Zobrazeno 1 - 10
of 11
pro vyhledávání: '"Vatee Pattaropong"'
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.
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:
Andrew Tasker, Andreas Reichelt, Yi-Ling Hu, Deanna Mohn, John McCarter, Ben Fisher, Robert M. Rzasa, Yi Chen, Julio C. Medina, Gang Yu, Sharon Wannberg, Brian Lucas, Ron C. Kelly, Jennifer Seganish, Felix Gonzalez-Lopez de Turiso, Xiaolin Hao, Kristin L. Andrews, Douglas A. Whittington, Matthew Frank Brown, Dawei Zhang, Youngsook Shin, Mario G. Cardozo, Jason Duquette, Robert C. Wahl, Leeanne Zalameda, Daniela Metz, Vatee Pattaropong, Michael G. Johnson, Tisha San Miguel, Randall W. Hungate, John Whoriskey, Lawrence R. McGee, Timothy D. Cushing, Kirk Henne, Liping H. Pettus, Xiao He
Publikováno v:
Journal of Medicinal Chemistry. 58:480-511
The development and optimization of a series of quinolinylpurines as potent and selective PI3Kδ kinase inhibitors with excellent physicochemical properties are described. This medicinal chemistry effort led to the identification of 1 (AMG319), a com
Autor:
Julia Winslow Lohman, David Fong, Michael G. Johnson, Xiaolin Hao, Gang Yu, Douglas A. Whittington, Helen J. McBride, Yi-Ling Hu, Vatee Pattaropong, Lawrence R. McGee, Sharon Wannberg, Kirk Henne, Jillian L. Simard, Xiao He, Deanna Mohn, Julio C. Medina, Kent Miner, Todd J. Kohn, Yi Chen, Felix Gonzalez-Lopez de Turiso, Jennifer Seganish, Mario G. Cardozo, Matthew Frank Brown, Daniela Metz, Youngsook Shin, Timothy D. Cushing
Publikováno v:
Journal of Medicinal Chemistry. 55:7667-7685
Structure-based rational design led to the synthesis of a novel series of potent PI3K inhibitors. The optimized pyrrolopyridine analogue 63 was a potent and selective PI3Kβ/δ dual inhibitor that displayed suitable physicochemical properties and pha
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:
Alexander S. Kiselyov, Jason Gerlak, Robin L. Rosler, Margarita Camara, James Fleming, Sui Ping Lee, Stan Mitelman, Asra Malikzay, Vatee Pattaropong, Ying Wang, Avdhoot Velankar, Evgueni L. Piatnitski, Leon M. Smith, Julia Winslow Lohman, Xiaoling Chen, Xiaohu Ouyang, David Surguladze, Joel Kawakami, M. Carolina Tuma, Marc Labelle, Jacqueline Doody, Hai-Ying He, Kai Zhou
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:1191-1196
Oxadiazole derivatives were synthesized and evaluated for their ability to inhibit tubulin polymerization and to cause mitotic arrest in tumor cells. The most potent compounds inhibited tubulin polymerization at concentrations below 1 microM. Lead an
Autor:
Hui-Hsien Chiang, Evgueni L. Piatnitski, Leon M. Smith, Xiaohu Ouyang, James Fleming, Paul Kussie, Yunyu Mao, Jason Gerlak, Vatee Pattaropong, M. Carolina Tuma, Asra Malikzay, Dhanvanthri S. Deevi, Wai C. Wong, Jacqueline Doody, Ki H. Kim, Xiaoling Chen, Sheetal Patel, Hai-Ying He, Marc Labelle, Robin L. Rolser, Daniel L. Milligan, Sui Ping Lee, Yang Yu, Ying Wang, John Kincaid, Alexander S. Kiselyov
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:5154-5159
A novel triazole-containing chemical series was shown to inhibit tubulin polymerization and cause cell cycle arrest in A431 cancer cells with EC(50) values in the single digit nanomolar range. Binding experiments demonstrated that representative acti
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:
Eugene Lvovich Piatnitski Chekler, Vatee Pattaropong, Ying Wang, Alexander S. Kiselyov, Xiaohu Ouyang, M. Carolina Tuma, Jacqueline Doody, Xiaoling Chen
In an effort to develop potent, orally bioavailable compounds for the treatment of neoplastic diseases, we developed a class of dual VEGFR-2 kinase and tubulin inhibitors. Targeting the VEGFR receptor kinase and tubulin structure allows for inhibitio
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5db507265fa4acd23e62fca7941b6653
https://europepmc.org/articles/PMC4007844/
https://europepmc.org/articles/PMC4007844/