Zobrazeno 1 - 10
of 29
pro vyhledávání: '"Daniel C-H Lin"'
Autor:
Yonghong Bai, Xinchao Yu, Hao Chen, Daniel Horne, Ryan White, Xiaosu Wu, Paul Lee, Yan Gu, Sudipa Ghimire-Rijal, Daniel C-H Lin, Xin Huang
Publikováno v:
eLife, Vol 9 (2020)
Transient receptor potential canonical (TRPC) proteins form nonselective cation channels that play physiological roles in a wide variety of cells. Despite growing evidence supporting the therapeutic potential of TRPC6 inhibition in treating pathologi
Externí odkaz:
https://doaj.org/article/b71d3676556f4790a50a9b6e9f6e309e
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:
Yan Gu, Daniel C-H Lin, Paul H. Lee, Ryan White, Xiaosu Wu, Daniel B. Horne, Yonghong Bai, Xinchao Yu, Hao Chen, Sudipa Ghimire-Rijal, Xin Huang
Publikováno v:
eLife
eLife, Vol 9 (2020)
eLife, Vol 9 (2020)
Transient receptor potential canonical (TRPC) proteins form nonselective cation channels that play physiological roles in a wide variety of cells. Despite growing evidence supporting the therapeutic potential of TRPC6 inhibition in treating pathologi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b5cea2718121b864c5ca48f8ee2ded6a
http://europepmc.org/articles/PMC7082128
http://europepmc.org/articles/PMC7082128
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:
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
Autor:
Daniel C.-H. Lin, Vincent Poitout
Publikováno v:
Drug Discovery Today. 18:1301-1308
The class A G-protein-coupled receptor GPR40 is predominantly expressed in pancreatic beta cells and plays a major part in fatty acid amplification of glucose-induced insulin secretion. GPR40 agonists are being developed for the treatment of type 2 d
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8e08e3afbe2f8c5b3a4335539091dd81
https://doi.org/10.1016/j.drudis.2013.09.003
https://doi.org/10.1016/j.drudis.2013.09.003
Autor:
Julio C. Medina, Jonathan B. Houze, Xianyun Jiao, Liusheng Zhu, Ying Sun, Vatee Pattaropong, Paul John Dransfield, Marc Vimolratana, Simon Wong, Frank Li, Qi Guo, Jinqian Liu, Jane Zhang, Jian Luo, Run Zhuang, Gayathri Swaminath, Daniel C.-H. Lin, Sean P. Brown
Publikováno v:
ACS Medicinal Chemistry Letters. 3:726-730
GPR40 (FFA1) is a G-protein-coupled receptor, primarily expressed in pancreatic islets, the activation of which elicits increased insulin secretion only in the presence of elevated glucose levels. A potent, orally bioavailable small molecule GPR40 ag
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::26e149414f63fde0f1bed3990e2b4b45
https://doi.org/10.1021/ml300133f
https://doi.org/10.1021/ml300133f
Autor:
Sean P. Brown, Jonathan B. Houze, Nigel J. M. Birdsall, Marc Vimolratana, Daniel C.-H. Lin, Jian Luo, Michael Chen, Yingcai Wang, Paul John Dransfield, Gayathri Swaminath, Jane Zhang, Qi Guo, Kathy Nguyen, Thanh Tran, Xian Yun Jiao
Publikováno v:
Molecular Pharmacology. 82:843-859
Activation of FFA1 (GPR40), a member of G protein-coupling receptor family A, is mediated by medium- and long-chain fatty acids and leads to amplification of glucose-stimulated insulin secretion, suggesting a potential role for free fatty acid 1 (FFA
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b03cd8c3310bbbcee919d767da4d907b
https://doi.org/10.1124/mol.112.079640
https://doi.org/10.1124/mol.112.079640