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GPCR Molecular Pharmacology and Drug Targeting Shifting Paradigms and New Directions

by: Gilchrist, Annette

GPCR Molecular Pharmacology and Drug Targeting Shifting Paradigms and New Directions

by: Gilchrist, Annette

ISBN 13:
9780470307786
ISBN 10:
0470307781
Edition: 1st
Format: Hardcover
Copyright: 08/09/2010
Publisher: Wiley

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Summary

G protein-coupled receptors (GPCRs) are a large protein family of transmembrane receptors vital in dictating cellular responses. GPCRs are involved in many diseases, but are also the target of around half of all modern medicinal drugs. Shifting Paradigms in G Protein Coupled Receptors takes a look at the way GPCRs are examined today, how they react, how their mutations lead to disease, and the many ways in which they can be screened for compounds that modulate them. Chemists, pharmacologists, and biologists will find essential information in this comprehensive reference.

The Evolution of Receptors: From On-Off Switches to Micro-Processors
Introduction
The Receptor as an On-Off Switch
Historical background and Classical Receptor Theory
The Operational Model of Drug Action
Receptor Antagonism
Specific Models of GPCRs (7TM receptors)
The Receptor as Microprocessor: Ternary Complex Models
Receptors as Basic Drug Recognition Units
Receptor Structure
Future Considerations
The Evolving Pharmacology of GPCRs
Agonists, neutral antagonists and inverse agonists
LDTRS/protean agonism
Molecular mechanisms of GPCR ligand binding
Two GPCR ligands binding at once- concept of allosterism
GPCR dimerisation
Future Perspectives
The Emergence of Allosteric Modulators for G Protein-Coupled Receptors
Introduction
Foundations of Allosteric Receptor Theory
Models for Understanding the Effects of Allosteric Modulators
Types of Allosteric Modulators and Their Properties
Detection and Quantification of Allosteric Interactions
Some Examples of GPCR Allosteric Modulators
Concluding Remarks
Receptor-mediated G protein activation: how, how many and where?
The mechanical problem - three different solutions
Receptor monomers - dimers - oligomers: one size fits all?
Corrals, fences, rafts - are there privileged places for GPCR activation?
Molecular Pharmacology of Frizzleds - with implications for possible therapy
Introduction
Frizzleds as WNT receptors
Frizzled signaling
Frizzleds? physiology & possible therapy
Secretin receptor dimerization: A possible functionally-important paradigm for Family B G protein-coupled receptors
Methodological approaches to GPCR oligomerization
Structural themes for GPCR oligomerization
Functional effects of GPCR oligomerization
Secretin receptor oligomerization
Past and Future Strategies for GPCR Deorphanization
Introduction
Current strategies to identify the ligand and function of orphan 7TM proteins
Functional assays for deorphanization
Future directions and new concepts
Controversial issues
High throughput GPCR screening technologies and the emerging importance of the cell phenotype
Introduction
How are GPCR drugs discovered?
GPCR dependence on G proteins
Technologies for GPCR compound screening and drug discovery
Importance of Target cells in GPCR HTS assays
Are "traditional" biochemical techniques out of fashion in the new era of GPCR pharmacology?
Overview
Receptor Binding Assays
Methods for Measurement of cAMP
Conclusions
Fluorescence and resonance energy transfer shine new light on GPCR function
Overview
Introduction
Labeling GPCRs with fluorescent tags
Detection of fluorescence and bioluminescence
Fluorescence-based assays to study receptor localization, trafficking and receptor function
Resonance energy transfer, a tool to get new insights into GPCR function
Analysis of steady state protein/protein interaction by means of RET
Kinetic analysis of protein/protein interactions by means of FRET
Detection of receptor function by fluorescence resonance energy
Integration of label-free detection methods in GPCR drug discovery
Overview
Introduction
Label free technologies -- past and present
A. Automated microscopes and microbalances
Discussion
Screening for allosteric modulators of G protein-coupled receptors
Introduction
The allosteric ternary complex model (ATCM), radioligand binding and affinity
Beyond affinity - functional assays, efficacy and allosteric agonism
Allosteric modulator titration curves
The impact of functional assay format on allosteric modulator screening
Taking advantage of structural understanding of allosteric binding sites
Summary and future directions
Ultra High Throughput Screening Assays for GPCRs
Introduction
Assay Types for GPCRs in uHTS
Summary
New techniques to express and crystallise G protein coupled receptors
Introduction
Key problems limiting production of 3D GPCR structures
History of GPCR structures
The search for other GPCR structures
Protein purification and solubilisation
In cubo crystallisation
Engineering receptor stability
Structures of the ß2 adrenergic receptor
The adenosine A2a receptor
Conclusions and Future developments
Structure and Modeling of GPCRs: Implications for drug discovery
Introduction
High resolution GPCR modeling
Constructing and Evaluating Homology Models of Other Receptor Types
Modeling GPCR Functional Features - Analysis of activation and signaling
Beyond Class A: modeling of other GPCR families
Summary and Conclusions
X-ray Structure Developments for GPCR Drug Targets
Overview
Introduction
Class A GPCRs
Class C GPCRs
Conclusions
Pharmacological Chaperones: Potential for the Treatment of Hereditary Diseases Caused by Mutations in G Protein-coupled Receptors
Overview
Introduction
Nephrogenic Diabetes Insipidus and the Vasopressin V2 Receptor
Retinitis Pigmentosa and the Rhodopsin Receptor
Idiopathic Hypogonadotropic Hypogonadism and the Gonadotropin-Releasing Hormone Receptor
Other Human Diseases Caused by Inactivating Mutations in GPCRs
Considerations for the Therapeutic Use of Pharmacological Chaperones
Concluding Remarks
Table of Contents provided by Publisher. All Rights Reserved.

Amazon no longer offers textbook rentals. We do!

GPCR Molecular Pharmacology and Drug Targeting Shifting Paradigms and New Directions

GPCR Molecular Pharmacology and Drug Targeting Shifting Paradigms and New Directions

9780470307786

0470307781

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Table of Contents

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