Info
- Utilizzare la checkbox di selezione a fianco di ciascun documento per attivare le funzionalità di stampa, invio email, download nei formati disponibili del (i) record.
G protein-coupled receptors as drug targets [[electronic resource] ] : analysis of activation and constitutive activity / / edited by Roland Seifert and Thomas Wieland
| G protein-coupled receptors as drug targets [[electronic resource] ] : analysis of activation and constitutive activity / / edited by Roland Seifert and Thomas Wieland |
| Pubbl/distr/stampa | Weinheim, : Wiley-VCH |
| Descrizione fisica | 1 online resource (305 p.) |
| Disciplina | 615.7 |
| Altri autori (Persone) |
SeifertRoland
WielandThomas |
| Collana | Methods and principles in medicinal chemistry |
| Soggetto topico |
Drug targeting
G proteins |
| Soggetto genere / forma | Electronic books. |
| ISBN |
1-280-85404-9
9786610854042 3-527-60734-X 3-527-60695-5 |
| Formato | Materiale a stampa  |
| Livello bibliografico | Monografia |
| Lingua di pubblicazione | eng |
| 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 |
| Record Nr. | UNINA-9910144275503321 |
| Weinheim, : Wiley-VCH | ||
| Materiale a stampa | ||
| Lo trovi qui: Univ. Federico II | ||
| ||
G protein-coupled receptors as drug targets [[electronic resource] ] : analysis of activation and constitutive activity / / edited by Roland Seifert and Thomas Wieland
| G protein-coupled receptors as drug targets [[electronic resource] ] : analysis of activation and constitutive activity / / edited by Roland Seifert and Thomas Wieland |
| Pubbl/distr/stampa | Weinheim, : Wiley-VCH |
| Descrizione fisica | 1 online resource (305 p.) |
| Disciplina | 615.7 |
| Altri autori (Persone) |
SeifertRoland
WielandThomas |
| Collana | Methods and principles in medicinal chemistry |
| Soggetto topico |
Drug targeting
G proteins |
| ISBN |
1-280-85404-9
9786610854042 3-527-60734-X 3-527-60695-5 |
| Formato | Materiale a stampa |
| Livello bibliografico | Monografia |
| Lingua di pubblicazione | eng |
| 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 |
| Record Nr. | UNINA-9910830452703321 |
| Weinheim, : Wiley-VCH | ||
| Materiale a stampa | ||
| Lo trovi qui: Univ. Federico II | ||
| ||
G protein-coupled receptors as drug targets : analysis of activation and constitutive activity / / edited by Roland Seifert and Thomas Wieland
| G protein-coupled receptors as drug targets : analysis of activation and constitutive activity / / edited by Roland Seifert and Thomas Wieland |
| Pubbl/distr/stampa | Weinheim, : Wiley-VCH |
| Descrizione fisica | 1 online resource (305 p.) |
| Disciplina | 615.7 |
| Altri autori (Persone) |
SeifertRoland
WielandThomas |
| Collana | Methods and principles in medicinal chemistry |
| Soggetto topico |
Drug targeting
G proteins |
| ISBN |
9786610854042
9781280854040 1280854049 9783527607341 352760734X 9783527606955 3527606955 |
| Formato | Materiale a stampa |
| Livello bibliografico | Monografia |
| Lingua di pubblicazione | eng |
| 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 |
| Record Nr. | UNINA-9911019482603321 |
| Weinheim, : Wiley-VCH | ||
| Materiale a stampa | ||
| Lo trovi qui: Univ. Federico II | ||
| ||
GPCR molecular pharmacology and drug targeting [[electronic resource] ] : shifting paradigms and new directions / / edited by Annette Gilchrist
| GPCR molecular pharmacology and drug targeting [[electronic resource] ] : shifting paradigms and new directions / / edited by Annette Gilchrist |
| Pubbl/distr/stampa | Hoboken, N.J., : Wiley, c2010 |
| Descrizione fisica | 1 online resource (544 p.) |
| Disciplina | 612/.015756 |
| Altri autori (Persone) | GilchristAnnette |
| Soggetto topico |
G proteins
Drug targeting |
| ISBN |
1-118-03517-8
1-282-68599-6 9786612685996 0-470-62732-8 0-470-62731-X |
| Formato | Materiale a stampa |
| Livello bibliografico | Monografia |
| Lingua di pubblicazione | eng |
| Nota di contenuto |
GPCR MOLECULAR PHARMACOLOGY AND DRUG TARGETING: SHIFTING PARADIGMS AND NEW DIRECTIONS; CONTENTS; PREFACE; CONTRIBUTORS; CHAPTER 1: The Evolution of Receptors: From On-Off Switches to Microprocessors; CHAPTER 2: The Evolving Pharmacology of GPCRs; CHAPTER 3: The Emergence of Allosteric Modulators for G Protein - Coupled Receptors; CHAPTER 4: Receptor-Mediated G Protein Activation: How, How Many, and Where?; CHAPTER 5: Molecular Pharmacology of Frizzleds-with Implications for Possible Therapy
CHAPTER 6: Secretin Receptor Dimerization: A Possible Functionally Important Paradigm for Family B G Protein-Coupled ReceptorsCHAPTER 7: Past and Future Strategies for GPCR Deorphanization; CHAPTER 8: High-Throughput GPCR Screening Technologies and the Emerging Importance of the Cell Phenotype; CHAPTER 9: Are "Traditional" Biochemical Techniques Out of Fashion in the New Era of GPCR Pharmacology?; CHAPTER 10: Fluorescence and Resonance Energy Transfer Shine New Light on GPCR Function; CHAPTER 11: Integration of Label-Free Detection Methods in GPCR Drug Discovery CHAPTER 12: Screening for Allosteric Modulators of G Protein-Coupled ReceptorsCHAPTER 13: Ultra-High-Throughput Screening Assays for GPCRs; CHAPTER 14: New Techniques to Express and Crystallize G Protein-Coupled Receptors; CHAPTER 15: Structure and Modeling of GPCRs: Implications for Drug Discovery; CHAPTER 16: X-Ray Structure Developments for GPCR Drug Targets; CHAPTER 17: Pharmacological Chaperones: Potential for the Treatment of Hereditary Diseases Caused by Mutations in G Protein-Coupled Receptors; INDEX |
| Record Nr. | UNINA-9910139201903321 |
| Hoboken, N.J., : Wiley, c2010 | ||
| Materiale a stampa | ||
| Lo trovi qui: Univ. Federico II | ||
| ||
GPCR molecular pharmacology and drug targeting : shifting paradigms and new directions / / edited by Annette Gilchrist
| GPCR molecular pharmacology and drug targeting : shifting paradigms and new directions / / edited by Annette Gilchrist |
| Edizione | [1st ed.] |
| Pubbl/distr/stampa | Hoboken, N.J., : Wiley, c2010 |
| Descrizione fisica | 1 online resource (544 p.) |
| Disciplina | 612/.015756 |
| Altri autori (Persone) | GilchristAnnette |
| Soggetto topico |
G proteins
Drug targeting |
| ISBN |
9786612685996
9781118035177 1118035178 9781282685994 1282685996 9780470627327 0470627328 9780470627310 047062731X |
| Formato | Materiale a stampa |
| Livello bibliografico | Monografia |
| Lingua di pubblicazione | eng |
| Nota di contenuto |
GPCR MOLECULAR PHARMACOLOGY AND DRUG TARGETING: SHIFTING PARADIGMS AND NEW DIRECTIONS; CONTENTS; PREFACE; CONTRIBUTORS; CHAPTER 1: The Evolution of Receptors: From On-Off Switches to Microprocessors; CHAPTER 2: The Evolving Pharmacology of GPCRs; CHAPTER 3: The Emergence of Allosteric Modulators for G Protein - Coupled Receptors; CHAPTER 4: Receptor-Mediated G Protein Activation: How, How Many, and Where?; CHAPTER 5: Molecular Pharmacology of Frizzleds-with Implications for Possible Therapy
CHAPTER 6: Secretin Receptor Dimerization: A Possible Functionally Important Paradigm for Family B G Protein-Coupled ReceptorsCHAPTER 7: Past and Future Strategies for GPCR Deorphanization; CHAPTER 8: High-Throughput GPCR Screening Technologies and the Emerging Importance of the Cell Phenotype; CHAPTER 9: Are "Traditional" Biochemical Techniques Out of Fashion in the New Era of GPCR Pharmacology?; CHAPTER 10: Fluorescence and Resonance Energy Transfer Shine New Light on GPCR Function; CHAPTER 11: Integration of Label-Free Detection Methods in GPCR Drug Discovery CHAPTER 12: Screening for Allosteric Modulators of G Protein-Coupled ReceptorsCHAPTER 13: Ultra-High-Throughput Screening Assays for GPCRs; CHAPTER 14: New Techniques to Express and Crystallize G Protein-Coupled Receptors; CHAPTER 15: Structure and Modeling of GPCRs: Implications for Drug Discovery; CHAPTER 16: X-Ray Structure Developments for GPCR Drug Targets; CHAPTER 17: Pharmacological Chaperones: Potential for the Treatment of Hereditary Diseases Caused by Mutations in G Protein-Coupled Receptors; INDEX |
| Record Nr. | UNINA-9910811243903321 |
| Hoboken, N.J., : Wiley, c2010 | ||
| Materiale a stampa | ||
| Lo trovi qui: Univ. Federico II | ||
| ||
The GTPase superfamily [[electronic resource] /] / [editors, Joan Marsh (organizer) and Jamie Goode]
| The GTPase superfamily [[electronic resource] /] / [editors, Joan Marsh (organizer) and Jamie Goode] |
| Pubbl/distr/stampa | Chichester ; ; New York, : Wiley, 1993 |
| Descrizione fisica | 1 online resource (302 p.) |
| Disciplina |
574.19
574.19245 |
| Altri autori (Persone) |
MarshJoan
GoodeJamie |
| Collana | Ciba Foundation symposium |
| Soggetto topico |
G proteins
Guanosine triphosphatase Guanosine triphosphatase genes |
| Soggetto genere / forma | Electronic books. |
| ISBN |
1-282-34785-3
9786612347856 0-470-51445-0 0-470-51446-9 |
| Formato | Materiale a stampa |
| Livello bibliografico | Monografia |
| Lingua di pubblicazione | eng |
| Nota di contenuto |
THE GTPase SUPERFAMILY; Contents; Introduction; Three-dimensional structure and properties of wild-type and mutant H-ras-encoded p21; Elongation factors in protein synthesis; RAS function and protein kinase cascades; Cell transformation by ras and regulation of its protein product; Identification of ras targets using a genetic approach; G proteins in signal transduction: the regulation of phospholipase C; The G protein cascade of visual transduction: kinetics and regulation; General discussion I Voltage-dependent Ca2+ channels as GAPS; Regulators of small GTPases
A GTPase cycle in initiation of protein translocation across the endoplasmic reticulum membraneA cell-physiological description of GE, a GTP-binding protein that mediates exocytosis; Dynamin, a GTPase involved in the initial stages of endocytosis; The VPS1 protein is a dynamin-like GTPase required for sorting proteins to the yeast vacuole; General discussion II : Ras-mediated signalling pathway during vulval development in Caenorhabditis elegans; The cycle of SEC4 function in vesicular transport; Mx proteins: GTPases involved in the interferon-induced antiviral state Should the tubulins be members of the GTPase superfamily?Final general discussion; Summing-up; Index of contributors; Subject index |
| Record Nr. | UNINA-9910144742803321 |
| Chichester ; ; New York, : Wiley, 1993 | ||
| Materiale a stampa | ||
| Lo trovi qui: Univ. Federico II | ||
| ||
The GTPase superfamily [[electronic resource] /] / [editors, Joan Marsh (organizer) and Jamie Goode]
| The GTPase superfamily [[electronic resource] /] / [editors, Joan Marsh (organizer) and Jamie Goode] |
| Pubbl/distr/stampa | Chichester ; ; New York, : Wiley, 1993 |
| Descrizione fisica | 1 online resource (302 p.) |
| Disciplina |
574.19
574.19245 |
| Altri autori (Persone) |
MarshJoan
GoodeJamie |
| Collana | Ciba Foundation symposium |
| Soggetto topico |
G proteins
Guanosine triphosphatase Guanosine triphosphatase genes |
| ISBN |
1-282-34785-3
9786612347856 0-470-51445-0 0-470-51446-9 |
| Formato | Materiale a stampa |
| Livello bibliografico | Monografia |
| Lingua di pubblicazione | eng |
| Nota di contenuto |
THE GTPase SUPERFAMILY; Contents; Introduction; Three-dimensional structure and properties of wild-type and mutant H-ras-encoded p21; Elongation factors in protein synthesis; RAS function and protein kinase cascades; Cell transformation by ras and regulation of its protein product; Identification of ras targets using a genetic approach; G proteins in signal transduction: the regulation of phospholipase C; The G protein cascade of visual transduction: kinetics and regulation; General discussion I Voltage-dependent Ca2+ channels as GAPS; Regulators of small GTPases
A GTPase cycle in initiation of protein translocation across the endoplasmic reticulum membraneA cell-physiological description of GE, a GTP-binding protein that mediates exocytosis; Dynamin, a GTPase involved in the initial stages of endocytosis; The VPS1 protein is a dynamin-like GTPase required for sorting proteins to the yeast vacuole; General discussion II : Ras-mediated signalling pathway during vulval development in Caenorhabditis elegans; The cycle of SEC4 function in vesicular transport; Mx proteins: GTPases involved in the interferon-induced antiviral state Should the tubulins be members of the GTPase superfamily?Final general discussion; Summing-up; Index of contributors; Subject index |
| Record Nr. | UNINA-9910831059003321 |
| Chichester ; ; New York, : Wiley, 1993 | ||
| Materiale a stampa | ||
| Lo trovi qui: Univ. Federico II | ||
| ||
The GTPase superfamily / / [editors, Joan Marsh (organizer) and Jamie Goode]
| The GTPase superfamily / / [editors, Joan Marsh (organizer) and Jamie Goode] |
| Pubbl/distr/stampa | Chichester ; ; New York, : Wiley, 1993 |
| Descrizione fisica | 1 online resource (302 p.) |
| Disciplina | 574.19/245 |
| Altri autori (Persone) |
MarshJoan
GoodeJamie |
| Collana | Ciba Foundation symposium |
| Soggetto topico |
G proteins
Guanosine triphosphatase Guanosine triphosphatase genes |
| ISBN |
9786612347856
9781282347854 1282347853 9780470514450 0470514450 9780470514467 0470514469 |
| Formato | Materiale a stampa |
| Livello bibliografico | Monografia |
| Lingua di pubblicazione | eng |
| Nota di contenuto |
THE GTPase SUPERFAMILY; Contents; Introduction; Three-dimensional structure and properties of wild-type and mutant H-ras-encoded p21; Elongation factors in protein synthesis; RAS function and protein kinase cascades; Cell transformation by ras and regulation of its protein product; Identification of ras targets using a genetic approach; G proteins in signal transduction: the regulation of phospholipase C; The G protein cascade of visual transduction: kinetics and regulation; General discussion I Voltage-dependent Ca2+ channels as GAPS; Regulators of small GTPases
A GTPase cycle in initiation of protein translocation across the endoplasmic reticulum membraneA cell-physiological description of GE, a GTP-binding protein that mediates exocytosis; Dynamin, a GTPase involved in the initial stages of endocytosis; The VPS1 protein is a dynamin-like GTPase required for sorting proteins to the yeast vacuole; General discussion II : Ras-mediated signalling pathway during vulval development in Caenorhabditis elegans; The cycle of SEC4 function in vesicular transport; Mx proteins: GTPases involved in the interferon-induced antiviral state Should the tubulins be members of the GTPase superfamily?Final general discussion; Summing-up; Index of contributors; Subject index |
| Record Nr. | UNINA-9911020450003321 |
| Chichester ; ; New York, : Wiley, 1993 | ||
| Materiale a stampa | ||
| Lo trovi qui: Univ. Federico II | ||
| ||
Ligand design for G protein-coupled receptors [[electronic resource] /] / edited by Didier Rognan
| Ligand design for G protein-coupled receptors [[electronic resource] /] / edited by Didier Rognan |
| Pubbl/distr/stampa | Weinheim ; ; [Great Britain], : Wiley, 2006 |
| Descrizione fisica | 1 online resource (286 p.) |
| Disciplina |
541.2242
615.19 |
| Altri autori (Persone) | RognanDidier |
| Collana | Methods and principles in medicinal chemistry |
| Soggetto topico |
Ligands (Biochemistry)
G proteins Drugs - Design |
| Soggetto genere / forma | Electronic books. |
| ISBN |
1-280-72349-1
9786610723492 3-527-60824-9 3-527-60826-5 |
| Formato | Materiale a stampa |
| Livello bibliografico | Monografia |
| Lingua di pubblicazione | eng |
| Nota di contenuto |
Ligand Design for G Protein-coupled Receptors; Contents; Preface; A Personal Foreword; List of Contributors; 1 G Protein-coupled Receptors in the Human Genome; 1.1 Introduction; 1.2 The Adhesion Family; 1.3 The Secretin Family; 1.4 The Frizzled/Taste 2 Family; 1.4.1 The Frizzled Receptor Cluster; 1.4.2 The Taste 2 Receptor Cluster; 1.5 The Glutamate Family; 1.6 The Rhodopsin Family; 1.6.1 The Rhodopsin α-Group; 1.6.1.1 The Prostaglandin Receptor Cluster; 1.6.1.2 The Amine Receptor Cluster; 1.6.1.3 The Opsin Receptor Cluster; 1.6.1.4 The Melatonin Receptor Cluster
1.6.1.5 The MECA Receptor Cluster1.6.1.6 Other Rhodopsin α-Receptors; 1.6.2 Rhodopsin β-Group; 1.6.3 Rhodopsin γ-Group; 1.6.3.1 The SOG Receptor Cluster; 1.6.3.2 The Melanocyte Concentrating Hormone Receptor Cluster; 1.6.3.3 The Chemokine Receptor Cluster; 1.6.3.4 Other Rhodopsin γ-Receptors; 1.6.4 The Rhodopsin δ-Group; 1.6.4.1 The MAS-related Receptor Cluster; 1.6.4.2 The Glycoprotein Receptor Cluster; 1.6.4.3 The Coagulation Factor Receptor Cluster; 1.6.4.4 The Purinergic Receptor Cluster; 1.6.4.5 The Olfactory Receptor Cluster; 1.6.4.6 Other Rhodopsin α-Receptors; 1.7 Other GPCRs 1.8 Future PerspectiveReferences; 2 Why G Protein-coupled Receptors Databases are Needed; 2.1 Introduction; 2.2 A Non-exhaustive List of the GPCR Data Models; 2.3 Using the Central Dogma of Biology; 2.4 Using the Tree of Life; 2.5 Using a Chemogenomic Approach; 2.6 Conclusion; References; 3 A Novel Drug Screening Assay for G Protein-coupled Receptors; 3.1 Introduction; 3.1.1 History; 3.1.2 Nuclear Translocation of Endogenous GPCRs; 3.1.3 The MOCA Method; 3.2 The MOCA Strategy Demonstrated with the D1 Dopamine Receptor; 3.2.1 Development of the Assay 3.2.2 Concentration-dependent Antagonist Blockade of Nuclear Transport3.2.3 Measurement of Receptor Cell Surface Expression: Antagonist Binding of Receptors at Cell Surface; 3.3 Development of Quantitative Methodology Suitable for High Throughput Analysis; 3.3.1 Nuclear Translocation of Orphan GPCRs; 3.4 Discussion of the MOCA Method; 3.5 Conclusion; References; 4 Importance of GPCR Dimerization for Function: The Case of the Class C GPCRs; 4.1 Introduction; 4.2 Class C GPCRs are Multidomain Proteins; 4.2.1 The VFT; 4.2.2 The CRD; 4.2.3 The HD; 4.2.4 C-Tail 4.3 Class C GPCRs are Constitutive Dimers4.4 Agonists Activate Class C GPCRs by Stabilizing the Closed State of the VFT; 4.5 Dimeric Functioning of the Dimer of VFTs; 4.5.1 Agonist Stoichiometry: Symmetry or Asymmetry?; 4.6 The Heptahelical Domain, the Target of Positive and Negative Allosteric Modulators, Behaves in a Manner Similar to Rhodopsin-like Class A GPCRs; 4.7 Allosteric Coupling Between the Extracellular and Heptahelical Domains within the Dimer; 4.7.1 Molecular Determinants of the Coupling Between the VFT and the HD; 4.7.2 Cis- and Trans-activation Can Exist within Class C GPCRs 4.8 Asymmetric Functioning of the HD Dimer |
| Record Nr. | UNINA-9910144274103321 |
| Weinheim ; ; [Great Britain], : Wiley, 2006 | ||
| Materiale a stampa | ||
| Lo trovi qui: Univ. Federico II | ||
| ||
Ligand design for G protein-coupled receptors [[electronic resource] /] / edited by Didier Rognan
| Ligand design for G protein-coupled receptors [[electronic resource] /] / edited by Didier Rognan |
| Pubbl/distr/stampa | Weinheim ; ; [Great Britain], : Wiley, 2006 |
| Descrizione fisica | 1 online resource (286 p.) |
| Disciplina |
541.2242
615.19 |
| Altri autori (Persone) | RognanDidier |
| Collana | Methods and principles in medicinal chemistry |
| Soggetto topico |
Ligands (Biochemistry)
G proteins Drugs - Design |
| ISBN |
1-280-72349-1
9786610723492 3-527-60824-9 3-527-60826-5 |
| Formato | Materiale a stampa |
| Livello bibliografico | Monografia |
| Lingua di pubblicazione | eng |
| Nota di contenuto |
Ligand Design for G Protein-coupled Receptors; Contents; Preface; A Personal Foreword; List of Contributors; 1 G Protein-coupled Receptors in the Human Genome; 1.1 Introduction; 1.2 The Adhesion Family; 1.3 The Secretin Family; 1.4 The Frizzled/Taste 2 Family; 1.4.1 The Frizzled Receptor Cluster; 1.4.2 The Taste 2 Receptor Cluster; 1.5 The Glutamate Family; 1.6 The Rhodopsin Family; 1.6.1 The Rhodopsin α-Group; 1.6.1.1 The Prostaglandin Receptor Cluster; 1.6.1.2 The Amine Receptor Cluster; 1.6.1.3 The Opsin Receptor Cluster; 1.6.1.4 The Melatonin Receptor Cluster
1.6.1.5 The MECA Receptor Cluster1.6.1.6 Other Rhodopsin α-Receptors; 1.6.2 Rhodopsin β-Group; 1.6.3 Rhodopsin γ-Group; 1.6.3.1 The SOG Receptor Cluster; 1.6.3.2 The Melanocyte Concentrating Hormone Receptor Cluster; 1.6.3.3 The Chemokine Receptor Cluster; 1.6.3.4 Other Rhodopsin γ-Receptors; 1.6.4 The Rhodopsin δ-Group; 1.6.4.1 The MAS-related Receptor Cluster; 1.6.4.2 The Glycoprotein Receptor Cluster; 1.6.4.3 The Coagulation Factor Receptor Cluster; 1.6.4.4 The Purinergic Receptor Cluster; 1.6.4.5 The Olfactory Receptor Cluster; 1.6.4.6 Other Rhodopsin α-Receptors; 1.7 Other GPCRs 1.8 Future PerspectiveReferences; 2 Why G Protein-coupled Receptors Databases are Needed; 2.1 Introduction; 2.2 A Non-exhaustive List of the GPCR Data Models; 2.3 Using the Central Dogma of Biology; 2.4 Using the Tree of Life; 2.5 Using a Chemogenomic Approach; 2.6 Conclusion; References; 3 A Novel Drug Screening Assay for G Protein-coupled Receptors; 3.1 Introduction; 3.1.1 History; 3.1.2 Nuclear Translocation of Endogenous GPCRs; 3.1.3 The MOCA Method; 3.2 The MOCA Strategy Demonstrated with the D1 Dopamine Receptor; 3.2.1 Development of the Assay 3.2.2 Concentration-dependent Antagonist Blockade of Nuclear Transport3.2.3 Measurement of Receptor Cell Surface Expression: Antagonist Binding of Receptors at Cell Surface; 3.3 Development of Quantitative Methodology Suitable for High Throughput Analysis; 3.3.1 Nuclear Translocation of Orphan GPCRs; 3.4 Discussion of the MOCA Method; 3.5 Conclusion; References; 4 Importance of GPCR Dimerization for Function: The Case of the Class C GPCRs; 4.1 Introduction; 4.2 Class C GPCRs are Multidomain Proteins; 4.2.1 The VFT; 4.2.2 The CRD; 4.2.3 The HD; 4.2.4 C-Tail 4.3 Class C GPCRs are Constitutive Dimers4.4 Agonists Activate Class C GPCRs by Stabilizing the Closed State of the VFT; 4.5 Dimeric Functioning of the Dimer of VFTs; 4.5.1 Agonist Stoichiometry: Symmetry or Asymmetry?; 4.6 The Heptahelical Domain, the Target of Positive and Negative Allosteric Modulators, Behaves in a Manner Similar to Rhodopsin-like Class A GPCRs; 4.7 Allosteric Coupling Between the Extracellular and Heptahelical Domains within the Dimer; 4.7.1 Molecular Determinants of the Coupling Between the VFT and the HD; 4.7.2 Cis- and Trans-activation Can Exist within Class C GPCRs 4.8 Asymmetric Functioning of the HD Dimer |
| Record Nr. | UNINA-9910831167703321 |
| Weinheim ; ; [Great Britain], : Wiley, 2006 | ||
| Materiale a stampa | ||
| Lo trovi qui: Univ. Federico II | ||
| ||
