J. Tata

发表

Discovery of aminoheterocycles as potent and brain penetrant prolylcarboxypeptidase inhibitors.

Michael E. Lassman, Shirly Pinto, M. Garcia-Calvo, 2012, Bioorganic & medicinal chemistry letters.

The discovery of non-benzimidazole and brain-penetrant prolylcarboxypeptidase inhibitors.

Michael E. Lassman, Shirly Pinto, M. Garcia-Calvo, 2012, Bioorganic & medicinal chemistry letters.

Discovery of a new class of potent prolylcarboxypeptidase inhibitors derived from alanine.

Michael E. Lassman, Shirly Pinto, M. Garcia-Calvo, 2012, Bioorganic & medicinal chemistry letters.

Discovery of benzimidazole pyrrolidinyl amides as prolylcarboxypeptidase inhibitors.

Michael E. Lassman, Shirly Pinto, M. Garcia-Calvo, 2011, Bioorganic & medicinal chemistry letters.

A combinatorial library of indinavir analogues and its in vitro and in vivo studies.

Yuan Cheng, Xin Xu, Lawrence C Kuo, 2002, Bioorganic & medicinal chemistry letters.

Discovery of orally bioavailable and novel urea agonists of the high affinity niacin receptor GPR109A.

Kenneth K. Wu, Q. Deng, Hong C Shen, 2007, Bioorganic & medicinal chemistry letters.

Agonist lead identification for the high affinity niacin receptor GPR109a.

Brian M. Smith, D. Connolly, S. Tamura, 2007, Bioorganic & medicinal chemistry letters.

Discovery of biaryl anthranilides as full agonists for the high affinity niacin receptor.

M. Forrest, Kenneth K. Wu, Q. Deng, 2007, Journal of medicinal chemistry.

3-(1H-tetrazol-5-yl)-1,4,5,6-tetrahydro-cyclopentapyrazole (MK-0354): a partial agonist of the nicotinic acid receptor, G-protein coupled receptor 109a, with antilipolytic but no vasodilatory activity in mice.

D. Connolly, S. Tamura, C. Sage, 2008, Journal of medicinal chemistry.

Discovery of pyrazolopyrimidines as the first class of allosteric agonists for the high affinity nicotinic acid receptor GPR109A.

Hong C Shen, J. Tata, S. Colletti, 2008, Bioorganic & medicinal chemistry letters.

Tetrahydro anthranilic acid as a surrogate for anthranilic acid: application to the discovery of potent niacin receptor agonists.

Hong C Shen, J. Tata, S. Colletti, 2008, Bioorganic & medicinal chemistry letters.

Effects of a niacin receptor partial agonist, MK-0354, on plasma free fatty acids, lipids, and cutaneous flushing in humans.

D. Connolly, J. Paolini, J. Wagner, 2008, Journal of clinical lipidology.

GPR109a agonists. Part 1: 5-Alkyl and 5-aryl-pyrazole-tetrazoles as agonists of the human orphan G-protein coupled receptor GPR109a.

J. Tata, S. Colletti, E. Carballo-Jane, 2009, Bioorganic & medicinal chemistry letters.

Discovery of novel tricyclic full agonists for the G-protein-coupled niacin receptor 109A with minimized flushing in rats.

Kenneth K. Wu, Q. Deng, Hong C Shen, 2009, Journal of medicinal chemistry.

Pyrazole acids as niacin receptor agonists for the treatment of dyslipidemia.

D. Blom, J. Tata, S. Colletti, 2009, Bioorganic & medicinal chemistry letters.

Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): a potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate.

M. Forrest, Kenneth K. Wu, Q. Deng, 2010, Journal of medicinal chemistry.

High-throughput purification platform in support of drug discovery.

P. Váchal, J. Tata, L. Xia, 2012, ACS combinatorial science.

(1aR,5aR)1a,3,5,5a-Tetrahydro-1H-2,3-diaza-cyclopropa[a]pentalene-4-carboxylic acid (MK-1903): a potent GPR109a agonist that lowers free fatty acids in humans.

D. Connolly, J. Knudsen, C. Sage, 2012, Journal of medicinal chemistry.

Synthesis and biological evaluation of platensimycin analogs.

M. Maccoss, Hong C Shen, S. Soisson, 2009, Bioorganic & medicinal chemistry letters.

A novel series of indazole-/indole-based glucagon receptor antagonists.

S. Qureshi, Bei B. Zhang, G. Salituro, 2015, Bioorganic & medicinal chemistry letters.

Niacin Lipid Efficacy Is Independent of Both the Niacin Receptor GPR109A and Free Fatty Acid Suppression

D. Rader, D. Connolly, Jiajun Liu, 2012, Science Translational Medicine.

Design and synthesis of conformationally constrained tri-substituted ureas as potent antagonists of the human glucagon receptor.

V. Ding, Bei B. Zhang, J. Tata, 2007, Bioorganic & medicinal chemistry letters.

Discovery of novel, potent, and orally active spiro-urea human glucagon receptor antagonists.

V. Ding, S. Qureshi, K. Chapman, 2005, Bioorganic & medicinal chemistry letters.

Discovery of pyrazolyl propionyl cyclohexenamide derivatives as full agonists for the high affinity niacin receptor GPR109A.

Hong C Shen, X. Tong, Qing Chen, 2010, Bioorganic & medicinal chemistry letters.

A novel glucagon receptor antagonist inhibits glucagon-mediated biological effects.

D. Moller, V. Ding, S. Qureshi, 2004, Diabetes.

Discovery of potent, orally active benzimidazole glucagon receptor antagonists.

V. Ding, S. Qureshi, D. Szalkowski, 2008, Bioorganic & medicinal chemistry letters.

Discovery and investigation of a novel class of thiophene-derived antagonists of the human glucagon receptor.

V. Ding, S. Qureshi, D. Szalkowski, 2005, Bioorganic & medicinal chemistry letters.

Discovery of benzofuran propanoic acid GPR120 agonists: From uHTS hit to mechanism-based pharmacodynamic effects.

Michael F. Finley, John J. Cummings, A. Crespo, 2016, Bioorganic & medicinal chemistry letters.

Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes.

S. Qureshi, S. Xu, Bei B. Zhang, 2012, Journal of medicinal chemistry.

Discovery and Pharmacology of a Novel Class of Diacylglycerol Acyltransferase 2 Inhibitors.

Shirly Pinto, D. McLaren, Sheng-ping Wang, 2015, Journal of medicinal chemistry.

From Screening to Targeted Degradation: Strategies for the Discovery and Optimization of Small Molecule Ligands for PCSK9.

Sujata Sharma, J. Lisnock, P. Orth, 2019, Cell chemical biology.

GPR109a agonists. Part 2: pyrazole-acids as agonists of the human orphan G-protein coupled receptor GPR109a.

J. Tata, S. Colletti, E. Carballo-Jane, 2010, Bioorganic & medicinal chemistry letters.

Anthranilic acid replacements in a niacin receptor agonist.

D. Blom, Hong C Shen, J. Tata, 2010, Bioorganic & medicinal chemistry letters.

The discovery of high affinity agonists of GPR109a with reduced serum shift and improved ADME properties.

J. Tata, S. Colletti, J. Imbriglio, 2011, Bioorganic & medicinal chemistry letters.

Comparison of rat and dog models of vasodilatation and lipolysis for the calculation of a therapeutic index for GPR109A agonists.

M. Forrest, M. E. Mccann, J. Tata, 2007, Journal of pharmacological and toxicological methods.

Novel N-arylpyrazolo[3,2-c]-based ligands for the glucocorticoid receptor: receptor binding and in vivo activity.

D. Zaller, Amjad Ali, Douglas K. Miller, 2004, Journal of medicinal chemistry.

Discovery of novel, potent, selective, and orally active human glucagon receptor antagonists containing a pyrazole core.

V. Ding, S. Qureshi, K. Chapman, 2011, Bioorganic & medicinal chemistry letters.

Discovery of N-aryl-2-acylindole human glucagon receptor antagonists.

V. Ding, S. Qureshi, D. Szalkowski, 2011, Bioorganic & medicinal chemistry letters.

Discovery of cyclic guanidines as potent, orally active, human glucagon receptor antagonists.

V. Ding, S. Qureshi, D. Szalkowski, 2011, Bioorganic & medicinal chemistry letters.

A strategy of employing aminoheterocycles as amide mimics to identify novel, potent and bioavailable soluble epoxide hydrolase inhibitors.

J. Berger, Gaochao Zhou, Bei B. Zhang, 2009, Bioorganic & medicinal chemistry letters.

Discovery of 3,3-disubstituted piperidine-derived trisubstituted ureas as highly potent soluble epoxide hydrolase inhibitors.

J. Berger, Gaochao Zhou, Bei B. Zhang, 2009, Bioorganic & medicinal chemistry letters.

Novel heterocyclic glucocorticoids: in vitro profile and in vivo efficacy.

D. Zaller, Amjad Ali, Douglas K. Miller, 2005, Bioorganic & medicinal chemistry letters.

The design and synthesis of orally active short duration spiroindane growth hormone secretagogues

Roy G. Smith, A. Patchett, G. Hickey, 1997 .

Structural Requirements for the Activation of the Human Growth Hormone Secretagogue Receptor by Peptide and Nonpeptide Secretagogues

D. Underwood, Roy G. Smith, J. Woods, 1997 .

Discovery of a highly potent, selective, and bioavailable soluble epoxide hydrolase inhibitor with excellent ex vivo target engagement.

J. Berger, Gaochao Zhou, Sanjeev Kumar, 2009, Journal of medicinal chemistry.

Location and chemical speciation of Cu in ZSM-5 during the water-gas shift reaction

J. Rodríguez, S. Senanayake, Dimitriy Vovchok, 2019, Catalysis Today.

Structural requirements for the activation of the human growth hormone secretagogue receptor by peptide and nonpeptide secretagogues.

D. Underwood, L. V. D. van der Ploeg, J. Woods, 1998, Molecular endocrinology.

Combinatorial library of indinavir analogues: replacement for the aminoindanol at P2'.

L. Kuo, W. Schleif, L. Gabryelski, 2002, Bioorganic & medicinal chemistry letters.

Solid phase synthesis of indinavir and its analogues.

K. Chapman, J. Tata, Z. Lu, 2000, Journal of combinatorial chemistry.

Combinatorial diversification of indinavir: in vivo mixture dosing of an HIV protease inhibitor library.

L. Kuo, W. Schleif, L. Gabryelski, 2000, Bioorganic & medicinal chemistry letters.

Highly potent, orally active diester macrocyclic human renin inhibitors.

R A Stearns, T. Halgren, A. Weber, 1992, Journal of medicinal chemistry.

HIV protease inhibitors with picomolar potency against PI-Resistant HIV-1 by extension of the P3 substituent.

Jiunn H. Lin, L. Kuo, W. Schleif, 2003, Bioorganic & medicinal chemistry letters.

Indinavir analogues with blocked metabolism sites as HIV protease inhibitors with improved pharmacological profiles and high potency against PI-resistant viral strains.

Yuan Cheng, Jiunn H. Lin, W. Schleif, 2002, Bioorganic & medicinal chemistry letters.

Synthesis and activity of novel HIV protease inhibitors with improved potency against multiple PI-resistant viral strains.

Jiunn H. Lin, L. Kuo, W. Schleif, 2002, Bioorganic & medicinal chemistry letters.

Direct observation (NMR) of the efficacy of glucagon receptor antagonists in murine liver expressing the human glucagon receptor.

V. Ding, Bei B. Zhang, G. Kaczorowski, 2006, Bioorganic & Medicinal Chemistry.

P1' oxadiazole protease inhibitors with excellent activity against native and protease inhibitor-resistant HIV-1.

W. Schleif, E. Emini, K. Chapman, 2004, Bioorganic & medicinal chemistry letters.

HIV-1 protease inhibitors with picomolar potency against PI-resistant HIV-1 by modification of the P1' substituent.

Jiunn H. Lin, L. Kuo, W. Schleif, 2003, Bioorganic & medicinal chemistry letters.

The design, synthesis and evaluation of novel HIV-1 protease inhibitors with high potency against PI-resistant viral strains.

Jiunn H. Lin, L. Kuo, W. Schleif, 2003, Bioorganic & medicinal chemistry letters.

The first stereoselective total synthesis of quinine.

J. Balkovec, G. Dake, R. Fujimoto, 2001, Journal of the American Chemical Society.

Design and biological activities of L-163,191 (MK-0677): a potent, orally active growth hormone secretagogue.

D. Johnston, A. Patchett, R. Nargund, 1995, Proceedings of the National Academy of Sciences of the United States of America.

P450 interaction with HIV protease inhibitors: relationship between metabolic stability, inhibitory potency, and P450 binding spectra.

J. Vacca, J. Lin, M. Chiba, 2001, Drug metabolism and disposition: the biological fate of chemicals.

The structure and kinetic reactivity of a pyrrolidine-derived vinylogous urethane lithium enolate

J. Tata, A. Adams, R. H. Schlessinger, 1986 .

The synthesis and activity of spiroindane growth hormone secretagogues

D. Johnston, Roy G. Smith, A. Patchett, 1997 .

Orally bioavailable highly potent HIV protease inhibitors against PI-resistant virus.

Jiunn H. Lin, W. Schleif, L. Gabryelski, 2005, Bioorganic & medicinal chemistry letters.

The synthesis and conformational analysis of amino acid-tetrahydroanthranilic acid hybrids

R. Mosley, R. Ball, J. Tata, 2008 .

Rapid Evolution of a Fragment-like Molecule to Pan-Metallo-Beta-Lactamase Inhibitors: Initial Leads toward Clinical Candidates

D. Wyss, A. Therien, T. Fischmann, 2022, Journal of Medicinal Chemistry.

Discovery of MK-1454: A Potent Cyclic Dinucleotide Stimulator of Interferon Genes Agonist for the Treatment of Cancer.

Andrew M Haidle, Matthew L. Maddess, J. Cumming, 2022, Journal of medicinal chemistry.

Novel glucocorticoids containing a 6,5-bicyclic core fused to a pyrazole ring: synthesis, in vitro profile, molecular modeling studies, and in vivo experiments.

D. Zaller, Amjad Ali, Douglas K. Miller, 2007, Bioorganic & medicinal chemistry letters.

A mass spectrometry-based proteome map of drug action in lung cancer cell lines

Andy Liaw, M. Glick, Benjamin Ruprecht, 2020, Nature Chemical Biology.

Peptidomimetic growth hormone secretagogues: synthesis and biological activities of analogs varied at the indole nucleus of the prototypical spiropiperidine L-162,752

Roy G. Smith, A. Patchett, R. Nargund, 1996 .

Substituted bridged phenyl piperidines: orally active growth hormone secretagogues.

A. Patchett, G. Hickey, Zhijian Lu, 2003, Bioorganic & medicinal chemistry letters.

Discovery of spirocyclic secondary amine-derived tertiary ureas as highly potent, selective and bioavailable soluble epoxide hydrolase inhibitors.

J. Berger, Gaochao Zhou, Sanjeev Kumar, 2009, Bioorganic & medicinal chemistry letters.

Potent and Selective Amidopyrazole Inhibitors of IRAK4 That Are Efficacious in a Rodent Model of Inflammation.

D. Tulshian, T. Fischmann, C. Garlisi, 2015, ACS medicinal chemistry letters.

Can We Make Small Molecules Lean? Optimization of a Highly Lipophilic TarO Inhibitor.

T. Roemer, S. Koseoglu, P. Tawa, 2017, Journal of medicinal chemistry.

Novel ketal ligands for the glucocorticoid receptor: in vitro and in vivo activity.

Scott K. Smith, D. Zaller, Amjad Ali, 2005, Bioorganic & medicinal chemistry letters.

Molecular modeling aided design of nicotinic acid receptor GPR109A agonists.

Ning Ren, Q. Deng, Steven L Colletti, 2008, Bioorganic & medicinal chemistry letters.

Highly potent growth hormone secretagogues.

A. Patchett, G. Hickey, Zhijian Lu, 2007, Bioorganic & medicinal chemistry letters.

Abstract 190: A Niacin Receptor Partial Agonist, MK-0354, Robustly Reduces Plasma Free Fatty Acids and Produces Little Flushing but Fails to Alter LDL-C, HDL-C, and Triglycerides in Humans

D. Connolly, J. Paolini, J. Wagner, 2007 .

Design, Synthesis, and Evaluation of Novel and Selective G-protein Coupled Receptor 120 (GPR120) Spirocyclic Agonists.

A. Crespo, E. Tozzo, F. Ujjainwalla, 2017, ACS medicinal chemistry letters.

Discovery of indazole aldosterone synthase (CYP11B2) inhibitors as potential treatments for hypertension.

M. Struthers, D. Macneil, D. Cully, 2017, Bioorganic & medicinal chemistry letters.

Discovery of Triazole CYP11B2 Inhibitors with in Vivo Activity in Rhesus Monkeys.

Michael E. Lassman, M. Struthers, Qingzhong Hu, 2015, ACS medicinal chemistry letters.

Discovery of Benzimidazole CYP11B2 Inhibitors with in Vivo Activity in Rhesus Monkeys.

Michael E. Lassman, Jeffrey T. Kuethe, M. Struthers, 2015, ACS medicinal chemistry letters.

Design and synthesis of highly potent HIV protease inhibitors with activity against resistant virus.

W. Schleif, L. Gabryelski, E. Emini, 2003, Bioorganic & medicinal chemistry letters.

Liquid dewetting of ultrathin polystyrene films: Is there a molecular architecture effect?

G. McKenna, J. Tata, Astrid K. Torres Arellano, 2020, Journal of Polymer Science.

Synthesis of novel HIV protease inhibitors (PI) with activity against PI-resistant virus.

W. Schleif, L. Gabryelski, E. Emini, 2007, Bioorganic & medicinal chemistry letters.

Discovery and Structure Enabled Synthesis of 2,6-Diaminopyrimidin-4-one IRAK4 Inhibitors.

D. Tulshian, T. Fischmann, C. Garlisi, 2015, ACS medicinal chemistry letters.

Discovery of Spirocyclic Aldosterone Synthase Inhibitors as Potential Treatments for Resistant Hypertension.

M. Struthers, D. Macneil, D. Cully, 2017, ACS medicinal chemistry letters.

Efforts towards the optimization of a bi-aryl class of potent IRAK4 inhibitors.

D. Tulshian, C. Garlisi, W. M. Seganish, 2016, Bioorganic & medicinal chemistry letters.

Niacin Lipid Efficacy Is Independent of Both the Niacin Receptor GPR109A and Free Fatty Acid Suppression

D. Rader, D. Connolly, Jiajun Liu, 2012, Science Translational Medicine.

From Screening to Targeted Degradation: Strategies for the Discovery and Optimization of Small Molecule Ligands for PCSK9.

Sujata Sharma, P. Orth, J. Shipman, 2021, Cell chemical biology.

Discovery of pyrazolyl propionyl cyclohexenamide derivatives as full agonists for the high affinity niacin receptor GPR109A.

Hong C Shen, X. Tong, Qing Chen, 2010, Bioorganic & medicinal chemistry letters.