G protein-coupled receptors (GPCRs): advances in structures, mechanisms, and drug discovery.

ABSTRACT: G protein-coupled receptors (GPCRs), the largest family of human membrane proteins and an important class of drug targets, play a role in maintaining numerous physiological processes. Agonist or antagonist, orthosteric effects or allosteric effects, and biased signaling or balanced signaling, characterize the complexity of GPCR dynamic features. In this study, we first review the structural advancements, activation mechanisms, and functional diversity of GPCRs. We then focus on GPCR drug discovery by revealing the detailed drug-target interactions and the underlying mechanisms of orthosteric drugs approved by the US Food and Drug Administration in the past five years. Particularly, an up-to-date analysis is performed on available GPCR structures complexed with synthetic small-molecule allo

SUBMITTER: Zhang M 

PROVIDER: S-EPMC11004190 | biostudies-literature | 2024 Apr

REPOSITORIES: biostudies-literature