Zobrazeno 1 - 10
of 41
pro vyhledávání: '"John S. Debenham"'
Autor:
Santhosh Satapati, Ying Qian, Margaret S. Wu, Aleksandr Petrov, Ge Dai, Sheng-ping Wang, Yonghua Zhu, Xiaolan Shen, Eric S. Muise, Ying Chen, Emanuel Zycband, Adam Weinglass, Jerry Di Salvo, John S. Debenham, Jason M. Cox, Ping Lan, Vinit Shah, Stephen F. Previs, Mark Erion, David E. Kelley, Liangsu Wang, Andrew D. Howard, Jin Shang
Publikováno v:
Journal of Lipid Research, Vol 58, Iss 8, Pp 1561-1578 (2017)
GPR40 and GPR120 are fatty acid sensors that play important roles in glucose and energy homeostasis. GPR40 potentiates glucose-dependent insulin secretion and demonstrated in clinical studies robust glucose lowering in type 2 diabetes. GPR120 improve
Externí odkaz:
https://doaj.org/article/1d5d6bb81f4b48f7aa3c095bb5ab4e88
Autor:
Wensheng Yu, Maofen Chen, Takao Suzuki, Zhiqi Qi, Bin Hu, Jianming Bao, John S. Debenham, Na Meng, Joseph L. Duffy, Robert Mazzola
Publikováno v:
The Journal of Organic Chemistry. 86:5560-5567
A mild condition via PPh3/I2/imidazole for the deoxygenation of substituted methanol derivatives has been identified. This metal-free process was found to proceed well on secondary or tertiary alcohols substituted with one or two heteroaryl groups, a
Autor:
Jerry Di Salvo, Santhosh Satapati, Mark D. Erion, Jin Shang, Stephen F. Previs, Adam B. Weinglass, John S. Debenham, Margaret Wu, Sheng-Ping Wang, Andrew D. Howard, Ying Chen, Aleksandr Petrov, Ge Dai, Yonghua Zhu, Liangsu Wang, David E. Kelley, Ying Qian, Xiaolan Shen, Eric S. Muise, Jason M. Cox, Ping Lan, Vinit Shah, Emanuel Zycband
Publikováno v:
Journal of Lipid Research, Vol 58, Iss 8, Pp 1561-1578 (2017)
GPR40 and GPR120 are fatty acid sensors that play important roles in glucose and energy homeostasis. GPR40 potentiates glucose-dependent insulin secretion and demonstrated in clinical studies robust glucose lowering in type 2 diabetes. GPR120 improve
Autor:
Julie A. DeMartino, James A. Milligan, Edward C. Sherer, Thomas F. Walsh, Richard Hajdu, Russell B. Lingham, Xinchun Tong, Michael Wolff, Denise M. Visco, Mikhail Reibarkh, Matthew J. Clements, Jeffrey T. Kuethe, Randy R. Miller, Christina B. Madsen-Duggan, Lisa M. Sonatore, Scott P. Salowe, Dominique Stickens, Jianmei Pang, Jeffrey J. Hale, Dan Zhou, John S. Debenham
Publikováno v:
Journal of medicinal chemistry. 59(24)
The discovery of novel 4-hydroxy-2-(heterocyclic)pyrimidine-5-carboxamide inhibitors of hypoxia-inducible factor (HIF) prolyl hydroxylases (PHD) is described. These are potent, selective, orally bioavailable across several species, and active in stim
Autor:
Yong Zhang, Jeffrey J. Hale, Andreas Verras, Shirly Pinto, Huaibing He, Zhu Shen, Urmi R. Bhatt, Elaine C. Tung, John S. Debenham, Matthew J. Clements, Dunlu Chen, Dong-Ming Shen, Wayne M. Geissler, Thomas H. Graham, JeanMarie Lisnock, Qing Chen, Suoyu Xu, Xiaohua Li, Margarita Garcia-Calvo, Wensheng Liu, Xinchun Tong, Judyann Wiltsie, Christina B. Madsen-Duggan, Jeffrey T. Kuethe
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:6228-6233
The synthesis, SAR, binding affinities and pharmacokinetic profiles are described for a series of cyclohexane-based prolylcarboxypeptidase (PrCP) inhibitors discovered by high throughput screening. Compounds show high levels of ex vivo target engagem
Autor:
John S. Debenham, Dann L. Parker, Birgit T. Priest, Ravi P. Nargund, Feroze Ujjainwalla, Randal M. Bugianesi, Michele Pachanski, Liangqin Guo, William K. Hagmann, George J. Eiermann, Yi Zang, Ramzi F. Sweis, Andrew D. Howard, Jenna L. Terebetski, Melissa Kirkland, Yue Feng, Gino Salituro, Derun Li, Christopher Joseph Sinz, Stan Mitelman, Maria E. Trujillo, Scott D. Edmondson, Karen H. Dingley, Jin Shang, Nicole Buist, Xiaofang Li, Weiguo Liu, Mary Ann Powles, Terri M. Kelly, Edward C. Sherer
GPR142 has been identified as a potential glucose-stimulated insulin secretion (GSIS) target for the treatment of type 2 diabetes mellitus (T2DM). A class of triazole GPR142 agonists was discovered through a high throughput screen. The lead compound
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::05666abdc0e69d7961b4edf099a12f0b
https://europepmc.org/articles/PMC5150677/
https://europepmc.org/articles/PMC5150677/
Autor:
Christopher Joseph Sinz, Sarah Souza, Aimie M. Ogawa, Dennis Leung, Eric R. Ashley, Brande Thomas-Fowlkes, Maria Madeira, Mary Ann Powles, Effie Tozzo, Hong D. Chu, Feroze Ujjainwalla, Melissa Kirkland, Matthew Lombardo, Clare London, Jerry Di Salvo, Keith Eagen, John S. Debenham, Jason M. Cox, Ping Lan, Alejandro Crespo, Adam B. Weinglass, Taro E. Akiyama, Nengxue Wang, Henry M. Vaccaro, Michele Pachanski, Shah Unmesh G, Zhongxiang Sun, Mariappan V. Chelliah, James R. Tata, Michael A. Plotkin, Candice Alleyne, Takao Suzuki, Srikanth Venkatraman
Publikováno v:
ACS medicinal chemistry letters. 8(1)
Type 2 diabetes mellitus (T2DM) is an ever increasing worldwide epidemic, and the identification of safe and effective insulin sensitizers, absent of weight gain, has been a long-standing goal of diabetes research. G-protein coupled receptor 120 (GPR
Autor:
Junying Wang, Richard G. Ball, Chun-Pyn Shen, Richard Z. Chen, Julie Lao, Vijay Bhasker G. Reddy, Xinchun Tong, Jeffrey J. Hale, Alison M. Strack, Jing Chen Xiao, Lauren P. Shearman, John S. Debenham, Tung M. Fong, D. Sloan Stribling, Christina B. Madsen-Duggan, Pei Huo, Lin Yan, Nancy N. Tsou, Thomas Bateman
Publikováno v:
Journal of Medicinal Chemistry. 53:4028-4037
This paper describes the discovery of N-[(4R)-6-(4-chlorophenyl)-7-(2,4-dichlorophenyl)-2,2-dimethyl-3,4-dihydro-2H-pyrano[2,3-b]pyridin-4-yl]-5-methyl-1H-pyrazole-3-carboxamide (MK-5596, 12c) as a novel cannabinoid-1 receptor (CB1R) inverse agonist
Autor:
Alison M. Strack, Xinchun Tong, Christina B. Madsen-Duggan, Lauren P. Shearman, Cathy R.-R.C. Huang, Mark T. Goulet, Thomas F. Walsh, Yue Feng, Jing Chen Xiao, D. Sloan Stribling, Junying Wang, John S. Debenham, Tung M. Fong, Chun-Pyn Shen, Sanjeev Kumar, Julie Lao, Donald J. Marsh, Richard B. Toupence
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:1448-1452
The synthesis, SAR and binding affinities of cannabinoid-1 receptor (CB1R) inverse agonists based on furo[2,3-b]pyridine scaffolds are described. Food intake, mechanism specific efficacy, pharmacokinetic, and metabolic evaluation of several of these
Autor:
Junying Wang, Jing Chen Xiao, D. Sloan Stribling, Marie-Therese Schaeffer, Alison M. Strack, Lauren P. Shearman, Cathy C. R.-R. Huang, D. Euan MacIntyre, Thomas F. Walsh, Christina B. Madsen-Duggan, Chun-Pyn Shen, John S. Debenham, Jeffrey J. Hale, Tung M. Fong, Julie Lao, Xinchun Tong
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:2591-2594
The synthesis, SAR and binding affinities are described for cannabinoid-1 receptor (CB1R) specific inverse agonists based on pyridopyrimidine and heterotricyclic scaffolds. Food intake and pharmacokinetic evaluation of several of these compounds indi