Review
G protein coupled receptor structure and activation

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Abstract

G protein coupled receptors (GPCRs) are remarkably versatile signaling molecules. The members of this large family of membrane proteins are activated by a spectrum of structurally diverse ligands, and have been shown to modulate the activity of different signaling pathways in a ligand specific manner. In this manuscript I will review what is known about the structure and mechanism of activation of GPCRs focusing primarily on two model systems, rhodopsin and the β2 adrenoceptor.

Abbreviations

β2AR
beta 2 adrenoceptor
GPCR
G protein coupled receptor
TM
transmembrane

Keywords

GPCR
7TM
Structure
Conformational change
Efficacy

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Amino acid numbering: The position of β2AR residues are followed by the Ballesteros general number [1] in superscript, in the form X.YY, where X refers to the TM segment and YY to the position relative to the most highly conserved amino acid in the TM segment, which is assigned an arbitrary position of 50.