Title G protein-coupled receptors in drug discovery / edited by Kenneth H. Lundstrom, Mark L. Chiu

Published Boca Raton : Taylor & Francis, 2006

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Description 1 online resource (362 pages) : illustrations Series Drug discovery series ; 4 Drug discovery series ; 4 Contents Introduction, K.H. Lundstrom and M.L. Chiu Biology of G Protein-Coupled Receptors, K. Lundstrom ; Introduction; Families of GPCRs; Coupling to G Proteins; GPCR Desensitization; Other Signaling Pathways; Trafficking of GPCRs; Resensitization; Conclusions; G Protein Coupled Receptors as Targets for Drug Discovery, T. Esbenshade ; Introduction; GPCR Family Overview; GPCR Tractability: Current Therapeutics; GPCR Drug Discovery; Novel GPCR Features and Impact on Drug Discovery Approaches; Conclusions; G Protein-Coupled Receptors as Cardiovascular Drug Targets, M. Scheinin and A. Snapir ; Cardiovascular Physiology, Pharmacology, and Therapeutics; Drugs in Development and Novel Drugs Targets; Receptor Subtypes as Novel Targets; Receptor Gene Polymorphisms; Concluding Remarks; G Protein-Coupled Receptors and Cancer, M.J. Smit and R.A Bakker ; Introduction; Family A GPCRs; Family C GPCRs; Frizzled/Smoothened Family of GPCRs; Virally Encoded GPCRs; Orphan GPCRs; Conclusions; G Protein-Coupled Receptors in Metabolic Disease, R.M. Reilly and C.A. Collins ; Introduction; Central Mediation of Feeding and Energy Homeostasis; Peripheral Signals Affecting Nutrient Sensing and Utilization; Conclusions; G Protein-Coupled Receptors in CNS Drug Discovery, R. Raddatz and D.S. Hartman ; Introduction; Psychiatric Diseases; Pain and Analgesia; Neurodegeneration; Neuroendocrine Function; Orphan GPCRs in the CNS; Conclusions; Recombinant G Protein-Coupled Receptors for Drug Discovery, K. Lundstrom ; Introduction; Cell-Free Translation; E Coli Expression; Other Prokaryotic Systems; Yeast Expression; Insect Cells; Mammalian Expression; Comparison of Expression Systems; Conclusions; High Throughput Screening Assays for G Protein-Coupled Receptors, U. Warrior, S. Gopalakrishnan, J. Vanhauwe, and D. Burns ; Introduction; Source of Material and Assay Diversity; High Throughput Screening; Receptor Binding Assays--General Considerations; Functional GPCR Assays; Inverse Agonists and Constitutive Activities; Microphysiometer Assays; Screening for Modulators of Orphan Receptors; Conclusions; Molecular Bioinformatics of Receptor Binding and Activation, K.P. Willey, H. Obermann, and J.B Procter ; Not All 7TM Receptors are GPCRs; Receptor Classification by Ligand Size; Ligand Diversity Conforms to Receptor Phylogeny; Structural Flexibilities of Membrane Receptors; Molecular Bioinformatics in Drug Discovery; Sequence and Structural Searches for an Activation Mechanism; The Cysteine Shuffle; Redox Control of Receptor Activation; Smells Rank as the Smallest 7TMR Agonists; Bioinformatics with Biological Sense; Structure and Dynamics of G Protein-Coupled Receptors, J. Klein-Seetharaman and M.C. Loewen ; Introduction; Structure, Stability, Dynamics, and Conformational Changes of Rhodopsin; Structures, Dynamics, and Conformational Changes of GPCRs; Conclusions; Towards Crystallization of G Protein-Coupled Receptors, M.L. Chiu and M.P MacWilliams ; Introduction; Overexpression and Purification; Detergent Selection; Sample Preparation; Crystallization Methods; Micelles and Bicelles; Lipidic Mesophases; Bicelles, Lipopeptides, and Nanodiscs; Crystallization; Case Study: Rhodopsin; Conclusions; Novel Solid-State NMR Methods for Structural Studies on G Protein-Coupled Receptors, A. Lange and M. Baldus ; Introduction; High-Resolution Solid State NMR; Sample Preparation; Applications; Conclusions and Outlook; Structural Genomics Initiatives, K. Lundstrom ; Introduction; Structural Genomics Programs on Membrane Proteins; Structural Genomics Initiatives Including GPCRs; MePNet Approach; Conclusions; Molecular Basis of Dimerization of Family A G Protein-Coupled Receptors, G Milligan ; Introduction; Quarternary Structure of Family A GPCRs; Consequences of the Dimerization of the Family A GPCRs; The Mechanisms of Dimerization of the Family A GPCRs; Conclusions; Orphan Receptors: Promising Targets for Drug Discovery, Y. Saito, Z. Wang, and O. Civelli ; Introduction; Search for Endogenous Ligands of Orphan GPCRs; Example of Deorphanization: The MCH Systems and Its Impact on Drug Discovery; Conclusions and Perspectives; Index Summary The contributors of these 16 papers use disease-oriented methods to describe the physiological roles of G protein-coupled receptors (GPRs) and their roles in target selection, screening and functional arrays. Topics include the biology of GPRs, their use as targets in cardiovascular drugs and metabolic disease, the possibilities for them in drug hi Bibliography Includes bibliographical references and index Notes Print version record Subject G proteins -- Receptors Drug development. Drugs -- Design. Receptors, G-Protein-Coupled Drug Delivery Systems Drug Design MEDICAL -- Biochemistry. Drugs -- Design Drug development G proteins -- Receptors Form Electronic book Author Lundstrom, Kenneth H Chiu, Mark L ISBN 1420028219 9781420028218 9780824725730 0824725735 9780429133794 0429133790

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