G protein-coupled receptors: from structure to function

by Giraldo, Jesús Pin, Jean-Philippe

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Title Statements

Full title :G protein-coupled receptors : from structure to function / edited by Jesus Giraldo and Jean-Philippe Pin.

Summary

G protein-coupled receptors (GPCRs) are the largest family of cell-surface receptors, with more than 800 members identified thus far in the human genome. They regulate the function of most cells in the body, and represent approximately 3% of the genes in the human genome. These receptors respond to a wide variety of structurally diverse ligands, ranging from small molecules, such as biogenic amines, nucleotides and ions, to lipids, peptides, proteins, and even light. Ligands (agonists and antagonists) acting on GPCRs are important in the treatment of numerous diseases, including cardiovascular and mental disorders, retinal degeneration, cancer, and AIDS. It is estimated that these receptors represent about one third of the actual identified targets of clinically used drugs. The determination of rhodopsin crystal structure and, more recently, of opsin, 1 and 2 adrenergic and A2A adenosine receptors provides both academia and industry with extremely valuable data for a better understanding of the molecular determinants of receptor function and a more reliable rationale for drug design. GPCR structure and function constitutes a hot topic. The book, which lies between the fields of chemical biology, molecular pharmacology and medicinal chemistry, is divided into three parts. The first part considers what receptor structures tell us about the mechanism of receptor activation. Part II focuses on receptor function. It 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 new insights on the link between structure and mechanism and their implications in drug design.

Edition Statements

Publication Date:2011.

Publication Statements

Publisher(s):Royal Society of Chemistry
Place of Publication:Cambridge
Language:eng
Publication Date:2011.

Notes

Includes index.

The Physical Object

Description:1 online resource (xxxv, 512 pages) : : illustrations (some color)

Edition Identifiers

ISBN:9781849733441, 1849733449
DOI:10.1039/9781849733441
oclc:ocn754110226
LC Classification:QP552.G16
Dewey Decimal:572.696

Section I: GPCR crystal structures on the arena; Structure and mechanism of G protein signalling through crystal structures of rhodopsin; Mechanism of receptor activation through the crystal structures of the ligand-free GPCR opsin;Crystal structure of the human ¯2 adrenergic G-protein-coupled receptor; Crystal structure of a ¯ 1 adrenergic G-protein-coupled receptorCrystal structure of a human A2A adenosine receptor bound to an antagonist; Class A GPCRs: Structural analysis of the binding domain of follicle stimulating hormone receptor; Class B GPCRs: Receptor activation involving ligand binding to two receptor domains; Class C GPCRs: Structures of the extracellular regions of metabotropic glutamate receptors; Section II: GPCRs are multifaceted functional machines; G protein-coupled receptor homo- and hetero-dimerization: contribution to pharmacology and function; Detection of heteromers formed by combinations of three different receptors; Cross-talk between ionotropic and

Metabotropic glutamate receptors; Structural and functional basis of the crosstalk between receptors; GPCRs assemble as oligomers in the membrane,

However a monomeric receptor is sufficient for G protein acti…

Subjects

Cell receptors -- Structure-activity re… Drug Discovery G proteins -- Receptors pharmacology Protéines G -- Récepteurs Récepteurs cellulaires -- Relations str… Receptors, G-Protein-Coupled -- drug ef… Receptors, G-Protein-Coupled -- genetics Receptors, G-Protein-Coupled -- physiol… Relations structure-activité (Biochimie) SCIENCE -- Life Sciences Structure-Activity Relationship Structure-activity relationships (Bioch…