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110928s2011 caua ob 001 0 eng |
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| 019 |
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|a 757677347
|a 968119032
|a 968997468
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| 020 |
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|a 9780123859525
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|a 0123859522
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|a 9780123859532
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|a (OCoLC)758952074
|z (OCoLC)757677347
|z (OCoLC)968119032
|z (OCoLC)968997468
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|a QP552.G16
|b P43 2011eb
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| 082 |
0 |
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|a 612.01575
|2 22
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| 049 |
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|a TXAM
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| 245 |
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|a Pharmacology of G protein coupled receptors /
|c edited by Richard R. Neubig.
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| 260 |
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|a San Diego, CA :
|b Elsevier,
|c ©2011.
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| 300 |
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|a 1 online resource (xvi, 270 pages) :
|b illustrations.
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| 336 |
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|a text
|b txt
|2 rdacontent
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| 337 |
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|a computer
|b c
|2 rdamedia
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| 338 |
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|a online resource
|b cr
|2 rdacarrier
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| 347 |
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|a text file
|2 rda
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| 490 |
1 |
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|a Advances in pharmacology ;
|v v. 62
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| 504 |
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|a Includes bibliographical references and index.
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| 520 |
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|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 |
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|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
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| 505 |
8 |
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|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
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| 505 |
8 |
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|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
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| 505 |
8 |
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|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
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| 505 |
8 |
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|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
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| 650 |
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0 |
|a G proteins.
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| 650 |
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0 |
|a Cell receptors.
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| 650 |
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0 |
|a Biochemistry.
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| 650 |
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2 |
|a GTP-Binding Proteins
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| 650 |
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2 |
|a Receptors, Cell Surface
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| 650 |
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2 |
|a Biochemistry
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| 650 |
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6 |
|a Protéines G.
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| 650 |
|
6 |
|a Récepteurs cellulaires.
|
| 650 |
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6 |
|a Biochimie.
|
| 650 |
|
7 |
|a biochemistry.
|2 aat
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| 650 |
|
7 |
|a Biochemistry
|2 fast
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| 650 |
|
7 |
|a Cell receptors
|2 fast
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| 650 |
|
7 |
|a G proteins
|2 fast
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| 650 |
1 |
7 |
|a G proteins
|x Receptors.
|2 bisacsh
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| 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 |
|
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|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 |
|
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|a BATCHLOAD
|
| 955 |
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|a Elsevier ScienceDirect 2026-2027
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| 994 |
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|a 92
|b TXA
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| 999 |
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|
| 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
|