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Med Sci (Paris)

Title:		[How do G-protein-coupled receptors work? The case of metabotropic glutamate and GABA receptors]
Author(s):		Galvez T; Pin JP;
Address:		"Center for Clinical Sciences Research, Department of Molecular Pharmacology, Stanford University Medical Center, 269, Campus Drive, Room 3230, Stanford, CA 94305, USA. galvez@stanford.edu"
Journal Title:		Med Sci (Paris)
Year:		2003
Volume:		19
Issue:		5
Page Number:		559 - 565
DOI:		10.1051/medsci/2003195559
ISSN/ISBN:		0767-0974 (Print) 0767-0974 (Linking)
Abstract:		"G-protein coupled receptors (GPCRs) represent the largest membrane proteins family in animal genomes. Being the receptors for most hormones and neurotransmitters, these proteins play a central role in intercellular communication. GPCRs can be classified into several groups based on the sequence similarity of their common structural feature: the heptahelical domain. The metabotropic receptors for the main neurotransmitters glutamate and gamma-aminobutyric acid (GABA) belong to the class III of GPCRs, together with others receptors for Ca2+, for sweet and amino acid taste compounds and for some pheromones, as well as for odorants in fish. Besides their transmembrane heptahelical domain responsible for G-protein activation, most of class III receptors possess a large extracellular domain responsible for ligand recognition. The recent resolution of the structure of this binding domain of one of these receptors, the mGlu1 receptor, together with the recent demonstration that these receptors are dimers, revealed an original mechanism of activation for these GPCRs. Such data open new possibilities to develop drugs aimed at modulating these receptors, and raised a number of interesting questions on the activation mechanism of other GPCRs"
Keywords:		"Animals Dimerization Enzyme Activation GTP-Binding Proteins/*physiology Glutamic Acid/physiology Guanosine Triphosphate/physiology Humans Models, Biological Models, Molecular Protein Conformation Protein Structure, Tertiary Receptors, GABA/*physiology Rec;"
Notes:		"MedlineGalvez, Thierry Pin, Jean-Philippe fre English Abstract Review France 2003/07/03 Med Sci (Paris). 2003 May; 19(5):559-65. doi: 10.1051/medsci/2003195559"