RT Journal Article
SR Electronic
T1 G Protein–Coupled Receptors Targeting Insulin Resistance, Obesity, and Type 2 Diabetes Mellitus
JF Pharmacological Reviews
JO Pharmacol Rev
FD American Society for Pharmacology and Experimental Therapeutics
SP 39
OP 67
DO 10.1124/pr.117.014373
VO 70
IS 1
A1 Riddy, Darren M.
A1 Delerive, Philippe
A1 Summers, Roger J.
A1 Sexton, Patrick M.
A1 Langmead, Christopher J.
A2 Barker, Eric L.
YR 2018
UL http://pharmrev.aspetjournals.org/content/70/1/39.abstract
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.