GPR21(m5) GPR21(m5)_P6.29A GPR21(m5)_β2AR
Ontology highlight
ABSTRACT: GPR21 is a class-A orphan G protein-coupled receptor (GPCR) and a potential therapeutic target for type 2 diabetes and other metabolic disorders. This receptor shows high basal activity in coupling to multiple G proteins in the absence of any known endogenous agonist or synthetic ligand. Here, we present the structures of ligand-free human GPR21 bound to heterotrimeric miniGs and miniG15 proteins, respectively. We identified an agonist-like motif in extracellular loop 2 (ECL2) that occupies the orthosteric pocket and promotes receptor activation. A side pocket that may be employed as a new ligand binding site was also uncovered.These findings will enable the design of modulators for GPR21 for understanding its signal transduction and exploring opportunity for deorphanization
ORGANISM(S): Homo Sapiens
SUBMITTER: Jie Zheng
PROVIDER: PXD038292 | iProX | Wed Nov 23 00:00:00 GMT 2022
REPOSITORIES: iProX
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