Drug discovery today
-
Drug discovery today · Dec 2013
ReviewModulating GPR40: therapeutic promise and potential in diabetes.
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. ⋯ 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.
-
Drug discovery today · Dec 2013
ReviewCentral nervous system biomarkers for antiobesity drug development.
With antiobesity agents, weight loss can emerge from an array of metabolic, cognitive and behavioural changes that translate into weight change over time. In early drug development, characterising these changes can actually be more informative than simply measuring weight loss. ⋯ In this review, we examine potential biomarkers for effects on metabolism and satiety, hedonics and motivation, and eating behaviour. We also review biomarkers for early detection of neuropsychiatric adverse effects.