TY - JOUR T1 - G Protein–Coupled Receptors Targeting Insulin Resistance, Obesity, and Type 2 Diabetes Mellitus JF - Pharmacological Reviews JO - Pharmacol Rev SP - 39 LP - 67 DO - 10.1124/pr.117.014373 VL - 70 IS - 1 AU - Darren M. Riddy AU - Philippe Delerive AU - Roger J. Summers AU - Patrick M. Sexton AU - Christopher J. Langmead A2 - Barker, Eric L. Y1 - 2018/01/01 UR - http://pharmrev.aspetjournals.org/content/70/1/39.abstract N2 - 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. ER -