• Drug discovery today · Dec 2013

    Review

    Modulating GPR40: therapeutic promise and potential in diabetes.

    • Vincent Poitout and Daniel C-H Lin.
    • Montreal Diabetes Research Center, CRCHUM, and Department of Medicine, Université de Montréal, Montréal, QC, Canada. Electronic address: vincent.poitout@umontreal.ca.
    • Drug Discov. Today. 2013 Dec 1; 18 (23-24): 1301-8.

    AbstractThe class A G-protein-coupled receptor GPR40 is predominantly expressed in pancreatic beta cells and plays a major part in fatty acid amplification of glucose-induced insulin secretion. GPR40 agonists are being developed for the treatment of type 2 diabetes. Preclinical studies have shown that GPR40 activation improves glucose control, and recent Phase II trials provided proof-of-concept for this approach. The pharmacology of GPR40 is only partially understood but recent findings suggest that full agonism of the receptor could, in addition to stimulating insulin release, engage the enteroinsular axis. Much remains to be discovered regarding the biology of the receptor to inform the development of GPR40-based drugs. Copyright © 2013 Elsevier Ltd. All rights reserved.

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