Therapeutic targets [electronic resource] : modulation, inhibition, and activation / edited by Luis M. Botana, Mabel Loza.

Hoboken, N.J. : John Wiley & Sons, c2012.
1 online resource (504 p.)
Drugs -- Design.
Pharmaceutical industry.
Electronic books.
The Latest Applications For Cellmechanism Research in Drug Discovery Designed 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 therapeutic drug targeting to help inform future avenues of drug research. Highly topical, this accessible edited volume features chapters contributed by respected experts from around the globe. The book helps postgraduate students and professional scientists working in a
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 α-Subunit Pore; The Inactivation Gate; Voltage Sensor; 3.2.3 Protein-Protein Modulation of Nav Channels; 3.2.4 β 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
4.3.1 Diversity of Voltage-Dependent Calcium Channels
Description based upon print version of record.
Includes bibliographical references and index.
Botana, Luis M.
Loza, Mabel.
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