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Therapeutic Targets : Modulation, Inhibition, and Activation.
The Latest Applications For Cellmechanism Research in Drug DiscoveryDesigned to connect research on cell mechanisms with the drug discovery process, Therapeutic Targets: Modulation, Inhibition, and Activation introduces readers to a range of new concepts and novel approaches to drug screening and th...
| Clasificación: | Libro Electrónico |
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| Autor principal: | |
| Otros Autores: | |
| Formato: | Electrónico eBook |
| Idioma: | Inglés |
| Publicado: |
Hoboken :
John Wiley & Sons,
2012.
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| Temas: | |
| Acceso en línea: | Texto completo |
Tabla de Contenidos:
- THERAPEUTIC TARGETS: MODULATION, INHIBITION, AND ACTIVATION; CONTENTS; Preface; Contributors; 1. cAMP-Specific Phosphodiesterases: Modulation, Inhibition, and Activation; 1.1 INTRODUCTION; 1.2 GENERAL CHARACTERISTICS OF PHOSPHODIESTERASES SPECIFIC FOR CYCLIC ADENOSINE MONOPHOSPHATE; 1.2.1 Modular Structure of cAMP-Specific PDEs; 1.2.2 PDE4s: Characterization and Regulation; Diversity of Isoforms; N-Terminal "Anchor"; UCR Regions; C-Terminal Site; Regulation of PDE4 Function by Posttranslation Modifications Other than Phosphorylation; 1.2.3 Inhibition of PDE4 as a Therapeutic Strategy.
- Pharmacologic Inhibition of the PDE4 Active SiteNovel Allosteric PDE4 Inhibitors; Alternative Strategies for Inhibition of Localized PDE4 Pools; PDE4 Knockout Mice; 1.2.4 PDE7; Characterization; Expression; Modulation; Inhibition; 1.2.5 PDE8; Characterization; Expression; Modulation; Inhibition; 1.3 CONCLUSIONS; ACKNOWLEDGMENTS; REFERENCES; 2. Protease-Activated Receptor 2; 2.1 INTRODUCTION; 2.2 OVERVIEW OF PAR2; 2.2.1 Activation; 2.2.2 Signal Transduction of PAR2; 2.2.3 Termination of PAR2 Signal; 2.3 PAR2 IN PHYSIOLOGY AND DISEASE; 2.3.1 PAR2 in Inflammation and Pain.
- 2.3.2 PAR2 in the Respiratory System2.3.3 PAR2 in Cardiovascular System; 2.3.4 PAR2 in the Gastrointestinal System; 2.3.5 PAR2 and Cancer; 2.3.6 PAR2 as a Therapeutic Target; 2.4 CONCLUSION; ACKNOWLEDGMENT; REFERENCES; 3. Voltage-Gated Sodium Channels as Therapeutic Targets; 3.1 INTRODUCTION; 3.2 INTRODUCTION TO VOLTAGE-GATED SODIUM CHANNELS; 3.2.1 The Nav Family; 3.2.2 Nav Channel Structure; The a-Subunit Pore; The Inactivation Gate; Voltage Sensor; 3.2.3 Protein-Protein Modulation of Nav Channels; 3.2.4 ß Subunits; 3.2.5 Therapeutic Relevance of Nav Channels; Pain and Inflammation.
- Muscle Channelopathies (Nav1.4)Cardiac Arrhythmias (Nav1.5); Nav Channels and Epilepsy; Migraine (Nav1.1); Cancer; Multiple Sclerosis and Immunomodulation; 3.3 Nav MODULATION WITH PEPTIDES AND SMALL MOLECULES; 3.3.1 Site-Specific Modulation of Nav Channels; Site 1: Pore Blockers; Sites 2 and 5: Intracellular Voltage-Dependent Gating Modulators; Sites 3 and 4: Extracellular Voltage-Dependent Gating Modulators; Site 6; 3.4 NEW THERAPEUTIC DIRECTIONS FOR NaV CHANNEL DRUG DISCOVERY; 3.4.1 Heterologous Expression of Nav; 3.4.2 Assay Technologies; Electrophysiology.
- Challenges with Automated Electrophysiology PlatformsCell-Based Functional Assay; Fluorescence-Based Assays; Cytotoxicity Assays; Binding Assays; Ion Flux Assays; 3.4.3 Label-Free Technology; 3.4.4 Venoms as Potent/Selective Drug Leads; 3.5 CONCLUSIONS; REFERENCES; 4. Multitarget Drugs for Stabilization of Calcium Cycling and Neuroprotection in Neurodegenerative Diseases and Stroke; 4.1 INTRODUCTION; 4.2 CALCIUM AS A UBIQUITOUS CELL MESSENGER; 4.2.1 Evolution of the Concept of Calcium Signaling; 4.2.2 Properties of Calcium that Make it an Ideal Cell Messenger; 4.3 CALCIUM ENTRY INTO CELLS.