Article
Bidirectional, iterative approach to the structural delineation of the functional "chemoprint" in GPR40 for agonist recognition.
Journal of medicinal chemistry - 28 Jun 2007
Tikhonova Irina G, Sum Chi Shing, Neumann Susanne, Thomas Craig J, Raaka Bruce M, Costanzi Stefano, Gershengorn Marvin C
Abstract excerpt
GPR40, free fatty acid receptor 1 (FFAR1), is a member of the GPCR superfamily and a possible target for the treatment of type 2 diabetes. In this work, we conducted a bidirectional iterative investigation, including computational modeling and site-directed mutagenesis, aimed at delineating amino acid residues forming the functional "chemoprint" of GPR40 for agonist recognition. The computational and experimental...
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