G Protein-Coupled Receptors

Now Published in the RSC Drug Discovery Series

G Protein-Coupled Receptors: From Structure to Function

Edited by Jesus Giraldo and Jean-Philippe Pin

G protein-coupled receptors regulate the function of most cells in the human body and represent approximately three percent of the genes in the human genome. These receptors respond to a wide variety of structurally diverse ligands, ranging from small molecules to lipids, peptides, proteins and even light. Ligands acting on GPCRs are commonly used in drug therapy for numerous diseases and it is estimated that these receptors represent about one third of actual identified targets of clinically used drugs.

This exemplary new book which is broken down into three main parts begins by considering what receptor structures tell us about the mechanism of receptor activation. Part two focuses on receptor function and discusses what the data from biophysical and mutational studies, and the analysis of the interactions of the receptor with ligands and regulator proteins tell us about the process of signal transduction. The final part on modelling and simulation details what new insights can be provided by theoretical studies and their implications for drug design.  The book will be essential reading for medicinal chemists, molecular and cell biologists, biochemists and pharmacologists.

http://www.rsc.org/shop/books/2011/9781849731836.asp

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