Determination of the endothelin-1 recognition sites of endothelin receptor type A by the directed-degeneration method.

ABSTRACT: G-protein coupled receptors (GPCRs) play indispensable physiological roles in cell proliferation, differentiation, and migration; therefore, identifying the mechanisms by which ligands bind to GPCRs is crucial for developing GPCR-targeting pharmaceutics and for understanding critical biological functions. Although some structural information is available regarding the interactions between GPCRs and their small molecule ligands, knowledge of how GPCRs interact with their corresponding macromolecule ligands, such as peptides and proteins, remains elusive. In this study, we have developed a novel strategy to investigate the precise ligand recognition mechanisms involved in the interaction of endothelin receptor type A (ET_A) with its ligand, endothelin-1 (ET-1); we call this method

SUBMITTER: Han SG 

PROVIDER: S-EPMC5548930 | biostudies-literature | 2017 Aug

REPOSITORIES: biostudies-literature