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Author : Brian Cox,Martin Gosling Publisher : Royal Society of Chemistry Page : 384 pages File Size : 55,8 Mb Release : 2014-09-24 Category : Medical ISBN : 9781849731867
Ion Channel Drug Discovery by Brian Cox,Martin Gosling Pdf
A rapidly growing field, this book covers the recent advances in screening technology, ion channel structure and modelling, with up-to-date case histories.
Ion Channels as Targets in Drug Discovery by Gary Stephens,Edward Stevens Pdf
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 by David J. Triggle,Murali Gopalakrishnan,David Rampe,Wei Zheng Pdf
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 by Valentin K. Gribkoff,Leonard K. Kaczmarek Pdf
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.
Targeting Ion Channels for Drug Discovery: Emerging Challenges for High Throughput Screening Technologies by Ciria Hernandez,Luis Eduardo Diaz Gimenez,Jean-Marc Taymans,Tim Strassmaier ,Marc Rogers Pdf
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 channel screening: advances in technologies and analysis by Ralf F. Kettenhofen,Dermott W. O’Callaghan,Juha Kammonen,Marzia Martina,Geoff A. Mealing Pdf
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 by Satya Prakash Gupta Pdf
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 by Jeffrey J. Clare,Derek J. Trezise Pdf
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.
Ion Channels in Health and Sickness by Fatima Shad Kaneez Pdf
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.
Ion channels play a vital role in basic physiological functions such as generation of electrical activity in nerves and muscle, control of cardiac excitability, intracellular signaling, hormone secretion, cell proliferation and many other biological processes. Because of their prevalence and the critical role they play in virtually all tissue types and organs, ion channels are also involved in a number of pathophysiological conditions. The aim of this volume is to review recent advances in the field of ion channel related diseases. Following an overview chapter summarizing the current state of ion channel screening technologies, five topics covering areas such as cancer, cardiac arrhythmias, cystic fibrosis, and pain have been selected, and the current state of knowledge is presented by leading experts in their field. Each chapter is structured to cover the biological rationale for the target, the current status in the development of agents to treat the disease, and future prospects and challenges facing each therapeutic area. The reader will receive a critical overview covering the progress made in the rapidly developing and complex field of ion channels and diseases.
Ion Channels Down Under, Volume 79 provides up-to-date information on ion channel pharmacology, their pharmacological modulators, and role in a diverse range of poorly treated medical conditions. Contributors include prominent scientists and highly-recognized experts with major accomplishments in the field of ion channel pharmacology. Topics covered include the role of ion channels in health and disease, ion channels as therapeutic targets and the molecular pharmacology of ion channels. Provides a must read book on ion channel pharmacology Contains up-to-date information on a number of ion channels, their pharmacological modulators, and their role in a diverse range of poorly treated medical conditions Contains contributions from prominent scientists and highly-recognized experts with major accomplishments in the field
Author : Peter C. Ruben Publisher : Springer Science & Business Media Page : 328 pages File Size : 55,9 Mb Release : 2014-04-15 Category : Medical ISBN : 9783642415883
Voltage Gated Sodium Channels by Peter C. Ruben Pdf
A number of techniques to study ion channels have been developed since the electrical basis of excitability was first discovered. Ion channel biophysicists have at their disposal a rich and ever-growing array of instruments and reagents to explore the biophysical and structural basis of sodium channel behavior. Armed with these tools, researchers have made increasingly dramatic discoveries about sodium channels, culminating most recently in crystal structures of voltage-gated sodium channels from bacteria. These structures, along with those from other channels, give unprecedented insight into the structural basis of sodium channel function. This volume of the Handbook of Experimental Pharmacology will explore sodium channels from the perspectives of their biophysical behavior, their structure, the drugs and toxins with which they are known to interact, acquired and inherited diseases that affect sodium channels and the techniques with which their biophysical and structural properties are studied.
Trp Channels in Drug Discovery by Tamaas Bairao Pdf
This volume in the Methods in Pharmacology and Toxicology series covers modeling methodologies involving disorders of the cardiovascular system, the brain, skin and metabolic system, as well as colitis, cancer, thermosensation and musculoskeletal disorders."