Zobrazeno 1 - 10
of 15
pro vyhledávání: '"Jason J. Wilkes"'
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
Discovery of Pyrrolidine-Containing GPR40 Agonists: Stereochemistry Effects a Change in Binding Mode
Autor:
William R. Ewing, Carrie Xu, Heng Liu, Brian J. Murphy, Neil Flynn, Tao Wang, Douglas B. Moore, Lori Kunselman, Bruce A. Ellsworth, Elizabeth A. Jurica, Kimberly A. Foster, Atsu Apedo, Yuan Tian, Yang Hong, Arvind Mathur, Bradley A. Zinker, Biji Jacob, Kristin N. Williams, Min Zhou, Brad D. Maxwell, Gary Cao, Andres S. Hernandez, Qin Sun, Hong Cai, Jean M. Whaley, Elizabeth A. Dierks, Joel C. Barrish, Dora M. Schnur, Ximao Wu, Doree F. Sitkoff, Mary Ellen Cvijic, Richard Rampulla, Chunshan Xie, David S. Nirschl, Reshma Panemangalore, Michael B. Hicks, Jeffrey A. Robl, Jason J. Wilkes
Publikováno v:
Journal of medicinal chemistry. 60(4)
A novel series of pyrrolidine-containing GPR40 agonists is described as a potential treatment for type 2 diabetes. The initial pyrrolidine hit was modified by moving the position of the carboxylic acid, a key pharmacophore for GPR40. Addition of a 4-
Multi-tissue, selective PPARγ modulation of insulin sensitivity and metabolic pathways in obese rats
Autor:
Shankar Subramaniam, Jason J. Wilkes, Jamie L. Resnik, Divya Thapar, Gene Hsiao, Jachelle M. Ofrecio, Dorothy D. Sears, Justin Chapman
Publikováno v:
American Journal of Physiology-Endocrinology and Metabolism. 300:E164-E174
Peroxisome proliferator-activated receptor-γ (PPARγ) ligands, including the insulin-sensitizing thiazolidinedione drugs, transcriptionally regulate hundreds of genes. Little is known about the relationship between PPARγ ligand-specific modulation
Publikováno v:
Diabetes
OBJECTIVE Insulin resistance develops in tandem with obesity. Ablating myostatin (Mstn) prevents obesity, so we investigated if Mstn deficiency could improve insulin sensitivity. A loss-of-function mutation (MstnLn) in either one or both alleles of t
Autor:
Elizabeth Nelson, M. T. Audrey Nguyen, Gautam Bandyopadhyay, Jerrold M. Olefsky, Jason J. Wilkes
Publikováno v:
American Journal of Physiology-Endocrinology and Metabolism. 289:E1015-E1022
We show that Topiramate (TPM) treatment normalizes whole body insulin sensitivity in high-fat diet (HFD)-fed male Wistar rats. Thus drug treatment markedly lowered glucose and insulin levels during glucose tolerance tests and caused increased insulin
Autor:
Jason J. Wilkes, Elizabeth Nelson, Melville C. Osborne, Jerrold M. Olefsky, Keith T. Demarest
Publikováno v:
American Journal of Physiology-Endocrinology and Metabolism. 288:E617-E624
We have studied the in vivo and in vitro effects of Topiramate (TPM) in female Zucker diabetic fatty (ZDF) rats. After weight matching, drug treatment had a marked effect to lower fasting glucose levels of relatively normoglycemic animals as well as
Autor:
Andrea L. Hevener, Gautam Bandyopadhyay, Weimin He, Jerrold M. Olefsky, Jamie Le, Yaacov Barak, Ronald M. Evans, Jason J. Wilkes, Peter Olson
Publikováno v:
Nature Medicine. 9:1491-1497
Thiazolidinediones (TZDs) are insulin-sensitizing drugs and are potent agonists of the nuclear peroxisome proliferator-activated receptor-gamma (PPAR-gamma). Although muscle is the major organ responsible for insulin-stimulated glucose disposal, PPAR
Autor:
Arend Bonen, Jason J. Wilkes
Publikováno v:
American Journal of Physiology-Endocrinology and Metabolism. 279:E912-E919
Insulin signaling was examined in muscle made insulin resistant by short-term (24-h) denervation. Insulin-stimulated glucose transport in vitro was reduced by 28% ( P < 0.05) in denervated muscle (DEN). In control muscle (SHAM), insulin increased lev
Publikováno v:
American Journal of Physiology-Endocrinology and Metabolism. 271:E477-E484
Ethanol consumption has been associated with glucose intolerance and insulin resistance and is suggested to be an independent risk factor in the development of non-insulin-dependent diabetes mellitus. We have investigated the long-term effects of eth
Autor:
Jamie L. Resnik, Jachelle M. Ofrecio, Jaap G. Neels, Joseph G. Yu, Philip D.G. Miles, Jason J. Wilkes, Saswata Talukdar, Kristen Johnson, Justin Chapman, Divya Thapar, Dorothy D. Sears
Publikováno v:
PLoS ONE
PLoS ONE, Vol 5, Iss 11, p e13959 (2010)
PLoS ONE, Vol 5, Iss 11, p e13959 (2010)
Background Insulin resistance is manifested in muscle, adipose tissue, and liver and is associated with adipose tissue inflammation. The cellular components and mechanisms that regulate the onset of diet-induced insulin resistance are not clearly def