Functional Characterization of Sodium Channel Inhibitors at the Delta-Opioid Receptor.

ABSTRACT: Existing pharmacotherapies acting on the opioid receptor system have been extensively used to treat chronic pain and addictive disorders. Nevertheless, the adverse side effects associated with opioid therapy underscore the need for concerted measures to develop safer analgesics. A promising avenue of research stems from the characterization of a sodium-dependent allosteric regulation site housed within the delta-opioid receptor and several other G protein-coupled receptors (GPCRs), thereby revealing the presence of a cluster of sodium and water molecules lodged in a cavity thought to be present only in the inactive conformation of the receptor. Studies into the structure-function relationship of said pocket demonstrated its critical involvement in the functional control of GPCR signaling.

SUBMITTER: Mohamud AO 

PROVIDER: S-EPMC9134235 | biostudies-literature | 2022 May

REPOSITORIES: biostudies-literature