Zobrazeno 1 - 10
of 38
pro vyhledávání: '"Jonathan B. Houze"'
Autor:
Jian Luo, Gayathri Swaminath, Sean P Brown, Jane Zhang, Qi Guo, Michael Chen, Kathy Nguyen, Thanhvien Tran, Lynn Miao, Paul J Dransfield, Marc Vimolratana, Jonathan B Houze, Simon Wong, Maria Toteva, Bei Shan, Frank Li, Run Zhuang, Daniel C-H Lin
Publikováno v:
PLoS ONE, Vol 7, Iss 10, p e46300 (2012)
Type 2 diabetes is characterized by impaired glucose homeostasis due to defects in insulin secretion, insulin resistance and the incretin response. GPR40 (FFAR1 or FFA1) is a G-protein-coupled receptor (GPCR), primarily expressed in insulin-producing
Externí odkaz:
https://doaj.org/article/0849b9dfe7b244fab2862894d2869154
Autor:
Daniel C-H Lin, Jane Zhang, Run Zhuang, Frank Li, Kathy Nguyen, Michael Chen, Thanhvien Tran, Edwin Lopez, Jenny Ying Lin Lu, Xiaoyan Nina Li, Liang Tang, George R Tonn, Gayathri Swaminath, Jeff D Reagan, Jin-Long Chen, Hui Tian, Yi-Jyun Lin, Jonathan B Houze, Jian Luo
Publikováno v:
PLoS ONE, Vol 6, Iss 11, p e27270 (2011)
Agonists of GPR40 (FFA1) have been proposed as a means to treat type 2 diabetes. Through lead optimization of a high throughput screening hit, we have identified a novel GPR40 agonist called AMG 837. The objective of these studies was to understand t
Externí odkaz:
https://doaj.org/article/729ea24e76304c709713d2c9927fb903
Autor:
Jonathan B. Houze, Andrea Boden, Ning Li, Dongming M. Liu, Xun Li, Jing Man Wong, Paul John Dransfield, Khanh Nguyen, Sridharan Rajamani, Gayathri Swaminath, Weston Sutherland, Yaping Sun, Ying Zhang, Vatee Pattaropong, Rhonda Chen, Vishnu Chintalgattu, Xiaochuan Ma, Murielle M. Véniant, Jim R. Turk, Ray W. Chui, Jinghong Wang, BaoXi Gao, Mark R. Fielden, Joyce Chi Yee Chan, Hugo M. Vargas, Kimberly M. Hoagland, Yinhong Chen, Yusheng Qu, Aarif Y. Khakoo, Shirley Mihardja, Qi Guo, Brandon Ason, Liaoyuan A. Hu, Ji Ma
Publikováno v:
JCI Insight
Heart failure (HF) remains a grievous illness with poor prognosis even with optimal care. The apelin receptor (APJ) counteracts the pressor effect of angiotensin II, attenuates ischemic injury, and has the potential to be a novel target to treat HF.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3042c04a79fb6373e3d1699adde8eb0a
https://pubmed.ncbi.nlm.nih.gov/32208384
https://pubmed.ncbi.nlm.nih.gov/32208384
Autor:
Jian Luo, Jinqian Liu, Jane Zhang, Jonathan B. Houze, Todd J. Kohn, Run Zhuang, Simon Wong, Michael D. Bartberger, Zhihua Ma, Daniel C.-H. Lin, Yingcai Wang, George Tonn, Jiwen Jim Liu, Frank Li, Liusheng Zhu, An-Rong Li, Julio C. Medina, Rajiv Sharma
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 26:15-20
As a follow-up to the GPR40 agonist AMG 837, which was evaluated in clinical trials for the treatment of type II diabetes, further optimization led to the discovery of AM-3189 (13k). AM-3189 is representative of a new class of compounds with minimal
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1fd9f66e7e014e23d509ba4642700f1c
https://doi.org/10.1016/j.bmcl.2015.11.050
https://doi.org/10.1016/j.bmcl.2015.11.050
Autor:
Paul John Dransfield, Simon Wong, Gayathri Swaminath, Vatee Pattaropong, Jian Luo, Liusheng Zhu, Jonathan B. Houze, Jane Zhang, Xianyun Jiao, Sean P. Brown, Daniel C.-H. Lin, Run Zhuang, Marc Vimolratana
Publikováno v:
ACS medicinal chemistry letters. 9(7)
[Image: see text] GPR40 (FFA1) is a G-protein-coupled receptor, primarily expressed in pancreatic islets and enteroendocrine L-cells, and, when activated, elicits increased insulin secretion only in the presence of elevated glucose levels. We recentl
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::26bbedd0ac22ff10e7062f8a3e38c225
https://pubmed.ncbi.nlm.nih.gov/30034614
https://pubmed.ncbi.nlm.nih.gov/30034614
Autor:
Jia-Nan Gong, Angela Coxon, Sean Caenepeel, Cyril H. Benes, Andrew W. Roberts, Tao Osgood, Donia M Moujalled, Elaina Cajulis, Andrew H. Wei, Regina K. Egan, Mario G. Cardozo, Pedro J. Beltran, Liusheng Zhu, Marc Vimolratana, Sean P. Brown, Brian Lucas, Xin Huang, Gordon Moody, Paul E. Hughes, David C.S. Huang, Giovanna Pomilio, Joshua Taygerly, Jan Sun, Danny Chui, Leszek Poppe, Jude Canon, Douglas A. Whittington, Yunxiao Li, Manuel Zancanella, Nick A. Paras, Joseph McClanaghan, Xianghong Wang, Alan C. Cheng, Kathleen S. Keegan, Jonathan B. Houze, Leah J. Damon, Patricia Greninger, Brian Belmontes
Publikováno v:
Cancer discovery. 8(12)
The prosurvival BCL2 family member MCL1 is frequently dysregulated in cancer. To overcome the significant challenges associated with inhibition of MCL1 protein–protein interactions, we rigorously applied small-molecule conformational restriction, w
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5ecf4086e51963a2ef56014b0508efb2
https://pubmed.ncbi.nlm.nih.gov/31262746
https://pubmed.ncbi.nlm.nih.gov/31262746
Autor:
Jason Duquette, Xin Huang, Dongyin Yu, Yun Ling, Jing Zhou, Yu Chung Wang, Daqing Sun, Sarah Wortman, John Eksterowicz, Qiuping Ye, Min Jiang, Jonathan D. Oliner, Lixia Jin, Alexander M. Long, Ana Z. Gonzalez, Peter Yakowec, Yihong Li, Steven H. Olson, Anne Y. Saiki, Hilary Plake Beck, Yosup Rew, Lawrence R. McGee, Julio C. Medina, Jonathan B. Houze, Jiasheng Fu, Jude Canon, Mcintosh Joel, Ada Chen, Brian M. Fox, Mei-Chu Lo, Xuelei Yan, Paul L. Shaffer, Zhihong Li, Tao Osgood, Xiaoning Zhao
Publikováno v:
Journal of Medicinal Chemistry. 57:10499-10511
Structure-based rational design and extensive structure-activity relationship studies led to the discovery of AMG 232 (1), a potent piperidinone inhibitor of the MDM2-p53 association, which is currently being evaluated in human clinical trials for th
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a6411aa1211e82e797ec19f5aeedd623
https://doi.org/10.1021/jm501550p
https://doi.org/10.1021/jm501550p
Autor:
Kevin Ronald Condroski, Susan P. Rhodes, Maralee McVean, Walter C. Voegtli, Christopher F. Kraser, Walter E. DeWolf, Lance A. Williams, Deborah Anderson, Hillary L. Sturgis, Boyd Steven A, Ronald Jay Hinklin, Jonathan B. Houze, Brian R. Baer, Thomas Daniel Aicher
Publikováno v:
Journal of Medicinal Chemistry. 57:8180-8186
Glucokinase (GK) is the rate-limiting step for insulin release from the pancreas in response to high levels of glucose. Flux through GK also contributes to reducing hepatic glucose output. Since many individuals with type 2 diabetes appear to have an
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a4219b54bd65bb5107d78fbd7952c7d1
https://doi.org/10.1021/jm501204z
https://doi.org/10.1021/jm501204z
Autor:
Ada Chen, Steven H. Olson, Alexander M. Long, John Eksterowicz, Michael D. Bartberger, Jing Zhou, Yosup Rew, Lawrence R. McGee, Mei-Chu Lo, Anne Y. Saiki, Dongyin Yu, Jason Duquette, Xuelei Yan, Ana Z. Gonzalez, Hilary Plake Beck, Jonathan B. Houze, Yun Ling, Mcintosh Joel, Jonathan D. Oliner, Sarah Wortman, Jude Canon, Daqing Sun, Dustin McMinn, Brian M. Fox, Paul L. Shaffer, Xiaoning Zhao, Tao Osgood, Lixia Jin, Xin Huang, Zhihong Li, David Chow, Qiuping Ye, Yihong Li, Jiasheng Fu, Peter Yakowec, Julio C. Medina
Publikováno v:
Journal of Medicinal Chemistry. 57:2472-2488
We previously reported the discovery of AMG 232, a highly potent and selective piperidinone inhibitor of the MDM2-p53 interaction. Our continued search for potent and diverse analogues led to the discovery of novel morpholinone MDM2 inhibitors. This
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::de1d3d1db724c5401afea1de13f776b9
https://doi.org/10.1021/jm401767k
https://doi.org/10.1021/jm401767k
Autor:
Run Zhuang, Qi Guo, Xianyun Jiao, Thanhvien Tran, Jonathan B. Houze, Frank Li, Paul John Dransfield, Jane Zhang, Jiwen Jim Liu, Richard V. Connors, Yongli Su, Jian Luo, Julio C. Medina, Marc Vimolratana, Xiaohui Du, Gayathri Swaminath, An-Rong Li, Ming Yu, Liusheng Zhu, Sean P. Brown, Todd J. Kohn, Zhongyu Wang, Yingcai Wang, Daniel C.-H. Lin, Simon Wong
Publikováno v:
ACS Medicinal Chemistry Letters. 5:384-389
We recently reported the discovery of a potent GPR40 full agonist AM-1638 (1). Herein, we describe our efforts in improving the drug-like properties of the full agonists through the systematic introduction of polar groups in the C-, D-, and A-rings.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::06439f1cb4f3cdf9f6fcdb67b8a2cf08
https://doi.org/10.1021/ml4005123
https://doi.org/10.1021/ml4005123