期刊
BIOLOGY OF THE CELL
卷 96, 期 5, 页码 335-342出版社
EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.biolcel.2004.03.005
关键词
GPCR; glutamate; GABA; calcium; G-protein; activation; dimer; allosteric modulator; Venus flytrap
类别
Class-C G-protein coupled receptors (GPCRs) represent a distant group among the large family of GPCRs. This class includes the receptors for the main neurotransmitters, glutamate and gamma-aminobutyric acid (GABA), and the receptors for Ca2+, some taste and pheromone molecules, as well as some orphan receptors. Like any other GPCRs, class-C receptors possess a heptahelical domain (HD) involved in heterotrimeric G-protein activation. but most of them also have a large extracellular domain (ECD) responsible for agonist recognition and binding. In addition, it is now well accepted that these receptors are dimers, either homo or heterodimers. This complex architecture raises a number of important questions. Here we will discuss our view of how agonist binding within the large ECD triggers the necessary change of conformation. or stabilize a specific conformation, of the heptahelical domain leading to G-protein activation. How ligands acting within the heptahelical domain can change the properties of these complex macromolecules. (C) 2004 Elsevier SAS. All rights reserved.
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