G protein-coupled receptors as drug targets [[electronic resource] ] : analysis of activation and constitutive activity / / edited by Roland Seifert and Thomas Wieland

• Pubblicazione: Weinheim, : Wiley-VCH; [Chichester, : John Wiley, distributor], c2005
• Descrizione fisica: 1 online resource (305 p.)
• Disciplina: 615.7
• Soggetto topico: Drug targeting; G proteins
• Altri autori: SeifertRoland WielandThomas
• Note generali: Description based upon print version of record.
• Nota di bibliografia: Includes bibliographical references and index.
• Nota di contenuto: G Protein-Coupled Receptors as Drug Targets; Table of Contents; Preface; A Personal Foreword; List of Contributors; Abbreviations and Terminology; I General Concepts; 1 Historical Background and Introduction; 2 The Nature of Constitutive Activity and Inverse Agonism; 2.1 Historical Perspective; 2.2 Theoretical Basis of Inverse Agonism: Relevance of Receptor Type; 2.3 The Interaction of Systems with Ligands; 2.4 Inverse Agonism as a Phenotypic Behavior; 2.5 Conclusion; 3 Molecular Mechanisms of GPCR Activation; 3.1 Introduction; 3.2 GPCR Structure and Ligand Recognition ; 3.3 Conformational Changes in the GPCR Activation Process3.4 Conversion to the Active Receptor State Involves Release of Stabilizing Intramolecular Interactions; 3.5 Kinetics of Agonist Binding and Receptor Activation; 3.6 GPCR Activation in an Oligomeric Context; 4 Molecular and Cellular Determinants of GPCR Splice Variant Constitutive Activity; 4.1 Introduction; 4.2 Constitutive Activation of Second Messenger Production by C-Terminal Splice Variants of GPCRs; 4.2.1 The Constitutive Activities of C-Terminal 5-HT(4) Receptor Splice Variants: the Shortest, the Strongest ; 4.2.2 The Constitutive Activities of mGlu(1)R and mGlu(5)R C-t Splice Variants: a Case for which a Physiological Control does exist4.2.3 Other Examples of GPCR C-t Splice Variants with Different Constitutive Activities; 4.3 Differential Constitutive Internalization of C-t GPCR Splice Variants; 4.3.1 The Thromboxane A2 Receptor TP(β)R, but not the TP(α)R Splice Variant, is Constitutively Internalized by Clathrin-dependent, GRK- and Arrestin-independent Mechanisms ; 4.3.2 The Prostaglandin F(2α) Receptor FP(B)R, but not the FP(A)R C-Terminal Splice Variant, is Constitutively Internalized by a Clathrin-independent, PI3-Kinase-dependent Mechanism4.4 Conclusion; 5 Naturally Occurring Constitutively Active Receptors: Physiological and Pharmacological Implications; 5.1 Introduction; 5.2 Wild-type Interspecies Homologues; 5.3 Wild-type Receptor Subtypes within a Given Species; 5.4 Wild-type Alternatively Spliced Receptors; 5.5 Polymorphisms in GPCRs; 5.6 GPCR Mutation-induced Disease; 5.7 Future Challenges ; 6 The Impact of G Proteins on Constitutive GPCR Activity6.1 Introduction; 6.2 The Contribution of G proteins to Constitutive Activity; 6.2.1 Basic Features; 6.2.2 The Distribution of G Proteins in the Plasma Membrane; 6.3 GPCR-G Protein Fusion Proteins; 6.3.1 Basic Features; 6.3.2 Modulation of the GPCR-G Protein Interface Alters Constitutive Activity; 6.3.3 Use of G Protein Variation to Detect Ligand Efficacy; 6.4 Conclusions; 7 (Patho)physiological and Therapeutic Relevance of Constitutive Activity and Inverse Agonism at G Protein-Coupled Receptors; 7.1 Introduction ; 7.2 Physiological Relevance of Constitutive Activity of GPCRs
• Sommario/riassunto: With its particular emphasis on the constitutive activity of G-protein-coupled receptors (GPCRs)s, this book comprehensively discusses an important biological process that has not yet been covered in such depth in any other existing books on GPCRs. The international team of highly distinguished authors addresses in detail current models and concepts, to introduce medicinal chemists, physiologists, pharmacologists, and medical researchers into the advances in the understanding of GPCR activation and constitutive activity. In addition, the book provides an overview on methods of investigating co
• Titolo autorizzato: G protein-coupled receptors as drug targets
• ISBN: 1-280-85404-9; 9786610854042; 3-527-60734-X; 3-527-60695-5
• Formato: Materiale a stampa
• Livello bibliografico: Monografia
• Lingua di pubblicazione: Inglese
• Record Nr.: 9910830452703321
• Lo trovi qui: Univ. Federico II
• Serie: Methods and principles in medicinal chemistry ; ; v. 24.