Structural insights into ligand recognition and selectivity of somatostatin receptors.

ABSTRACT: Somatostatin receptors (SSTRs) play versatile roles in inhibiting the secretion of multiple hormones such as growth hormone and thyroid-stimulating hormone, and thus are considered as targets for treating multiple tumors. Despite great progress made in therapeutic development against this diverse receptor family, drugs that target SSTRs still show limited efficacy with preferential binding affinity and conspicuous side-effects. Here, we report five structures of SSTR2 and SSTR4 in different states, including two crystal structures of SSTR2 in complex with a selective peptide antagonist and a non-peptide agonist, respectively, a cryo-electron microscopy (cryo-EM) structure of G_i1-bound SSTR2 in the presence of the endogenous ligand SST-14, as well as two cryo-EM structures of G

SUBMITTER: Zhao W 

PROVIDER: S-EPMC9343605 | biostudies-literature | 2022 Aug

REPOSITORIES: biostudies-literature