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G protein-coupled receptors : from structure to function

Author: Jesús Giraldo; Jean-Philippe Pin; Royal Society of Chemistry (Great Britain)
Publisher: Cambridge : Royal Society of Chemistry, 2011.
Series: RSC drug discovery series.
Edition/Format:   eBook : Document : EnglishView all editions and formats
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  Read more...
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Genre/Form: Electronic books
Additional Physical Format: Print version:
G protein-coupled receptors.
Cambridge : Royal Society of Chemistry, 2011
(OCoLC)751724450
Material Type: Document, Internet resource
Document Type: Internet Resource, Computer File
All Authors / Contributors: Jesús Giraldo; Jean-Philippe Pin; Royal Society of Chemistry (Great Britain)
ISBN: 9781849733441 1849733449
OCLC Number: 754110226
Notes: Includes index.
Description: 1 online resource (xxxv, 512 pages) : illustrations (some color).
Contents: 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 activation; Optical techniques to analyze real-time activation and signaling of G-protein-coupled receptors; Molecular basis of agonism revealed by fluorescence resonance energy studies; Metabotropic glutamate receptors: A paradigm of structural and functional receptor complexity; Lipid-protein interactions in GPCR-associated signaling; The role of cholesterol in GPCR signaling; Cholesterol-dependent GPCR signaling efficacy; Modulating receptor function through RAMPs: can they represent drug targets in themselves?; GRK2 Activation by Receptors; GRK2-Dependent Desensitization Downstream of G Proteins; Arrestins as multi-functional signaling adaptors; Enzyme regulation of -Arrestin-dependent signalling and trafficking of GPCRs; Section III: Modelling GPCR structure and function; Analyzing the activation mechanism of GPCRs by biophysical and computational methods; Modelling the activation mechanism of free fatty acid receptor 1; Prediction of opioid receptor oligomerization; Structural and dynamic effects of cholesterol at preferred sites of interaction with rhodopsin identified from molecular dynamics simulations; Quantifying GPCR function; Mathematical modelling of metabotropic glutamate receptors function; Modelling of G-protein-coupled receptor signaling pathways; From Structure to function to drug discovery: the view-point of a medicinal chemist
Series Title: RSC drug discovery series.
Responsibility: edited by Jesus Giraldo and Jean-Philippe Pin.

Abstract:

This book considers the relationship between structure and function in G protein-coupled receptors (GPCRs) and the implications for drug design.  Read more...

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Drug discovery and development requires the active collaborations of researches from many scientific disciplines and sub-disciplines and the RSC has created a great opportunity to provide the Read more...

 
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