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Mol Cell Endocrinol. 1999 May 25;151(1-2):181-93.

Structural basis of G protein-coupled receptor function.

Author information

  • 1Institut für Pharmakologie, Freie Universität Berlin, Germany. schoberg@zedat.fu-berlin.de

Abstract

The vast majority of extracellular signaling molecules, like hormones and neurotransmitters, interact with a class of membranous receptors characterized by a uniform molecular architecture of seven transmembrane alpha-helices linked by extra- and intracelluar peptide loops. In a reversible manner, binding of diverse agonists to heptahelical receptors leads to activation of a limited repertoire of heterotrimeric guanine nucleotide-binding proteins (G proteins) forwarding the signal to intracellular effectors such as enzymes and ion channels. Proper functioning of a G protein-coupled receptor is based on a complex interplay of structural determinants which are ultimately responsible for receptor folding, trafficking and transmembrane signaling. Applying novel biochemical and molecular biological methods interesting insights into receptor structure/function relationships became available. These studies have a significant impact on our understanding of the molecular basis of human diseases and may eventually lead to novel therapeutic strategies.

PMID:
10411333
[PubMed - indexed for MEDLINE]
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