Zobrazeno 1 - 10
of 14
pro vyhledávání: '"Xianyun Jiao"'
Autor:
Jesse D. Vargas, Kenny Lou, Kristy C. Perez, Han-Jie Zhou, Yangzhong Tang, Mary-Kamala Menon, Mark Rolfe, Ronan Le Moigne, Xianyun Jiao, Peter K Buchowiecki, Ariel Pios, Antonett Madriaga, Daniel Anderson, Grace J. Lee, Bing Yao, Laura K. Shawver, Zhi Yong Wu, Victoria A. Assimon
Publikováno v:
ACS chemical biology. 14(2)
RUVBL1 and RUVBL2 are ATPases associated with diverse cellular activities (AAAs) that form a complex involved in a variety of cellular processes, including chromatin remodeling and regulation of gene expression. RUVBLs have a strong link to oncogenes
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
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.
Autor:
Anne Chai, Stuart Donald Jones, Andrew K. Shiau, Marc Labelle, Frank Kayser, Peter Coward, Juan C. Jaen, Xianyun Jiao, Ben Fisher, Martin James Harrison, Patrick Escaron, David J. Kopecky, Derek E. Piper, Sharon McKendry, Jean Danao
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:5966-5970
The present report describes our efforts to convert an existing LXR agonist into an LXR antagonist using a structure-based approach. A series of benzenesulfonamides was synthesized based on structural modification of a known LXR agonist and was deter
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
Autor:
Joanne Greenberg, Jiwen Liu, Gayathri Swaminath, Mario G. Cardozo, Peter Jaeckel, Jennifer Weiszmann, Xianyun Jiao, Ralf Schwandner, Hui Tian, Frank Kayser, Yang Li, TaeWeon Lee, Yingcai Wang, Hongfei Ge
Publikováno v:
Molecular Pharmacology. 74:1599-1609
FFA2 (GPR43) has been identified as a receptor for short-chain fatty acids (SCFAs) that include acetate and propionate. FFA2 is highly expressed in islets, a subset of immune cells, and adipocytes. Although the potential roles of FFA2 activation in t
Autor:
Vatee Pattaropong, Jaehyeon Park, Xianyun Jiao, Mark Joseph Chicarelli, Thanhvien Tran, Bencsik Josef Roland, Paul John Dransfield, Kevin Ronald Condroski, Sujen Lai, Julio C. Medina, Brian R. Baer, Boyd Steven A, Mohr Peter, Deborah A. Anderson, Jonathan B. Houze, Walter E. DeWolf, Yumei Xiong, Marion Conn, Zice Fu, Jasmine Davda, Lixia Jin, Xiaohui Du, Jerry Yang, Peter Coward, Bin Wang, Murielle M. Véniant, Ronald Jay Hinklin, Todd J. Kohn, David Chow, Thomas Daniel Aicher
Glucokinase (GK) activators represent a class of type 2 diabetes therapeutics actively pursued due to the central role that GK plays in regulating glucose homeostasis. Herein we report a novel C5-alkyl-2-methylurea-substituted pyridine series of GK a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cf1181d36e9b23087fdb1a05de5f3410
https://europepmc.org/articles/PMC4265826/
https://europepmc.org/articles/PMC4265826/
Autor:
Frank Li, Xianyun Jiao, Qi Guo, Julio C. Medina, Sean P. Brown, Jian Luo, Daniel C.-H. Lin, Jonathan B. Houze, Lynn Miao, Yingcai Wang, Liusheng Zhu, Tiffany L. Correll, Michael D. Bartberger, Jane Zhang, Run Zhuang, Jiwen Jim Liu, Yongli Su, David Chow, Gayathri Swaminath, An-Rong Li, Paul John Dransfield, Khanh Nguyen, Zhongyu Wang, Simon Wong, Marc Vimolratana, Xiaohui Du, Ming Yu, Thanhvien Tran, Vatee Pattaropong, Annie Kasparian
GPR40 (FFAR1 or FFA1) is a target of high interest being pursued to treat type II diabetes due to its unique mechanism leading to little risk of hypoglycemia. We recently reported the discovery of AM-1638 (2), a potent full agonist of GPR40. In this
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::57cc725905f00876cc74627d7371cf38
https://europepmc.org/articles/PMC4027505/
https://europepmc.org/articles/PMC4027505/
Autor:
Jeff D. Reagan, Julio C. Medina, Xianyun Jiao, Leping Li, Run Zhuang, Mami Yamazaki, Mike Lizarzaburu, Sujen Lai, Jonathan B. Houze, Jiwen Jim Liu, Daniel C.-H. Lin, Alykhan Motani, Ryo Okuyama, Peter Fan, Ying Zhang, Futoshi Nara, Michiko Murakoshi, Angela Fu, Nobuaki Watanabe, Yumei Xiong, Zice Fu, Xiaohui Du, Qingxiang Liu, Ming Yu, Kozo Oda
Publikováno v:
ACS medicinal chemistry letters. 4(9)
Herein, we report the lead optimization of amrinone–phenylalanine based GPR142 agonists. Structure–activity relationship studies led to the discovery of aminopyrazole–phenylalanine carboxylic acid 22, which exhibited good agonistic activity, hi
Autor:
Shou-Hua Xiao, Shyun Li, Juan C. Jaen, Frank Kayser, Ellyn Farrelly, Zhulun Wang, Xianyun Jiao, Rajiv Sharma, Nigel Walker, Mario G. Cardozo, David J. Kopecky, Jinsong Liu, Holger Wesche, Jinqian Liu
Publikováno v:
Bioorganicmedicinal chemistry letters. 22(19)
Two classes of ACK1 inhibitors, 4,5,6-trisubstituted furo[2,3-d]pyrimidin4-amines and 4,5,6-trisubstituted 7H-pyrrolo[2,3-d]pyrimidin-4-amines, were discovered and evaluated as ACK1 inhibitors. Further structural refinement led to the identification