11, pg 536, 2015) (2015) (6)
The neurotoxicity of misonidazole: potential modifying role of dexamethasone. (1980) (6)
Modern Cancer Drug Discovery (2014) (6)
Corrigendum: The promise and peril of chemical probes. (2015) (5)
PI3 Kinase in Cancer: From Biology to Clinic. (2012) (5)
Drugging the cancer genome: new challenges of infrequent and combinatorial targets. (2007) (5)
The relevance of pharmacology in clinical oncology practice. The moderator thinks that.... (1993) (5)
In vivo Biological Activity of the Histone Deacetylase Inhibitor LAQ824 Is detectable with 3¶-Deoxy-3¶-( 18 F)Fluorothymidine (2006) (5)
A phase I trial of the heat shock protein 90 (HSP90) inhibitor 17-dimethylaminoethylamino-17-demethoxygeldanamycin (17- DMAG, alvespimycin) administered weekly (2007) (5)
Bottlenecks in Anticancer Drug Discovery and Development: In vivo Pharmacokinetic and Pharmacodynamic Issues and the Potential Role of PET (1995) (5)
Inhibition of phospholipid signalling and proliferation of Swiss 3T3 cells by the wortmannin analogue demethoxyviridin. (1997) (5)
Phase I study of BW12C in combination with mitomycin C in patients with advanced gastrointestinal cancer. (1992) (5)
Synthesis and antiproliferative activity of tyrphostins containing quinoline moieties. (1996) (5)
Interaction of nitroimidazole sensitizers with drug metabolizing enzymes--spectral and kinetic studies. (1986) (5)
Exploiting Cancer Dependence on Molecular Chaperones: HSP90 Inhibitors Past, Present, and Future (2014) (5)
Pharmacokinetic contribution to the improved therapeutic selectivity of a novel bromoethylamino prodrug (RB 6145) of the mixed-function hypoxic cell sensitizer/cytotoxin α-(1-aziridinomethyl)-2-nitro-1H-imidazole-1-ethanol (RSU 1069) (2004) (5)
Modulation of pancreatic cancer cell sensitivity to FOLFIRINOX through microRNA-mediated regulation of DNA damage (2021) (5)
Altered pharmacokinetics in the mechanism of chemosensitization: effects of nitroimidazoles and other chemical modifiers on the pharmacokinetics, antitumour activity and acute toxicity of selected nitrogen mustards (2004) (5)
High-performance liquid chromatography of chlorambucil analogues. (1987) (4)
Sensitization of (colon) cancer cells to death receptor related therapies (2012) (4)
The role of dexamethasone in the modification of misonidazole pharmacokinetics. (1983) (4)
Discovery and Design of Inhibitors of Oncogenic Tyrosine Kinases (1994) (4)
Effects of the xanthine oxidase inhibitor allopurinol on the renal clearance of nitroimidazoles. (1982) (4)
Patterns of cross-sensitivity in the responses of clonal subpopulations isolated from the RIF-1 mouse sarcoma to selected nitrosoureas and nitrogen mustards. (1984) (4)
Solution structure of the Hop TPR2A domain and investigation of target druggability by NMR, biochemical and in silico approaches (2020) (4)
Corrigendum: ATP-competitive inhibitors block protein kinase recruitment to the Hsp90-Cdc37 system (2013) (4)
Interactions of hyperthermia with hypoxic cell sensitisers. (1988) (4)
Coronavirus canSAR – a Data-Driven, AI-Enabled, Drug Discovery Resource for the Research Community (2020) (4)
Drug Discovery Strategies: Technologies to Accelerate Translation from Target to Drug (2004) (4)
Targeting hypoxia inducible factor-1. (2004) (4)
Evolution of kinase polypharmacology across HSP90 drug discovery (2020) (4)
Estimating the kinetic parameters for enzymatic drug metabolism in the whole animal. (1986) (4)
A comparative study of Ro 03-8799: racemic mixture and enantiomers. (1986) (4)
New drugs and novel agents. (1989) (4)
Pharmacokinetics of BW12C and mitomycin C, given in combination in a phase 1 study in patients with advanced gastrointestinal cancer (1993) (3)
Anti-cancer drug success emerges from molecular biology origins. (2001) (3)
Corrigendum: Drugging the PI3 kinome (2006) (3)
New class of antibiotics (2001) (3)
A phase I trial of the heat shock protein 90 (HSP90) inhibitor alvespimycin (17-dimethylaminoethylamino-17-demethoxygeldanamycin 17-DMAG) administered weekly, intravenously, to patients with advanced, solid tumors (2007) (3)
In vitro nuclear magnetic resonance spectroscopy metabolic biomarkers for the combination of temozolomide with PI3K inhibition in paediatric glioblastoma cells (2017) (3)
Emerging from a crisis in anticancer drug discovery? Screening versus design: confessions of an optimistic fence-sitter. (1992) (3)
Glutathione metabolism in human lymphocytes by flow cytometry (1988) (3)
The Novel Protein HSF1 Stress Pathway Inhibitor Bisamide CCT361814 Demonstrates Pre-Clinical Anti-Tumor Activity in Myeloma (2017) (3)
CB 1954 revisited (2004) (3)
Inhibition of cellular esterases by the antitumour imidazotetrazines mitozolomide and temozolomide: demonstration by flow cytometry and conventional spectrofluorimetry (2004) (3)
Abstract 2433:In vitroandin vivoantitumor activity of the next generation HSP90 inhibitor, AT13387, in both hormone-sensitive and castration-resistant prostate cancer models. (2013) (3)
Developments in Cancer Chemotherapy Volume II (1990) (3)
Abstract 4355: Elucidation of the different roles of CDK8 and CDK19 in colorectal cancer (CRC) using CRISPR gene editing technology (2016) (3)
Emerging Molecular Therapies: Drugs Interfering With Signal Transduction Pathways (2008) (3)
The off-target kinase landscape of clinical PARP inhibitors (2019) (3)
New targets for Crohn's disease. (2001) (3)
Effects of the histone deacetylase inhibitor (HDACI) LAQ824 on histone acetylation, Hsp70 and c-Raf in peripheral blood lymphocytes from patients with advanced solid tumours enrolled in a phase I clinical trial. (2004) (3)
Optimised Treatment Modalities for Hypoxic Tumour Cells (1989) (3)
Signalling pathways in afferent and efferent arms of angiogenesis induced by activation of c-erbB receptors (2002) (2)
Inhibition of the Epigenetic Modifier EZH2 Upregulates Cell Cycle Control Genes to Inhibit Myeloma Cell Growth and Overcome High-Risk Disease Features (2016) (2)
Commentary Finding the needle in the haystack: why high-throughput screening is good for your health (2002) (2)
Antitumour Ether Lipids and Platelet-Activating Factor Analogues Have Different Cytotoxic Profiles and Calcium Mobilizing Effects — a Structure-Activity Study (1993) (2)
Signal Transduction Pathways A Goldmine for Therapeutic Targets (2000) (2)
Induction of Hsp70 and depletion of the client protein c-Raf-1 measured by ELISA following cellular exposure to the novel Hsp90 ATPase inhibitor, CCT018159 (2003) (2)
347 Biological evaluation of a novel, synthetic pyrazole class of Hsp90 inhibitors (2004) (2)
New cancer drugs on the horizon. (2005) (2)
Successes for UK cancer partnership (2014) (2)
Inhibition of the Molecular Chaperone Heat Shock Protein 90 in Cancer: Consequences for the Regulation of Survival Signaling and Induction of Cell Death (2008) (2)
Structural and functional characterisation of human RNA helicase DHX8 provides insights into the mechanism of RNA-stimulated ADP release. (2019) (2)
Measurement of Enzyme Kinetics by Flow Cytometry (1993) (2)
More review content in TiPS 2003 (2003) (2)
HSP90 inhibitors: targeting the cancer chaperone for combinatorial blockade of oncogenic pathways (2008) (2)
322 Novel isoquinoline-5-sulfonamides as biochemical and cellular inhibitors of PKB/AKt (2004) (2)
Inhibitors of Heat Shock Protein 72 Induction Enhance Apoptosis Induced by Hsp90 Inhibitors (2008) (2)
Abstract B74: The dual FLT3-Aurora inhibitor CCT241736 overcomes resistance to selective FLT3 inhibition driven by FLT3 ligand and FLT3 point mutations in acute myeloid leukemia. (2011) (2)
Cancer - 21st century solutions (2002) (2)
Correction: In vitro Biological Characterization of a Novel, Synthetic Diaryl Pyrazole Resorcinol Class of Heat Shock Protein 90 Inhibitors. (2019) (2)
Can flow cytoenzymology be applied to measure membrane-bound enzyme kinetics? Assessment by analysis of gamma-glutamyl transpeptidase activity. (1993) (2)
Cell-signaling targets for antitumour drug development (2004) (2)
Effects of cimetidine, antipyrine, and pregnenolone carbonitrile on misonidazole pharmacokinetics. (1983) (2)
Discovering and Developing PI3 Kinase Inhibitors for Cancer: Rapid Progress through Academic-Biotech-Pharma Interactions (2011) (2)
Proceedings: The role of alkaline phosphatase in the release of p-hydroxy aniline mustard from its phosphate conjugate. (1975) (2)
Emerging Molecular Therapies: Small-Molecule Drugs (2000) (2)
DRUGGING THE HSP90 MOLECULAR CHAPERONE MACHINE FOR CANCER TREATMENT (2007) (2)
Rational Drug Design of Small Molecule Anticancer Agents: Preclinical Discovery (2007) (2)
Resistance to Selective FLT3 Inhibitors, Driven by FLT3 Ligand and FLT3 Point Mutations, Can Be Overcome with the Dual FLT3-Aurora Kinase Inhibitor CCT241736, (2011) (2)
Emerging Molecular Therapies (2000) (2)
New Trends in Targeted Cancer Chemotherapy (1987) (2)
Abstract #3863: Derivatives of seliciclib with improved potency both in vitro and in vivo as novel cyclin dependent kinase (CDK) inhibitors (2009) (2)
Validation of liquid chromatography assay for the quantitation of (Z)-3-[2,4-dimethyl-5-(2-oxo-1,2-dihydro-indol-3-ylidenemethyl)-1H-pyrrol-3-yl]propionic acid (SU006668) in human plasma and its application to a phase I clinical trial. (2003) (2)
Minimizing bias in target selection by exploiting multidisciplinary Big Data and the protein interactome. (2016) (2)
Corrigendum: New approaches to molecular cancer therapeutics (2007) (2)
AT13148, an orally bioavailable AKT kinase inhibitor with potent anti-tumor activity in both in vitro and in vivo models exhibiting AKT pathway deregulation. (2007) (2)
Corrigendum: Revealing the delta lady (2010) (2)
Pharmacokinetic and metabolism studies of a novel synthetic series of heat shock protein 90 (Hsp90) inhibitors (2003) (2)
Characterization of CCT129202, a novel Aurora kinase inhibitor and in vivo quantification of biological activity (2007) (2)
Native size exclusion chromatography-based mass spectrometry (SEC-MS) identifies novel components of the Heat Shock Protein 90-dependent proteome (2022) (1)
Pancreas Cancer Molecular Targets for Therapy (2011) (1)
Effects of elevated temperature on misonidazole O-demethylation by mouse liver microsomes: kinetic and stability studies of a model mixed-function oxidase reaction (2004) (1)
A liquid chromatographic-tandem mass spectrometric method for the determination of two selective thymidylate synthase inhibitors, BGC945 and BGC638, in mouse plasma. (2005) (1)
375 POSTER Downstream mechanistic markers of HDAC inhibition for drug discovery and clinical evaluation (2006) (1)
Enhancing access to innovative cancer drugs: cross-sector consensus on a way forward to benefit patients (2021) (1)
Abstract ND08: NXP800: A first-in-class orally active, small-molecule HSF1 pathway inhibitor (2022) (1)
Abstract 3025: Discovery of preclinical development candidate inhibitors of the mediator complex-associated kinases CDK8 and CDK19 and evaluation of their therapeutic potential (2016) (1)
Correction to: Reflections and Outlook on Targeting HSP90, HSP70 and HSF1 in Cancer: A Personal Perspective. (2020) (1)
Abstract 4977: MIR1307 mediates pancreatic cancer resistance to FOLFIRINOX chemotherapy by affecting response to DNA damage (2018) (1)
568 POSTER In vitro and in vivo pharmacological properties of the potent phosphatidylinositol 3-kinase (P13K) family inhibitor Pl103 (2006) (1)
Abstract 2962: Histone H3.3 mutations drive paediatric glioblastoma through upregulation of MYCN. (2013) (1)
Development and validation of a sensitive solid-phase-extraction and high-performance liquid chromatography assay for the bioreductive agent tirapazamine and its major metabolites in mouse and human plasma for pharmacokinetically guided dose escalation (1995) (1)
Pharmacological properties of the PI3 kinase (PI3K) inhibitors PI-540 and PI-620 (2008) (1)
Cancer Therapy : Preclinical AT 13148 Is a Novel , Oral Multi-AGC Kinase Inhibitor with Potent Pharmacodynamic and Antitumor Activity (2012) (1)
Discovery and validation of biomarkers to support clinical development of NXP800: A first-in-class orally active, small-molecule HSF1 pathway inhibitor (2022) (1)
Abnormal clinical pharmacokinetics of the developmental radiosensitizers pimonidazole (Ro 03-8799) and etanidazole (SR 2508). (1990) (1)
Drugging the cancer genome – discovery of small-molecule targeted therapeutics for personalized, precision medicine (2014) (1)
Combinatorial targets for the treatment of ovarian cancers with phosphatidylinositol-3-kinase inhibitors (2016) (1)
Abstract 2730: RNAi knockdown or chemical inhibition of anaphase-promoting complex components is synthetic lethal with HSP90 inhibition (2014) (1)
Preface - Hot topic: Hsp90 Molecular Chaperone Inhibitors: Opportunities and Challenges (Guest Editor: Paul Workman) (2003) (1)
NVP-AUY922 / VER-52296: A novel 3,4 diarylisoxazole Hsp90 chaperone inhibitor discovered via structure-based drug design (2007) (1)
Paul Workman--at the cutting edge of drug discovery (interview by Dorothy Bonn). (2001) (1)
Abstract 928: The novel clinical candidate AT13148 is an oral multi-AGC kinase inhibitor with potent pharmacodynamic and antitumor activity and demonstrates a mechanism of action distinct from AKT inhibitors (2012) (1)
Faculty Opinions recommendation of Cancer proliferation gene discovery through functional genomics. (2008) (1)
Abstract 3554: CCT137690, a dual inhibitor of Aurora and FLT3 kinases, sensitizes FLT3-ITD positive acute myeloid leukemia and overcomes resistance to selective FLT3-inhibition (2011) (1)
HSP90 Inhibition as an Anticancer Strategy: Novel Approaches and Future Directions (2009) (1)
Lack of stereoselectivity in the pharmacokinetics and metabolism of the radiosensitizer Ro 03-8799 in man (2004) (1)
605 POSTER Modulation of the HSP90 co-chaperone AHA1 affects client protein activity and increases cellular sensitivity to the HSP90 inhibitor 17-allylamino-17-demethoxygeldanamycin (17-AAG) (2006) (1)
319 Factors that govern the cell death response induced by inhibition of the molecular chaperone heat shock protein 90 (2004) (1)
The era of high-quality chemical probes (2022) (1)
Fragment docking supported by NMR shift perturbations (2014) (1)
MEK 1 / 2 inhibition decreases lactate in BRAF-driven human cancer cells (2013) (1)
Deletion Mutations in Pediatric High-Grade Glioma and Response to Targeted Therapy in Pediatric Glioma Cell Lines (2009) (1)
Author response: Assessing the mechanism and therapeutic potential of modulators of the human Mediator complex-associated protein kinases (2016) (1)
TRANSLATIONAL — BILIARY MIR 21 Drives Resistance to Heat Shock Protein 90 Inhibition in Cholangiocarcinoma (2018) (1)
Synthesis of Resorcinylic Macrocycles Related to Radicicol via Ring-Closing Metathesis. (2006) (1)
Signal Transduction Pathways (2001) (1)
Mechanism of action of a novel series of inhibitors of the Hsp90 molecular chaperone (2004) (1)
Targeting HSP90 in pediatric malignancies by the European Consortium "Innovative Therapies for Children with Cancer" (2007) (1)
Rational Drug Design of Small Molecule Anticancer Agents: Early Clinical Development (2007) (1)
Proceedings: A comparison of chemical and microbiological methods for estimating alkylating agent concentration. (1974) (1)
Novel cyclin dependent kinase (CDK) inhibitors induce down regulation of Mcl-1 and apoptosis in multiple myeloma cells (2006) (1)
Differential mechanisms of temozolomide resistance in pediatric glioma cell lines (2008) (1)
C MRS and DNA microarray analysis demonstrate increased phosphatidylcholine breakdown following inhibition of the PI3K signalling pathway in HCT116 colon cancer cells (2004) (1)
Establishment and Characterization of Acquired Resistance to the Farnesyl Protein Transferase Inhibitor R 115777 in a Human Colon Cancer Cell Line 1 (2002) (1)
Comprar Principles of Molecular Oncology | Bronchud, Miguel H. | 9781934115251 | Springer (2008) (1)
Orally Active 2-Amino Thienopyrimidine Inhibitors of the Hsp90 Chaperone (2009) (1)
Genomics and drug development (2003) (1)
PtdIns 3-kinase (2011) (1)
Use of gene expression microarrays to identify novel pharmacodynamic biomarkers of phosphatidylinositide-3’-kinase (PI3K) inhibition (2008) (1)
Dual Inhibition of Aurora and FLT3 Kinases by CCT137690: A Novel Treatment Strategy Against FLT3-ITD Positive AML In Vitro and In Vivo (2010) (1)
379 Characterisation of a novel class I isoform selective phosphatidyl-inositol 3-kinase inhibitor in glioma (2004) (1)
Cell cycle independent activity of cyclin D1. (2003) (1)
Human Hsp90-alpha with 9-Butyl-8-(2,5-dimethoxy-benzyl)-2-fluoro-9H-purin-6-ylamine (2004) (0)
HSF1 Pathway Inhibitor Clinical Candidate (CCT361814/NXP800) Developed from a Phenotypic Screen as a Potential Treatment for Refractory Ovarian Cancer and Other Malignancies (2023) (0)
Macrophage Stimulating 1 Receptor (2011) (0)
EGFRVIII deletion mutations in pediatric high-grade glioma and response to erlotinib in pediatric glioma cell lines (2008) (0)
The Chemical Probes Portal: an enhanced public resource providing expert advice on chemical tools for cancer research (2022) (0)
Abstract B166: A RNA helicase siRNA screen to identify potential therapeutic targets in castration-resistant prostate cancer (2015) (0)
PKA-S6K1 Chimera Apo (2013) (0)
Abstract 4549: Proteomic analysis of ubiquitination identifies the interplay between HSP90 inhibition and CUL5 in the control of autophagy (2016) (0)
Characterization of a potent inhibitor of class 1 phosphatidylinositide-3’-kinases (PI3K) in human glioma (2007) (0)
HUMAN HSP90 WITH 4-CHLORO-6-(4-(4-(4-METHANESULPHONYL-BENZYL)- PIERAZIN-1-YL)-1H-PYRAZOL-3-YL)-BENZENE-1,3-DIOL (2006) (0)
Signal Transduction Pathway Targeting (2005) (0)
canSAR: update to the cancer translational research and drug discovery knowledgebase (2022) (0)
Abstract 3242: CCT271850, a novel, selective, highly potent and orally bioavailable Mps1 kinase inhibitor. (2013) (0)
Q&A: Paul Workman on big data and large biases. (2013) (0)
The kinase polypharmacology landscape of clinical PARP inhibitors (2019) (0)
Reply to ‘Assembling the brain trust: the multidisciplinary imperative in neuro-oncology’ (2019) (0)
Design of drugs targeting the cell cycle (2003) (0)
Pyranone DNA-PK inhibitors, for treating cancer (2002) (0)
STRUCTURE OF PKB-BETA (AKT2) COMPLEXED WITH THE INHIBITOR A-443654 (2007) (0)
HUMAN HSP90 WITH 4-(4-(2,3-Dihydro-benzol(1,4)dioxin-6-yl)-5-methyl- 1H-pyrazol-3-yl)-6-ethyl-benzene-1,3-diol (2006) (0)
Array technology in the molecular pharmacology of anticancer agents (1999) (0)
PKA-S6K1 Chimera with Staurosporine bound (2013) (0)
Abstract 1817: Characterisation of CCT251455, a novel, selective and highly potent Mps1 kinase inhibitor (2012) (0)
H3F3A MUTATIONS IN PAEDIATRIC GLIOBLASTOMA REGULATE A SELF-RENEWAL GENE SIGNATURE (2012) (0)
Abstract A024: Probe Miner: objective, quantitative, data-driven assessment of chemical probes for target validation (2018) (0)
BRAF inhibition promotes BRAF mutant human melanoma cell survival under nutrient-deprived conditions through activation of mitochondrial metabolism (2016) (0)
140 POSTER Macrolactone based inhibitors of Heat Shock Protein 90 (2008) (0)
PKA-S6K1 Chimera with compound 21a (CCT196539) bound (2013) (0)
Structure of PKA-PKB chimera complexed with C-(4-(4-Chlorophenyl)-1-(7H-pyrrolo(2,3-d)pyrimidin-4-yl)piperidin-4-yl)methylamine (2008) (0)
Abstract 3517: Changes in plasma components of β-oxidation as a pharmacodynamic (PD) biomarker of PI3K inhibition by GDC-0941, a potent, pan-inhibitor of Class I phosphatidyl-inositol-3-kinase (PI3K). (2013) (0)
Abstract 1133: Synthetic lethal screen identifies candidates that modulate cancer cell sensitivity in response to HSP90 inhibition. (2013) (0)
Abstract 4749: Insights into the molecular mechanism of HSP90 binding of methoxy-substituted resorcinylic isoxazole amide inhibitors reveal different isoform selectivity profiles (2012) (0)
R-loop editing by DNA cytosine deaminase APOBEC3B determines the activity of estrogen receptor enhancers (2022) (0)
Abstract C7: Sensitization of human colorectal cancer cells to TRAIL induced‐apoptosis following inhibition of PI3K or HSP90 (2009) (0)
Correction to: An in vitro and in vivo study of the combination of the heat shock protein inhibitor 17-allylamino-17-demethoxygeldanamycin and carboplatin in human ovarian cancer models (2018) (0)
Abstract 4164: The druggable proteome: Identifying novel target families for cancer (2014) (0)
Abstract 1828: A genomic-transcriptomic-phosphoproteomic study to interrogate lapatinib resistance in an HER2 over expressing SKBR3 human breast cancer cell line model (2014) (0)
The Antisignaling Agent SC- (cid:1)(cid:1)(cid:2) 9, 4-(Benzyl-(2-[(2,5-diphenyloxazole-4-carbonyl)amino]ethyl)carbamoyl)-2-decanoylaminobutyricAcid,IsaStructurallyUniquePhospholipidAnaloguewithPhospholipaseCInhibitoryActivity (2002) (0)
Essays In Biochemistry: 61 (5) (2017) (0)
Dodgy malaria drugs. (2001) (0)
Chapter 1 – Absorption and distribution of anticancer drugs (1993) (0)
Pharmacological Targets Database (PTbase) (2002) (0)
Correction: A chemical inhibitor of PPM1D that selectively kills cells overexpressing PPM1D (2020) (0)
Increase of oleic acid in erythrocytes associated with malignancies (1985) (0)
Designing new cancer drugs: the science, the art and team sport (2008) (0)
Paul A. J. Speth, M.D. (1989) (0)
HIGH GRADE GLIOMAS AND DIPG (2014) (0)
Abstract 5083: Inhibition of MEK1/2 signaling in humanBRAFV600Emelanoma cells reduces glucose uptake and lactate dehydrogenase activity resulting in a time-dependent decrease in lactate production (2010) (0)
Sequencing of prostate cancers identifies new cancer genes, routes of progression and drug targets (2018) (0)
Crystal structure of DHX8 helicase domain bound to ADP at 2.3 Angstrom (2019) (0)
PKA-S6K1 Chimera with compound 1 (NU1085) bound (2013) (0)
Abstract 2976: Confirmation of in-cell target engagement using the proteolysis targeting chimeras (PROTACs) against pirin (2018) (0)
Tumours in the Brain: A Special Case for Drug Delivery (1990) (0)
Pharmacokinetics in experimental and clinical chemotherapy (2004) (0)
Structure of PKA-PKB chimera complexed with (1S)-2-amino-1-(4- chlorophenyl)-1-(4-(1H-pyrazol-4-yl)phenyl)ethan-1-ol (2012) (0)
251 ORAL The phosphatidylinositide 3-kinase (P13-kinase) inhibitor Pl103 sensitises some ovarian carcinoma (OC) cell lines to paclitaxel or carboplatin (2006) (0)
426 POSTER A high throughput screen and secondary assays for the identification and evaluation of histone methyltransferase inhibitors (2006) (0)
Microarray gene expression studies to discover novel determinants of sensitivity to gefitinib in squamous cell carcinoma of the head and neck (2008) (0)
841 Non-invasive Imaging of Response to MEK Inhibition With Selumetinib (AZD6244, ARRY-142886) in a Human Colorectal Cancer Xenograft Using Diffusion-Weighted MRI (2012) (0)
Bioreductive drugs in phase I — How to evaluate (1993) (0)
Paul Workman: Drugging the Cancer Genome (2016) (0)
562 POSTER Inhibition of MEK 1/2 signalling with Cl-1040 in human melanoma cells leads to alterations in phosphocholine metabolism (2006) (0)
Abstract A187: Exploring isoform-dependent functions of the mediator kinases in colorectal cancer (2018) (0)
Structure of cAMP-dependent protein kinase complexed with (4R,2S)-5'-(4-(4-Chlorobenzyloxy)pyrrolidin-2-ylmethanesulfonyl)isoquinoline (2005) (0)
Cassette dosing in tumor bearing animals for the discovery of NVP-AUY922, a novel HSP90 inhibitor. (2007) (0)
Primary Cancer Site (2011) (0)
42 New inhibitors targeting critical cancer dependencies: Progress and challenges (2010) (0)
Anakinra for arthritis. (2001) (0)
Mitomycin C under Aerobic but not Hypoxic Conditions Impaired Drug Activation in a Mammalian Cell Line Resistant to Decreased NADPH : Cytochrome P-450 Reductase Activity and Updated (2006) (0)
Abstract 4383: SOCRATES: integrating ex vivo and in silico analysis to identify optimal drug combinations for patients (2016) (0)
Human Hsp90-alpha with 8-Benzo[1,3]dioxol-,5-ylmethyl-9-butyl-2-fluoro-9H-purin-6-ylamine (2004) (0)
Abstract 2807: HER3 is an actionable target in advanced prostate cancer (2022) (0)
First disclosure of the chemical structure of a selective fibroblast growth factor receptor ( FGFr ) inhibitor lead series from Astex ’ s collaboration with Janssen Pharmaceutica (0)
Pharmacological intervention with multistep oncogenesis: potential role for HSP90 inhibitors (2004) (0)
Structure of PKA-PKB chimera complexed with ISOQUINOLINE-5-SULFONIC ACID (2-(2-(4-CHLOROBENZYLOXY) ETHYLAMINO)ETHYL)AMIDE (2007) (0)
Native Size-Exclusion Chromatography–Based Mass Spectrometry Reveals New Components of the Early Heat Shock Protein 90 Inhibition Response Among Limited Global Changes (2022) (0)
Benzopyranone DNA-PK inhibitors (2002) (0)
Hsp90 Inhibitors Deliver a Death Signal Via the Endoplasmic Reticulum Stress Pathway in Myeloma. (2006) (0)
Gene Microarray Technologies for Cancer Drug Discovery and Development (2005) (0)
Effects of the hydroxamic acid histone deacetylase inhibitors trichostatin A (TSA), suberoylanilide hydroxamic acid (SAHA) and LAQ824 on histone and protein acetylation. (2003) (0)
Abstract #4677: NVP-BEP795 and NVP-BEP800: Novel, fragment derived orally bioavailable small molecule Hsp90 inhibitors with potent antitumor activity (2009) (0)
Abstract 2501: Inhibition of the PI3K pathway potentiates temozolomide effects in pediatric glioblastoma and results in alterations in glucose and choline metabolism detected by MRS (2012) (0)
Screening for novel anticancer drugs in an academic environment: the right time and the right place? (2003) (0)
Abstract 1130: Unveiling the metabolic response of BRAF mutant melanoma cells to BRAF inhibition (2015) (0)
Crystal structure of DHX8 helicase bound to single stranded poly-adenine RNA (2019) (0)
Small-molecule targeting of brachyury transcription factor addiction in chordoma (2019) (0)
331 Key roles for HSP90 in tumour neoangiogenesis (2004) (0)
Abstract 293: Screening the druggable genome for synthetic lethal interactions with the CHK1 inhibitor PNT737 (2017) (0)
237 INVITED Strategies to transfer success in the development of molecularly targeted therapy to the challenge of paediatric cancers (2006) (0)
HSP-90 Inhibition is a Promising Therapeutic Strategy in Cholangiocarcinoma and MIR-21 may Serve as a Biomarker of Sensitivity (2016) (0)
Human Hsp90-alpha with 8-Benzo[1,3]dioxol-,5-ylmethyl-9-butyl-9H-purin-6-ylamine (2004) (0)
Characterisation of the 4q12 amplicon in pediatric gliomas (2008) (0)
Novel therapeutic strategies (2002) (0)
Development of PI3 kinase inhibitors for cancer treatment (2005) (0)
Human Hsp90-alpha with 9-Butyl-8-(2-chloro-3,4,5-trimethoxy-benzyl)-9H-purin-6-ylamine (2004) (0)
The Encyclopedia of Cancer (2008) (0)
Elemental mapping of fluorine using electron spectroscopic imaging for the intracellular localisation of an anthracycline drug (ME2303) in human ovarian cancer cells. (1993) (0)
Structure of PKA-PKB chimera complexed with A-443654 (2007) (0)
Abstract SY06-03: Exploiting the dependency of cancer cells on molecular chaperone systems (2011) (0)
Development and characterisation of a cell-based system for identification of novel HIF-1 inhibitors. (2003) (0)
Abstract 4481: First report of preclinical pharmacology of two novel potent AKT inhibitors and development of pharmacodynamic (PD) biomarkers in tumor and surrogate tissue (2010) (0)
Screening in an academic environment: The right time and the right place? (2003) (0)
PKA-S6K1 Chimera with compound 21e (CCT239066) bound (2013) (0)
Japan-U.S. Joint seminar on toxicity of chlorinated biphenyls, dibenzofurans, dibenzodioxins, and related compounds. April 25-28, 1983, Fukuoka, Japan. (1985) (0)
Correction: Silencing of HSP90 Cochaperone AHA1 Expression Decreases Client Protein Activation and Increases Cellular Sensitivity to the HSP90 Inhibitor 17-Allylamino-17-Demethoxygeldanamycin. (2019) (0)
346 Pharmacodynamic markers for the choline kinase inhibitor MN58b in human breast cancer model by magnetic resonance spectroscopy (2004) (0)
Cancer esearch apeutics , Targets , and Chemical Biology MT-Independent Temozolomide Resistance in Pediatric blastoma Cells Associated with a PI 3-Kinase – Mediated R / Stem Cell Gene Signature (2010) (0)
Abstract B99: Targeting TPR cochaperones of the Hsp90 molecular chaperone complex for specific inhibition. (2011) (0)
The View From Here: Drugging the cancer genome (2009) (0)
Molecular profiling and combinatorial activity of CCT068127 (2017) (0)
Monthly pill. (2001) (0)
A prospective study to evaluate the role of gene expression profiles (GEP) in predicting clinical outcome of patients (pts) receiving preoperative chemotherapy for oesophagogastric (OG) cancer (2007) (0)
Correction: Signalling involving MET and FAK supports cell division independent of the activity of the cell cycle-regulating CDK4/6 kinases (2020) (0)
CHAPTER 4:Exploiting the Dependency of Cancer Cells on Molecular Chaperones (2013) (0)
Abstract 1775: Identification of small molecule inhibitors of HSF1 stress pathway activation in cancer cells (2014) (0)
540 Vemurafenib alters glucose utilization in BRAF-driven human melanoma cells (2014) (0)
Pharmacology of the Hypoxic cell Radiosensitizers Ro 03-8799 and SR 2508 in Human Gliomas and Brain Tissue (1987) (0)
Paul D. Workman Photograph Collection- Accession 1109 (2003) (0)
149 POSTER Acetylation of molecular chaperones by histone deactylase inhibitors (HDACI) (2008) (0)
145 POSTER Hsp90 inhibitors target addiction to mutant oncoproteins in colorectal cancer (2008) (0)
764 Prioritising PK/PD endpoints for molecular imaging (2003) (0)
PKA-S6K1 Chimera with compound 15e (CCT147581) bound (2013) (0)
Twenty-ninth annual meeting of the British Association for Cancer Research in conjunction with the third annual meeting of the Association of Cancer Physicians. March 21-24, 1988, Norwich, U.K. Abstracts. (1988) (0)
Structure of PKA-PKB chimera complexed with (1-(9H-Purin-6-yl) piperidin-4-yl)methanamine (2008) (0)
Paul Workman on the challenges of cancer drug development. Interview by Katharine E. Pestell. (2003) (0)
Abstract 2843: Resistance to ERK inhibitors as a result of an acquired novel P-loop mutation of ERK2 (2015) (0)
PI3 kinase inhibitory drugs: fantasy or reality? (2009) (0)
Iceland's genome fits another piece in schizophrenia puzzle (2002) (0)
Inhibition of the molecular chaperone Hsp90 in cancer: consequences for the regulation of survival signalling and induction of cell death (2005) (0)
Abstract 1158: Real-time assessment of uptake and utilization of lactate in intact human breast cancer cells using a 1H-NMR-based assay (2015) (0)
Human Hsp90-alpha with 8-(2,5-dimethoxy-benzyl)-2-fluoro-9H-purin-6-ylamine (2004) (0)
Structure of cAMP-dependent protein kinase complexed with A-443654 (2007) (0)
1 INVITED Translating basic research into patient benefit: The druggable cancer genome (2007) (0)
Feeling forgetful? (2001) (0)
New drug design and development in cancer: present status and future perspectives (2004) (0)
111 Development and validation of a mass spectrometric assay to evaluate drug-drug interaction in human liver microsomes. Application to anticancer agents (2004) (0)
Emerging molecular therapies: drugs affecting signal transduction (2004) (0)
9411 The novel HSP90 inhibitor NVP-AUY922 demonstrates activity in rhabdomyosarcoma cell lines (2009) (0)
Changes in choline metabolism as potential biomarkers of HSP 90 inhibition in NEU / HER 2-driven mammary carcinoma Oncomouse ® cells (2009) (0)
Crystal structure of DHX8 helicase domain bound to ADP at 2.6 angstrom (2019) (0)
Abstract 5277: Non-invasive metabolic biomarkers of histone deacetylase inhibition in human colon cancer cells and tumors (2011) (0)
Structure of PKA complexed with 4-(4-Chlorobenzyl)-1-(7H-pyrrolo(2,3- d)pyrimidin-4-yl)piperidin-4-ylamine (2008) (0)
Human Hsp90-beta with PU3 (9-Butyl-8(3,4,5-trimethoxy-benzyl)-9H-purin-6-ylamine) (2004) (0)
The novel potent PI3 Kinase inhibitors, PI-540 and PI-620: Activity in vitro and in vivo (2008) (0)
Molecular Medicine in Practice The Association of PI 3 Kinase Signaling and Chemoresistance in Advanced Ovarian Cancer (2012) (0)
Loss of Spindly sensitizes EML4-ALK v3 lung cancer cells to HSP90 inhibitors (2022) (0)
Inhibition of the HSP90 molecular chaperone in vitro and in vivo by novel, synthetic, potent resorcinylic pyrazole, isoxazole amide analogs (2007) (0)
Effects of HSP90 inhibitor 17-allylamino-17-demethoxygeldanamycin (17-AAG) on NEU/HER2 overexpressing mammary tumours in MMTV-NEU-NT mice monitored by Magnetic Resonance Spectroscopy (2012) (0)
News & CommentFree? journals (2001) (0)
Abstract 4772: Addiction to chaperones: Investigating the role of HSP70 isoforms in cancer (2016) (0)
Abstract 5399: Inhibition of the PI3K/mTOR pathway potentiates irradiation effects in paediatric glioblastoma inducing metabolic alterations detected by MRS. (2013) (0)
Abstract LB-304: Discovery of chemical probe CCT251236: An orally bioavailable efficacious pirin ligand from an HSF1 phenotypic screen (2017) (0)
80 POSTER Inhibition of MEK1/2 signalling results in decreased levels of intracellular lactate in human melanoma and colorectal cancer cells as observed with magnetic resonance spectroscopy (2008) (0)
Target in Renal Cell Carcinoma A HIF-Regulated VHL-PTP 1 B-Src Signaling Axis Identifies a Therapeutic (2011) (0)
Signalling targets for the development of cancer drugs. (1994) (0)
Combined action of hypoxic sensitisers and hyperthermia on the emt6 tumour. Abstr. (1977) (0)
Non-invasive Imaging of Response to MEK Inhibition With Selumetinib (AZD6244, ARRY-142886) in a Human Colorectal Cancer Xenograft Using Diffusion-Weighted MRI (2012) (0)
Abstract LB234: Activation of the integrated stress response by the developmental HSF1 pathway inhibitor NXP800 (2023) (0)
Targeting the proteasome: a new route to anticancer treatment (2002) (0)
HUMAN HSP90 WITH 5-(5-CHLORO-2,4-DIHYDROXY-PHENYL)-4-PIPERAZIN-1-YL- 2H-PYRAZOLE-3-CARBOXYLIC ACID ETHYLAMIDE (2006) (0)
In Brief (2002) (0)
Abstract B83: Modulation of the HSP90 cochaperone carboxy‐terminus HSC70‐interacting protein (CHIP) increases cellular sensitivity to heat shock protein 90 (HSP90) inhibition (2009) (0)
Drugging the cancer genome: Advances, challenges, and the pharmacologic audit trail (2006) (0)
Advances in Enzyme-Regulation. Vol. 31 (1992) (0)
Notable Developments in Genomic Profiling Have Enhanced Personalized Cancer Care (2014) (0)
HSP72 with adenosine-derived inhibitor (2016) (0)
Abstract IA16: Targeting molecular chaperone and stress pathways to hit multiple hallmarks and overcome resistance (2017) (0)
Correction: Discovery of 4,6-disubstituted pyrimidines as potent inhibitors of the heat shock factor 1 (HSF1) stress pathway and CDK9. See DOI: 10.1039/c6md00159a (2016) (0)
P0282 : The long non coding RNA UC.158 modulates growth of Wnt/β;-catenin driven hepatocellular carcinoma (HCC) (2015) (0)
O.101 ADVENTURES IN TARGETED CANCER THERAPY: FROM TUMOUR HYPOXIA TO THE CANCER GENOME (2006) (0)
Therapeutics , Targets , and Chemical Biology MEK 1 / 2 Inhibition Decreases Lactate in BRAF-Driven Human Cancer Cells (2013) (0)
CCT068127 in complex with CDK2 (2017) (0)
453 Plasma metabolomic signature of novel signal transduction inhibitors from preclinical identification to clinical validation (2014) (0)
8P NXP800 versus cisplatin in ARID1a-mutated ovarian clear cell carcinoma xenograft models (2023) (0)
Targeting of multiple signalling pathways 90 molecular chaperone inhibitors (2007) (0)
Abstract 1069: MiR-21 may serve as a predictive biomarker of response in the assessment of efficacy of HSP-90 inhibition in gastrointestinal (GI) cancers (2016) (0)
New face at TiPS (2001) (0)
Fragment-based screening of HSP70 sheds light on the functional role of ATP-binding site residues (2016) (0)
Abstract PR02: Identification of a potent and selective chemical probe for exploring the role of CDK8/19 in cancer biology (2015) (0)
Heat shock protein 90 inhibitors modulate choline phospholipid profiles and metabolizing enzymes in human melanoma cells (2008) (0)
Abstract LB-48: Non-invasive imaging of response to MEK Inhibition with AZD6244 (ARRY-142886) in a human melanoma xenograft monitored by diffusion-weighted MRI (2010) (0)
104 Plasma metabolomic analysis of genetic and pharmacological manipulation of PI 3-kinase pathway activation in mice using liquid chromatography coupled to mass spectrometry (LC-MS) (2010) (0)
Population Candidate Gene Association Study (2011) (0)
Purine derivatives and their use as antiproliferative agent (2003) (0)
Abstract 3869: Phosphoproteomic-based identification of CDK8/CDK19 substrates in colorectal cancer (2016) (0)
109 Identification of small molecule inhibitors of PKB/AKT in a high throughput screen (2004) (0)
A flow cytofluorimetric assay for cellular esterases in populations of single cells. Abstr. (1978) (0)
L5.2 Drugging the Cancer Genome: Opportunities and Challenges (2012) (0)
NVP-AUY922, a novel diarylisoxazole resorcinol HSP90 inhibitor, potently inhibits growth and metastasis of human tumor xenografts (2007) (0)
/ Stem Cell Gene Signature HOX Mediated − Glioblastoma Cells Associated with a PI 3-Kinase MGMT-Independent Temozolomide Resistance in Pediatric (2010) (0)
Development and Validation of RP-HPLC Method for the Estimation of Ivabradine Hydrochloride in Tablets (2010) (0)
Upregulation of MYCN Histone H 3 . 3 Mutations Drive Pediatric Glioblastoma through (2013) (0)
Ninth International Conference on Chemical Modifiers of Cancer Treatment, August 22-26, 1995, Christ Church, Oxford, UK (1996) (0)
Phase I safety, pharmacokinetic, and pharmacogenomic trial of ES-285, a novel marine cytotoxic agent administered as an infusion over 24 h every 21 days in patients with solid tumors (2007) (0)
Abstract 129: Assessing the mechanism and therapeutic potential of modulators of the human mediator complex-associated protein kinases CDK8 and CDK19 (2017) (0)
Structure of cAMP-dependent protein kinase complexed with Isoquinoline-5-sulfonic acid (2-(2-(4-chlorobenzyloxy)ethylamino) ethyl)amide (2005) (0)
Human Hsp90-alpha with 9-Butyl-8-(3,4,5-trimethoxy-benzyl)-9H-purin-6-ylamine (2004) (0)
Placebo effect? (2001) (0)
New in neurology (2001) (0)
News & CommentIn briefs (2002) (0)
Allison's trail of destruction. (2001) (0)
Array technology in the molecular pharmacology of anticancer agents (1999) (0)
Good news for sick Kenyans. (2001) (0)
Vascular biology researcher honoured (2001) (0)
330 Magnetic resonance spectroscopy confirms the mechanism of action of the choline kinase inhibitor MN58b in human breast cancer cells (2004) (0)
Clinical trial safety. (2001) (0)
Abstract 2677: A detailed analysis of protein binding and biological activity of methoxy-substituted resorcinylic isoxazole amide HSP90 inhibitors (2010) (0)
Targeting Hsp90: The Cancer Super-Chaperone (2007) (0)
Human Hsp90-alpha with 8-(2-chloro-3,4,5-trimethoxy-benzyl)-2-fluoro-9-pent-4-ylnyl-9H-purin-6-ylamine (2004) (0)
Abstract BSF2-1: Molecular Chaperones: Cancer Dependence and Druggability (2010) (0)
Histone deacetylase inhibitors (HDACIs) induce HIF-1 transcriptional activity. (2006) (0)
Abstract 2998: Molecular and cellular effects of individual and combinatorial silencing of HSP90 paralogs (2016) (0)
European School of Oncology Task Force Report. New approaches in cancer pharmacology: drug design and development (Part 2). (1994) (0)
3 INVITED Signalling pathways as targets for therapy in angiogenesis and metastasis (2007) (0)
Human Hsp90-alpha with 8-(2,5-dimethoxy-benzyl)-2-fluoro-9-pent-9H-purin-6-ylamine (2004) (0)
Abstract 4428: A novel imidazo[4,5-b]pyridine Aurora kinase inhibitor with anti-leukemic activity (2010) (0)
229 INVITED The role of genomics and proteomics in targeted drug development: discovery and use of biomarkers (2006) (0)
Abstract 2896: A genome-wide CRISPR/Cas9 pooled screen identifies EML4-ALK variant-specific synthetic lethal partners of HSP90 inhibitors (2018) (0)
Paul Workman's Paris (1999) (0)
37 INVITED Drugging the cancer chaperone Hsp90: From chemical biology with natural products to active drugs in the clinic (2008) (0)
HUMAN HSP90 WITH 4-CHLORO-6-(4-PIPERAZIN-1-YL-1H-PYRAZOL-3-YL)- BENZENE-1,2-DIOL (2006) (0)
Acquired resistance to HSP90 inhibitor 17-allylamino-17-demethoxygeldanamycin (17-AAG) in adult and pediatric glioblastoma cell lines (2008) (0)
O1.2Drugging the cancer genome to overcome drug resistance (2015) (0)
Microbots in the body. (2001) (0)
Abstract 2925: Mechanism-based combinatorial treatment of KRAS mutant colorectal cancer with MEK and PI3K pathway inhibitors (2014) (0)
Pharmacological Intervention With Multistep Oncogenesis (2004) (0)
6 Genomics and proteomics in drug development (2004) (0)
An in vitro and in vivo study of the combination of the heat shock protein inhibitor 17-allylamino-17-demethoxygeldanamycin and carboplatin in human ovarian cancer models (vol 62, pg 769, 2008) (2018) (0)
Abstract A239: MPS1 (TTK) kinase inhibition selectively kills aneuploid cells (2009) (0)

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