Coverart for item
The Resource G protein-coupled receptors : from structure to function, edited by Jesus Giraldo and Jean-Philippe Pin

G protein-coupled receptors : from structure to function, edited by Jesus Giraldo and Jean-Philippe Pin

Label
G protein-coupled receptors : from structure to function
Title
G protein-coupled receptors
Title remainder
from structure to function
Statement of responsibility
edited by Jesus Giraldo and Jean-Philippe Pin
Contributor
Subject
Language
eng
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
Member of
Cataloging source
UKRSC
Dewey number
572.696
Illustrations
illustrations
Index
index present
LC call number
QP552.G16
LC item number
G77 2011
Literary form
non fiction
Nature of contents
  • dictionaries
  • bibliography
NLM call number
  • 2012 A-122
  • QV 38
http://library.link/vocab/relatedWorkOrContributorName
  • Giraldo, Jesús
  • Pin, Jean-Philippe
  • Royal Society of Chemistry (Great Britain)
Series statement
RSC drug discovery
http://library.link/vocab/subjectName
  • G proteins
  • Cell receptors
  • Receptors, G-Protein-Coupled
  • Receptors, G-Protein-Coupled
  • Drug Discovery
  • Receptors, G-Protein-Coupled
  • Structure-Activity Relationship
  • SCIENCE
  • Pharmacology
  • Cell receptors
  • G proteins
Label
G protein-coupled receptors : from structure to function, edited by Jesus Giraldo and Jean-Philippe Pin
Instantiates
Publication
Note
Includes index
Bibliography note
Includes bibliographical references and index
Carrier category
online resource
Carrier category code
  • cr
Carrier MARC source
rdacarrier
Color
multicolored
Content category
text
Content type code
  • txt
Content type MARC source
rdacontent
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
Control code
754110226
Dimensions
unknown
Extent
1 online resource (xxxv, 512 pages)
Form of item
online
Isbn
9781849733441
Media category
computer
Media MARC source
rdamedia
Media type code
  • c
Other control number
10.1039/9781849733441
Other physical details
illustrations (some color)
http://library.link/vocab/ext/overdrive/overdriveId
t3514
Specific material designation
remote
System control number
(OCoLC)754110226
Label
G protein-coupled receptors : from structure to function, edited by Jesus Giraldo and Jean-Philippe Pin
Publication
Note
Includes index
Bibliography note
Includes bibliographical references and index
Carrier category
online resource
Carrier category code
  • cr
Carrier MARC source
rdacarrier
Color
multicolored
Content category
text
Content type code
  • txt
Content type MARC source
rdacontent
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
Control code
754110226
Dimensions
unknown
Extent
1 online resource (xxxv, 512 pages)
Form of item
online
Isbn
9781849733441
Media category
computer
Media MARC source
rdamedia
Media type code
  • c
Other control number
10.1039/9781849733441
Other physical details
illustrations (some color)
http://library.link/vocab/ext/overdrive/overdriveId
t3514
Specific material designation
remote
System control number
(OCoLC)754110226

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