Zobrazeno 1 - 10
of 110
pro vyhledávání: '"Jeffrey A Robl"'
Autor:
Ricardo A García, Debra J Search, John A Lupisella, Jacek Ostrowski, Bo Guan, Jian Chen, Wen-Pin Yang, Amy Truong, Aiqing He, Rongan Zhang, Mujing Yan, Samuel E Hellings, Peter S Gargalovic, Carol S Ryan, Linda M Watson, Robert A Langish, Petia A Shipkova, Nancy L Carson, Joseph R Taylor, Richard Yang, George C Psaltis, Thomas W Harrity, Jeffrey A Robl, David A Gordon
Publikováno v:
PLoS ONE, Vol 8, Iss 2, p e53192 (2013)
BACKGROUND: Chronic glucocorticoid excess has been linked to increased atherosclerosis and general cardiovascular risk in humans. The enzyme 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) increases active glucocorticoid levels within tissues by
Externí odkaz:
https://doaj.org/article/6bd68584051f4497b56fefb3bbb8522c
Autor:
James Kempson, Xiaoping Hou, Jung-Hui Sun, Michael Wong, Joseph Pawluczyk, Jianqing Li, Subramaniam Krishnananthan, Eric M. Simmons, Yi Hsiao, Yi-Xin Li, Dawn Sun, Dauh-Rurng Wu, Wei Meng, Saleem Ahmad, Lidet Negash, Robert Brigance, Huji Turdi, Jon J. Hangeland, R. Michael Lawrence, Pratik Devasthale, Jeffrey A. Robl, Arvind Mathur
Publikováno v:
Organic Process Research & Development. 26:1327-1335
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::35fda97669790a07bfdfb80a55523b6b
https://doi.org/10.1021/acs.oprd.2c00036
https://doi.org/10.1021/acs.oprd.2c00036
Autor:
Yan Shi, Ying Wang, Wei Meng, Robert P. Brigance, Denis E. Ryono, Scott Bolton, Hao Zhang, Sean Chen, Rebecca Smirk, Shiwei Tao, Joseph A. Tino, Kristin N. Williams, Richard Sulsky, Laura Nielsen, Bruce Ellsworth, Michael K. Y. Wong, Jung-Hui Sun, Leslie W. Leith, Dawn Sun, Dauh-Rurng Wu, Anuradha Gupta, Richard Rampulla, Arvind Mathur, Bang-Chi Chen, Aiying Wang, Helen G. Fuentes-Catanio, Lori Kunselman, Michael Cap, Jacob Zalaznick, Xiaohui Ma, Heng Liu, Joseph R. Taylor, Rachel Zebo, Beverly Jones, Stephen Kalinowski, Joann Swartz, Ada Staal, Kevin O’Malley, Lisa Kopcho, Jodi K. Muckelbauer, Stanley R. Krystek, Steven A. Spronk, Jovita Marcinkeviciene, Gerry Everlof, Xue-Qing Chen, Carrie Xu, Yi-Xin Li, Robert A. Langish, Yanou Yang, Qi Wang, Kamelia Behnia, Aberra Fura, Evan B. Janovitz, Nicola Pannacciulli, Steven Griffen, Bradley A. Zinker, John Krupinski, Mark Kirby, Jean Whaley, Robert Zahler, Joel C. Barrish, Jeffrey A. Robl, Peter T. W. Cheng
Publikováno v:
Journal of Medicinal Chemistry. 65:4291-4317
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::cc68196d2f5ecc2fc360366195341ffb
https://doi.org/10.1021/acs.jmedchem.1c02110
https://doi.org/10.1021/acs.jmedchem.1c02110
Autor:
Brian J. Murphy, Daniel Smith, Julia Sapuppo, Giridhar S. Tirucherai, Lawrence J. Kennedy, Ching-Hsuen Chu, Anthony V. Azzara, Shiwei Tao, Glenn D. Rosen, Subramaniam Krishnananthan, Jun Li, Victor R. Guarino, Lisa Burns, Joseph R. Taylor, Milinda Ziegler, Lakshmi Sivaraman, Bruce A. Ellsworth, Selvakumar Kumaravel, Hao Zhang, Tao Wang, Jun Shi, Atsu Apedo, Dhanusu Suresh, Kathy Mosure, Gerry Everlof, David A. Gordon, Lisa Zhang, Michael Gill, Chen-Pin Hung, Jianqing Li, Peter T. W. Cheng, Robert F. Kaltenbach, Sutjano Jusuf, Ying Wang, Stephanie Boehm, Mary Ellen Cvijic, Matthew G. Soars, Chi Shing Sum, Yan Shi, Jeffrey A. Robl, Reddigunta Ramesh Babu, Bradley A. Zinker, Yanou Yang, Stephen S. Kalinowski, Carrie Xu, Steven J. Walker, Sarah C. Traeger, Rebekah Heiry, Kimberley A. Lentz, Qian Ruan
Publikováno v:
Journal of Medicinal Chemistry. 64:15549-15581
The oxycyclohexyl acid BMS-986278 (33) is a potent lysophosphatidic acid receptor 1 (LPA1) antagonist, with a human LPA1 Kb of 6.9 nM. The structure-activity relationship (SAR) studies starting from the LPA1 antagonist clinical compound BMS-986020 (1
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::c00ce908946d21bafba2486eb2e08c90
https://doi.org/10.1021/acs.jmedchem.1c01256
https://doi.org/10.1021/acs.jmedchem.1c01256
Autor:
Shu Chang, Anthony V. Azzara, Yi-Xin Li, Marta Dabros, James Kempson, Reshma Panemangelor, Huji Turdi, Kimberly A. Foster, William J. Keim, Jean M. Whaley, Jeffrey A. Robl, Fang Moore, Luping Chen, Mary Jane Cullen, Xiaoping Hou, Atsu Apedo, R. Michael Lawrence, Arvind Mathur, David G. Harden, Wei Meng, Kevin O'Malley, Mary Ann Pelleymounter, Hannguang Chao, Pratik Devasthale, Jon J. Hangeland, Zhengping Ma, Dauh-Rurng Wu, Robert Paul Brigance, Guohua Zhao, Lynn M. Abell, Qi Gao, Susan Harvey, Lisa M. Kopcho, Dong Cheng, Elizabeth A. Dierks, Ching-Hsuen Chu, Suzanne Rooney, Xiang-Yang Ye, Saleem Ahmad, Wei Wang
Publikováno v:
Journal of Medicinal Chemistry. 64:14773-14792
MGAT2 inhibition is a potential therapeutic approach for the treatment of metabolic disorders. High-throughput screening of the BMS internal compound collection identified the aryl dihydropyridinone compound 1 (hMGAT2 IC50 = 175 nM) as a hit. Compoun
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::40e90999a2854f1a395c0459b5cd876d
https://doi.org/10.1021/acs.jmedchem.1c01356
https://doi.org/10.1021/acs.jmedchem.1c01356
Autor:
Mary Jane Cullen, Qian Xiang, Jeffrey A. Robl, Philip M. Sher, Brian J. Murphy, Keith J. Miller, Timothy M. Harper, Andrew Alt, Emily Luk, Sarah E. Malmstrom, Dean A. Wacker, Ginger Wu, Kimberly A. Foster, John M. Fevig, Joseph Carpenter, Robert L. Bertekap, Mary F. Grubb, Ying Wang, Karen A. Rossi, Gang Wu, Christian L. Morales, Jianxin Feng, Xiang Yang Ye, Anthony V. Azzara, Matthias Broekema
Publikováno v:
Journal of Medicinal Chemistry. 60:6166-6190
Agonism of the 5-HT2C receptor represents one of the most well-studied and clinically proven mechanisms for pharmacological weight reduction. Selectivity over the closely related 5-HT2A and 5-HT2B receptors is critical as their activation has been sh
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::9ab408370d6568ec38a8faeab8daced5
https://doi.org/10.1021/acs.jmedchem.7b00385
https://doi.org/10.1021/acs.jmedchem.7b00385
Autor:
Jeffrey A. Robl, Michael Thomas, Mary Ann Pelleymounter, Brian Gemzik, Anthony V. Azzara, Brian J. Murphy, Sharon N. Bisaha, Helen E. Godonis, Daniel Longhi, Neil Flynn, William N. Washburn, Kenneth W. Rohrbach, Khehyong Ngu, Saleem Ahmad, Susan Harvey, Christine Huang, Evan B. Janovitz, Andres S. Hernandez, James Devenny, Hongwei Zhang, Lisa Zhang, Susan Glick, Suzanne Rooney, Wei Wang
Publikováno v:
Journal of Medicinal Chemistry. 59:8848-8858
The potent MCHR1 in vitro and in vivo antagonist activity of a series of cyclic tertiary alcohols derived from compound 2b is described. Subsequent pharmacokinetic and pharmacodynamic studies identified BMS-814580 (compound 10) as a highly efficaciou
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::b952b4585a825fd9a757591676fa67d8
https://doi.org/10.1021/acs.jmedchem.6b00676
https://doi.org/10.1021/acs.jmedchem.6b00676
Autor:
Paul E. Morin, Haixia Wang, Lawrence J. Kennedy, Stephen P. O'connor, James J. Li, Akbar Nayeem, Vidhyashankar Ramamurthy, Steven Sheriff, Nathan Morgan, Steven J. Walker, Xiang-Yang Ye, Frederick Moulin, Brad D. Maxwell, Thomas Harrity, Jeffrey A. Robl, Stephanie Y. Chen, Timothy W. Harper, Rachel Zebo, Jun Li, Zhenqiu Hong, Shung Wu, Mengmeng Wang, Randolph P. Ponticiello, David A. Gordon, Rajasree Golla, Ramakrishna Seethala, Daniel M. Camac, Joseph R. Taylor, David S. Yoon
[Image: see text] BMS-823778 (2), a 1,2,4-triazolopyridinyl-methanol derived analog, was identified as a potent and selective inhibitor of human 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD-1) enzyme (IC(50) = 2.3 nM) with >10,000-fold selectiv
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::537bf023154f9aff48423a9bc7df61b2
https://europepmc.org/articles/PMC6295842/
https://europepmc.org/articles/PMC6295842/
Autor:
Gary G. Cao, Min Zhou, Ramya Jayaram, Douglas B. Moore, Andres S. Hernandez, Tao Wang, Jean M. Whaley, Yue-Zhong Shu, Carrie Xu, Lori Kunselman, Atsu Apedo, William R. Ewing, Reshma Panemangalore, Qi Gao, Arvind Mathur, Richard Rampulla, Bradley A. Zinker, Lauren Haque, Mary Ellen Cvijic, Marta Dabros, Arun Kumar Gupta, Heng Liu, Jeffrey A. Robl, Bruce A. Ellsworth, Jun Shi, Zhengxiang Gu, Jason J. Wilkes, Akin H. Davulcu, Kristin N. Williams, Elizabeth A. Dierks, John Krupinski, Zhenqiu Hong, Edward J. Brady, Ximao Wu, Qin Sun, Hong Cai, Chunshan Xie, Elizabeth A. Jurica, Kimberly A. Foster
Publikováno v:
Journal of medicinal chemistry. 61(3)
G protein-coupled receptor 40 (GPR40) has become an attractive target for the treatment of diabetes since it was shown clinically to promote glucose-stimulated insulin secretion. Herein, we report our efforts to develop highly selective and potent GP
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0fbe81ca0de7013eecb9cd7ee4d58d5d
https://pubmed.ncbi.nlm.nih.gov/29316397
https://pubmed.ncbi.nlm.nih.gov/29316397
Autor:
Neil Flynn, Mary Jane Cullen, Hongwei Zhang, Wei Wang, Susan Glick, Lisa Zhang, Jeffrey A. Robl, Pratik Devasthale, Andres S. Hernandez, Christian Caporuscio, Brian J. Murphy, Suzanne Rooney, Ning Huang, Mary Ann Pelleymounter, Kenneth W. Rohrbach, Kishore Renduchintala, Anthony V. Azzara, Helen E. Godonis, Yi-Xin Li, Radhakrishnan Sridhar, Michael Thomas, Susan Harvey, Paul Stetsko, Mary F. Grubb, Chris Freeden, Fang Moore, Christine Huang, James Devenny, Daniel Longhi, William N. Washburn
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 25:2793-2799
Our investigation of the structure–activity and structure–liability relationships for dihydropyrrolopyrazol-6-one MCHR1 antagonists revealed that off-rate characteristics, inferred from potencies in a FLIPR assay following a 2 h incubation, can i
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::17121b519c7b9c469d07059362c3d928
https://doi.org/10.1016/j.bmcl.2015.05.008
https://doi.org/10.1016/j.bmcl.2015.05.008