G protein-coupled receptors in drug discovery. (2006)

• Record Type: Book
• Further Information: Note: Edited by Kenneth H. Lundstrom, Mark L. Chiu.
• Other Names: Lundstrom, Kenneth H; Chiu, Mark L
• 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
• Publisher Details: Boca Raton : Taylor & Francis
• Publication Date: 2006
• Extent: 1 online resource (362 pages), illustrations
• Subjects: 612/.01575; G proteins -- Receptors; Drug development; Receptors, G-Protein-Coupled; Drug Delivery Systems; Drug Design; MEDICAL -- Biochemistry; Drug development; G proteins -- Receptors; Electronic books
• Languages: English
• ISBNs: 1420028219; 9781420028218; 9780824725730; 0824725735
• Related ISBNs: 0824725735
• Notes: Note: Includes bibliographical references and index.; Note: Print version record.
• Access Rights: Legal Deposit; Only available on premises controlled by the deposit library and to one user at any one time; The Legal Deposit Libraries (Non-Print Works) Regulations (UK).
• Access Usage: Restricted: Printing from this resource is governed by The Legal Deposit Libraries (Non-Print Works) Regulations (UK) and UK copyright law currently in force.