Voltage-Gated Ion Channels as Drug Targets

Triggle, David J. / Gopalakrishnan, Murali / Rampe, David / Zheng, Wei (Editor)

Methods and Principles in Medicinal Chemistry (Series Nr. 29)

1. Edition February 2006
XII, 480 Pages, Hardcover
121 Pictures
48 tables
Monograph

ISBN: 978-3-527-31258-0

Wiley-VCH, Weinheim

Wiley Online Library Content Sample Chapter Index List of Contributors

Short Description

Edited by prominent researchers in the field, this is a unique resource for drug developers and physiologists seeking a molecular-level understanding of ion channel pharmacology.

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Edited by the most prominent person in the field and top researchers at US pharmaceutical companies, this is a unique resource for drug developers and physiologists seeking a molecular-level understanding of ion channel pharmacology.
After an introduction to the topic, the authors evaluate the structure and function of ion channels, as well as related drug interaction. A section on assay technologies is followed by a section each on calcium, sodium and potassium channels. Further chapters cover genetic and acquired channelopathies, before the book closes with a look at safety issues in ion channel drug development.
For medicinal and pharmaceutical chemists, biochemists, molecular biologists and those working in the pharmaceutical industry.

Introduction
Structure and Function of Ion Channels
Drug Interaction at Ion Channels
Assay Technologies
Binding Studies
Ion Fluxes
Fluorescence Studies
Patch Clamping
Calcium Channels
Overview
T-type Channels
L-type Channels
N-type Channels
Sodium Channels
Overview
Channel Subtype Selectivity
Potassium Channels
Overview
Kv1.3
Kv1.5
Ca-activated channels
K(ATP)
KCNQ
Genetic and Acquired Channelopathies
Overview
HERG
Long QT Syndrome
Safety Issues in Ion Channel Drug Development

"The present book will be indispensable for all libraries of pharmaceutical companies. University libraries and researchers with an interest in the subject will also certainly wish to acquire this book."
Angewandte Chemie

"This volume makes an excellent case for initiating, continuing, or broadening studies to identify voltage-gated ion channel agonists. [...] Given these findings and the advances made in developing more rapid and reliable lead validation assays, this volume should be of interest to a broad range of medicinal chemists and pharmacologists."
Journal of Medicinal Chemistry

David J. Triggle is a Professor for Pharmacy at the State University of New York at Buffalo, USA, where he is investigating drug-receptor interactions and has specialized in ion channel pharmacology. He is the author of several books, has contributed around 350 papers, chapters and reviews, and has presented over 1,000 lectures worldwide.

David Rampe is currently head of the Safety Pharmacology Department at Sanofi-Aventis Pharmaceuticals in Bridgewater, NJ, USA. Over the past 17 years he has worked in both the discovery and development areas of the pharmaceutical industry.

Wei Zheng is a Group Leader at the NIH Chemical Genomics Center. He was previously a Group Leader at Merck's centralized screening center. Over the past 12 years he has being working in the area of assay development and high throughput screening.

Murali Gopalakrishnan is a Project Leader in the Neuroscience Research Division of Abbott Laboratories, Illinois, USA. Over the past 12 years he has been engaged in various drug discovery programs in the areas of central nervous system, urology and pain.

D. J. Triggle, State University of New York, Buffalo, USA; M. Gopalakrishnan, Abbott Laboratories, Abbott Park, USA; D. Rampe, Aventis Pharmaceuticals, Bridgewater, USA; W. Zheng, Merck & Co., North Wales, USA