Crystal structures of human ETB receptor provide mechanistic insight into receptor activation and partial activation

Abstract

Signalling through the endothelin receptor ETB, a class A GPCR, induces nitric oxide-mediated vasorelaxation. Here the authors present the crystal structures of the human ETB receptor bound to the peptide hormone endothelin-3 and in complex with the ETB-selective partial agonist IRL1620 and discuss mechanistic implications for receptor activation.