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Insights into the structure of class B GPCRs.

ABSTRACT: The secretin-like (class B) family of G protein-coupled receptors (GPCRs) are key players in hormonal homeostasis and are interesting drug targets for the treatment of several metabolic disorders (such as type 2 diabetes, osteoporosis, and obesity) and nervous system diseases (such as migraine, anxiety, and depression). The recently solved crystal structures of the transmembrane domains of the human glucagon receptor and human corticotropin-releasing factor receptor 1 have opened up new opportunities to study the structure and function of class B GPCRs. The current review shows how these structures offer more detailed explanations to previous biochemical and pharmacological studies of class B GPCRs, and provides new insights into their interactions with ligands.

SUBMITTER: Hollenstein K

PROVIDER: S-EPMC3931419 | biostudies-literature | 2014 Jan

REPOSITORIES: biostudies-literature

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Insights into the structure of class B GPCRs.

Hollenstein Kaspar K de Graaf Chris C Bortolato Andrea A Wang Ming-Wei MW Marshall Fiona H FH Stevens Raymond C RC

Trends in pharmacological sciences 20131218 1

The secretin-like (class B) family of G protein-coupled receptors (GPCRs) are key players in hormonal homeostasis and are interesting drug targets for the treatment of several metabolic disorders (such as type 2 diabetes, osteoporosis, and obesity) and nervous system diseases (such as migraine, anxiety, and depression). The recently solved crystal structures of the transmembrane domains of the human glucagon receptor and human corticotropin-releasing factor receptor 1 have opened up new opportun ...[more]

PMID: 24359917

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