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Encyclopedia of Life Sciences

DOI: 10.1038/npg.els.0000118

Anesthetic Pharmacology, p. 17-27

DOI: 10.1017/cbo9780511781933.003

Wiley, British Journal of Pharmacology, (164), p. S5-S113, 2011

DOI: 10.1111/j.1476-5381.2011.01649_3.x

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G Protein-Coupled Receptors

Journal article published in 2013 by Husseini K. Manji, P. H. M. Torres, Elizabath C. Warburton, R. H. de Rijk, Hans-Joachim Wittmann, Joachim D. Uys, Harriet de Wit, Gorkem Yararbas, Andrew Young, Sophie Tambour, Andrea Strasser, Etienne Sibille, John Shine, Will Spooren, W. J. Thomsen and other authors.
This paper is made freely available by the publisher.
This paper is made freely available by the publisher.

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Abstract

The G protein-coupled receptors (GPCRs) constitute the largest superfamily of proteins encoded by the human genome. These receptors are membrane proteins which share a common structure of seven transmembrane helices and are involved in the cellular signal transduction through activation of heterotrimeric protein (G protein) in intracellular environment. This activation signal, mediated by the agonist binding to the extracellular domain of the receptor, is transmitted into the cell and activates many signaling cascades in different physiological events such as neurotransmission, growth, metabolism, differentiation of the cell, secretion and immune defense. As a consequence, these receptors are described as therapeutic targets for more than 50% of drugs sold worldwide. Thus, the study of the molecular mechanism involving GPCRs has become essential to understand the cellular signaling and, consequently, the rational design of new therapeutic agents, e.g. antihypertensive drugs. Therefore, this review reports the structural characteristics, the activation mechanism, the G protein activation and the classification of these membrane proteins of huge physiological and pathophysiological importance.