BACE

This book covers virtually all aspects of the rapidly developing field of beta secretase (BACE), from the original isolation and cloning of BACE, to the discovery of various classes of BACE inhibitors, to challenges in clinical development.

Informationen zum Autor VARGHESE JOHN is Director of Alzheimer's Drug Discovery at the Buck Institute for Age Research. He is a chemist with many years of pharmaceutical industry experience in discovery and development of drugs for CNS diseases with a primary focus on Alzheimer's disease (AD). Dr. John has many publications and patents to his credit. Klappentext BACE inhibitors and their use in the treatment of Alzheimer's DiseaseBACE (²-site of APP cleaving enzyme) is a critical component in Alzheimer's Disease (AD), and the development of BACE inhibitors shows great potential as a therapy for the disease. BACE: Lead Target for Orchestrated Therapy of Alzheimer's Disease covers virtually all aspects of BACE from initial identification, discovery of inhibitors, and challenges in clinical development, while providing a global understanding essential for productive and successful drug discovery.This book details the story of the discovery of BACE and its role in AD and comprehensively discusses:* The development of BACE inhibitors as therapeutics for Alzheimer's disease* The research that led to the identification of BACE* New BACE inhibitors currently being clinically tested* ADME (absorption, distribution, metabolism, excretion) and clinical trial design--topics not addressed in current field literature* Cutting-edge technology such as high-throughput screening, structure-based drug design, and QSAR in context of BACE inhibitors and Alzheimer's drug discovery* Other approaches to BACE inhibition based on interaction with the precursor protein APPBy enhancing the reader's understanding of the various aspects of the BACE drug-discovery process, this much-needed reference will serve as a key resource for all scientists involved in Alzheimer's research--and inspire new approaches to treatment of AD.Note: CD-ROM/DVD and other supplementary materials are not included as part of eBook file. Zusammenfassung This book covers virtually all aspects of the rapidly developing field of beta secretase (BACE), from the original isolation and cloning of BACE, to the discovery of various classes of BACE inhibitors, to challenges in clinical development. Inhaltsverzeichnis PREFACE.ACKNOWLEDGMENTS.CONTRIBUTORS.CHAPTER 1 BACE, APP PROCESSING, AND SIGNAL TRANSDUCTION IN ALZHEIMER'S DISEASE (Dale E. Bredesen and Edward H. Koo).1.1 Introduction.1.2 BACE Cleavage of APP as a Molecular Switching Mechanism.1.3 AD: An Imbalance in Cellular Dependence?1.4 BACE Cleavage, Caspase Cleavage, and Neuronal Trophic Dependence.1.5 BACE Cleavage of APP, Dependence Receptors, and Alzheimer Pathology.1.6 Key Mutations Proximal of APP Processing to A².1.7 Final Remarks.CHAPTER 2 IDENTIFICATION OF BACE AS A TARGET IN ALZHEIMER'S DISEASE (Robert L. Heinrikson and Sukanto Sinha).2.1 Introduction.2.2 The Search for 2-Secretase.2.3 Validation of the BACE Target.2.4 Final Remarks.CHAPTER 3 BACE BIOLOGICAL ASSAYS (Alfredo G. Tomasselli and Michael J. Bienkowski).3.1 Introduction.3.2 Clinical and Physiological Hallmarks of Alzheimer's Disease (AD).3.3 APP Processing.3.4 Aspartyl Protease Classifi cation.3.5 BACE Structure.3.6 Mechanism, Kinetics, Inhibition, and Specifi city.3.7 Assay Strategies for Inhibitor Finding and Development.3.8 Common Assays Used to Identify and Study Inhibitors.3.9 BACE Assays.3.10 Final Remarks.CHAPTER 4 PEPTIDIC, PEPTIDOMIMETIC, AND HTS-DERIVED BACE INHIBITORS (James P. Beck and Dustin J. Mergott).4.1 Introduction.4.2 Elan/Pharmacia (Pfizer).4.3 Oklahoma Medical Research Foundation (OMRF)/Multiple Collaborators.4.4 Eli Lilly.4.5 Merck.4.6 GlaxoSmithKline.4.7 Schering Plough.4.8 Bristol-Myers Squibb.4.9 Novartis.4.10 Amgen.4.11 Wyeth.4.12 Final Remarks.CHAPTER 5 FRAGMENT-BASED APPROACHES FOR IDENTIFICATION OF BACE INHIBITORS (Andreas Kuglstatter and Michael Hennig).5.1 Introduction.5.2 Biophysical ...

Autorentext
VARGHESE JOHN is Director of Alzheimer's Drug Discovery at the Buck Institute for Age Research. He is a chemist with many years of pharmaceutical industry experience in discovery and development of drugs for CNS diseases with a primary focus on Alzheimer's disease (AD). Dr. John has many publications and patents to his credit.

Klappentext
BACE inhibitors and their use in the treatment of Alzheimer's Disease BACE (²-site of APP cleaving enzyme) is a critical component in Alzheimer's Disease (AD), and the development of BACE inhibitors shows great potential as a therapy for the disease. BACE: Lead Target for Orchestrated Therapy of Alzheimer's Disease covers virtually all aspects of BACE from initial identification, discovery of inhibitors, and challenges in clinical development, while providing a global understanding essential for productive and successful drug discovery. This book details the story of the discovery of BACE and its role in AD and comprehensively discusses: * The development of BACE inhibitors as therapeutics for Alzheimer's disease * The research that led to the identification of BACE * New BACE inhibitors currently being clinically tested * ADME (absorption, distribution, metabolism, excretion) and clinical trial design--topics not addressed in current field literature * Cutting-edge technology such as high-throughput screening, structure-based drug design, and QSAR in context of BACE inhibitors and Alzheimer's drug discovery * Other approaches to BACE inhibition based on interaction with the precursor protein APP By enhancing the reader's understanding of the various aspects of the BACE drug-discovery process, this much-needed reference will serve as a key resource for all scientists involved in Alzheimer's research--and inspire new approaches to treatment of AD. Note: CD-ROM/DVD and other supplementary materials are not included as part of eBook file.

Inhalt
PREFACE. ACKNOWLEDGMENTS. CONTRIBUTORS. CHAPTER 1 BACE, APP PROCESSING, AND SIGNAL TRANSDUCTION IN ALZHEIMER'S DISEASE (Dale E. Bredesen and Edward H. Koo). 1.1 Introduction. 1.2 BACE Cleavage of APP as a Molecular Switching Mechanism. 1.3 AD: An Imbalance in Cellular Dependence? 1.4 BACE Cleavage, Caspase Cleavage, and Neuronal Trophic Dependence. 1.5 BACE Cleavage of APP, Dependence Receptors, and Alzheimer Pathology. 1.6 Key Mutations Proximal of APP Processing to A². 1.7 Final Remarks. CHAPTER 2 IDENTIFICATION OF BACE AS A TARGET IN ALZHEIMER'S DISEASE (Robert L. Heinrikson and Sukanto Sinha). 2.1 Introduction. 2.2 The Search for 2-Secretase. 2.3 Validation of the BACE Target. 2.4 Final Remarks. CHAPTER 3 BACE BIOLOGICAL ASSAYS (Alfredo G. Tomasselli and Michael J. Bienkowski). 3.1 Introduction. 3.2 Clinical and Physiological Hallmarks of Alzheimer's Disease (AD). 3.3 APP Processing. 3.4 Aspartyl Protease Classifi cation. 3.5 BACE Structure. 3.6 Mechanism, Kinetics, Inhibition, and Specifi city. 3.7 Assay Strategies for Inhibitor Finding and Development. 3.8 Common Assays Used to Identify and Study Inhibitors. 3.9 BACE Assays. 3.10 Final Remarks. CHAPTER 4 PEPTIDIC, PEPTIDOMIMETIC, AND HTS-DERIVED BACE INHIBITORS (James P. Beck and Dustin J. Mergott). 4.1 Introduction. 4.2 Elan/Pharmacia (Pfizer). 4.3 Oklahoma Medical Research Foundation (OMRF)/Multiple Collaborators. 4.4 Eli Lilly. 4.5 Merck. 4.6 GlaxoSmithKline. 4.7 Schering Plough. 4.8 Bristol-Myers Squibb. 4.9 Novartis. 4.10 Amgen. 4.11 Wyeth. 4.12 Final Remarks. CHAPTER 5 FRAGMENT-BASED APPROACHES FOR IDENTIFICATION OF BACE INHIBITORS (Andreas Kuglstatter and Michael Hennig). 5.1 Introduction. 5.2 Biophysical Methods Applied to BACE Fragment Screens. 5.3 BACE Inhibitors Identifi ed by Fragment Screening. 5.4 Final Remarks. CHAPTER 6 STRUCTURE-BASED DESIGN OF BACE INHIBITORS: TECHNICAL AND PR…

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