Zobrazeno 1 - 10
of 22
pro vyhledávání: '"Edward J. Brady"'
Autor:
James Mu, Sajjad A Qureshi, Edward J Brady, Eric S Muise, Mari Rios Candelore, Guoqiang Jiang, Zhihua Li, Margaret S Wu, Xiaodong Yang, Qing Dallas-Yang, Corey Miller, Yusheng Xiong, Ronald B Langdon, Emma R Parmee, Bei B Zhang
Publikováno v:
PLoS ONE, Vol 7, Iss 11, p e49572 (2012)
Hyperglucagonemia is implicated in the pathophysiology of hyperglycemia. Antagonism of the glucagon receptor (GCGR) thus represents a potential approach to diabetes treatment. Herein we report the characterization of GRA1, a novel small-molecule GCGR
Externí odkaz:
https://doaj.org/article/d41be1e4e3c94bbbb634399a73d5972e
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:
Steve Mock, Guoquiang Jiang, Song Zheng, James R. Tata, Dong-Ming Shen, Kevin T. Chapman, Xiaodong Yang, Sajjad A. Qureshi, Xiaolan Shen, Edward J. Brady, Bei B. Zhang, Margaret E. McCann, Xinchun Tong, Emma R. Parmee, Mari R. Candelore, Laurie Tota, William P. Feeney, Victor D.-H. Ding, Michael Wright, Richard Saperstein, Qing Dallas-Yang
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:76-81
A novel class of 1,3,5-pyrazoles has been discovered as potent human glucagon receptor antagonists. Notably, compound 26 is orally bioavailable in several preclinical species and shows selectivity towards cardiac ion channels, other family B receptor
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::598a01439adc406e046e5ad6d160d2f0
https://doi.org/10.1016/j.bmcl.2010.11.074
https://doi.org/10.1016/j.bmcl.2010.11.074
Autor:
Constantin Tamvakopolous, Rui Liang, Emma R. Parmee, Lauren Abrardo, Song Zheng, Bei B. Zhang, Sharon Tong, James R. Tata, Steve Mock, Michael Wright, Mari R. Candelore, Victor D.-H. Ding, Edward J. Brady, Richard Saperstein, Laurie Tota
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:587-592
A series of conformationally constrained tri-substituted ureas were synthesized, and their potential as glucagon receptor antagonists was evaluated. This effort resulted in the identification of compound 4a, which had a binding IC50 of 4.0 nM and was
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1fa30cbe651c82bd44e412b97a827a15
https://doi.org/10.1016/j.bmcl.2006.11.014
https://doi.org/10.1016/j.bmcl.2006.11.014
Autor:
Xiaodong Yang, Guoqiang Jiang, Emma R. Parmee, Songnian Lin, James R. Tata, Gary G. Chicchi, Laurie Tota, Bei B. Zhang, Maria E. Trujillo, Corey Miller, Fengqi Zhang, Edward J. Brady, Alka Bansal, Sajjad A. Qureshi, Gino Salituro
Publikováno v:
Bioorganicmedicinal chemistry letters. 25(19)
A novel, potent series of glucagon receptor antagonists (GRAs) was discovered. These indazole- and indole-based compounds were designed on an earlier pyrazole-based GRA lead MK-0893. Structure–activity relationship (SAR) studies were focused on the
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::002b78d75ac42fc8e60e6fc67fe968e9
https://pubmed.ncbi.nlm.nih.gov/26303893
https://pubmed.ncbi.nlm.nih.gov/26303893
Autor:
Rui Liang, Lauri M. Tota, Kevin T. Chapman, Joseph L. Duffy, Xiaodong Yang, Frank Xiaoqing Liu, Guoqiang Jiang, Edward J. Brady, Brian A. Kirk, Song Zheng, Zenon Konteatis, James R. Tata, Mari R. Candelore, Deborah Szalkowski, Sharon Tong, Bei B. Zhang, Victor D.-H. Ding, Elizabeth Louise Campbell, Richard Saperstein, Sajjad A. Qureshi, Dan Xie, Peter Zafian
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:1401-1405
A novel class of antagonists of the human glucagon receptor (hGCGR) has been discovered. Systematic modification of the lead compound identified substituents that were essential for activity and those that were amenable to further optimization. This
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::02875fe32941a428c96a4c4eb4d22e48
https://doi.org/10.1016/j.bmcl.2005.01.003
https://doi.org/10.1016/j.bmcl.2005.01.003
Autor:
Victor D.-H. Ding, Dan Xie, Kun Liu, Dawn E. Biazzo-Ashnault, Libo Xu, Xiaolan Shen, James V. Heck, Su Er W Huskey, A. Brian Jones, David E. Moller, Richard Saperstein, Zhihua Li, Bei B. Zhang, Deborah Szalkowski, Edward J. Brady, Gino Salituro, Sajjad A. Qureshi
Publikováno v:
Journal of Biological Chemistry. 275:36590-36595
We recently described the identification of a non-peptidyl fungal metabolite (l-783,281, compound 1), which induced activation of human insulin receptor (IR) tyrosine kinase and mediated insulin-like effects in cells, as well as decreased blood gluco
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9d4d1ebd322ee3b57f91142ab2688833
https://doi.org/10.1074/jbc.m006287200
https://doi.org/10.1074/jbc.m006287200
Autor:
Catherine D. Strader, M J Forrest, Jennifer E. Hutchins, R R Miller, Shuet Hing L Chiu, D. E. Macintyre, G J Hom, R A Stearns, T J Bach, Margaret A. Cascieri, Linda J. Kelly, A M Amend, Joseph M. Metzger, D Carroll, Mari R. Candelore, Xiao-Ming Guan, B Hegarty-Friscino, E R Parmee, Edward J. Brady, Liping Deng, Robert J. Mathvink, Richard Saperstein, M. H. Fisher, J M Barker, H O Ok
Publikováno v:
Journal of Clinical Investigation. 101:2387-2393
Activation of beta3 adrenergic receptors on the surface of adipocytes leads to increases in intracellular cAMP and stimulation of lipolysis. In brown adipose tissue, this serves to up-regulate and activate the mitochondrial uncoupling protein 1, whic
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6f1404accbdc3cd2636c4cec78d6c417
https://doi.org/10.1172/jci2496
https://doi.org/10.1172/jci2496
Autor:
Zhihua Li, Bei B. Zhang, Corey Miller, James Mu, Emma R. Parmee, Guoqiang Jiang, Eric S. Muise, Margaret Wu, Sajjad A. Qureshi, Xiong Yusheng, Edward J. Brady, Mari R. Candelore, Ronald B. Langdon, Xiaodong Yang, Qing Dallas-Yang
Publikováno v:
PLoS ONE
PLoS ONE, Vol 7, Iss 11, p e49572 (2012)
PLoS ONE, Vol 7, Iss 11, p e49572 (2012)
Hyperglucagonemia is implicated in the pathophysiology of hyperglycemia. Antagonism of the glucagon receptor (GCGR) thus represents a potential approach to diabetes treatment. Herein we report the characterization of GRA1, a novel small-molecule GCGR
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4bb3d4fb72faaf4add1a0c774c067ef5
https://pubmed.ncbi.nlm.nih.gov/23185367
https://pubmed.ncbi.nlm.nih.gov/23185367
Autor:
Richard Saperstein, Terry Reisine, Byron H. Arison, William J. Paleveda, Roger M. Freidinger, Edward J. Brady, Stephen F. Brady, Karen Raynor, D. F. Veber
Publikováno v:
Tetrahedron. 49:3449-3466
In testing and refining our model of the receptor-bound conformation of the potent small-ring somatostatin analog cyclo-(Pro6-Phe7-D-Trp8-Lys9-Thr10-Phe11), we have investigated structures constrained within bicyclic systems. Specifically, we have in
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::8994517db01b2dfdf048ef82df13560c
https://doi.org/10.1016/s0040-4020(01)90206-6
https://doi.org/10.1016/s0040-4020(01)90206-6