P. Kym

发表

Analgesic potential of TRPV1 antagonists.

P. Kym, M. Kort, C. Hutchins, 2009, Biochemical pharmacology.

Selective blockade of TRPA1 channel attenuates pathological pain without altering noxious cold sensation or body temperature regulation

J. Segreti, S. Baker, Robert G. Schmidt, 2011, PAIN.

Identification and characterization of amino-piperidinequinolones and quinazolinones as MCHr1 antagonists.

M. Maguire, Courtney A. Cullis, C. Blackburn, 2006, Bioorganic & medicinal chemistry letters.

Total synthesis of erythromycin B

A. Hodgson, P. Hergenrother, P. Kym, 2007 .

Prospects for obesity treatment: MCH receptor antagonists.

C. Collins, P. Kym, C. A. Collins, 2003, Current opinion in investigational drugs.

TRPV1 ligands with hyperthermic, hypothermic and no temperature effects in rats

A. Gomtsyan, J. Segreti, Robert G. Schmidt, 2015, Temperature.

Synthesis and biological evaluation of 5-substituted and 4,5-disubstituted-2-arylamino oxazole TRPV1 antagonists.

A. Gomtsyan, Chih-Hung Lee, Robert G. Schmidt, 2010, Bioorganic & medicinal chemistry.

Repeated dosing of ABT-102, a potent and selective TRPV1 antagonist, enhances TRPV1-mediated analgesic activity in rodents, but attenuates antagonist-induced hyperthermia

A. Gomtsyan, P. Mantyh, J. Sullivan, 2009, Pain.

TRPA1 in Drug Discovery

P. Kym, Jun Chen, S. McGaraughty, 2012 .

Pore dilation occurs in TRPA1 but not in TRPM8 channels

Donghee Kim, C. Faltynek, P. Kym, 2009, Molecular pain.

Diacylglycerol Acyltransferase 1 Inhibition Lowers Serum Triglycerides in the Zucker Fatty Rat and the Hyperlipidemic Hamster

A. Souers, J. Segreti, A. King, 2009, Journal of Pharmacology and Experimental Therapeutics.

Evaluation of a highly efficient aryl azide photoaffinity labeling reagent for the progesterone receptor.

J. Katzenellenbogen, K. Carlson, P. Kym, 1995, Bioconjugate chemistry.

In vivo efficacy of acyl CoA: diacylglycerol acyltransferase (DGAT) 1 inhibition in rodent models of postprandial hyperlipidemia.

A. Souers, J. Segreti, A. King, 2010, European journal of pharmacology.

Hepatic Glucocorticoid Receptor Antagonism Is Sufficient to Reduce Elevated Hepatic Glucose Output and Improve Glucose Control in Animal Models of Type 2 Diabetes

L. Öhman, D. Edgerton, A. Cherrington, 2005, Journal of Pharmacology and Experimental Therapeutics.

Fluorine-18-labeled progestin ketals: synthesis and target tissue uptake selectivity of potential imaging agents for receptor-positive breast tumors.

M. Welch, J. Katzenellenbogen, H. VanBrocklin, 1993, Journal of medicinal chemistry.

trans-Activation and repression properties of the novel nonsteroid glucocorticoid receptor ligand 2,5-dihydro-9-hydroxy-10-methoxy-2,2,4-trimethyl-5-(1-methylcyclohexen-3-y1)-1H-[1]benzopyrano[3,4-f]quinoline (A276575) and its four stereoisomers.

M. Nakane, J. Kuk, G. Carter, 2002, Molecular pharmacology.

Identification and preliminary characterization of a potent, safe, and orally efficacious inhibitor of acyl-CoA:diacylglycerol acyltransferase 1.

Steven C. Cullen, P. Hajduk, A. Souers, 2012, Journal of medicinal chemistry.

Validation of diacyl glycerolacyltransferase I as a novel target for the treatment of obesity and dyslipidemia using a potent and selective small molecule inhibitor.

A. Souers, G. Diaz, H. Sham, 2008, Journal of medicinal chemistry.

Species Comparison and Pharmacological Characterization of Human, Monkey, Rat, and Mouse TRPA1 Channels

P. Kym, Jun Chen, Xufeng Zhang, 2012, Journal of Pharmacology and Experimental Therapeutics.

Analgesic potential of TRPV3 antagonists.

P. Kym, R. Reilly, 2011, Current topics in medicinal chemistry.

Design, Synthesis, and Conformational Analysis of a Proposed Type I β-Turn Mimic.

J. Katzenellenbogen, B. Fink, P. Kym, 1998 .

Electrophysiologic characterization of a novel hERG channel activator.

G. Gintant, A. Souers, G. Diaz, 2009, Biochemical pharmacology.

Synthesis and characterization of non-steroidal ligands for the glucocorticoid receptor: selective quinoline derivatives with prednisolone-equivalent functional activity.

M. Nakane, S. Elmore, P. Kym, 2001, Journal of medicinal chemistry.

Discovery and SAR of 4-Aminopyrrolidine-2-carboxylic Acid Correctors of CFTR for the Treatment of Cystic Fibrosis.

A. Bogdan, A. Swensen, Ashvani K. Singh, 2022, Bioorganic & medicinal chemistry letters.

Synthesis and evaluation of 2-amino-8-alkoxy quinolines as MCHr1 antagonists. Part 1.

A. Vasudevan, A. Souers, C. Collins, 2004, Bioorganic & medicinal chemistry letters.

Discovery and SAR development of thienopyridones: a class of small molecule AMPK activators.

L. Kifle, H. Sham, P. Kym, 2007, Bioorganic & medicinal chemistry letters.

Discovery of (R)-1-(7-chloro-2,2-bis(fluoromethyl)chroman-4-yl)-3-(3-methylisoquinolin-5-yl)urea (A-1165442): a temperature-neutral transient receptor potential vanilloid-1 (TRPV1) antagonist with analgesic efficacy.

A. Gomtsyan, J. Segreti, A. King, 2014, Journal of medicinal chemistry.

A-995662 [(R)-8-(4-methyl-5-(4-(trifluoromethyl)phenyl)oxazol-2-ylamino)-1,2,3,4-tetrahydronaphthalen-2-ol], a novel, selective TRPV1 receptor antagonist, reduces spinal release of glutamate and CGRP in a rat knee joint pain model

S. Baker, T. Neelands, P. Honore, 2010, PAIN.

Pharmacology of Modality-Specific Transient Receptor Potential Vanilloid-1 Antagonists That Do Not Alter Body Temperature

A. Gomtsyan, P. Mantyh, J. Segreti, 2012, Journal of Pharmacology and Experimental Therapeutics.

TRPV1 antagonists: clinical setbacks and prospects for future development.

P. Kym, M. Kort, 2012, Progress in medicinal chemistry.

Nonsteroidal selective glucocorticoid modulators: the effect of C-10 substitution on receptor selectivity and functional potency of 5-allyl-2,5-dihydro-2,2,4-trimethyl-1H-[1]benzopyrano[3,4-f]quinolines.

S. Elmore, M. Nakane, J. Miner, 2003, Journal of medicinal chemistry.

Synthesis and structure-activity relationships of a novel series of tricyclic dihydropyridine-based KATP openers that potently inhibit bladder contractions in vitro.

J. Sullivan, R. Henry, M. Gopalakrishnan, 2004, Journal of medicinal chemistry.

Aminopiperidine indazoles as orally efficacious melanin concentrating hormone receptor-1 antagonists.

Ju Gao, Anil Vasudevan, John K Lynch, 2005, Bioorganic & medicinal chemistry letters.

Synthesis and biological evaluation of novel, selective, nonsteroidal glucocorticoid receptor antagonists.

I. Akritopoulou‐Zanze, Jyoti R. Patel, P. Kym, 2004, Bioorganic & medicinal chemistry letters.

Discovery and characterization of aminopiperidinecoumarin melanin concentrating hormone receptor 1 antagonists.

Thomas Fey, Robin Shapiro, Ju Gao, 2005, Journal of medicinal chemistry.

Process Development of a Diacyl Glycerolacyltransferase-1 Inhibitor

Brian J. Kotecki, A. Souers, P. Kym, 2010 .

Synthesis and Structure−Activity Relationships of a Novel Series of 2,3,5,6,7,9-Hexahydrothieno[3,2-b]quinolin-8(4H)-one 1,1-Dioxide KATP Channel Openers: Discovery of (−)-(9S)-9-(3-Bromo-4-fluorophenyl)-2,3,5,6,7,9- hexahydrothieno[3,2-b]quinolin-8(4H)-one 1,1-Dioxide (A-278637), a Potent KATP Open

J. Sullivan, R. Henry, J. Brioni, 2004 .

Novel approach to the zaragozic acids. Enantioselective total synthesis of 6,7-dideoxysqualestatin H5.

S. Liras, P. Kym, S. Martin, 2002, The Journal of organic chemistry.

Design, Synthesis, and Conformational Analysis of a Proposed Type I β-Turn Mimic

John A. Katzenellenbogen, J. Katzenellenbogen, B. Fink, 1998 .

Stereoselective Synthesis of a Dipyridyl Transient Receptor Potential Vanilloid-3 (TRPV3) Antagonist.

A. Gomtsyan, Robert G. Schmidt, P. Kym, 2016, The Journal of organic chemistry.

TRPV1 antagonists that cause hypothermia, instead of hyperthermia, in rodents: Compounds’ pharmacological profiles, in vivo targets, thermoeffectors recruited and implications for drug development

A. A. Romanovsky, A. Gomtsyan, E. Pintér, 2018, Acta physiologica.

THE EFFECT OF ACCEPTOR GROUP VARIATION ON THE SOLVATOCHROMISM OF DONOR‐ACCEPTOR FLUOROPHORES

J. Katzenellenbogen, K. Carlson, K. Hwang, 1993, Photochemistry and photobiology.

Synthesis and Pharmacology of (Pyridin-2-yl)methanol Derivatives as Novel and Selective Transient Receptor Potential Vanilloid 3 Antagonists.

Bruce Clapham, Bin Li, A. Gomtsyan, 2016, Journal of medicinal chemistry.

An evaluation of 3,4-methylenedioxy phenyl replacements in the aminopiperidine chromone class of MCHr1 antagonists.

A. Souers, G. Diaz, H. Sham, 2007, Bioorganic & medicinal chemistry letters.

Fueling the Pipeline via Innovations in Organic Synthesis.

P. Kym, E. Voight, Stephen N. Greszler, 2021, ACS medicinal chemistry letters.

Pharmacology of Modality-Specific TRPV1 Antagonists That Do Not Alter Body Temperature

A. Gomtsyan, P. Mantyh, J. Segreti, 2012 .

Identification of 2-(4-benzyloxyphenyl)-N- [1-(2-pyrrolidin-1-yl-ethyl)-1H-indazol-6-yl]acetamide, an orally efficacious melanin-concentrating hormone receptor 1 antagonist for the treatment of obesity.

Robin Shapiro, Ju Gao, Anil Vasudevan, 2005, Journal of medicinal chemistry.

Benz[a]anthracene diols: Predicted carcinogenicity and structure-estrogen receptor binding affinity relationships

P. Kym, G. Anstead, 1995, Steroids.

Targeting TRP channels for pain relief.

A. Szallasi, Jill-Desiree Brederson, P. Kym, 2013, European journal of pharmacology.

The Asymmetric Synthesis of Erythromycin B

A. Hodgson, P. Kym, S. Martin, 1997 .

Recent Progress in the Discovery and Development of Small-Molecule Modulators of CFTR.

P. Kym, Xueqing Wang, M. Pizzonero, 2018, Progress in medicinal chemistry.

Discovery of potent, selective, orally bioavailable stearoyl-CoA desaturase 1 inhibitors.

Bo Liu, Gang Liu, Hongyu Zhao, 2007, Journal of medicinal chemistry.

Identification and characterization of a small molecule AMPK activator that treats key components of type 2 diabetes and the metabolic syndrome.

L. Kifle, Gang Zhao, K. Marsh, 2006, Cell metabolism.

A novel antiinflammatory maintains glucocorticoid efficacy with reduced side effects.

M. Nakane, S. Elmore, R. Turner, 2003, Molecular endocrinology.

Biological Characterization of F508delCFTR Protein Processing by the CFTR Corrector ABBV-2222/GLPG2222

C. Tse, D. Cyr, A. Swensen, 2019, The Journal of Pharmacology and Experimental Therapeutics.

TRPV3 modulates nociceptive signaling through peripheral and supraspinal sites in rats.

A. Gomtsyan, Jill-Desiree Brederson, Robert G. Schmidt, 2017, Journal of neurophysiology.

P. Chandran, M. Jarvis, P. Kym, 2011, Brain Research.

TRPA1 modulation of spontaneous and mechanically evoked firing of spinal neurons in uninjured, osteoarthritic, and inflamed rats

P. Kym, M. Kort, S. Didomenico, 2010, Molecular pain.

Discovery of 4-[(2R,4R)-4-({[1-(2,2-Difluoro-1,3-benzodioxol-5-yl)cyclopropyl]carbonyl}amino)-7-(difluoromethoxy)-3,4-dihydro-2H-chromen-2-yl]benzoic Acid (ABBV/GLPG-2222), a Potent Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) Corrector for the Treatment of Cystic Fibrosis.

A. Bogdan, C. Tse, A. Swensen, 2018, Journal of medicinal chemistry.

Transient Receptor Potential Channel Ankyrin-1 Is Not a Cold Sensor for Autonomic Thermoregulation in Rodents

A. A. Romanovsky, V. Tékus, K. Pohóczky, 2014, The Journal of Neuroscience.

Molecular Determinants of Species-Specific Activation or Blockade of TRPA1 Channels

P. Hajduk, J. R. Huth, Chaohong Sun, 2008, The Journal of Neuroscience.

Foslevodopa/Foscarbidopa: A New Subcutaneous Treatment for Parkinson's Disease

M. Facheris, Geoff G. Z. Zhang, F. Jameel, 2021, Annals of neurology.

Optimization of chromone-2-carboxamide melanin concentrating hormone receptor 1 antagonists: assessment of potency, efficacy, and cardiovascular safety.

G. Diaz, E. Bush, H. Sham, 2006, Journal of medicinal chemistry.

Discovery of ABBV/GLPG-3221, a Potent Corrector of CFTR for the Treatment of Cystic Fibrosis.

A. Bogdan, C. Tse, A. Swensen, 2019, ACS medicinal chemistry letters.

Identification of ortho-amino benzamides and nicotinamides as MCHr1 antagonists.

Anil Vasudevan, Christopher Blackburn, A. Vasudevan, 2005, Bioorganic & medicinal chemistry letters.

TRPA1: the species difference

P. Kym, Jun Chen, 2009, The Journal of general physiology.

TRPA 1 : the species difference

P. Kym, Jun Chen, 2022 .

Capsaicin-induced inhibition of platelet aggregation is not mediated by transient receptor potential vanilloid type 1

A. King, P. Kym, M. Kort, 2012, Blood coagulation & fibrinolysis : an international journal in haemostasis and thrombosis.

Antagonism of TRPV1 receptors indirectly modulates activity of thermoregulatory neurons in the medial preoptic area of rats

J. Segreti, R. Fryer, C. Faltynek, 2009, Brain Research.

Synthesis and evaluation of urea-based indazoles as melanin-concentrating hormone receptor 1 antagonists for the treatment of obesity.

Robin Shapiro, Ju Gao, A. Souers, 2005, Bioorganic & medicinal chemistry letters.

Molecular structures, conformational analysis, and preferential modes of binding of 3-aroyl-2-arylbenzo[b]thiophene estrogen receptor ligands: LY117018 and aryl azide photoaffinity labeling analogs.

J. Katzenellenbogen, S. R. Wilson, P. Kym, 1993, Journal of medicinal chemistry.

Progestin 16 alpha, 17 alpha-dioxolane ketals as molecular probes for the progesterone receptor: synthesis, binding affinity, and photochemical evaluation.

J. Katzenellenbogen, K. Carlson, P. Kym, 1993, Journal of medicinal chemistry.

Identification of aminopiperidine benzamides as MCHr1 antagonists.

A. Vasudevan, A. Souers, C. Blackburn, 2005, Bioorganic & medicinal chemistry letters.

Synthesis and evaluation of 2-amino-8-alkoxy quinolines as MCHr1 antagonists. Part 2.

Anil Vasudevan, A. Vasudevan, A. Souers, 2004, Bioorganic & medicinal chemistry letters.

Synthesis and evaluation of 2-amino-8-alkoxy quinolines as MCHr1 antagonists. Part 3.

Ju Gao, Anil Vasudevan, A. Vasudevan, 2004, Bioorganic & medicinal chemistry letters.

Lead optimization of melanin concentrating hormone receptor 1 antagonists with low hERG channel activity.

A. Souers, P. Kym, A. Judd, 2008, Current topics in medicinal chemistry.

Lead optimization strategies and tactics applied to the discovery of melanin concentrating hormone receptor 1 antagonists.

A. Vasudevan, A. Souers, P. Kym, 2007, Current topics in medicinal chemistry.

Lack of efficacy of melanin-concentrating hormone-1 receptor antagonists in models of depression and anxiety.

A. Vasudevan, A. Souers, G. Fox, 2006, European journal of pharmacology.

Liver-selective glucocorticoid antagonists: a novel treatment for type 2 diabetes.

K. Koehler, L. Hagberg, C. Jakob, 2004, Journal of medicinal chemistry.

Identification of diamino chromone-2-carboxamides as MCHr1 antagonists with minimal hERG channel activity.

G. Gintant, A. Souers, G. Diaz, 2007, Bioorganic & medicinal chemistry letters.

Constrained 7-fluorocarboxychromone-4-aminopiperidine based Melanin-concentrating hormone receptor 1 antagonists: the effects of chirality on substituted indan-1-ylamines.

A. Souers, G. Diaz, E. Bush, 2007, Bioorganic & medicinal chemistry letters.

The pursuit of differentiated ligands for the glucocorticoid receptor.

S. Elmore, P. Kym, M. Kort, 2003, Current topics in medicinal chemistry.

534 Defining a mechanistic link between TRPV3 activity and psoriasis through IL-1α and EGFR signaling pathways

S. Gauld, T. Neelands, L. Miller, 2016 .

The PTPN2/PTPN1 inhibitor ABBV-CLS-484 unleashes potent anti-tumour immunity

Yi Yang, M. Rees, K. Yates, 2023, Nature.

Discovery of (R)-(3-fluoropyrrolidin-1-yl)(6-((5-(trifluoromethyl)pyridin-2-yl)oxy)quinolin-2-yl)methanone (ABBV-318) and analogs as small molecule Nav1.7/ Nav1.8 blockers for the treatment of pain.

G. Gintant, R. Gum, T. Neelands, 2022, Bioorganic & medicinal chemistry.

Screening for cardiovascular safety: a structure-activity approach for guiding lead selection of melanin concentrating hormone receptor 1 antagonists.

Ju Gao, Anil Vasudevan, John K Lynch, 2006, Journal of medicinal chemistry.

Free Energy Perturbation Approach for Accurate Crystalline Aqueous Solubility Predictions.

Richard S. Hong, Shailendra V. Bordawekar, Lingle Wang, 2023, Journal of medicinal chemistry.

Synthesis and Pharmacology of (Pyridin-2-yl)methanol Derivatives as Novel and Selective Transient Receptor Potential Vanilloid 3 Antagonists.

A. Gomtsyan, J. Segreti, R. Henry, 2016, Journal of medicinal chemistry.

TRPV3 modulates nociceptive signaling through peripheral and supraspinal sites in rats.

A. Gomtsyan, Robert G. Schmidt, P. Kym, 2017, Journal of neurophysiology.