-transparent.png){kind=logo}
AMG 837: a potent, orally bioavailable GPR40 agonist. 2012
Jonathan B Houze, and
Liusheng Zhu, and
Ying Sun, and
Michelle Akerman, and
Wei Qiu, and
Alex J Zhang, and
Rajiv Sharma, and
Michael Schmitt, and
Yingcai Wang, and
Jiwen Liu, and
Jinqian Liu, and
Julio C Medina, and
Jeff D Reagan, and
Jian Luo, and
George Tonn, and
Jane Zhang, and
Jenny Ying-Lin Lu, and
Michael Chen, and
Edwin Lopez, and
Kathy Nguyen, and
Li Yang, and
Liang Tang, and
Hui Tian, and
Steven J Shuttleworth, and
Daniel C-H Lin
Amgen Inc. 1120 Veterans Blvd., South San Francisco, CA 94080, USA. jhouze@amgen.com
The discovery that certain long chain fatty acids potentiate glucose stimulated insulin secretion through the previously orphan receptor GPR40 sparked interest in GPR40 agonists as potential antidiabetic agents. Optimization of a series of β-substituted phenylpropanoic acids led to the identification of (S)-3-(4-((4'-(trifluoromethyl)biphenyl-3-yl)methoxy)phenyl)hex-4-ynoic acid (AMG 837) as a potent GPR40 agonist with a superior pharmacokinetic profile and robust glucose-dependent stimulation of insulin secretion in rodents.
Related Publications
Jonathan B Houze, and
Liusheng Zhu, and
Ying Sun, and
Michelle Akerman, and
Wei Qiu, and
Alex J Zhang, and
Rajiv Sharma, and
Michael Schmitt, and
Yingcai Wang, and
Jiwen Liu, and
Jinqian Liu, and
Julio C Medina, and
Jeff D Reagan, and
Jian Luo, and
George Tonn, and
Jane Zhang, and
Jenny Ying-Lin Lu, and
Michael Chen, and
Edwin Lopez, and
Kathy Nguyen, and
Li Yang, and
Liang Tang, and
Hui Tian, and
Steven J Shuttleworth, and
Daniel C-H Lin
March 2015,
ACS medicinal chemistry letters,
Jonathan B Houze, and
Liusheng Zhu, and
Ying Sun, and
Michelle Akerman, and
Wei Qiu, and
Alex J Zhang, and
Rajiv Sharma, and
Michael Schmitt, and
Yingcai Wang, and
Jiwen Liu, and
Jinqian Liu, and
Julio C Medina, and
Jeff D Reagan, and
Jian Luo, and
George Tonn, and
Jane Zhang, and
Jenny Ying-Lin Lu, and
Michael Chen, and
Edwin Lopez, and
Kathy Nguyen, and
Li Yang, and
Liang Tang, and
Hui Tian, and
Steven J Shuttleworth, and
Daniel C-H Lin
September 2010,
ACS medicinal chemistry letters,
Jonathan B Houze, and
Liusheng Zhu, and
Ying Sun, and
Michelle Akerman, and
Wei Qiu, and
Alex J Zhang, and
Rajiv Sharma, and
Michael Schmitt, and
Yingcai Wang, and
Jiwen Liu, and
Jinqian Liu, and
Julio C Medina, and
Jeff D Reagan, and
Jian Luo, and
George Tonn, and
Jane Zhang, and
Jenny Ying-Lin Lu, and
Michael Chen, and
Edwin Lopez, and
Kathy Nguyen, and
Li Yang, and
Liang Tang, and
Hui Tian, and
Steven J Shuttleworth, and
Daniel C-H Lin
February 2018,
Journal of medicinal chemistry,
Jonathan B Houze, and
Liusheng Zhu, and
Ying Sun, and
Michelle Akerman, and
Wei Qiu, and
Alex J Zhang, and
Rajiv Sharma, and
Michael Schmitt, and
Yingcai Wang, and
Jiwen Liu, and
Jinqian Liu, and
Julio C Medina, and
Jeff D Reagan, and
Jian Luo, and
George Tonn, and
Jane Zhang, and
Jenny Ying-Lin Lu, and
Michael Chen, and
Edwin Lopez, and
Kathy Nguyen, and
Li Yang, and
Liang Tang, and
Hui Tian, and
Steven J Shuttleworth, and
Daniel C-H Lin
January 2011,
PloS one,
Jonathan B Houze, and
Liusheng Zhu, and
Ying Sun, and
Michelle Akerman, and
Wei Qiu, and
Alex J Zhang, and
Rajiv Sharma, and
Michael Schmitt, and
Yingcai Wang, and
Jiwen Liu, and
Jinqian Liu, and
Julio C Medina, and
Jeff D Reagan, and
Jian Luo, and
George Tonn, and
Jane Zhang, and
Jenny Ying-Lin Lu, and
Michael Chen, and
Edwin Lopez, and
Kathy Nguyen, and
Li Yang, and
Liang Tang, and
Hui Tian, and
Steven J Shuttleworth, and
Daniel C-H Lin
March 2021,
Journal of medicinal chemistry,
Jonathan B Houze, and
Liusheng Zhu, and
Ying Sun, and
Michelle Akerman, and
Wei Qiu, and
Alex J Zhang, and
Rajiv Sharma, and
Michael Schmitt, and
Yingcai Wang, and
Jiwen Liu, and
Jinqian Liu, and
Julio C Medina, and
Jeff D Reagan, and
Jian Luo, and
George Tonn, and
Jane Zhang, and
Jenny Ying-Lin Lu, and
Michael Chen, and
Edwin Lopez, and
Kathy Nguyen, and
Li Yang, and
Liang Tang, and
Hui Tian, and
Steven J Shuttleworth, and
Daniel C-H Lin
May 2013,
Bioorganic & medicinal chemistry letters,
Jonathan B Houze, and
Liusheng Zhu, and
Ying Sun, and
Michelle Akerman, and
Wei Qiu, and
Alex J Zhang, and
Rajiv Sharma, and
Michael Schmitt, and
Yingcai Wang, and
Jiwen Liu, and
Jinqian Liu, and
Julio C Medina, and
Jeff D Reagan, and
Jian Luo, and
George Tonn, and
Jane Zhang, and
Jenny Ying-Lin Lu, and
Michael Chen, and
Edwin Lopez, and
Kathy Nguyen, and
Li Yang, and
Liang Tang, and
Hui Tian, and
Steven J Shuttleworth, and
Daniel C-H Lin
March 2011,
Organic letters,
Jonathan B Houze, and
Liusheng Zhu, and
Ying Sun, and
Michelle Akerman, and
Wei Qiu, and
Alex J Zhang, and
Rajiv Sharma, and
Michael Schmitt, and
Yingcai Wang, and
Jiwen Liu, and
Jinqian Liu, and
Julio C Medina, and
Jeff D Reagan, and
Jian Luo, and
George Tonn, and
Jane Zhang, and
Jenny Ying-Lin Lu, and
Michael Chen, and
Edwin Lopez, and
Kathy Nguyen, and
Li Yang, and
Liang Tang, and
Hui Tian, and
Steven J Shuttleworth, and
Daniel C-H Lin
April 2017,
Journal of medicinal chemistry,
Jonathan B Houze, and
Liusheng Zhu, and
Ying Sun, and
Michelle Akerman, and
Wei Qiu, and
Alex J Zhang, and
Rajiv Sharma, and
Michael Schmitt, and
Yingcai Wang, and
Jiwen Liu, and
Jinqian Liu, and
Julio C Medina, and
Jeff D Reagan, and
Jian Luo, and
George Tonn, and
Jane Zhang, and
Jenny Ying-Lin Lu, and
Michael Chen, and
Edwin Lopez, and
Kathy Nguyen, and
Li Yang, and
Liang Tang, and
Hui Tian, and
Steven J Shuttleworth, and
Daniel C-H Lin
January 2023,
ACS medicinal chemistry letters,
Jonathan B Houze, and
Liusheng Zhu, and
Ying Sun, and
Michelle Akerman, and
Wei Qiu, and
Alex J Zhang, and
Rajiv Sharma, and
Michael Schmitt, and
Yingcai Wang, and
Jiwen Liu, and
Jinqian Liu, and
Julio C Medina, and
Jeff D Reagan, and
Jian Luo, and
George Tonn, and
Jane Zhang, and
Jenny Ying-Lin Lu, and
Michael Chen, and
Edwin Lopez, and
Kathy Nguyen, and
Li Yang, and
Liang Tang, and
Hui Tian, and
Steven J Shuttleworth, and
Daniel C-H Lin
February 2018,
Bioorganic & medicinal chemistry letters,
