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PDBsum entry 6pb1
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Signaling protein
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PDB id
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6pb1
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Contents |
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281 a.a.
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40 a.a.
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227 a.a.
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338 a.a.
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57 a.a.
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126 a.a.
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References listed in PDB file
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Key reference
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Title
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Molecular basis for hormone recognition and activation of corticotropin-Releasing factor receptors.
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Authors
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S.Ma,
Q.Shen,
L.H.Zhao,
C.Mao,
X.E.Zhou,
D.D.Shen,
P.W.De waal,
P.Bi,
C.Li,
Y.Jiang,
M.W.Wang,
P.M.Sexton,
D.Wootten,
K.Melcher,
Y.Zhang,
H.E.Xu.
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Ref.
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Mol Cell, 2020,
77,
669.
[DOI no: ]
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PubMed id
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Abstract
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Corticotropin-releasing factor (CRF) and the three related peptides urocortins
1-3 (UCN1-UCN3) are endocrine hormones that control the stress responses by
activating CRF1R and CRF2R, two members of class B G-protein-coupled receptors
(GPCRs). Here, we present two cryoelectron microscopy (cryo-EM) structures of
UCN1-bound CRF1R and CRF2R with the stimulatory G protein. In both structures,
UCN1 adopts a single straight helix with its N terminus dipped into the receptor
transmembrane bundle. Although the peptide-binding residues in CRF1R and CRF2R
are different from other members of class B GPCRs, the residues involved in
receptor activation and G protein coupling are conserved. In addition, both
structures reveal bound cholesterol molecules to the receptor transmembrane
helices. Our structures define the basis of ligand-binding specificity in the
CRF receptor-hormone system, establish a common mechanism of class B GPCR
activation and G protein coupling, and provide a paradigm for studying membrane
protein-lipid interactions for class B GPCRs.
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