The G Protein-Coupled Receptors Handbook

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Lakshmi A. Devi
Springer Science & Business Media, 1 Mar 2008 - 412 halaman
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A comprehensive survey of the many recent advances in the field of G protein-coupled receptors (GPCR). The authors describe the current knowledge of GPCR receptor structure and function, the different mechanisms involved in the regulation of GPCR function, and the role of pharmacological chaperones in GPCR folding and maturation. They also present new findings about how GPCR dimerization/oligomerization modifies the properties of individual receptors and show how recent developments are leading to significant advances in drug discovery, such as the detection of ligands for orphan GPCRs. Also discussed are the most recent developments that could lead to new drug discoveries: the role of GPCRs in mediating pain, the development of receptor-type selective drugs based on the structural plasticity of receptor activation, and the identification of natural ligands of orphan GPCRs (deorphanization) as possible drug targets.
 

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Isi

Molecular Mechanisms Involved in the Activation
33
The Effect of Pharmacological
71
Regulated Membrane Trafficking and Proteolysis of GPCRs
95
GPCRACTIVITY AND ITS REGULATORS
107
Orchestration of Multiple Signaling Pathways
135
G ProteinCoupled Receptor Kinases
149
The Arrestins
159
Classes Assembly and Functions
199
Functional Complementation and the Analysis of GPCR
267
The Role of Oligomerization in G ProteinCoupled Receptor
287
Receptor Oligomerization and Trafficking
309
Modulation of Receptor Pharmacology
323
RECENT DEVELOPMENTS IN DRUG DISCOVERY
347
DeOrphanizing GPCRs and Drug Development
389
Index
403
Hak Cipta

Biophysical and Biochemical Methods
217

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