The G Protein-Coupled Receptors HandbookLakshmi A. Devi Springer Science & Business Media, 1 Mar 2008 - 412 halaman 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. |
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 |
403 | |
Biophysical and Biochemical Methods | 217 |
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Acad Sci USA activation agonist amino acid antagonists appears arrestin associated binding Biochem Biol Chem BRET calnexin cell surface cells changes channel chaperones complex conformational conserved constitutive activity coupling cytoplasmic demonstrated desensitization determined dimerization domain dopamine receptor effects endocytosis energy enhanced et al evidence example exist expression folding formation function fusion G protein GABAB receptor glycosylation GPCRs GRKs helices helix heterodimerization heterodimers hormone human identified important inactive increase induced inhibition interaction internalization intracellular involved kinase leads levels ligand loop mechanism mediated membrane modulate molecular motif mutant Natl Acad Sci Nature observed occurs oligomerization oligomers opioid receptor pathway peptide Pharmacol pharmacological phosphorylation potential presence Proc Natl Acad protein-coupled receptor recent recep receptor activation region regulation residues response rhodopsin role selective sequence showed shown signaling specific stimulation structure studies suggesting tion trafficking transmembrane whereas wild-type