PT  - JOURNAL ARTICLE
AU  - Darren M. Riddy
AU  - Philippe Delerive
AU  - Roger J. Summers
AU  - Patrick M. Sexton
AU  - Christopher J. Langmead
ED  - Barker, Eric L.
TI  - G Protein–Coupled Receptors Targeting Insulin Resistance, Obesity, and Type 2 Diabetes Mellitus
AID  - 10.1124/pr.117.014373
DP  - 2018 Jan 01
TA  - Pharmacological Reviews
PG  - 39--67
VI  - 70
IP  - 1
4099  - http://pharmrev.aspetjournals.org/content/70/1/39.short
4100  - http://pharmrev.aspetjournals.org/content/70/1/39.full
SO  - Pharmacol Rev2018 Jan 01; 70
AB  - G protein–coupled receptors (GPCRs) continue to be important discovery targets for the treatment of type 2 diabetes mellitus (T2DM). Many GPCRs are directly involved in the development of insulin resistance and β-cell dysfunction, and in the etiology of inflammation that can lead to obesity-induced T2DM. This review summarizes the current literature describing a number of well-validated GPCR targets, but also outlines several new and promising targets for drug discovery. We highlight the importance of understanding the role of these receptors in the disease pathology, and their basic pharmacology, which will pave the way to the development of novel pharmacological probes that will enable these targets to fulfill their promise for the treatment of these metabolic disorders.