G protein-coupled receptors

Hanna Pincas, Javier González-Maeso, Frederique Ruf-Zamojski, Stuart C. Sealfon

Research output: Chapter in Book/Report/Conference proceedingChapterpeer-review

3 Scopus citations

Abstract

G protein-coupled receptors (GPCRs) include one of the largest gene families in the mammalian genome. The diversity of receptor binding sites and coupling mechanisms provides the signaling specificity necessary to maintain homeostasis. Various G protein-coupled receptors are critical for the functioning of every endocrine system in health and disease, and these proteins are the predominant targets of therapeutic drugs. GPCRs are grouped by primary sequence into different families that all have a canonical seven alpha helical transmembrane domain structure. In recent years, solving the crystal structure for an increasing number of these receptors has helped to resolve the molecular mechanisms of ligand interaction and activation. Despite their name, they couple to cellular signaling via both heterotrimeric G proteins and G protein-independent mechanisms. Receptor and signaling regulatory mechanisms contribute to controlling the level of the cellular responses elicited. A variety of endocrine and systemic diseases are caused by specific receptor mutations.

Original languageEnglish
Title of host publicationEndocrinology (Switzerland)
PublisherSpringer Science and Business Media Deutschland GmbH
Pages85-120
Number of pages36
DOIs
StatePublished - 2018

Publication series

NameEndocrinology (Switzerland)
ISSN (Print)2510-1927
ISSN (Electronic)2510-1935

Keywords

  • Crystallography
  • Genetics
  • Pharmacology
  • Regulation
  • Signal transduction

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