The secretin-like class B family of G protein-coupled receptors (GPCRs) are key players in hormonal homeostasis. Recent structures of various receptors in complex with a variety of orthosteric and allosteric ligands provide fundamental new insights into the function and mechanism of class B GPCRs, including: (i) ligand-induced changes in the relative orientation of the extracellular and transmembrane receptor domains; (ii) intramolecular interaction networks that stabilize conformational changes to accommodate intracellular G protein binding; and (iii) allosteric modulation of receptor activation. This review provides a comprehensive analysis of the structural, biochemical, and pharmacological data on class B GPCRs for understanding ligand–receptor interaction and modulation mechanisms and assessing the potential implications for drug discovery for the secretin-like GPCR family.

G蛋白偶联受体（GPCR）的促胰液素样B类家族是激素稳态的关键因素。与各种正构和变构配体复合的各种受体的最新结构为B类GPCR的功能和机制提供了基本的新见解，包括：（i）配体诱导的细胞外和跨膜受体域相对方向的变化；（ii）稳定构象变化以适应细胞内G蛋白结合的分子内相互作用网络；（iii）受体活化的变构调节。这篇评论对结构，生化，