GPR1 is a
#chemerin receptor, but is Gi signaling elicited upon binding to the chemerin
#adipokine? The
#cryoEM structure of the GPR1-Gi complex bound to chemerin confirms Gi signaling and a ‘two-site’ activation mechanism
#PLOSBiology https://plos.io/4hr0s6a
Structure of G protein-coupled receptor GPR1 bound to full-length chemerin adipokine reveals a chemokine-like reverse binding mode
GPR1 is a chemerin receptor, but whether Gi signaling is elicited upon binding to the chemerin adipokine remains unclear. This study reports a cryo-EM structural analysis of the GPR1-Gi complex bound to chemerin, confirming Gi signaling and a ‘two-site’ activation mechanism.
The
#GPCR CMKLR1 responds to the
#adipokine #chemerin and is abundant in
#InnateImmune cells. Structure of CMKLR1 in complex with
#Gprotein and a peptide agonist (+ mutagenesis & simulations) reveals mechanisms of action
#PLOSBiology https://plos.io/4a6Igvd
Structural basis of G protein–Coupled receptor CMKLR1 activation and signaling induced by a chemerin-derived agonist
Chemokine-like receptor 1 (CMKLR1) responds to the adipokine chemerin and is highly expressed in innate immune cells. A high-resolution structure of CMKLR1 in complex with G protein and a peptide agonist, together with mutagenesis and computational simulations studies, reveals mechanisms of peptide agonist recognition, receptor activation, and G protein-coupling.
PLOS Biology
