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Ion Channel Drug Discovery

Ion Channel Drug Discovery
Author: Brian Cox
Publisher: Royal Society of Chemistry
Total Pages: 384
Release: 2014-09-03
Genre: Science
ISBN: 1849735085

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Ion channel drug discovery is a rapidly evolving field fuelled by recent, but significant, advances in our understanding of ion channel function combined with enabling technologies such as automated electrophysiology. The resurgent interest in this target class by both pharmaceutical and academic scientists was clearly highlighted by the over-subscribed RSC/BPS 'Ion Channels as Therapeutic Targets' symposium in February 2009. This book builds on the platform created by that meeting, covering themes including advances in screening technology, ion channel structure and modelling and up-to-date case histories of the discovery of modulators of a range of channels, both voltage-gated and non-voltage-gated channels. The editors have built an extensive network of contacts in the field through their first-hand scientific experience, collaborations and conference participation and the organisation of the meeting at Novartis, Horsham, increased the network enabling the editors to draw on the experience of eminent researchers in the field. Interest and investment in ion channel modulation in both industrial and academic settings continues to grow as new therapeutic opportunities are identified and realised for ion channel modulation. This book provides a reference text by covering a combination of recent advances in the field, from technological and medicinal chemistry perspectives, as well as providing an introduction to the new 'ion channel drug discoverer'. The book has contributions from highly respected academic researchers, industrial researchers at the cutting edge of drug discovery and experts in enabling technology. This combination provides a complete picture of the field of interest to a wide range of readers.


Ion Channels as Targets in Drug Discovery

Ion Channels as Targets in Drug Discovery
Author: Gary Stephens
Publisher: Springer
Total Pages: 0
Release: 2024-05-19
Genre: Medical
ISBN: 9783031521966

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This book is built around ion channel research and, more specifically, ion channels as important therapeutic drug targets. Under the editorial leadership of Gary Stephens in academic research and Edward Stevens from industry, the aim is to bring these strands together to provide a cutting-edge translational reference on ion channel drug discovery. Exploiting our knowledge of ion channel structure and function has clear current and future potential to intervene and correct the pathophysiology associated with debilitating conditions, including cardiovascular disease, diabetes, cystic fibrosis, pain, epilepsy, and neurodegenerative disorders. Individual chapters have a disease focus, also providing a “case study story” that will also appeal to a clinical audience, while background information on a given ion channel is presented to provide a solid reference for undergraduate and postgraduate teaching.


Voltage-Gated Ion Channels as Drug Targets

Voltage-Gated Ion Channels as Drug Targets
Author: David J. Triggle
Publisher: John Wiley & Sons
Total Pages: 492
Release: 2006-08-21
Genre: Science
ISBN: 3527607749

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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.


Structure, Function, and Modulation of Neuronal Voltage-Gated Ion Channels

Structure, Function, and Modulation of Neuronal Voltage-Gated Ion Channels
Author: Valentin K. Gribkoff
Publisher: John Wiley & Sons
Total Pages: 505
Release: 2008-12-09
Genre: Science
ISBN: 0470429895

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This book discusses voltage-gated ion channels and their importance in drug discovery and development. The book includes reviews of the channel genome, the physiological bases of targeting ion channels in disease, the unique technologies developed for ion channel drug discovery, and the increasingly important role of ion channel screening in cardiac risk assessment. It provides an important reference for research scientists and drug discovery companies.


Ion channel screening: advances in technologies and analysis

Ion channel screening: advances in technologies and analysis
Author: Ralf F. Kettenhofen
Publisher: Frontiers E-books
Total Pages: 103
Release:
Genre:
ISBN: 2889190358

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Ion channel research has increased tremendously in the past 35 years since the first publication of the patch clamp technique by Neher and Sakmann in 1976. This is documented by the rising number of publications listed in Pubmed (http://www.ncbi.nlm.nih.gov/pubmed) including the keyword ‘ion channel’ from just 186 hits in 1976 to almost 180,000 hits today. Ion channels attract this great interest due to their pivotal role in the control of fundamental physiological processes in a plethora of different tissues. Moreover, their importance in a wide range of inherited and drug-induced pathologies spanning all major therapeutic areas makes them attractive targets for pharmacological drug screening and potential risk factors when assessing drug safety (Ashcroft, 2006; Clare, 2010; Dunlop 2008; Milligan 2009). Several methods and technologies have been developed to meet the analytical needs for studying ion channels. These approaches have addressed ion channel function directly as well as in the context of the cell and tissue. Scaling of these technologies has allowed ion channel analysis to be carried out on high throughput and high content assay systems. In this Research Topic we want to provide an up-to-date collection of the latest developments and improvements in ion channel screening; defining the cutting edge and indicating further developments required in the future.


Ion Channels and Their Inhibitors

Ion Channels and Their Inhibitors
Author: Satya Prakash Gupta
Publisher: Springer Science & Business Media
Total Pages: 358
Release: 2011-06-21
Genre: Science
ISBN: 3642199224

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Being the crucial components of living cells, ion channels are important targets of therapeutic agents. Historically, it has been challenging to develop drugs on this target class. A major issue with target based ion channel drug development is the identification of effective small chemical leads for medicinal chemistry optimization to the clinical candidate status. Thus enough attention has been paid to the study of structure and functions of ion channels and their potential inhibitors. The present book compiles important chapters authored by eminent workers in the field to cover important recent advances in the studies of the structure and functions of ion channels and their inhibitors, such as sodium ion, potassium ion, chloride ion, calcium ion channel inhibitors. The book may be of great use to the students and scientists working in the area of molecular biology, biochemistry, physiology, neurobiology, and medicinal chemistry.


Expression and Analysis of Recombinant Ion Channels

Expression and Analysis of Recombinant Ion Channels
Author: Jeffrey J. Clare
Publisher: John Wiley & Sons
Total Pages: 302
Release: 2006-08-21
Genre: Science
ISBN: 3527607935

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Filling the gap created over the past five years, during which many new techniques have entered the market, this book is directed at both the new and the experienced ion channel researcher wishing to learn more about the considerations and methods for studying recombinant ion channels. These latest developments are covered here for the first time, contributed by editors and authors working for major pharmaceutical companies and who routinely apply these techniques in their daily work. The first three chapters cover the use of the Xenopus oocyte expression system for structure-function studies, from basic approaches for manipulating ion channel cDNAs to more specialized but powerful techniques. This is followed by reviews of strategies and methodologies available for expressing channels in mammalian cells and for their analysis by patch-clamp electrophysiology. Chapters 6 to 8 review the latest methodologies for ion channel drug discovery, including high throughput screening using fluorescence and luminescence, as well as automated planar array electrophysiology. The remaining two chapters focus on approaches for determining ion channel crystal structures and on computational approaches to understanding channel mechanisms at atomic resolution. Rather than provide detailed protocols, indicated by references in each chapter, the authors provide a comprehensive and easily accessible overview of the techniques involved, reviewing underlying principles and providing working guidelines as well as an understanding of the key theoretical and practical considerations associated with each topic. In each case, this practical advice is illustrated by real life examples, taken either from the author's own experience or from key examples in the literature, providing valuable practical hints not found elsewhere. The result is a compendium of practical ion channel information that will prove a valuable resource to academic and industrial workers alike.


Targeting Ion Channels for Drug Discovery: Emerging Challenges for High Throughput Screening Technologies

Targeting Ion Channels for Drug Discovery: Emerging Challenges for High Throughput Screening Technologies
Author: Ciria Hernandez
Publisher: Frontiers Media SA
Total Pages: 153
Release: 2024-06-07
Genre: Science
ISBN: 2832550169

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Ligand and voltage-gated ion channels are highly regulated protein molecules that cross the cell membrane allowing ion flow from one side of the membrane to the other. They are ubiquitously expressed in human tissues and consist of one of the largest and best understood functional groups of proteins, with more than 400 members spanning nearly 1% of the human genome. They are involved in a variety of fundamental physiological processes, and their malfunction causes numerous diseases. In terms of the challenges faced in the effort to discover specific drugs in ancient and emerging diseases, ion channels are the third-largest class of target proteins after G-protein-coupled receptors (GPCRs) and kinases. 15% of small molecule drug targets have been reported to be voltage- or ligand-gated ion channels, resulting in approximately 150 new drug candidates in preclinical and clinical studies. Of the ion channel targeting drugs found on the market, these were identified more than a decade ago, and many of the current studies are at various stages of scientific approval. Overcoming these challenges has led the field of ion channel drug discovery to transform over the past 15 years through major advancements in genetic target detection, validation, structure-based drug design, and drug modeling of cell-based diseases.


Ion Channels in Health and Sickness

Ion Channels in Health and Sickness
Author: Fatima Shad Kaneez
Publisher: BoD – Books on Demand
Total Pages: 204
Release: 2018-10-10
Genre: Science
ISBN: 1789842271

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Ion channels are proteins that make pores in the membranes of excitable cells present both in the brain and the body. These cells are not only responsible for converting chemical and mechanical stimuli into the electrical signals but are also liable for monitoring vital functions. All our activities, from the blinking of our eyes to the beating of our heart and all our senses from smell to sight, touch, taste and hearing are regulated by the ion channels. This book will take us on an expedition describing the role of ion channels in congenital and acquired diseases and the challenges and limitations scientist are facing in the development of drugs targeting these membrane proteins.