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

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

NATURE STRUCTURAL & MOLECULAR BIOLOGY（2017）

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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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关键词

Drug discovery,G protein-coupled receptors,Metabolic diseases,X-ray crystallography,Life Sciences,general,Biochemistry,Protein Structure,Membrane Biology,Biological Microscopy

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