Structural basis for the cooperative allosteric activation of the free fatty acid receptor GPR40

被引：0
|
作者：
Jun Lu
Noel Byrne
John Wang
Gerard Bricogne
Frank K Brown
Harry R Chobanian
Steven L Colletti
Jerry Di Salvo
Brande Thomas-Fowlkes
Yan Guo
Dawn L Hall
Jennifer Hadix
Nicholas B Hastings
Jeffrey D Hermes
Thu Ho
Andrew D Howard
Hubert Josien
Maria Kornienko
Kevin J Lumb
Michael W Miller
Sangita B Patel
Barbara Pio
Christopher W Plummer
Bradley S Sherborne
Payal Sheth
Sarah Souza
Srivanya Tummala
Clemens Vonrhein
Maria Webb
Samantha J Allen
Jennifer M Johnston
Adam B Weinglass
Sujata Sharma
Stephen M Soisson
机构：
[1] Merck Research Laboratories,Department of Structural Chemistry
[2] Merck Research Laboratories,Department of Screening and Protein Science
[3] Merck Research Laboratories,Department of In vitro Pharmacology
[4] Global Phasing Limited,Department of Medicinal Chemistry
[5] Merck Research Laboratories,Department of Cardiometabolic Disease
[6] Merck Research Laboratories,undefined
来源：
Nature Structural & Molecular Biology | 2017年 / 24卷
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摘要：
Crystal structures of hGPR40, a target for treatment of type 2 diabetes, bound to a partial and an allosteric agonist explain the binding cooperativity between these ligands and present new opportunities for structure-guided drug design.
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页码：570 / 577
页数：7
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