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Article

Rearrangement of a polar core provides a conserved mechanism for constitutive activation of class B G protein-coupled receptors.

The Journal of biological chemistry - 16 Jun 2017

Yin Yanting, de Waal Parker W, He Yuanzheng, Zhao Li-Hua, Yang Dehua, Cai Xiaoqing, Jiang Yi, Melcher Karsten, Wang Ming-Wei, Xu H Eric

Abstract excerpt

The glucagon receptor (GCGR) belongs to the secretin-like (class B) family of G protein-coupled receptors (GPCRs) and is activated by the peptide hormone glucagon. The structures of an activated class B GPCR have remained unsolved, preventing a mechanistic understanding of how these receptors are activated. Using a combination of structural modeling and mutagenesis studies, we present here two modes of...

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Identifiers

PMID: 28356352
DOI: 10.1074/jbc.M117.782987
PMCID: PMC5473240

Genes

GCGR

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