Alternative splicing of G protein–coupled receptors: relevance to pain management

FA Oladosu, W Maixner, AG Nackley - Mayo Clinic Proceedings, 2015 - Elsevier
FA Oladosu, W Maixner, AG Nackley
Mayo Clinic Proceedings, 2015Elsevier
Drugs that target G protein–coupled receptors (GPCRs) represent the primary treatment
strategy for patients with acute and chronic pain; however, there is substantial individual
variability in both the efficacy and adverse effects associated with these drugs. Variability in
drug responses is due, in part, to individuals' diversity in alternative splicing of pain-relevant
GPCRs. G protein–coupled receptor alternative splice variants often exhibit distinct tissue
distribution patterns, drug-binding properties, and signaling characteristics that may impact …
Abstract
Drugs that target G protein–coupled receptors (GPCRs) represent the primary treatment strategy for patients with acute and chronic pain; however, there is substantial individual variability in both the efficacy and adverse effects associated with these drugs. Variability in drug responses is due, in part, to individuals’ diversity in alternative splicing of pain-relevant GPCRs. G protein–coupled receptor alternative splice variants often exhibit distinct tissue distribution patterns, drug-binding properties, and signaling characteristics that may impact disease pathology as well as the extent and direction of analgesic effects. We review the importance of GPCRs and their known splice variants to the management of pain.
Elsevier