Doriano Fabbro

Q: What Schools Are Affiliated With Doriano Fabbro

Doriano Fabbro is affiliated with the following schools: Medical University of Vienna, University of Milan, University of Strasbourg, Stanford University

Doriano Fabbro's AcademicInfluence.com Rankings

Doriano Fabbro

Computer Science

#7847

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#8256

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Algorithms

#309

World Rank

#313

Historical Rank

Computational Linguistics

#1655

World Rank

#1672

Historical Rank

Machine Learning

#3049

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#3087

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Computer Science

Doriano Fabbro's Degrees

PhD Computer Science University of Milan
Bachelors Computer Science University of Milan

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Doriano Fabbro's Published Works

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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

The IUPHAR/BPS Guide to PHARMACOLOGY in 2018: updates and expansion to encompass the new guide to IMMUNOPHARMACOLOGY (2017) (1500)
Characterization of AMN107, a selective inhibitor of native and mutant Bcr-Abl. (2005) (1471)
Identification and characterization of NVP-BEZ235, a new orally available dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor with potent in vivo antitumor activity (2008) (1150)
The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands (2015) (1100)
Inhibition of mutant FLT3 receptors in leukemia cells by the small molecule tyrosine kinase inhibitor PKC412. (2002) (613)
THE CONCISE GUIDE TO PHARMACOLOGY 2017/18: Enzymes (2017) (606)
In vivo antitumor activity of NVP-AEW541-A novel, potent, and selective inhibitor of the IGF-IR kinase. (2004) (571)
The Concise Guide to PHARMACOLOGY 2015/16: Enzymes (2015) (559)
A novel antisense oligonucleotide targeting survivin expression induces apoptosis and sensitizes lung cancer cells to chemotherapy. (2000) (514)
PKC zeta is a molecular switch in signal transduction of TNF‐alpha, bifunctionally regulated by ceramide and arachidonic acid. (1995) (506)
Identification and Characterization of NVP-BKM120, an Orally Available Pan-Class I PI3-Kinase Inhibitor (2011) (468)
THE CONCISE GUIDE TO PHARMACOLOGY 2019/20: Enzymes (2019) (443)
Antitumor activity of a phosphorothioate antisense oligodeoxynucleotide targeted against C-raf kinase (1996) (415)
A derivative of staurosporine (CGP 41 251) shows selectivity for protein kinase C inhibition and In vitro anti‐proliferative as well as In vivo anti‐tumor activity (1989) (406)
Requirement of Src kinases Lyn, Hck and Fgr for BCR-ABL1-induced B-lymphoblastic leukemia but not chronic myeloid leukemia (2004) (403)
Allosteric inhibitors of Bcr-abl–dependent cell proliferation (2006) (347)
The crystal structure of a c-Src complex in an active conformation suggests possible steps in c-Src activation. (2005) (315)
AEE788: a dual family epidermal growth factor receptor/ErbB2 and vascular endothelial growth factor receptor tyrosine kinase inhibitor with antitumor and antiangiogenic activity. (2004) (315)
Discovery of NVP-BYL719 a potent and selective phosphatidylinositol-3 kinase alpha inhibitor selected for clinical evaluation. (2013) (313)
Protein kinases as targets for anticancer agents: from inhibitors to useful drugs. (2002) (304)
THE CONCISE GUIDE TO PHARMACOLOGY 2019/20: Introduction and Other Protein Targets (2019) (295)
Different susceptibility of protein kinases to staurosporine inhibition. Kinetic studies and molecular bases for the resistance of protein kinase CK2. (1995) (293)
PKC412--a protein kinase inhibitor with a broad therapeutic potential. (2000) (281)
THE CONCISE GUIDE TO PHARMACOLOGY 2017/18: Overview (2017) (266)
Activation mutations of human c-KIT resistant to imatinib mesylate are sensitive to the tyrosine kinase inhibitor PKC412. (2005) (248)
Ten things you should know about protein kinases: IUPHAR Review 14 (2015) (244)
PKC412 overcomes resistance to imatinib in a murine model of FIP1L1-PDGFRα-induced myeloproliferative disease. (2003) (234)
Imatinib: a selective tyrosine kinase inhibitor. (2002) (232)
Structural biology contributions to the discovery of drugs to treat chronic myelogenous leukaemia (2006) (231)
PKC412 inhibits in vitro growth of neoplastic human mast cells expressing the D816V-mutated variant of KIT: comparison with AMN107, imatinib, and cladribine (2CdA) and evaluation of cooperative drug effects. (2006) (230)
The epsilon isoform of protein kinase C is an oncogene when overexpressed in rat fibroblasts. (1993) (226)
Induction of apoptosis in small-cell lung cancer cells by an antisense oligodeoxynucleotide targeting the Bcl-2 coding sequence. (1997) (219)
Extended kinase profile and properties of the protein kinase inhibitor nilotinib. (2010) (212)
Discovery of a potent and selective protein kinase CK2 inhibitor by high-throughput docking. (2003) (204)
THE CONCISE GUIDE TO PHARMACOLOGY 2019/20: Catalytic receptors (2019) (198)
Discovery of Asciminib (ABL001), an Allosteric Inhibitor of the Tyrosine Kinase Activity of BCR-ABL1. (2018) (193)
Prediction of Resistance to Small Molecule FLT3 Inhibitors (2004) (192)
Trends in kinase drug discovery: targets, indications and inhibitor design (2021) (186)
Phosphorylation Specificities of Protein Kinase C Isozymes for Bovine Cardiac Troponin I and Troponin T and Sites within These Proteins and Regulation of Myofilament Properties* (1996) (185)
International Union of Basic and Clinical Pharmacology. XC. Multisite Pharmacology: Recommendations for the Nomenclature of Receptor Allosterism and Allosteric Ligands (2014) (183)
THE CONCISE GUIDE TO PHARMACOLOGY 2017/18: Catalytic receptors (2017) (181)
Dramatic inhibition of retinal and choroidal neovascularization by oral administration of a kinase inhibitor. (1999) (176)
Specific CLK Inhibitors from a Novel Chemotype for Regulation of Alternative Splicing (2011) (175)
PKC412 inhibits the zinc finger 198-fibroblast growth factor receptor 1 fusion tyrosine kinase and is active in treatment of stem cell myeloproliferative disorder. (2004) (172)
Effect of VEGF receptor inhibitor PTK787/ZK222548 combined with ionizing radiation on endothelial cells and tumour growth (2001) (171)
Imatinib (STI571) resistance in chronic myelogenous leukemia: molecular basis of the underlying mechanisms and potential strategies for treatment. (2004) (170)
Selective regulation of expression of protein kinase C (PKC) isoenzymes in multidrug-resistant MCF-7 cells. Functional significance of enhanced expression of PKC alpha. (1993) (168)
Inhibition of Growth of Human Tumor Cell Lines in Nude Mice by an Antisense Oligonucleotide Inhibitor of Protein Kinase C-α Expression (1996) (166)
The Concise Guide to PHARMACOLOGY 2015/16: Catalytic receptors (2015) (164)
Advances in kinase targeting: current clinical use and clinical trials. (2014) (162)
THE CONCISE GUIDE TO PHARMACOLOGY 2021/22: Enzymes (2021) (161)
Second Generation of Antisense Oligonucleotides: From Nuclease Resistance to Biological Efficacy in Animals (1996) (152)
Protein Kinase C βII Specifically Binds to and Is Activated by F-actin* (1996) (151)
Insulin-stimulated Protein Kinase B Phosphorylation on Ser-473 Is Independent of Its Activity and Occurs through a Staurosporine-insensitive Kinase* (2001) (150)
FGFR3 activates RSK2 to mediate hematopoietic transformation through tyrosine phosphorylation of RSK2 and activation of the MEK/ERK pathway. (2006) (149)
The Concise Guide to Pharmacology 2013/14: Overview (2013) (143)
A public-private partnership to unlock the untargeted kinome. (2013) (142)
A small synthetic peptide, which inhibits the p53-hdm2 interaction, stimulates the p53 pathway in tumour cell lines. (2000) (140)
Inhibition of Protein Kinase c-Src Reduces the Incidence of Breast Cancer Metastases and Increases Survival in Mice: Implications for Therapy (2006) (138)
Biochemical and three-dimensional-structural study of the specific inhibition of protein kinase CK2 by [5-oxo-5,6-dihydroindolo-(1,2-a)quinazolin-7-yl]acetic acid (IQA). (2003) (137)
Sequence-specific antitumor activity of a phosphorothioate oligodeoxyribonucleotide targeted to human C-raf kinase supports an antisense mechanism of action in vivo. (1996) (135)
Biosynthesis and posttranslational modifications of protein kinase C in human breast cancer cells. (1989) (134)
Dual-specific Src and Abl kinase inhibitors, PP1 and CGP76030, inhibit growth and survival of cells expressing imatinib mesylate-resistant Bcr-Abl kinases. (2003) (131)
Targeting cancer with small-molecular-weight kinase inhibitors. (2012) (131)
Expression of four protein kinase C isoforms in rat fibroblasts. Distinct subcellular distribution and regulation by calcium and phorbol esters. (1992) (127)
Classical PKC isoforms in cancer. (2007) (127)
Inhibitors of protein kinases: CGP 41251, a protein kinase inhibitor with potential as an anticancer agent. (1999) (125)
Platelet-derived growth factor and angiotensin II stimulate the mitogen-activated protein kinase cascade in renal mesangial cells: comparison of hypertrophic and hyperplastic agonists. (1995) (121)
Selective ceramide binding to protein kinase C-alpha and -delta isoenzymes in renal mesangial cells. (1998) (120)
The small molecule tyrosine kinase inhibitor AMN107 inhibits TEL-PDGFRbeta and FIP1L1-PDGFRalpha in vitro and in vivo. (2005) (120)
Synthesis and target identification of hymenialdisine analogs. (2004) (116)
Structure-activity relationships in a series of substituted indolocarbazoles: topoisomerase I and protein kinase C inhibition and antitumoral and antimicrobial properties. (1996) (116)
25 Years of Small Molecular Weight Kinase Inhibitors: Potentials and Limitations (2015) (115)
SRC family kinases: potential targets for the treatment of human cancer and leukemia. (2003) (113)
The RET kinase inhibitor NVP-AST487 blocks growth and calcitonin gene expression through distinct mechanisms in medullary thyroid cancer cells. (2007) (111)
Protein kinase C and mammary cell differentiation: involvement of protein kinase C alpha in the induction of beta-casein expression. (1994) (106)
Inhibition of mutant FLT 3 receptors in leukemia cells by the small molecule tyrosine kinase inhibitor PKC 412 (2002) (104)
Beneficial effects of combining nilotinib and imatinib in preclinical models of BCR-ABL+ leukemias. (2007) (101)
Effects of PKC412, nilotinib, and imatinib against GIST-associated PDGFRA mutants with differential imatinib sensitivity. (2006) (100)
EGF induces biphasic S6 kinase activation: Late phase is protein kinase C-dependent and contributes to mitogenicity (1989) (99)
FGFR3 as a therapeutic target of the small molecule inhibitor PKC412 in hematopoietic malignancies (2005) (98)
The Binding Properties and Biological Activities of Bcl-2 and Bax in Cells Exposed to Apoptotic Stimuli* (1998) (97)
5-(4,6-Dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine (PQR309), a Potent, Brain-Penetrant, Orally Bioavailable, Pan-Class I PI3K/mTOR Inhibitor as Clinical Candidate in Oncology. (2017) (96)
Correlation between hormone dependency and the regulation of epidermal growth factor receptor by tumor promoters in human mammary carcinoma cells. (1986) (95)
Alpha-thrombin stimulates nuclear diglyceride levels and differential nuclear localization of protein kinase C isozymes in IIC9 cells. (1992) (94)
Selective in vivo and in vitro effects of a small molecule inhibitor of cyclin-dependent kinase 4. (2001) (93)
NMR reveals the allosteric opening and closing of Abelson tyrosine kinase by ATP-site and myristoyl pocket inhibitors (2013) (92)
Immunological quantitation of phospholipid/CA2+‐dependent protein kinase of human mammary carcinoma cells: Inverse relationship to estrogen receptors (1987) (92)
Binding or bending: distinction of allosteric Abl kinase agonists from antagonists by an NMR-based conformational assay. (2010) (91)
Second-generation antisense oligonucleotides: structure-activity relationships and the design of improved signal-transduction inhibitors. (1996) (91)
Activation of protein kinase C subtypes alpha, gamma, delta, epsilon, zeta, and eta by tumor-promoting and nontumor-promoting agents. (1997) (88)
Hormone- and phorbol ester-activated protein kinase C isozymes mediate a reorganization of the actin cytoskeleton associated with prolactin secretion in GH4C1 cells. (1992) (87)
RET/PTC-induced cell growth is mediated in part by epidermal growth factor receptor (EGFR) activation: evidence for molecular and functional interactions between RET and EGFR. (2008) (87)
FLT3 internal tandem duplication mutations induce myeloproliferative or lymphoid disease in a transgenic mouse model (2005) (85)
Expression of four protein kinase C isoforms in rat fibroblasts. Differential alterations in ras-, src-, and fos-transformed cells. (1992) (83)
Syntheses and biological activities (topoisomerase inhibition and antitumor and antimicrobial properties) of rebeccamycin analogues bearing modified sugar moieties and substituted on the imide nitrogen with a methyl group. (1997) (81)
Possible regulatory functions of protein kinase C-alpha and -epsilon isoenzymes in rat renal mesangial cells. Stimulation of prostaglandin synthesis and feedback inhibition of angiotensin II-stimulated phosphoinositide hydrolysis. (1991) (80)
Synergistic growth-inhibitory effects of two tyrosine kinase inhibitors, dasatinib and PKC412, on neoplastic mast cells expressing the D816V-mutated oncogenic variant of KIT (2007) (79)
Protein tyrosine kinase inhibitors: new treatment modalities? (2002) (79)
THE CONCISE GUIDE TO PHARMACOLOGY 2021/22: Catalytic receptors (2021) (79)
Pyrrolopyrimidine c-Src inhibitors reduce growth, adhesion, motility and invasion of prostate cancer cells in vitro. (2003) (78)
The phosphatidylinositide 3'-kinase/Akt survival pathway is a target for the anticancer and radiosensitizing agent PKC412, an inhibitor of protein kinase C. (2001) (77)
THE CONCISE GUIDE TO PHARMACOLOGY 2021/22: Introduction and Other Protein Targets (2021) (75)
Deconvolution of Buparlisib's mechanism of action defines specific PI3K and tubulin inhibitors for therapeutic intervention (2017) (75)
Reduction of c-Src activity by substituted 5,7-diphenyl-pyrrolo[2,3-d]-pyrimidines induces osteoclast apoptosis in vivo and in vitro. Involvement of ERK1/2 pathway. (2004) (73)
Phenylamino‐Pyrimidine (PAP) Derivatives: A New Class of Potent and Selective Inhibitors of Protein Kinase C (PKC) (1996) (73)
Epidermal growth factor binding and protein kinase C activities in human breast cancer cell lines: possible quantitative relationship. (1986) (72)
Structural insights into the conformational selectivity of STI-571 and related kinase inhibitors. (2004) (71)
PQR309 Is a Novel Dual PI3K/mTOR Inhibitor with Preclinical Antitumor Activity in Lymphomas as a Single Agent and in Combination Therapy (2017) (71)
Different translocation of three distinct PKC isoforms with tumor-promoting phorbol ester in human platelets. (1991) (69)
bcl‐xl antisense treatment induces apoptosis in breast carcinoma cells (2000) (69)
Stable expression of small interfering RNA sensitizes TEL-PDGFbetaR to inhibition with imatinib or rapamycin. (2004) (68)
Targeting protein kinases in cancer therapy. (2002) (66)
7,8-Dichloro-1-oxo-β-carbolines as a Versatile Scaffold for the Development of Potent and Selective Kinase Inhibitors with Unusual Binding Modes (2011) (63)
Selective translocation of protein kinase C-delta in PC12 cells during nerve growth factor-induced neuritogenesis. (1995) (62)
Nitric Oxide Induces Degradation of the Neutral Ceramidase in Rat Renal Mesangial Cells and Is Counterregulated by Protein Kinase C* (2002) (62)
Optimization of a Dibenzodiazepine Hit to a Potent and Selective Allosteric PAK1 Inhibitor. (2015) (62)
Antitumor activity of a PKC-alpha antisense oligonucleotide in combination with standard chemotherapeutic agents against various human tumors transplanted into nude mice. (1998) (61)
Effect of tumour-promoting phorbol ester, thrombin and vasopressin on translocation of three distinct protein kinase C isoforms in human platelets and regulation by calcium. (1992) (60)
Tracing pathway activities with kinase inhibitors and reverse phase protein arrays (2009) (58)
Immunocharacterization of δ‐ and ζ‐isoenzymes of protein kinase C in rat renal mesangial cells (1992) (58)
Differential p53-dependent mechanism of radiosensitization in vitro and in vivo by the protein kinase C-specific inhibitor PKC412. (2001) (58)
Protein kinase C desensitization by phorbol esters and its impact on growth of human breast cancer cells. (1986) (57)
Differential Activation of the Phosphatidylinositol 3′-Kinase/Akt Survival Pathway by Ionizing Radiation in Tumor and Primary Endothelial Cells (2004) (55)
The ceramide kinase inhibitor NVP‐231 inhibits breast and lung cancer cell proliferation by inducing M phase arrest and subsequent cell death (2014) (55)
Protein kinase C in human renal cell carcinomas: role in invasion and differential isoenzyme expression (2000) (55)
Antitumor activity of a C-raf antisense oligonucleotide in combination with standard chemotherapeutic agents against various human tumors transplanted subcutaneously into nude mice. (1997) (55)
Inhibitors of the Abl kinase directed at either the ATP- or myristate-binding site. (2010) (55)
PI3K/mTOR Pathway Inhibition: Opportunities in Oncology and Rare Genetic Diseases (2019) (55)
Effect of Potent and Selective Inhibitors of the Grb2 SH2 Domain on Cell Motility* (1999) (55)
Phosphorylation regulates transcriptional activity of PAX3/FKHR and reveals novel therapeutic possibilities. (2008) (54)
Continuous synthesis of two protein-kinase-C-related proteins after down-regulation by phorbol esters. (1988) (54)
PREDICTIVE VALUE OF EGF RECEPTOR IN BREAST CANCER (1988) (54)
Immunocharacterization of protein kinase C isoenzymes in rat kidney glomeruli, and cultured glomerular epithelial and mesangial cells. (1993) (54)
Discovery and Preclinical Characterization of 5-[4,6-Bis({3-oxa-8-azabicyclo[3.2.1]octan-8-yl})-1,3,5-triazin-2-yl]-4-(difluoromethyl)pyridin-2-amine (PQR620), a Highly Potent and Selective mTORC1/2 Inhibitor for Cancer and Neurological Disorders. (2018) (53)
The protein kinase C inhibitor CGP41251 suppresses cytokine release and extracellular signal-regulated kinase 2 expression in cancer patients. (1999) (52)
Identification and characterization of NVP-BKM 120 , an orally available pan class I PI 3-Kinase inhibitor (2011) (51)
The novel, catalytic mTORC1/2 inhibitor PQR620 and the PI3K/mTORC1/2 inhibitor PQR530 effectively cross the blood-brain barrier and increase seizure threshold in a mouse model of chronic epilepsy (2018) (51)
Structural biology contributions to tyrosine kinase drug discovery. (2009) (50)
The 27,000 daltons stress proteins are phosphorylated by protein kinase C during the tumor promoter-mediated growth inhibition of human mammary carcinoma cells. (1988) (49)
Patupilone Acts as Radiosensitizing Agent in Multidrug-Resistant Cancer Cells In vitro and In vivo (2005) (48)
Targeting protein kinases in cancer therapy: a success? (2004) (46)
Syntheses and biological activities of rebeccamycin analogues. Introduction of a halogenoacetyl substituent. (1999) (46)
Inhibition of growth of human tumor cell lines in nude mice by an antisense of oligonucleotide inhibitor of protein kinase C-alpha expression. (1996) (43)
A novel treatment approach for low grade lymphoproliferative disorders using PKC412 (CGP41251), an inhibitor of protein kinase C. (2002) (42)
Antisense oligonucleotides as inhibitors of signal transduction: development from research tools to therapeutic agents. (1996) (42)
Protein kinase C inhibitor and irradiation-induced apoptosis: relevance of the cytochrome c-mediated caspase-9 death pathway. (2000) (40)
Syntheses and Biological Evaluation of Indolocarbazoles, Analogues of Rebeccamycin, Modified at the Imide Heterocycle (1998) (38)
Protein kinase C down-regulation enhances cAMP-mediated induction of urokinase-type plasminogen activator mRNA in LLC-PK1 cells. (1991) (37)
Chemical and biological profile of dual Cdk1 and Cdk2 inhibitors. (2003) (37)
Selective redistribution of protein kinase C isozymes by thapsigargin and staurosporine. (1992) (37)
( S)-4-(Difluoromethyl)-5-(4-(3-methylmorpholino)-6-morpholino-1,3,5-triazin-2-yl)pyridin-2-amine (PQR530), a Potent, Orally Bioavailable, and Brain-Penetrable Dual Inhibitor of Class I PI3K and mTOR Kinase. (2019) (37)
Inhibitory activity and selectivity of staurosporine derivatives towards protein kinase C (1994) (36)
Effects of tumor promoters on growth and on cellular redistribution of phospholipid/CA2+‐dependent protein kinase in human breast cancer cells (1986) (34)
Inhibition of the growth of glioblastomas by CGP 41251, an inhibitor of protein kinase C, and by a phorbol ester tumor promoter. (1996) (33)
Subcellular distribution of protein kinase C of GH3 cells: quantitation and characterization by polyacrylamide gel electrophoresis. (1985) (31)
New sesquiterpene quinols from a Micronesian sponge, Aka sp. (2003) (31)
Targeting Sphingosine Kinase 1 in Carcinoma Cells Decreases Proliferation and Survival by Compromising PKC Activity and Cytokinesis (2012) (29)
In-vitro antiproliferative activities and kinase inhibitory potencies of glycosyl-isoindigo derivatives (2007) (29)
Ceramide induces translocation of protein kinase C-alpha to the Golgi compartment of human embryonic kidney cells by interacting with the C2 domain. (2003) (28)
Therapeutically targeted anticancer agents: inhibitors of receptor tyrosine kinases. (2004) (27)
Synergistic Growth-Inhibitory Effects of Two Tyrosine Kinase Inhibitors, Dasatinib and PKC412, on Neoplastic Mast Cells Expressing the D816V-Mutated Oncogenic Variant of KIT. (2006) (27)
Syntheses, biochemical and biological evaluation of staurosporine analogues from the microbial metabolite rebeccamycin. (1998) (27)
Synthesis, mode of action, and biological activities of rebeccamycin bromo derivatives. (1999) (27)
In-vitro antiproliferative activities and kinase inhibitory potencies of meridianin derivatives (2008) (27)
Upregulation of the S1P3 receptor in metastatic breast cancer cells increases migration and invasion by induction of PGE2 and EP2/EP4 activation. (2016) (26)
Differential phosphoprofiles of EGF and EGFR kinase inhibitor-treated human tumor cells and mouse xenografts (2004) (24)
Phorbol ester and epidermal growth factor receptors in human breast cancer. (1987) (24)
Synthesis and biological evaluation of diversely substituted indolin-2-ones. (2008) (24)
Preclinical Development of PQR514, a Highly Potent PI3K Inhibitor Bearing a Difluoromethyl–Pyrimidine Moiety (2019) (23)
Regulation of protein kinase C isozymes in kidney regeneration. (1993) (23)
Antisense oligonucleotide inhibitors of isozymes of protein kinase C: in vitro and in vivo activity, and clinical development as anti-cancer therapeutics. (1997) (22)
Differential recovery of protein kinase C-α and -ɛ isozymes after long-term phorbol ester treatment in rat renal mesangial cells (1991) (22)
Kinase inhibition by deoxy analogues of the resorcylic lactone L-783277. (2011) (22)
Effect of hypothyroidism and thyroid hormone replacement on the level of protein kinase C and protein kinase A in rat liver (1991) (21)
Calcium transients in human platelets monitored by aequorin, fura-2 and quin-2: effects of protein kinase C activation and inhibition. (1987) (21)
Comparison of different tumour promoters and bryostatin 1 on protein kinase C activation and down-regulation in rat renal mesangial cells. (1994) (21)
A Conformational Restriction Strategy for the Identification of a Highly Selective Pyrimido-Pyrrolo-Oxazine mTOR Inhibitor. (2019) (20)
Homogeneous purification of human recombinant GST-Akt/PKB from Sf9 cells. (1999) (19)
Discovery of allosteric BCR-ABL inhibitors from phenotypic screen to clinical candidate. (2014) (19)
IL‐8‐mediated angiogenic responses of endothelial cells to lipid antigen activation of iNKT cells depend on EGFR transactivation (2011) (19)
Chemical genetic approach identifies microtubule affinity‐regulating kinase 1 as a leucine‐rich repeat kinase 2 substrate (2015) (19)
Protein kinase C isozyme expression and down-modulation in growing, quiescent, and transformed renal proximal tubule epithelial cells. (1994) (19)
The Phosphodiesterase Inhibitor SQ 20006 Selectively Blocks Mitogen Activation of p70S6k and Transition to S Phase of the Cell Division Cycle without Affecting the Steady State Phosphorylation of eIF-4E (*) (1995) (18)
The cytosolic phorboid receptor correlates with hormone dependency in six mammary carcinoma cell lines. (1985) (18)
Ontogeny of the adenosine-3':5'-phosphate-dependent protein-kinase system during early uterine development. Inverse relationship with the estrogen receptors. (1979) (16)
Altered protein kinase C in a mast cell variant defective in exocytosis. (1987) (16)
Platelet-derived growth factor stimulates de-novo synthesis of mitogen-activated protein kinase in renal mesangial cells. (1995) (16)
Phorbol ester inhibits erythropoietin production in human hepatoma cells (Hep G2). (1992) (16)
Syntheses and biological evaluation of indolocarbazoles, analogues of rebeccamycin, modified at the imide heterocycle. (1998) (15)
Feedback regulation of extracellular ATP-stimulated phosphoinositide hydrolysis by protein kinase C-alpha in bovine glomerular endothelial cells. (1997) (15)
Extended kinase profiling of the Bcr-Abl inhibitor nilotinib (2007) (15)
Overexpression of protein kinase C beta I in a murine keratinocyte cell line produces effects on cellular growth, morphology and differentiation. (1994) (14)
Novel brain permeant mTORC1/2 inhibitors are as efficacious as rapamycin or everolimus in mouse models of acquired partial epilepsy and tuberous sclerosis complex (2020) (14)
The Substrate-Activity-Screening methodology applied to receptor tyrosine kinases: a proof-of-concept study. (2012) (14)
4-(Difluoromethyl)-5-(4-((3R,5S)-3,5-dimethylmorpholino)-6-((R)-3-methylmorpholino)-1,3,5-triazin-2-yl)pyridin-2-amine (PQR626), a Potent, Orally Available, and Brain-Penetrant mTOR Inhibitor for the Treatment of Neurological Disorders. (2020) (13)
Estrogen stimulates growth of mammary tumor cells ZR-75 without activation of S6 kinase and S6 phosphorylation. Difference from epidermal growth factor and alpha-transforming growth-factor-induced proliferation. (1987) (13)
Cyclic AMP-dependent protein kinase type I and type II and cyclic AMP binding in human mammary tumors. (1980) (13)
Protein Tyrosine Kinases as Targets for Cancer and Other Indications (2006) (13)
Corrigendum to “Discovery of NVP-BYL719 a potent and selective phosphatidylinositol-3 kinase alpha inhibitor selected for clinical evaluation” [Bioorg. Med. Chem. Lett. 23 (2013) 3741–3748] (2013) (12)
BCR-ABL signaling: A new STATus in CML. (2012) (12)
The small molecule tyrosine kinase inhibitor AMN 107 inhibits TEL-PDGFR and FIP 1 L 1-PDGFR in vitro and in vivo (2005) (12)
Overexpression of the alpha-type protein kinase (PK) C in LLC-PK1 cells does not lead to a proportional increase in the induction of two 12-O-tetradecanoylphorbol-13-acetate-inducible genes. (1991) (12)
Involvement of protein kinase C in the growth regulation of human breast cancer cells. (1992) (11)
The Novel TORC1/2 Kinase Inhibitor PQR620 Has Anti-Tumor Activity in Lymphomas as a Single Agent and in Combination with Venetoclax (2019) (11)
Expression and partial characterization of rat protein kinase C-delta and protein kinase C-zeta in insect cells using recombinant baculovirus. (1992) (11)
Brain-penetrant PQR620 mTOR and PQR530 PI3K/mTOR inhibitor reduce huntingtin levels in cell models of HD (2020) (10)
Notch Inhibition in Cancer: Challenges and Opportunities. (2020) (10)
Translocation of protein kinase C is not required to inhibit the antigen-induced increase of cytosolic calcium in a mast cell line. (1987) (10)
Advances in Brief Prediction of Resistance to Small Molecule FLT 3 Inhibitors : Implications for Molecularly Targeted Therapy of Acute Leukemia (2004) (10)
Targeted Therapy with Imatinib: An Exception or a Rule? (2005) (9)
Staurosporine stimulates expression of the urokinase‐type (u‐PA) plasminogen activator in LLC‐PK1 cells (1989) (9)
Consequences of the inhibition of Hdm2 expression in human osteosarcoma cells using antisense oligonucleotides. (2000) (9)
Cyclic adenosine monophosphate-dependent protein kinases of human seminal plasma: origin and characteristics of multiple forms. (1982) (8)
Growth-promoting effect of a protein-free hemodialysate used in situations of hypoxia and for tissue repair as measured via stimulation of S6-kinase. (1992) (8)
In vitro cultures of epithelial cells from healthy breast tissues and cells from breast carcinomas. (1989) (8)
Phosphorylation, Signaling, and Cancer: Targets and Targeting (2015) (8)
Hypoxia-induced accumulation of erythropoietin mRNA in isolated hepatocytes is inhibited by protein kinase C (2004) (8)
Tumor-promoting phorbol ester and activated Ha-ras synergistically reduce the interleukin 3 requirement in a mast cell line. (1991) (8)
PKC412, inhibitor of the KIT tyrosine kinase, demonstrates efficacy in mast cell leukemia with the D816V KIT mutation. (2003) (7)
Characterization of kinase inhibitors using reverse phase protein arrays. (2011) (7)
AEE788 (2004) (7)
Unphosphorylated α‐PKC exhibits phorbol ester binding but lacks protein kinase activity in vitro (1993) (7)
The Dawn of Allosteric BCR-ABL1 Drugs: From a Phenotypic Screening Hit to an Approved Drug. (2022) (7)
Progesterone and estrogen receptors in GH3 cells. (1980) (7)
Synergistic growth inhibition mediated by dual PI3K/mTOR pathway targeting and genetic or direct pharmacological AKT inhibition in human glioblastoma models (2020) (7)
Acylated-acyl carrier protein stabilizes the Pseudomonas aeruginosa WaaP lipopolysaccharide heptose kinase (2018) (7)
Book Review: Protein Tyrosine Kinases. from Inhibitors to Useful Drugs (2006) (6)
Synthesis and antimicrobial activities of monoindolyl- and bisindolyloximes (1999) (6)
Author Correction: Trends in kinase drug discovery: targets, indications and inhibitor design (2021) (5)
The lipophilic muramyltripeptide MTP-PE, a biological response modifier, is an activator of protein kinase C. (1986) (5)
The IUPHAR Guide to Immunopharmacology: connecting immunology and pharmacology (2020) (5)
Ribosomal protein S6 kinase and PKC in human mammary tumor cells. (1989) (4)
(S)-4-(Difluoromethyl)-5-(4-(3-methylmorpholino)-6-morpholino-1,3,5-triazin-2-yl)pyridin-2-amine (PQR530), a Potent, Orally Bioavailable, and Brain-Penetrable Dual Inhibitor of Class I PI3K and mTOR Kinase. (2019) (4)
Expression and purification of human recombinant GST-FGF receptor-1. (2001) (4)
Differential recovery of protein kinase C-alpha and -epsilon isozymes after long-term phorbol ester treatment in rat renal mesangial cells. (1991) (4)
Synthesis and biological evaluation of monoindolyl and indolocarbazolyl oxazolones and imidazolones. (1997) (4)
Inhibitors of protein kinases. (2013) (4)
cAMP-dependent protein kinases of rat pituitary GH3 cells. (1985) (4)
Subject Index, Vol. 14, 1981 (1981) (4)
Abstract 4514: PQR309: A potent, brain-penetrant, dual pan-PI3K/mTOR inhibitor with excellent oral bioavailability and tolerability (2015) (4)
Nilotinib, in Comparison to Both Dasatinib and Imatinib, Possesses a Greatly Prolonged Residence Time When Bound to the BCR-ABL Kinase SH1 Domain (2011) (4)
A derivative of staurosporine (CGP 41:251) shows selectivity for PKC inhibition and in vitro antiproliferative effects as well as in vivo antitumor activity. Int. J. Cancer, 43, 851–866 (1989) (1999) (4)
cAMP-dependent protein kinases, their subunits, and cAMP-binding protein from four sources: a comparison of physical characteristics determined by polyacrylamide gel electrophoresis. (1981) (4)
High-Resolution Seminal Plasma Protein Patterns in Normal and Infertile Men (1982) (4)
Abstract 671: BKM120-mediated G2 arrest: Structural and functional segregation of off-target action and PI3K inhibition (2015) (3)
AMD107: Efficacy as a Selective Inhibitor of the Tyrosine Kinase Activity of BCR-ABL in Murine Leukemia Models. (2004) (3)
Abstract 2664: PQR309: Structure-based design, synthesis and biological evaluation of a novel, selective, dual pan-PI3K/mTOR inhibitor (2015) (3)
Role of Protein Kinase C (PKC) in Short‐ and Long‐Term Cellular Responses: Inhibition of Agonist‐Mediated Calcium Transients and Down‐Regulation of PKC (1988) (3)
In vivo activity of AMN107, as selective Bcr-Abl kinase inhibitor, in murine leukemia models (2005) (3)
Immunocharacterization of delta- and zeta-isoenzymes of protein kinase C in rat renal mesangial cells. (1992) (3)
AMN107: Inhibitory profile against non-mutated and mutated forms of the Bcr-Abl tyrosine kinase (2005) (3)
Protein Tyrosine Kinases (2006) (3)
Antisense- and antigene-based drug design strategies in oncology (1998) (2)
Phenylamino-pyrimidine (PAP) Derivatives: A New Class of Potent and Selective Inhibitors of Protein Kinase C (PKC) (1996) (2)
Correlation of estrogen receptors and charge alterations of regulatory subunits of cAMP-dependent protein kinases in human mammary tumor cells. (1984) (2)
Nuclear protein kinases of GH3 cells. (1981) (2)
an Inhibitor of Protein Kinase C Target for the Anticancer and Radiosensitizing Agent PKC 412 ,-Kinase / Akt Survival Pathway Is a ′ The Phosphatidylinositide 3 Updated (2001) (2)
Abstract 159: Pharmacological characterization of the selective, orally bioavailable, potent dual PI3K/mTORC1/2 inhibitor PQR530 (2017) (2)
An ELISA for PDGFR phosphorylation: Comparison of effects of STI571 on cellular Bcr-Abl, c-Kit and PDGFR-β protein kinases (2004) (2)
The PKC inhibitor CGP 41251 reverses P-gp mediated multidrug resistance and synergizes with adriamycin: 64 (1994) (2)
Abstract 140: Discovery and biological evaluation of PQR530, a highly potent dual pan-PI3K/mTORC1/2 inhibitor (2017) (2)
CONTRIBUTIONS TO THE DISCOVERY OF DRUGS TO TREAT CHRONIC MYELOGENOUS LEUKEMIA (2)
Chemical and Biological Profile of Dual Cdk 1 and Cdk 2 Inhibitors (2011) (2)
The Dual PI3K/mTOR Inhibitor PQR309 Has Synergistic Activity with Other Targeted Agents in Diffuse Large B Cell Lymphomas (2015) (2)
Zonal gene expression in human colon assessed by laser microdissection (LMD) and quantitative real-time RT-PCR (2001) (2)
Pharmacological profile of the FLT3-Tyrosine Kinase Inhibitor AST487 (2005) (1)
Cyclic AMP-dependent protein kinases in semen from men with subnormal sperm motility or morphology (1983) (1)
The Novel PI3K/mTOR Dual Inhibitor PQR309 in Pre-Clinical Lymphoma Models: Demonstration of Anti-Tumor Activity As Single Agent and in Combination and Identification of Gene Expression Signatures Associated with Response (2014) (1)
PKC412 Effectively Inhibits Constitutively Activated FGFR3 Mutants in Murine Leukemia Models and t(4;14) Myeloma Cell Lines. (2004) (1)
Abstract 1922: 2-Aminothiazoles as potent and selective PI3Kalpha inhibitors: Discovery of NVP-BYL719 and structural basis for the isoform selectivity (2012) (1)
Abstract 378: Exploring intermittent dosing schedules for the Pan PI3K/mTor inhibitor PQR309 (2016) (1)
Unphosphorylated alpha-PKC exhibits phorbol ester binding but lacks protein kinase activity in vitro. (1993) (1)
Substrate profiling of IGF-1R and InsR: identification of a potent pentamer substrate. (2011) (1)
Cancer Biology and the Principles of Targeted Cancer Drug Discovery (2017) (1)
Abstract 2652: Pre-clinical activity and mechanism of action of the novel dual PI3K/mTOR inhibitor PQR309 in B-cell lymphomas (2015) (1)
Synthesis and Antimicrobial Activities of Monoindolyl- and Bisindolyloximes. (1999) (1)
Antisense oligonucleotides and their anticancer activities (1998) (1)
Epidermal Growth Factor Receptor and Calcium/Phospholipid-Dependent Protein Kinase Activities in Human Mammary Tumor Cells1 (1986) (1)
Phosphorylation of cAMP-dependent protein kinases in normal and abnormal human sperm. (1984) (1)
Inhibitors of Protein Kinases and Protein Phosphates Contributors (2005) (1)
The novel mTORC1/2 inhibitor PQR620 has in vitro and in vivo activity in lymphomas (2016) (1)
Abstract 1336: Structure-activity relationship studies, synthesis, and biological evaluation of PQR620, a highly potent and selective mTORC1/2 inhibitor (2016) (1)
8th International Conference on Inhibitors of Protein Kinases (IPK '2014). (2015) (1)
PKC412 Inhibits In Vitro Growth of Neoplastic Mast Cells Expressing the D816V-Mutated Variant of KIT: Comparison with AMN107 and Imatinib, and Evaluation of Drug-Interactions. (2005) (1)
Fingolimod (FTY720) Inhibits BCR-ABL Signaling Allosterically by Binding to the Myristate Binding Site (2011) (1)
Abstract 393A: Pharmacological characterization of the selective, orally bioavailable, potent mTORC1/2 inhibitor PQR620 (2016) (1)
Abl kinase domain in complex with NVP-AEG082 (2007) (0)
Targeting the PI3K/mTOR Pathway in Lymphoma with PQR309 and PQR620: Single Agent Activity and Synergism with the BCL2 Inhibitor Venetoclax (2016) (0)
Author Correction: Acylated-acyl carrier protein stabilizes the Pseudomonas aeruginosa WaaP lipopolysaccharide heptose kinase (2018) (0)
Abstract A117: An integrated phosphoproteomic approach to dissect the mechanism of action of the novel dual PI3K/mTOR inhibitor PQR309 in B-cell lymphomas (2015) (0)
Human Abl kinase domain in complex with imatinib (STI571, Glivec) (2007) (0)
Regulation of ribosomal protein S6 kinase in human mammary tumor cells: Effect of estrogen, growth factors and phorbol ester (1988) (0)
Endocrine therapy of breast cancer : experimental and clinical aspects (1986) (0)
Medullary Thyroid Cancer Cells inCalcitonin Gene Expression through Distinct Mechanisms The RET Kinase Inhibitor NVP-AST 487 Blocks Growth and Updated (2007) (0)
Author Correction: Acylated-acyl carrier protein stabilizes the Pseudomonas aeruginosa WaaP lipopolysaccharide heptose kinase (2018) (0)
P11.45 Synergistic growth inhibition mediated by dual PI3K/mTOR pathway targeting and genetic or direct pharmacological AKT inhibition in human glioblastoma models (2019) (0)
PNAS Plus Significance Statements (2013) (0)
Cell Line Synergistically Reduce the Interleukin 3 Requirement in a Mast ras Tumor-promoting Phorbol Ester and Activated Ha-Updated (2006) (0)
PQR309, idelalisib, duvelisib and ibrutinib lead to similar gene expression changes in activated B-cell like (ABC) diffuse large B-cell lymphoma (DLBCL) (2016) (0)
Title Page / Contents / Sponsors of the Conference / Foreword (1986) (0)
Abstract #3715: The inhibition of ABL kinase activity by nilotinib and imatinib, but not dasatinib, is time-dependent (2009) (0)
Book Review: Immunotherapy of Cancer (2006) (0)
L10 Two novel mtor and PI3K/mTOR inhibitors induce autophagy and reduce the amount of aggregated mutant huntingtin in cell models of HD (2016) (0)
653 Optimization of novel antiangiogenic treatment modalities in combination with ionizing radiation (2004) (0)
Cyclic AMP-dependent protein kinases in semen from men with subnormal sperm motility or morphology. (1984) (0)
Identification and validation of MARK1 as a LRRK2 substrate (2014) (0)
L 3 Differences in the kinase binding modes of imatinib , nilotinib and dasatinib are reflected in Abl transphosphorylation assays (2009) (0)
A cell-based screening strategy predicts Bcr-Abl mutations that cause resistance toward the second-generation Abl kinase inhibitor AMN107 (2005) (0)
Correction: Targeting Sphingosine Kinase 1 in Carcinoma Cells Decreases Proliferation and Survival by Compromising PKC Activity and Cytokinesis (2013) (0)
The International Union of Basic and Clinical Pharmacology Committee on Receptor Nomenclature and Drug Classification (NC-IUPHAR): Relevance to pharmacology today and challenges for the future (2018) (0)
Human ABL kinase in complex with nilotinib (2008) (0)
Strategies toward identification of novel and selective protein kinase inhibitors (1998) (0)
Expression of protein kinase C isoenzymes and correlation with tumor invasiveness in vitro (2007) (0)
73 Tailoring molecular radiosensitizers (2006) (0)
7.01 – Cancer Biology (2007) (0)
Inhibition of the NPM-ALK Fusion Tyrosine Kinase in Hematopoietic Neoplasia by the Small Molecule Tyrosine Kinase Antagonist TAE684. (2006) (0)
Abl kinase domain unligated and in complex with tetrahydrostaurosporine (2007) (0)
Contents, Vol. 14, 1981 (1981) (0)
Abstract 382: Concomitant administration of acid reducing agents can impact the pharmacokinetics of the balanced pan-PI3K and mTOR inhibitor PQR309 (2016) (0)
Characterization of a novel, small molecular weight IGFI-R inhibitor (2005) (0)
Pyrimidylaminobenzamide derivatives for use in the treatment of a myeloproliferative disease induced by TEL-PDGFR-beta (2006) (0)
Author errata. (1999) (0)
CSIG-26. MOLECULAR DETERMINANTS OF SENSITIVITY TO PI3K/AKT/mTOR PATHWAY INHIBITION IN GLIOBLASTOMA (2018) (0)
Lipids as Targets for Renal Cell Carcinoma Therapy (2023) (0)
Protein kinase inhibitors as antileukemic agents (2003) (0)
PKC412 Inhibits the ZNF198-FGFR1 Fusion Tyrosine Kinase and Is Efficacious in Treatment of t(8;13)(p11;q12) Associated Stem Cell Myeloproliferative Disease. (2004) (0)
Inhibition of Cell Growth by Antisense Oligonucleotides Targeting the Growth-Related Protein Kinase c-raf. (2000) (0)
537 Multidrug-resistant tumors treated with Epothilone B in combination with clinically relevant doses of ionizing radiation (2004) (0)
Use of protein kinase inhibitors to dissect the regulation of protein kinase B [PKB-Akt] by upstream kinases (2001) (0)
STI571 (IMATINIB): structural and enzymatic studies of interactions with ABL kinase and resistance mutants (2002) (0)
Contents, Vol. 12, 1980 (1980) (0)
Abstract 665: Discovery and preclinical characterization of PQR626: A potent, orally available, and brain-penetrant mTOR inhibitor for the treatment of tuberous sclerosis complex (2020) (0)
Subject Index, Vol. 12, 1980 (1980) (0)
Inhibitors of cyclin dependent protein kinases (1998) (0)
Correlation between steroid receptors estrogen receptor and progesterone receptor and epidermal growth factor receptor in human mammary breast cancer (1986) (0)
Abstract B041: PQR309-containing combinations show synergistic antilymphoma activity (2018) (0)
Structure of unphosphorylated c-Src in complex with an inhibitor (2005) (0)
Abstract 153: Tricyclic fused pyrimidinopyrrolo-oxazines reveal conformational preferences of morpholine for PI3K hinge region binding (2017) (0)
IUBMB focused meeting: 10thconference Inhibitors of Protein Kinases. Kinase inhibitors in target biology and disease (IPK2019) (2020) (0)
Protein Kinase C Inhibitor and Irradiation-induced Apoptosis : Relevance of the Cytochrome c-mediated Caspase-9 Death Pathway 1 (2000) (0)
Early preclinical development of PQR309, a novel balanced dual PI3K/mTOR inhibitor for treatment of various cancer types (2015) (0)
Abstract 380: The dual PI3K/MTOR inhibitor PQR309 is active in mature B cell lymphoma cell lines bearing resistance to the PI3K-delta inhibitor idelalisib and specific gene expression features (2016) (0)
Improvement of breast cancer metastasis-free survlval by anti c-Src therapy (2006) (0)
The modulation of multidrug resistance by CGP41251 in B-chronic lymphocytic leukaemia cells in vitro. (1997) (0)
Abl kinase domain in complex with PD180970 (2007) (0)
The modulation of multidrug resistance and induction of apoptotic cell death by a PKC inhibitor CGP41251 in B-CLL cells in vitro (1997) (0)
Preface [Hot topic: New Insights in Protein Kinase Inhibitors: Chemogenomics, Phosphoproteomics, Structural Based Approaches and the Emergence of Resistance Executive Editor: Doriano Fabbro ] (2004) (0)
Cooperative in vivo cytotoxicity of ionizing radiation and the protein kinase C-inhibitor PKC412 in p53-deficient, radioresistant tumor cells (1999) (0)
Author Correction: Trends in kinase drug discovery: targets, indications and inhibitor design (2021) (0)
Different translocation and calcium dependence of protein kinase C isoforms induced by phorbol ester in human platelets (1991) (0)
Acylated-acyl carrier protein stabilizes the Pseudomonas aeruginosa WaaP lipopolysaccharide heptose kinase (2018) (0)

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