Details

Autor(en) / Beteiligte

• Poitout, Vincent
• Lin, Daniel C.-H.

Titel

Modulating GPR40: therapeutic promise and potential in diabetes

Ist Teil von

• Drug discovery today, 2013-12, Vol.18 (23-24), p.1301-1308

Ort / Verlag

England: Elsevier Ltd

Erscheinungsjahr

2013

Quelle

MEDLINE

Beschreibungen/Notizen

• •GPR40 is a fatty acid receptor expressed in pancreatic beta cells.•GPR40 largely mediates fatty acid amplification of glucose-induced insulin secretion.•GPR40 agonists are being developed for the treatment of type 2 diabetes.•Encouraging Phase II trials with the GPR40 agonist TAK875 were recently disclosed.•The pharmacology of GPR40 is still only partially understood. The 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.