Pharmacology of G protein coupled receptors /

G protein coupled receptors remain the most important class of therapeutic targets in medicine. In the last 5 years, tremendous advances have been made in our understanding of the structure and mechanism of this critical family of drug targets. The present volume explores the modern experimental and...

Full description

Bibliographic Details
Corporate Author: ScienceDirect (Online service)
Other Authors: Neubig, Richard R.
Format: eBook
Language:English
Published: San Diego, CA : Elsevier, ©2011.
Series:Advances in pharmacology (San Diego, Calif.) ; v. 62.
Subjects:
Online Access:Connect to the full text of this electronic book

MARC

Tag First Indicator Second Indicator Subfields
LEADER 00000cam a2200000 a 4500
001 in00005748721
005 20260326190432.3
006 m o d
007 cr mnu---uuaaa
008 110928s2011 caua ob 001 0 eng
040 |a AU@  |b eng  |e pn  |c AU@  |d CDX  |d OCLCQ  |d QCL  |d OPELS  |d OCLCQ  |d OPELS  |d OCLCF  |d OCLCQ  |d UAB  |d D6H  |d OCLCQ  |d LEAUB  |d OL$  |d OCLCO  |d OCLCQ  |d OCLCO  |d OCLCL  |d OCLCQ  |d OCLCL  |d OCLCQ  |d FEM  |d SFB 
019 |a 757677347  |a 968119032  |a 968997468 
020 |a 9780123859525  |q (electronic bk.) 
020 |a 0123859522  |q (electronic bk.) 
020 |a 9780123859532  |q (electronic bk.) 
020 |a 0123859530 
035 |a (OCoLC)758952074  |z (OCoLC)757677347  |z (OCoLC)968119032  |z (OCoLC)968997468 
050 4 |a QP552.G16  |b P43 2011eb 
082 0 4 |a 612.01575  |2 22 
049 |a TXAM 
245 0 0 |a Pharmacology of G protein coupled receptors /  |c edited by Richard R. Neubig. 
260 |a San Diego, CA :  |b Elsevier,  |c ©2011. 
300 |a 1 online resource (xvi, 270 pages) :  |b illustrations. 
336 |a text  |b txt  |2 rdacontent 
337 |a computer  |b c  |2 rdamedia 
338 |a online resource  |b cr  |2 rdacarrier 
347 |a text file  |2 rda 
490 1 |a Advances in pharmacology ;  |v v. 62 
504 |a Includes bibliographical references and index. 
520 |a G protein coupled receptors remain the most important class of therapeutic targets in medicine. In the last 5 years, tremendous advances have been made in our understanding of the structure and mechanism of this critical family of drug targets. The present volume explores the modern experimental and conceptual framework for drug discovery for G protein coupled receptors. It explores advances in structure determination and structure-based drug design as well as new concepts of allosteric modulation, functional selectivity/biased agonism, and pharmacological chaperones. In addition, emerging drug targets such as receptor families for fatty acids, carboxylic acids, lipid mediators, etc. are included. Final chapters cover novel mechanisms of signal regulation through PDZ domains and RGS proteins. This volume will bring an up-to-date perspective on the G protein coupled receptor field to both academic and industry scientists. The present volume explores the modern experimental and conceptual framework for drug discovery for G protein coupled receptors. It explores advances in structure determination and structure-based drug design as well as new concepts of allosteric modulation, functional selectivity/biased agonism, and pharmacological chaperones. This volume will bring an up-to-date perspective on the G protein coupled receptor field to both academic and industry scientists. 
505 0 |a Front Cover; Pharmacology of G Protein Coupled Receptors; Copyright; Contents; Contributors; Preface; Chapter 1: The Use of GPCR Structures in Drug Design; I. Introduction; II. Technology Developments Enabling GPCR Structure Determination; A. Optimizing Expression, Purification, and Stability; B. New Techniques for GPCR Crystallization; III. GPCR Structures; A. Rhodopsin as the Prototypical Receptor; B. Aminergic Receptors; 1. Antagonist Binding; 2. Agonist Binding; C. Adenosine A2A Receptor; D. Chemokine Receptor CXCR4; E. Family B Extracellular Domain Structures 
505 8 |a IV. GPCR Structures in Drug DiscoveryA. Relevance of Information from GPCR Crystal Structures to Native GPCRs; B. Virtual Screening Approaches to GPCR Drug Discovery; C. Utilizing GPCR Structures in Lead Optimization; D. Using Structures to Enable Fragment Screening Approaches; V. Conclusion; Acknowledgments; References; Chapter 2: Allosteric Modulation of Metabotropic Glutamate Receptors; I. Introduction; II. Metabotropic Glutamate Receptors; A. Structural Features of Metabotropic Glutamate Receptors; B. Localization and Functional Roles of the mGlus; 1. Group I mGlus; 2. Group II mGlus 
505 8 |a 3. Group III mGlusIII. Pharmacological Profiles of mGlu Allosteric Modulators; A. Group I mGlus; B. Group II mGlus; C. Group III mGlus; IV. Quantifying Allosteric Interactions; V. Structural Determinants of mGlu Allosteric Modulator Binding; A. Common Allosteric Sites on the mGlus; B. Multiple Allosteric Sites Within a mGlu Subtype; VI. Functional Selectivity of mGlu Allosteric Modulation; VII. Therapeutic Potential of mGlu Allosteric Modulators; A. mGlu1 NAMs for Pain; B. mGlu5 NAMs for Anxiety, Depression, and Fragile X Syndrome; C. mGlu5 PAMs for Schizophrenia 
505 8 |a D. mGlu2 PAMs for Schizophrenia, Anxiety Disorders, and Drug DependenceE. mGlu3 PAMs for Neuroprotection; F. Group II NAMs for Cognitive Enhancement; G. mGlu4 PAMs for Parkinson's Disease; VIII. Conclusion; Acknowledgments; References; Chapter 3: Refining Efficacy: ExploitingFunctional Selectivity forDrug Discovery; I. Introduction; II. GPCRs as Conformational Ensembles; III. The Pluridimensional Nature of GPCR Efficacy; IV. Functionally Selective GPCR Agonism; A. Biased Activation of GPCR Effectors; B. Spatial and Temporal Bias of GPCR Signaling 
505 8 |a V. Functional Selectivity and Pharmaceutical DevelopmentVI. Functional Selectivity at the Parathyroid Hormone Receptor; A. The Biological Actions of Parathyroid Hormone; B. Biased Activation of the PTH1R by Synthetic PTH Analogues; C. PTH1R Functional Selectivity in vivo; VII. Conclusion; Acknowledgments; References; Chapter 4: Pharmacological Chaperones for Misfolded Gonadotropin-Releasing Hormone Receptors; I. Introduction; II. The Endoplasmic Reticulum Quality Control System; III. Misfolding of GPCRs and Disease; IV. Mutations in the Human GnRHR; A. Structural Features of the GnRHR 
650 0 |a G proteins. 
650 0 |a Cell receptors. 
650 0 |a Biochemistry. 
650 2 |a GTP-Binding Proteins 
650 2 |a Receptors, Cell Surface 
650 2 |a Biochemistry 
650 6 |a Protéines G. 
650 6 |a Récepteurs cellulaires. 
650 6 |a Biochimie. 
650 7 |a biochemistry.  |2 aat 
650 7 |a Biochemistry  |2 fast 
650 7 |a Cell receptors  |2 fast 
650 7 |a G proteins  |2 fast 
650 1 7 |a G proteins  |x Receptors.  |2 bisacsh 
655 7 |a Electronic books.  |2 local 
655 4 |a Pharmacology; Biology; Molecular Biology. 
700 1 |a Neubig, Richard R. 
710 2 |a ScienceDirect (Online service) 
758 |i has work:  |a Pharmacology of G protein coupled receptors (Text)  |1 https://id.oclc.org/worldcat/entity/E39PCGT3xKR7Rt6Xf8RJxTYJj3  |4 https://id.oclc.org/worldcat/ontology/hasWork 
830 0 |a Advances in pharmacology (San Diego, Calif.) ;  |v v. 62. 
856 4 0 |u http://proxy.library.tamu.edu/login?url=https://www.sciencedirect.com/science/bookseries/10543589/62  |z Connect to the full text of this electronic book  |t 0 
936 |a BATCHLOAD 
955 |a Elsevier ScienceDirect 2026-2027 
994 |a 92  |b TXA 
999 f f |i a0865845-b17b-4c64-a16b-c5edd48d4a26  |s bf3600a0-7706-439a-a94d-a807d7c1f8b1  |t 0 
952 f f |a Texas A&M University  |b College Station  |c Electronic Resources  |s www_evans  |d Available Online  |t 0  |e QP552.G16 P43 2011eb  |h Library of Congress classification 
998 f f |a QP552.G16 P43 2011eb  |t 0  |l Available Online