James T. Dalton

Q: What Schools Are Affiliated With James T. Dalton

James T. Dalton is affiliated with the following schools: University of Alabama, University of Cincinnati, University of California, Berkeley, Ohio State University, University of Michigan, University of Tennessee, Stanford University, Baylor College of Medicine, University of Toronto, University of California, San Francisco, University of Tennessee Health Science Center

James T. Dalton's AcademicInfluence.com Rankings

James T. Dalton

Chemistry

#4470

World Rank

#5553

Historical Rank

Organic Chemistry

#936

World Rank

#1049

Historical Rank

chemistry Degrees

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Chemistry

James T. Dalton's Degrees

PhD Pharmaceutical Sciences University of California, San Francisco
Masters Chemistry Stanford University
Bachelors Chemistry University of California, Berkeley

Why Is James T. Dalton Influential?

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According to Wikipedia, James Tilmon Dalton is an American pharmacist and drug discovery scientist. He is Executive Vice President & Provost at the University of Alabama. Career As a pharmacy intern and then pharmacist, Dalton worked at Kettering Medical Center. After earning his PhD, Dalton was appointed as assistant professor in the Department of Pharmaceutical Sciences at the University of Tennessee. As a professor at the University of Tennessee, Dalton led the research group that first reported selective androgen receptor modulators . In 1997, Dalton’s group published the first report on SARMs, which was used to research and create a class of potential drugs to treat age and disease-related muscle loss. Dalton also led the research group that invented sabizabulin, a tubulin inhibitor under development for the treatment of cancer and SARS-CoV-2 .

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James T. Dalton'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

Flavopiridol administered using a pharmacologically derived schedule is associated with marked clinical efficacy in refractory, genetically high-risk chronic lymphocytic leukemia. (2007) (404)
Chemistry and structural biology of androgen receptor. (2005) (380)
Structural basis for antagonism and resistance of bicalutamide in prostate cancer (2005) (371)
Effects of enobosarm on muscle wasting and physical function in patients with cancer: a double-blind, randomised controlled phase 2 trial. (2013) (371)
The selective androgen receptor modulator GTx-024 (enobosarm) improves lean body mass and physical function in healthy elderly men and postmenopausal women: results of a double-blind, placebo-controlled phase II trial (2011) (294)
Muscle wasting in cancer cachexia: clinical implications, diagnosis, and emerging treatment strategies. (2011) (291)
Drug Insight: testosterone and selective androgen receptor modulators as anabolic therapies for chronic illness and aging (2006) (291)
Selective androgen receptor modulators in preclinical and clinical development (2008) (233)
Discovery of nonsteroidal androgens. (1998) (198)
Nonsteroidal selective androgen receptor modulators (SARMs): dissociating the anabolic and androgenic activities of the androgen receptor for therapeutic benefit. (2009) (192)
Favorable effects of weak acids on negative-ion electrospray ionization mass spectrometry. (2004) (186)
Expanding the therapeutic use of androgens via selective androgen receptor modulators (SARMs). (2007) (183)
Pharmacokinetics of chlorpheniramine, phenytoin, glipizide and nifedipine in an individual homozygous for the CYP2C9*3 allele. (1999) (179)
Structural Basis for Accommodation of Nonsteroidal Ligands in the Androgen Receptor* (2005) (179)
Clinical response and pharmacokinetics from a phase 1 study of an active dosing schedule of flavopiridol in relapsed chronic lymphocytic leukemia. (2009) (170)
Selective androgen receptor modulator treatment improves muscle strength and body composition and prevents bone loss in orchidectomized rats. (2005) (166)
FTY720 demonstrates promising preclinical activity for chronic lymphocytic leukemia and lymphoblastic leukemia/lymphoma. (2008) (158)
Discovery of 4-substituted methoxybenzoyl-aryl-thiazole as novel anticancer agents: synthesis, biological evaluation, and structure-activity relationships. (2009) (157)
Pharmacodynamics of Selective Androgen Receptor Modulators (2003) (146)
Development of selective androgen receptor modulators (SARMs) (2017) (137)
Design, synthesis, and biological characterization of metabolically stable selective androgen receptor modulators. (2004) (127)
Synthesis and antiproliferative activity of 2-aryl-4-oxo-thiazolidin-3-yl-amides for prostate cancer. (2004) (122)
Discovery and therapeutic promise of selective androgen receptor modulators. (2005) (121)
Structural Determinants of P-Glycoprotein-Mediated Transport of Glucocorticoids (2003) (120)
Study Design and Rationale for the Phase 3 Clinical Development Program of Enobosarm, a Selective Androgen Receptor Modulator, for the Prevention and Treatment of Muscle Wasting in Cancer Patients (POWER Trials) (2016) (120)
Key structural features of nonsteroidal ligands for binding and activation of the androgen receptor. (2003) (108)
Discovery of novel 2-aryl-4-benzoyl-imidazoles targeting the colchicines binding site in tubulin as potential anticancer agents. (2010) (108)
Crystal Structure of the T877A Human Androgen Receptor Ligand-binding Domain Complexed to Cyproterone Acetate Provides Insight for Ligand-induced Conformational Changes and Structure-based Drug Design* (2007) (107)
Estrogen Receptor-β-selective Ligands Alleviate High-fat Diet- and Ovariectomy-induced Obesity in Mice (2010) (105)
Comparison of the pharmacological effects of a novel selective androgen receptor modulator, the 5alpha-reductase inhibitor finasteride, and the antiandrogen hydroxyflutamide in intact rats: new approach for benign prostate hyperplasia. (2004) (103)
Pharmacokinetics of intravesical mitomycin C in superficial bladder cancer patients. (1991) (101)
Steroidogenic Enzyme AKR1C3 Is a Novel Androgen Receptor-Selective Coactivator that Promotes Prostate Cancer Growth (2013) (98)
Selective Androgen Receptor Modulator (SARM) Treatment Prevents Bone Loss and Reduces Body Fat in Ovariectomized Rats (2007) (98)
Discovery of antiandrogen activity of nonsteroidal scaffolds of marketed drugs (2007) (97)
TMPRSS2:ERG gene fusion predicts subsequent detection of prostate cancer in patients with high-grade prostatic intraepithelial neoplasia. (2014) (96)
Mdr1 limits CYP3A metabolism in vivo. (2000) (93)
Design, synthesis, and SAR studies of 4-substituted methoxylbenzoyl-aryl-thiazoles analogues as potent and orally bioavailable anticancer agents. (2011) (92)
Pharmacokinetics and Pharmacodynamics of Nonsteroidal Androgen Receptor Ligands (2006) (91)
Bladder wall penetration of intravesical mitomycin C in dogs. (1991) (91)
Discovery of 2-arylthiazolidine-4-carboxylic acid amides as a new class of cytotoxic agents for prostate cancer. (2005) (90)
Homology modeling using multiple molecular dynamics simulations and docking studies of the human androgen receptor ligand binding domain bound to testosterone and nonsteroidal ligands. (2001) (84)
Chemistry and Structural Biology of Androgen Receptor (2005) (82)
Discovery of novel 2-aryl-4-benzoyl-imidazole (ABI-III) analogues targeting tubulin polymerization as antiproliferative agents. (2012) (80)
Design, Synthesis, and Biological Evaluation of Stable Colchicine Binding Site Tubulin Inhibitors as Potential Anticancer Agents (2014) (79)
Enantioselective binding of Casodex to the androgen receptor. (1996) (77)
A Selective Androgen Receptor Modulator for Hormonal Male Contraception (2005) (77)
A ligand-based approach to identify quantitative structure-activity relationships for the androgen receptor. (2004) (72)
The Para Substituent of S-3-(Phenoxy)-2-hydroxy-2-methyl-N-(4-nitro-3-trifluoromethyl-phenyl)-propionamides Is a Major Structural Determinant of in Vivo Disposition and Activity of Selective Androgen Receptor Modulators (2005) (71)
Steroidal androgens and nonsteroidal, tissue-selective androgen receptor modulator, S-22, regulate androgen receptor function through distinct genomic and nongenomic signaling pathways. (2008) (68)
Clinical pharmacokinetics of 5-aminolevulinic acid in healthy volunteers and patients at high risk for recurrent bladder cancer. (2002) (67)
A Potent, Metabolically Stable Tubulin Inhibitor Targets the Colchicine Binding Site and Overcomes Taxane Resistance. (2018) (64)
Novel nonsteroidal ligands with high binding affinity and potent functional activity for the androgen receptor. (2002) (64)
Synthesis and antiproliferative activity of thiazolidine analogs for melanoma. (2007) (63)
Selective androgen receptor modulators for the prevention and treatment of muscle wasting associated with cancer (2013) (62)
Effects of a novel selective androgen receptor modulator on dexamethasone-induced and hypogonadism-induced muscle atrophy. (2010) (61)
Phosphatase and tensin homologue deleted on chromosome ten (PTEN) as a molecular target in lung epithelial wound repair (2007) (60)
Estrogen regulates histone deacetylases to prevent cardiac hypertrophy (2013) (58)
Synthesis and antiproliferative activity of novel 2-aryl-4-benzoyl-imidazole derivatives targeting tubulin polymerization. (2011) (58)
FTY720 Shows Promising In vitro and In vivo Preclinical Activity by Downmodulating Cyclin D1 and Phospho-Akt in Mantle Cell Lymphoma (2010) (57)
MicroRNAs Are Mediators of Androgen Action in Prostate and Muscle (2010) (56)
Discovery of 4-Aryl-2-benzoyl-imidazoles as tubulin polymerization inhibitor with potent antiproliferative properties. (2013) (55)
Chiral nonsteroidal affinity ligands for the androgen receptor. 1. Bicalutamide analogues bearing electrophilic groups in the B aromatic ring. (2000) (53)
Preclinical characterization of a (S)-N-(4-cyano-3-trifluoromethyl-phenyl)-3-(3-fluoro, 4-chlorophenoxy)-2-hydroxy-2-methyl-propanamide: a selective androgen receptor modulator for hormonal male contraception. (2009) (53)
Selective Androgen Receptor Modulators (SARMs) Negatively Regulate Triple-Negative Breast Cancer Growth and Epithelial:Mesenchymal Stem Cell Signaling (2014) (53)
Flavopiridol Pharmacogenetics: Clinical and Functional Evidence for the Role of SLCO1B1/OATP1B1 in Flavopiridol Disposition (2010) (52)
Pharmacology, Pharmacokinetics, and Metabolism of Acetothiolutamide, a Novel Nonsteroidal Agonist for the Androgen Receptor (2003) (51)
Use of Intravenous Valproate in Three Pediatric Patients with Nonconvulsive or Convulsive Status Epilepticus (1999) (49)
17-β estradiol protects ARPE-19 cells from oxidative stress through estrogen receptor-β. (2010) (48)
Androgen Receptor: A Complex Therapeutic Target for Breast Cancer (2016) (48)
Novel Tubulin Polymerization Inhibitors Overcome Multidrug Resistance and Reduce Melanoma Lung Metastasis (2012) (47)
Therapeutic potential of the SARMs: revisiting the androgen receptor for drug discovery (2006) (46)
Synthesis and antiproliferative activity of imidazole and imidazoline analogs for melanoma. (2008) (45)
A novel liposomal formulation of flavopiridol. (2009) (44)
Effect of B-ring substitution pattern on binding mode of propionamide selective androgen receptor modulators. (2008) (43)
Role of Nuclear Receptors in Lipid Dysfunction and Obesity-Related Diseases (2013) (41)
Combination bortezomib and rituximab treatment affects multiple survival and death pathways to promote apoptosis in mantle cell lymphoma (2009) (40)
Ockham's razor and selective androgen receptor modulators (SARMs): are we overlooking the role of 5alpha-reductase? (2007) (40)
Pharmacokinetics of S-3-(4-acetylamino-phenoxy)-2-hydroxy-2-methyl-N-(4-nitro- 3-trifluoromethyl-phenyl)-propionamide in rats, a non-steroidal selective androgen receptor modulator (2004) (39)
Mass spectrometric characterization of urinary metabolites of the selective androgen receptor modulator S-22 to identify potential targets for routine doping controls. (2011) (39)
Creation of Polarized Cells Coexpressing CYP3A4, NADPH Cytochrome P450 Reductase and MDR1/P-glycoprotein (2004) (38)
Unexpected binding orientation of bulky-B-ring anti-androgens and implications for future drug targets. (2011) (36)
Novel Selective Agents for the Degradation of Androgen Receptor Variants to Treat Castration-Resistant Prostate Cancer. (2017) (35)
Characterization of in vitro generated metabolites of the selective androgen receptor modulators S-22 and S-23 and in vivo comparison to post-administration canine urine specimens. (2010) (35)
Population Pharmacokinetics of Humanized Monoclonal Antibody HuCC49ΔCH2 and Murine Antibody CC49 in Colorectal Cancer Patients (2007) (35)
Synthesis, in vitro structure-activity relationship, and in vivo studies of 2-arylthiazolidine-4-carboxylic acid amides as anticancer agents. (2010) (34)
Biological activity of 4-substituted methoxybenzoyl-aryl-thiazole: an active microtubule inhibitor. (2011) (34)
Identification of a novel phosphorylation site in human androgen receptor by mass spectrometry. (2001) (34)
A phase I/II dose escalation study of apolizumab (Hu1D10) using a stepped-up dosing schedule in patients with chronic lymphocytic leukemia and acute leukemia (2009) (33)
Pharmacologic activation of estrogen receptor α increases mitochondrial function, energy expenditure, and brown adipose tissue (2017) (33)
Comparative lipoprotein metabolism of myristate, palmitate, and stearate in normolipidemic men. (1996) (33)
ERβ selective agonist inhibits angiotensin-induced cardiovascular pathology in female mice. (2013) (32)
CHARACTERIZATION OF THE IN VITRO METABOLISM OF SELECTIVE ANDROGEN RECEPTOR MODULATOR USING HUMAN, RAT, AND DOG LIVER ENZYME PREPARATIONS (2005) (32)
PHARMACOKINETICS AND METABOLISM OF A SELECTIVE ANDROGEN RECEPTOR MODULATOR IN RATS: IMPLICATION OF MOLECULAR PROPERTIES AND INTENSIVE METABOLIC PROFILE TO INVESTIGATE IDEAL PHARMACOKINETIC CHARACTERISTICS OF A PROPANAMIDE IN PRECLINICAL STUDY (2006) (32)
Development and Validation of a Highly Sensitive Liquid Chromatography/Mass Spectrometry Method for Simultaneous Quantification of Lenalidomide and Flavopiridol in Human Plasma (2008) (32)
Pharmacokinetic Optimization of 4-Substituted Methoxybenzoyl-aryl-thiazole and 2-Aryl-4-benzoyl-imidazole for Improving Oral Bioavailability (2011) (31)
Tip110, the Human Immunodeficiency Virus Type 1 (HIV-1) Tat-interacting Protein of 110 kDa as a Negative Regulator of Androgen Receptor (AR) Transcriptional Activation* (2004) (31)
Pharmacokinetics of aminolevulinic acid after oral and intravenous administration in dogs. (1999) (30)
Arylisothiocyanato selective androgen receptor modulators (SARMs) for prostate cancer. (2006) (29)
Affinity labeling of the androgen receptor with nonsteroidal chemoaffinity ligands. (1999) (28)
Androgen receptor antagonists: a patent review (2008 – 2011) (2012) (28)
A novel rhodamine-riboflavin conjugate probe exhibits distinct fluorescence resonance energy transfer that enables riboflavin trafficking and subcellular localization studies. (2004) (27)
Predictive Ability of Level A in Vitro-in Vivo Correlation for RingCap Controlled-Release Acetaminophen Tablets (2001) (26)
Nonsteroidal Selective Androgen Receptor Modulators Enhance Female Sexual Motivation (2010) (26)
Effects of Selective Androgen Receptor Modulator (SARM) Treatment in Osteopenic Female Rats (2009) (26)
Selective androgen receptor modulators as improved androgen therapy for advanced breast cancer (2014) (26)
Cancer cachexia therapy: a key weapon in the fight against cancer (2011) (26)
Enobosarm: A targeted therapy for metastatic, androgen receptor positive, breast cancer. (2014) (25)
Estrogen receptor β selective nonsteroidal estrogens: seeking clinical indications (2010) (25)
Structure-activity relationship studies of arylthiazolidine amides as selective cytotoxic agents for melanoma. (2007) (25)
Toremifene – a promising therapy for the prevention of prostate cancer and complications of androgen deprivation therapy (2006) (25)
Discovery and mechanistic characterization of a novel selective nuclear androgen receptor exporter for the treatment of prostate cancer. (2010) (24)
Competitive mass spectrometry binding assay for characterization of three binding sites of tubulin. (2010) (23)
Antikinetoplastid antimitotic activity and metabolic stability of dinitroaniline sulfonamides and benzamides. (2006) (23)
A novel bis-indole destabilizes microtubules and displays potent in vitro and in vivo antitumor activity in prostate cancer (2011) (22)
Discovery and Preclinical Characterization of Novel Small Molecule TRK and ROS1 Tyrosine Kinase Inhibitors for the Treatment of Cancer and Inflammation (2013) (21)
Domain Structure and DNA Binding Regions of β Protein from Bacteriophage λ* (2006) (21)
SAR studies of 2-arylthiazolidine-4-carboxylic acid amides: a novel class of cytotoxic agents for prostate cancer. (2005) (21)
Synthesis of novel iodo derived bicalutamide analogs (2004) (21)
Flavopiridol Administered as a Pharmacologically-Derived Schedule Demonstrates Marked Clinical Activity in Refractory, Genetically High Risk, Chronic Lymphocytic Leukemia (CLL). (2004) (21)
In Vivo Metabolism and Final Disposition of a Novel Nonsteroidal Androgen in Rats and Dogs (2006) (21)
Hydroxysteroid Dehydrogenase (17β -HSD3, 17β-HSD5, and 3α-HSD3) Inhibitors:Extragonadal Regulation of Intracellular Sex Steroid Hormone Levels (2007) (21)
Inhibitors of Tubulin Assembly Identified through Screening a Compound Library (2008) (20)
In vitro and in vivo structure-activity relationships of novel androgen receptor ligands with multiple substituents in the B-ring. (2005) (20)
A Method to Study Drug Concentration–Depth Profiles in Tissues: Mitomycin C in Dog Bladder Wall (1991) (19)
Selective androgen receptor modulators (2003) (19)
Time‐Variant Increase in Methylprednisolone Clearance in Patients with Acute Respiratory Distress Syndrome: A Population Pharmacokinetic Study (2001) (19)
Selective androgen receptor modulators for the treatment of late onset male hypogonadism (2014) (19)
Evidence of significant absorption of sodium salicylate from urinary bladder of rats. (1991) (18)
Ostarine increases lean body mass and improves physical performance in healthy elderly subjects: Implications for cancer cachexia patients (2007) (18)
INTERSPECIES DIFFERENCES IN PHARMACOKINETICS AND METABOLISM OF S-3-(4-ACETYLAMINO-PHENOXY)-2-HYDROXY-2-METHYL-N-(4-NITRO-3-TRIFLUOROMETHYLPHENYL)-PROPIONAMIDE: THE ROLE OF N-ACETYLTRANSFERASE (2006) (18)
Pharmacokinetic drug interactions of the selective androgen receptor modulator GTx-024(Enobosarm) with itraconazole, rifampin, probenecid, celecoxib and rosuvastatin (2016) (18)
Medetomidine analogs as alpha 2-adrenergic ligands. 3. Synthesis and biological evaluation of a new series of medetomidine analogs and their potential binding interactions with alpha 2-adrenoceptors involving a "methyl pocket". (1997) (17)
Apoptosis induced by novel aldehyde calpain inhibitors in human tumor cell lines. (2006) (17)
Synthesis and biological evaluation of novel cytotoxic phospholipids for prostate cancer. (2004) (17)
Selective estrogen receptor alpha agonist GTx-758 decreases testosterone with reduced side effects of androgen deprivation therapy in men with advanced prostate cancer. (2015) (16)
Orally Bioavailable Tubulin Antagonists for Paclitaxel-Refractory Cancer (2012) (16)
I-387, a Novel Antimitotic Indole, Displays a Potent In vitro and In vivo Antitumor Activity with Less Neurotoxicity (2010) (16)
Synthesis of irreversibly binding bicalutamide analogs for imaging studies. (2005) (15)
The long and winding road for selective androgen receptor modulators. (2017) (15)
Development and validation of a sensitive liquid chromatography/mass spectrometry method for quantitation of flavopiridol in plasma enables accurate estimation of pharmacokinetic parameters with a clinically active dosing schedule. (2008) (15)
Drug Metabolism and Pharmacokinetics of 4-Substituted Methoxybenzoyl-aryl-thiazoles (2010) (14)
Pharmacologically derived schedule of flavopiridol has significant efficacy in refractory, genetically high risk chronic lymphocytic leukemia (CLL). (2006) (14)
Pre-systemic metabolism prevents in vivo antikinetoplastid activity of N1,N4-substituted 3,5-dinitro sulfanilamide, GB-II-150. (2006) (14)
Cytochrome P-450 2C9 Sensitizes Human Prostate Tumor Cells to Cyclophosphamide via a Bystander Effect (2000) (14)
Synthesis, calpain inhibitory activity, and cytotoxicity of P2-substituted proline and thiaproline peptidyl aldehydes and peptidyl alpha-ketoamides. (2006) (14)
Role and pharmacologic significance of cytochrome P‐450 2D6 in oxidative metabolism of toremifene and tamoxifen (2013) (14)
β-LGND2, an ERβ selective agonist, inhibits pathologic retinal neovascularization. (2012) (13)
Structure determination of chiral sulfoxide in diastereomeric bicalutamide derivatives. (2009) (13)
High-performance liquid chromatographic determination of mitomycin C in rat and human plasma and urine. (1989) (12)
Enobosarm and lean body mass in patients with non-small cell lung cancer. (2014) (12)
Absorption, distribution, metabolism and excretion of the novel SARM GTx-024 [(S)-N-(4-cyano-3-(trifluoromethyl)phenyl)-3-(4-cyanophenoxy)-2-hydroxy-2-methylpropanamide] in rats (2013) (12)
Molecular Target Characterization and Antimyeloma Activity of the Novel, Insulin-like Growth Factor 1 Receptor Inhibitor, GTx-134 (2011) (11)
Nonsteroidal Tissue‐Selective Androgen Receptor Modulators (2008) (11)
Efficient Microwave‐Enhanced Synthesis of 4‐Thiazolidinones. (2005) (11)
Comparison of high-dose intermittent and low-dose continuous oral artemisinin in dogs with naturally occurring tumors. (2014) (11)
Cesium fluoride and tetra-n-butylammonium fluoride mediated 1,4-N-->O shift of disubstituted phenyl ring of a bicalutamide derivative. (2006) (11)
Selective androgen receptor modulators activate the canonical prostate cancer androgen receptor program and repress cancer growth. (2021) (11)
Pharmacologic activation of estrogen receptor α increases mitochondrial function, energy expenditure, and brown adipose tissue. (2017) (11)
Efficient microwave enhanced synthesis of 4-thiazolidinones (2004) (11)
Alanine Aminotransferase Regulation by Androgens in Non-hepatic Tissues (2012) (10)
Recombinant expression and purification of human androgen receptor in a baculovirus system. (2001) (10)
Preclinical Pharmacology of a Nonsteroidal Ligand for Androgen Receptor-Mediated Imaging of Prostate Cancer (2006) (9)
Medetomidine analogs as alpha 2-adrenergic ligands. 2. Design, synthesis, and biological activity of conformationally restricted naphthalene derivatives of medetomidine. (1996) (9)
An overview on selective androgen receptor modulators: Focus on enobosarm (2013) (9)
GTx-822, an ER{beta}-selective agonist, protects retinal pigment epithelium (ARPE-19) from oxidative stress by activating MAPK and PI3-K pathways. (2010) (9)
Domain structure and DNA binding regions of beta protein from bacteriophage lambda. (2006) (9)
A bifunctional colchicinoid that binds to the androgen receptor (2007) (9)
Synthesis of oxazolidinedione derived bicalutamide analogs. (2006) (8)
Biotransformation of a Novel Antimitotic Agent, I-387, by Mouse, Rat, Dog, Monkey, and Human Liver Microsomes and In Vivo Pharmacokinetics in Mice (2011) (8)
2-Arylthiazolidine-4-carboxylic acid amides (ATCAA) target dual pathways in cancer cells: 5'-AMP-activated protein kinase (AMPK)/mTOR and PI3K/Akt/mTOR pathways. (2010) (8)
Flavopiridol given as a 30-min intravenous (IV) bolus followed by 4-hr continuous IV infusion (CIVI) results in clinical activity and tumor lysis in refractory chronic lymphocytic leukemia (CLL). (2004) (8)
Chronic restraint via tail immobilization of mice: effects on corticosterone levels and other physiologic indices of stress. (2002) (7)
Preclinical characterization of a novel diphenyl benzamide selective ERα agonist for hormone therapy in prostate cancer. (2012) (7)
Evidence of significant absorption of antipyrine from urinary bladder of rats. (1992) (7)
Mdr 1 Limits CYP 3 A Metabolism in Vivo (2000) (6)
2',3'-Dideoxyinosine is not metabolized in human placenta. (1993) (6)
Drug interaction potential of toremifene and N-desmethyltoremifene with multiple cytochrome P450 isoforms (2011) (6)
Standard Pentostatin Dose Reductions in Renal Insufficiency Are Not Adequate: Selected Patients with Steroid-Refractory Acute Graft-Versus-Host Disease (2013) (6)
Combination Bortezomib (PS341, Velcade) and Rituximab Treatment Affects Multiple Survival and Death Pathways To Promote Apoptosis in Mantle Cell Lymphoma. (2005) (6)
Development and validation of a rapid and sensitive high-performance liquid chromatography-mass spectroscopy assay for determination of 17-(allylamino)-17-demethoxygeldanamycin and 17-(amino)-17-demethoxygeldanamycin in human plasma. (2008) (6)
Pharmacokinetics, biodistribution and metabolism of a novel selective androgen receptor modulator designed for prostate cancer imaging. (2009) (6)
High-performance liquid chromatographic determination of pentamidine in plasma. (1993) (6)
Mass spectrometric characterization of the human androgen receptor ligand-binding domain expressed in Escherichia coli. (2001) (6)
Flavopiridol (alvocidib) in chronic lymphocytic leukemia (2009) (5)
Pentamidine congeners. 4. DNA binding affinity and anti-Pneumocystis carinii activity of butamidine analogues (1996) (5)
Clinical Activity of Flavopiridol in Relapsed and Refractory Chronic Lymphocytic Leukemia (CLL) with High-Risk Cytogenetic Abnormalities: Updated Data on 89 Patients (Pts). (2007) (5)
Flavopiridol Can Be Safely Dose Escalated in Relapsed CLL Patients: Achievement of Target C max Results in Improved Clinical Activity. (2006) (5)
Effects of bladder resorption on pharmacokinetic data analysis (1994) (5)
Synthesis and Antiproliferative Activity of 2‐Aryl‐4‐oxo‐thiazolidin‐3‐yl‐amides for Prostate Cancer. (2005) (4)
Final Results of a Dose Escalation Study of Flavopiridol in Acute Leukemias Using a Novel Treatment Schedule. (2007) (4)
Preliminary Results of a Phase II Study of Flavopiridol (Alvocidib) in Relapsed Chronic Lymphocytic Leukemia (CLL): Confirmation of Clinical Activity in High-Risk Patients and Achievement of Complete Responses (CR). (2007) (4)
Pharmacokinetics of Aminolevulinic Acid After Intravesical Administration to Dogs (2004) (4)
Flavopiridol in Chronic Lymphocytic Leukemia (2007) (4)
Relationship of CYP2D6 status and toremifene metabolism. (2011) (3)
Phase I study of a novel, pharmacokinetically derived schedule of flavopiridol in acute leukemias: Clinical efficacy including hyperacute tumor lysis, pharmacokinetics, and pharmacodynamics. (2006) (3)
Genitourinary tumors, prostate (2012) (3)
Pharmacodynamics of Selective Androgen Receptor Modulators ( SARMs ) (2002) (3)
Abstract P5-09-21: Selective androgen receptor modulators (SARMs): Enobosarm as targeted therapy for the treatment of androgen receptor-positive breast cancer (2013) (3)
FTY720 Demonstrates Promising in-Vitro and in-Vivo Pre-Clinical Activity by Down-Modulation of Cyclin D1 and Pakt in Mantle Cell Lymphoma. (2009) (2)
Effect of para halogen modification of S-3-(phenoxy)-2-hydroxy-2-methyl-N-(4-nitro-3-trifluoromethyl-phenyl)-propionamides on metabolism and clearance (2014) (2)
FTY 720 Shows Promising In vitro and In vivo Preclinical Activity by Downmodulating Cyclin D 1 and Phospho-Akt in Mantle Cell Lymphoma (2010) (2)
Aldo-keto reductase (AKR) 1C3 as an androgen receptor coactivator. (2013) (2)
Effect of GTx-758, an ERα agonist, on serum-free testosterone and serum PSA in men with advanced prostate cancer. (2013) (2)
The free hormone hypothesis: Correlation of decreases in PSA with free testosterone rather than total testosterone in men with advanced prostate cancer treated with GTx-758. (2013) (1)
Abstract 2788: GTx-230: an orally available novel tubulin inhibitor that disrupts tumor vasculature and displays single-agent antitumor efficacy in multidrug-resistant prostate cancer with less neurotoxicity (2012) (1)
Abstract 1350: Novel ABI analogs target the colchicine site in tubulin and overcome multidrug resistance in metastatic melanoma (2011) (1)
102 GTx-758, an ERα agonist, reduces serum free testosterone lower than can be achieved by leuprolide with a significantly lower rate of hot flashes in men with advanced prostate cancer (2013) (1)
2048 ERG GENE TRANSLOCATION PREDICTS PROGRESSION OF HIGH GRADE PROSTATIC INTRAEPITHELIAL NEOPLASIA TO PROSTATE CANCER (2013) (1)
Abstract 730: Targeting colchicine binding site in tubulin for the treatment of advanced melanoma (2010) (1)
1448 ORAL ADMINISTRATION OF GTX-758, A SELECTIVE ERα AGONIST, INDUCES CHEMICAL CASTRATION BUT NOT GYNECOMASTIA IN MALE MONKEYS (2011) (1)
The effect of low-dose GTx-758 on free testerone levels in men with metastatic castration resistant prostate cancer (mCRPC). (2014) (1)
2008 Medicinal Chemistry DiVision Award Address Nonsteroidal Selective Androgen Receptor Modulators (SARMs): Dissociating the Anabolic and Androgenic Activities of the Androgen Receptor for Therapeutic Benefit (2009) (1)
MP70-17 OPTIMAL TESTOSTERONE SUPPRESSION ON MEDICAL ANDROGEN DEPRIVATION THERAPY SHOULD STRIVE TO SUPPRESS FREE TESTOSTERONE LEVELS, TO LEVELS SIMILAR TO ORCHIECTOMY--WHAT IS THAT VALUE? (2014) (1)
SELECTIVE ANDROGEN RECEPTOR MODULATORS AS IMPROVED ANDROGEN THERAPY FOR WOMEN (2013) (1)
Pharmacokinetic Optimization of 4-Substituted Methoxybenzoyl-Aryl-Thiazole (SMART) and 2-Aryl-4-Benzoyl-Imidazole (ABI) for Improving Oral Bioavailability (2011) (1)
Pharmacokinetics, pharmacodynamics and metabolism of a novel anticancer agent for prostate cancer. (2012) (1)
Excessive Neurotoxicity in a Phase II Trial of Combined Bortezomib and Rituximab in Patients with Relapsed/Refractory Mantle Cell (MCL) and Follicular (FL) Non-Hodgkin’s Lymphoma. (2006) (1)
Medetomidine Analogues as α2-Adrenergic Ligands. Part 3. Synthesis and Biological Evaluation of a New Series of Medetomidine Analogues and Their Potential Binding Interactions with α2- Adrenoceptors Involving a “Methyl Pocket”. (1997) (1)
Effect of para halogen modification of S-3-(phenoxy)-2-hydroxy-2-methyl-N-(4-nitro-3-trifluoromethyl-phenyl)-propionamides on metabolism and clearance (2013) (0)
Updated Results of a Phase I Study of Flavopiridol in Acute Leukemias Using a Novel, Pharmacokinetically Derived Schedule: Clinical Activity Including Hyperacute Tumor Lysis Syndrome (TLS), Pharmacokinetics (PK), and Pharmacodynamics (PD). (2006) (0)
Varicella-zoster meningitis with a late-onset of skin eruption: A case report (2014) (0)
Compound for treating cancer (2009) (0)
GTX-758, An Oral ERa Agonist, Increases Sex Hormone Binding Globulin, Reduces Free T and Decreases PSA in Patients with Castration Resistant Prostate Cancer (2012) (0)
Modulation of the Androgen Receptor Axis (0)
Alanine Aminotransferase Regulation by Androgens in Non-hepatic Tissues (2011) (0)
GTx-878, a Selective Estrogen Receptor Modulator (SERM) Inhibits Retinal Neovascularization in the Mouse Model of Oxygen Induced Retinopathy (2010) (0)
Novel Tubulin Polymerization Inhibitors Overcome Multidrug Resistance and Reduce Melanoma Lung Metastasis (2012) (0)
Crystal Structure Of The Androgen Receptor Ligand Binding Domain T877A Mutant In Complex With S-1 (2005) (0)
Synthesis and Antiproliferative Activity of Thioazolidine Analogues for Melanoma. (2007) (0)
Crystal structure of the T877A androgen receptor ligand binding domain in complex with (S)-N-(4-Cyano-3-(trifluoromethyl)phenyl)-3-(4-cyanonaphthalen-1-yloxy)-2-hydroxy-2-methylpropanamide (2011) (0)
Estradiol Protects RPE Cells From Oxidative Stress by Induction of ER- β (2009) (0)
Diagnostic tools like ANDROTEST have estimated a disease incidence of 10%–40% in men aged over 45 years and suggest that up to 60 million men in the United States, Europe and Japan suffer (2020) (0)
Pharmacology of N,N-di(n-butyl)adriamycin-14-valerate in the rat (2009) (0)
Crystal Structure of the Androgen Receptor Ligand-binding Domain W741L Mutant Complex with R-bicalutamide (2005) (0)
Agonists and antagonists of lpa receptors and use procedures. (2001) (0)
Baseline characteristics from two ongoing phase III trials for the prevention and treatment of muscle wasting in NSCLC. (2013) (0)
Selective modulators of andro genrezeptors and methods for their use (2001) (0)
Crystal Structure Of The Androgen Receptor Ligand Binding Domain In Complex With S-1 (2005) (0)
Crystal Structure Of The Androgen Receptor Ligand Binding Domain T877A Mutant In Complex With Hydroxyflutamide (2005) (0)
Halogenated selective modulators of the androgen receptor and methods of use thereof. (2003) (0)
Molecular Cancer apeutics apeutic Discovery 7 , a Novel Antimitotic Indole , Displays a Potent In vitro and Ther ivo Antitumor Activity with Less Neurotoxicity (2010) (0)
Treatment of symptoms of the kidney disease with the selective androgen receptor modulators (SARM) (2006) (0)
Crystal Structure Of The Androgen Receptor Ligand Binding Domain W741L Mutant In Complex With S-1 (2005) (0)
Abstract #4416: 2-arylthiazolidine-4-carboxylic acid amides (ATCAA) target dual pathways: Effects on the 5\#8217;-AMP-activated protein kinase (AMPK) and Akt pathways. (2009) (0)
Abstract #LB-262: A Randomized Placebo-Controlled Trial of a Selective Androgen Receptor Modulator in patients with cancer cachexia (2009) (0)
Selective Estrogen Receptor Modulators (SERMs) and Selective Androgen Receptor Modulators (SARMs) (2015) (0)
Drug Metabolism and Pharmacokinetics of 4-Substituted Methoxybenzoyl-aryl-thiazoles □ S (2010) (0)
Crystal structure of the human androgen receptor T877A mutant ligand-binding domain with cyproterone acetate (2007) (0)
POD-03.06 GTx-758, an Oral ER? Agonist Being Developed for ADT, Lowers Serum Testosterone (2011) (0)
Orally Bioavailable Tubulin Antagonists for Paclitaxel-Refractory Cancer (2012) (0)
Serum IGF-1 levels in men with advanced prostate cancer treated with the ERα agonist, GTx-758. (2013) (0)
MP52-02 A NOVEL ORAL ? AND ? TUBULIN INHIBITOR, VERU-111, HAS POTENT ACTIVITY AGAINST PACLITAXEL SENSITIVE AND RESISTANT PROSTATE CANCER (2018) (0)
Crystal structure of the androgen receptor ligand binding domain in complex with SARM C-23 (2008) (0)
multisubstituted selective modulators of the androgen receptor and methods of use thereof (2003) (0)
DMD # 9985R 1 IN VIVO METABOLISM AND FINAL DISPOSITION OF A NOVEL NONSTEROIDAL ANDROGEN IN RATS AND DOGS (2006) (0)
(2-(1-h-indolyl)imidazol-4-yl)(3,4,5-trimethoxyphenyl)methanone useful for the treatment of cancer (2009) (0)
Selective androgen receptor modulators activate the canonical prostate cancer androgen receptor program and repress cancer growth. (2021) (0)
Original article Novel nonsteroidal ligands with high binding affinity and potent functional activity for the androgen receptor (2002) (0)
A Selective Androgen Receptor Modulator (SARM) for Hormonal Male Contraception (2004) (0)
LB-S&T-06 NOVEL DUAL-BINDING SELECTIVE DEGRADERS OF FULL LENGTH AND SPLICE VARIANT ANDROGEN RECEPTORS FOR THE TREATMENT OF CASTRATION-RESISTANT PROSTATE CANCER (2016) (0)
Halogenated selektiveandrogenrezeptormodulatoren and procedures for their application (2003) (0)
SUBSTITUTED AND ACYLANILIDER methods of use thereof (2007) (0)
G2-M block, apoptosis, and cytotoxicity are potently induced by novel bis-indoles in prostate cancer cells (2005) (0)
Importance of CYP2D6 metabolism in the in vitro antiestrogenic activity of toremifene and tamoxifen. (2011) (0)
Pharmacokinetic and pharmacodynamic correlations of flavopiridol in the treatment of chronic lymphocytic leukemia. (2016) (0)
Plenary paper Flavopiridol administered using a pharmacologically derived schedule is associated with marked clinical efficacy in refractory, genetically high-risk chronic lymphocytic leukemia (2006) (0)
Agonists and antagonists for the LPA receptor and application methods (2001) (0)
high-risk chronic lymphocytic leukemia associated with marked clinical efficacy in refractory, genetically Flavopiridol administered using a pharmacologically derived schedule is (2013) (0)
Activity of VERU-111, an novel oral α and β tubulin inhibitor, against paclitaxel sensitive and resistant prostate cancer. (2018) (0)
Crystal structure of DJ-101 in complex with tubulin protein (2017) (0)
Gtx-822 a Selective Estrogen Receptor β (erβ) Ligand Protects Mitochondria in Arpe-19 Cells Through Genomic and Non-Genomic Pathways (2010) (0)
Optimal testosterone suppression on medical ADT should strive to suppress free testosterone levels to levels similar to orchiectomy: What is that value? (2014) (0)
Pharmacokinetic and pharmacodynamic implications of drug absorption from urinary bladder (1990) (0)
UP-02.076 GTx-758, an Oral ER? Agonist Being Developed for Advanced Prostate Cancer Avoids Many Estrogen Deficiency Side Effects Commonly Observed with ADT (2011) (0)
Crystal Structure Of The Androgen Receptor Ligand Binding Domain In Complex With R-3 (2005) (0)
JPET #94334 1 Preclinical pharmacology of a nonsteroidal ligand for androgen receptor mediated imaging of prostate cancer (2006) (0)
Microsoft Word-85670376-file00 (2010) (0)
FTY720 (2-Amino-2-[2-(4-octylphenyl) ethyl] Propane 1, 3-diol hydrochloride), Mediates Cytotoxicity through Caspase Independent and Protein Phosphatase 2A Dependent Mechanisms in Chronic Lymphocytic Leukemia and Lymphoblastic Leukemia/Lymphoma. (2006) (0)
Rate of hot flashes in patients with advanced prostate cancer treated with GTx-758. (2013) (0)
Abstract 5684: Target tubulin polymerization with novel reverse ABI analogs interacting with the colchicine binding site. (2013) (0)
SAR Studies of 2-Arylthiazolidine-4-carboxylic Acid Amides (I): A Novel Class of Cytotoxic Agents for Prostate Cancer. (2005) (0)
Effect of the ERα agonist GTx-758 on bone turnover markers in men with advanced prostate cancer. (2013) (0)
863 Low dose GTx-758 decreases free testosterone to levels similar to orchiectomy in men with metastatic castration resistant prostate cancer (mCRPC) (2014) (0)
VERU-111, an novel oral α and β tubulin inhibitor, has potent activity against paclitaxel sensitive and resistant prostate cancer (2018) (0)
Bladder absorption and pharmacokinetics of mitomycin c mmc in trans urethral resection patients (1989) (0)
Title: Nonsteroidal Selective Androgen Receptor Modulators Enhance Female Sexual Motivation Running Title Page Running Title: Sarms Enhance Female Sexual Motivation (2010) (0)

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