Targeting Ion Channels For Drug Discovery Emerging Challenges For High Throughput Screening Technologies

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

Ciria Hernandez,Luis Eduardo Diaz Gimenez,Jean-Marc Taymans,Tim Strassmaier ,Marc Rogers
Targeting Ion Channels for Drug Discovery Emerging Challenges for High Throughput Screening Technologies Book PDF

Author : Ciria Hernandez,Luis Eduardo Diaz Gimenez,Jean-Marc Taymans,Tim Strassmaier ,Marc Rogers
Publisher : Frontiers Media SA
Page : 153 pages
File Size : 54,8 Mb
Release : 2024-06-07
Category : Science
ISBN : 9782832550168

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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 Drug Discovery

Brian Cox,Martin Gosling
Ion Channel Drug Discovery Book PDF

Author : Brian Cox,Martin Gosling
Publisher : Royal Society of Chemistry
Page : 384 pages
File Size : 52,6 Mb
Release : 2014-09-24
Category : Medical
ISBN : 9781849731867

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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.

Voltage-Gated Ion Channels as Drug Targets

David J. Triggle,Murali Gopalakrishnan,David Rampe,Wei Zheng
Voltage Gated Ion Channels as Drug Targets Book PDF

Author : David J. Triggle,Murali Gopalakrishnan,David Rampe,Wei Zheng
Publisher : John Wiley & Sons
Page : 492 pages
File Size : 53,5 Mb
Release : 2006-08-21
Category : Science
ISBN : 9783527607747

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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.

High Throughput Screening

William P. Janzen,Paul Bernasconi
High Throughput Screening Book PDF

Author : William P. Janzen,Paul Bernasconi
Publisher : Methods in Molecular Biology
Page : 290 pages
File Size : 43,6 Mb
Release : 2009-07-09
Category : Juvenile Nonfiction
ISBN : UOM:39015075677206

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High Throughput Screening by William P. Janzen,Paul Bernasconi Pdf

Featuring new screening technologies as well as many well established methods, this book offers comprehensive treatment of the activities directly related to High Throughput Screening (HTS), such as compound library management, data handling, and robotics.

Ion Channels and Disease

Frances M. Ashcroft
Ion Channels and Disease Book PDF

Author : Frances M. Ashcroft
Publisher : Academic Press
Page : 505 pages
File Size : 55,9 Mb
Release : 1999-10-20
Category : Science
ISBN : 9780080535210

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Ion Channels and Disease by Frances M. Ashcroft Pdf

Ion channels are membrane proteins that act as gated pathways for the movement of ions across cell membranes. They play essential roles in the physiology of all cells. In recent years, an ever-increasing number of human and animal diseases have been found to result from defects in ion channel function. Most of these diseases arise from mutations in the genes encoding ion channel proteins, and they are now referred to as the channelopathies. Ion Channels and Disease provides an informative and up-to-date account of our present understanding of ion channels and the molecular basis of ion channel diseases. It includes a basic introduction to the relevant aspects of molecular biology and biophysics and a brief description of the principal methods used to study channelopathies. For each channel, the relationship between its molecular structure and its functional properties is discussed and ways in which genetic mutations produce the disease phenotype are considered. This book is intended for research workers and clinicians, as well as graduates and advanced undergraduates. The text is clear and lively and assumes little knowledge, yet it takes the reader to frontiers of what is currently known about this most exciting and medically important area of physiology. Introduces the relevant aspects of molecular biology and biophysics Describes the principal methods used to study channelopathies Considers single classes of ion channels with summaries of the physiological role, subunit composition, molecular structure and chromosomal location, plus the relationship between channel structure and function Looks at those diseases associated with defective channel structures and regulation, including mutations affecting channel function and to what extent this change in channel function can account for the clinical phenotype

High-Throughput Screening in Drug Discovery

Jörg Hüser
High Throughput Screening in Drug Discovery Book PDF

Author : Jörg Hüser
Publisher : John Wiley & Sons
Page : 362 pages
File Size : 40,9 Mb
Release : 2006-12-13
Category : Science
ISBN : 9783527609369

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High-Throughput Screening in Drug Discovery by Jörg Hüser Pdf

Backed by leading authorities, this is a professional guide to successful compound screening in pharmaceutical research and chemical biology, including the chemoinformatic tools needed for correct data evaluation. Chapter authors from leading pharmaceutical companies as well as from Harvard University discuss such factors as chemical genetics, binding, cell-based and biochemical assays, the efficient use of compound libraries and data mining using cell-based assay results. For both academics and professionals in the pharma and biotech industries working on small molecule screening.

A Practical Guide to Assay Development and High-Throughput Screening in Drug Discovery

Taosheng Chen
A Practical Guide to Assay Development and High Throughput Screening in Drug Discovery Book PDF

Author : Taosheng Chen
Publisher : CRC Press
Page : 291 pages
File Size : 44,8 Mb
Release : 2009-12-21
Category : Medical
ISBN : 9781420070514

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A Practical Guide to Assay Development and High-Throughput Screening in Drug Discovery by Taosheng Chen Pdf

The development of suitable assays, the integration of appropriate technology, and the effective management of the essential infrastructure are all critical to the success of any high-throughput screening (HTS) endeavor. However, few scientists have the multidisciplinary experience needed to control all aspects of an HTS drug discovery project. A P

Ionic Channels of Excitable Membranes

Bertil Hille
Ionic Channels of Excitable Membranes Book PDF

Author : Bertil Hille
Publisher : Sinauer Associates, Incorporated
Page : 632 pages
File Size : 44,9 Mb
Release : 1992
Category : Excitable membranes
ISBN : UOM:39015024124383

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Ionic Channels of Excitable Membranes by Bertil Hille Pdf

This new, fully revised and expanded edition of Ionic Channels of Excitable Membranes includes new chapters on fast chemical synapses, modulation through G protein coupled receptors and second messenger systems, molecules cloning, site directed mutagenesis, and cell biology. It begins with the classical biophysical work of Hodgkin and Huxley and then weaves a description of the known ionic channels together with their biological functions. The book continues by developing the physical and molecular principles needed for explaining permeation, gating, pharmacological modification, and molecular diversity, and ends with a discussion of channel evolution. Ionic Channels of Excitable Membranes is written to be accessible and interesting to biological and physical scientists of all kinds.

Drug Discovery and Evaluation

Hans G. Vogel,Wolfgang H. Vogel
Drug Discovery and Evaluation Book PDF

Author : Hans G. Vogel,Wolfgang H. Vogel
Publisher : Springer Science & Business Media
Page : 790 pages
File Size : 50,7 Mb
Release : 2013-04-17
Category : Medical
ISBN : 9783662033333

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Drug Discovery and Evaluation by Hans G. Vogel,Wolfgang H. Vogel Pdf

This reference book contains a comprehensive selection of the most frequently used assays for reliably detecting pharmacological effects of potential drugs, including tests for cardiovascular, analgesic, psychotropic, metabolic, endocrine, respiratory, renal, and immunomodulatory activities. Each of the over 700 assays comprises a detailed protocol with the purpose and rationale of the method, a description of the experimental procedure, a critical assessment of the results and their pharmacological and clinical relevance, and pertinent references. Identification of specific tests is facilitated by the enclosed CD-ROM which allows for a quick and full text research. An appendix with guidelines and legal regulations for animal experiments in various countries will help to plan these experiments properly in accordance with the welfare of laboratory animals.

Handbook of Drug Screening

Ramakrishna Seethala,Prabhavathi Fernandes
Handbook of Drug Screening Book PDF

Author : Ramakrishna Seethala,Prabhavathi Fernandes
Publisher : CRC Press
Page : 619 pages
File Size : 53,6 Mb
Release : 2001-07-24
Category : Medical
ISBN : 9780824741440

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Handbook of Drug Screening by Ramakrishna Seethala,Prabhavathi Fernandes Pdf

A presentation of screening techniques, modern technologies, and high-capacity instrumentation for increased productivity in the development and discovery of new drugs, chemical compounds, and targeted delivery of pharmaceuticals. It contains practical applications and examples of strategies in cell-based and cell-free screens as well as homogeneous, fluorescence, chemiluminescence, and radioactive-based technologies.

Comprehensive Medicinal Chemistry III

Anonim
Comprehensive Medicinal Chemistry III Book PDF

Author : Anonim
Publisher : Elsevier
Page : 4609 pages
File Size : 43,5 Mb
Release : 2017-06-03
Category : Technology & Engineering
ISBN : 9780128032015

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Comprehensive Medicinal Chemistry III by Anonim Pdf

Comprehensive Medicinal Chemistry III, Eight Volume Set provides a contemporary and forward-looking critical analysis and summary of recent developments, emerging trends, and recently identified new areas where medicinal chemistry is having an impact. The discipline of medicinal chemistry continues to evolve as it adapts to new opportunities and strives to solve new challenges. These include drug targeting, biomolecular therapeutics, development of chemical biology tools, data collection and analysis, in silico models as predictors for biological properties, identification and validation of new targets, approaches to quantify target engagement, new methods for synthesis of drug candidates such as green chemistry, development of novel scaffolds for drug discovery, and the role of regulatory agencies in drug discovery. Reviews the strategies, technologies, principles, and applications of modern medicinal chemistry Provides a global and current perspective of today's drug discovery process and discusses the major therapeutic classes and targets Includes a unique collection of case studies and personal assays reviewing the discovery and development of key drugs

Calcium Signaling

Md. Shahidul Islam
Calcium Signaling Book PDF

Author : Md. Shahidul Islam
Publisher : Springer Nature
Page : 1110 pages
File Size : 54,5 Mb
Release : 2019-10-23
Category : Medical
ISBN : 9783030124571

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Calcium Signaling by Md. Shahidul Islam Pdf

This volume contains a unique selection of chapters covering a wealth of contemporary topics in this ubiquitous and diverse system of cell signaling. It offers much more than the accessibility and authority of a primary text book, exploring topics ranging from the fundamental aspects of calcium signaling to its varied clinical implications. It presents comprehensive discussion of cutting-edge research alongside detailed analysis of critical issues, at the same time as setting out testable hypotheses that point the way to future scientific endeavors. The contributions feature material on theoretical and methodological topics as well as related subjects including mathematical modeling and simulations. They examine calcium signaling in a host of contexts, from mammalian cells to bacteria, fruit fly and zebrafish. With much of interest to newcomers to the field as well as seasoned experts, this new publication is both wide-ranging and authoritative. The chapter “Calcium Signaling: From Basic to Bedside” is available open access under a Creative Commons Attribution 4.0 International License via link.springer.com.

Computer Applications in Pharmaceutical Research and Development

Sean Ekins
Computer Applications in Pharmaceutical Research and Development Book PDF

Author : Sean Ekins
Publisher : John Wiley & Sons
Page : 840 pages
File Size : 43,8 Mb
Release : 2006-07-11
Category : Medical
ISBN : 9780470037225

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Computer Applications in Pharmaceutical Research and Development by Sean Ekins Pdf

A unique, holistic approach covering all functions and phases of pharmaceutical research and development While there are a number of texts dedicated to individual aspects of pharmaceutical research and development, this unique contributed work takes a holistic and integrative approach to the use of computers in all phases of drug discovery, development, and marketing. It explains how applications are used at various stages, including bioinformatics, data mining, predicting human response to drugs, and high-throughput screening. By providing a comprehensive view, the book offers readers a unique framework and systems perspective from which they can devise strategies to thoroughly exploit the use of computers in their organizations during all phases of the discovery and development process. Chapters are organized into the following sections: * Computers in pharmaceutical research and development: a general overview * Understanding diseases: mining complex systems for knowledge * Scientific information handling and enhancing productivity * Computers in drug discovery * Computers in preclinical development * Computers in development decision making, economics, and market analysis * Computers in clinical development * Future applications and future development Each chapter is written by one or more leading experts in the field and carefully edited to ensure a consistent structure and approach throughout the book. Figures are used extensively to illustrate complex concepts and multifaceted processes. References are provided in each chapter to enable readers to continue investigating a particular topic in depth. Finally, tables of software resources are provided in many of the chapters. This is essential reading for IT professionals and scientists in the pharmaceutical industry as well as researchers involved in informatics and ADMET, drug discovery, and technology development. The book's cross-functional, all-phases approach provides a unique opportunity for a holistic analysis and assessment of computer applications in pharmaceutics.

Handbook of Ion Channels

Jie Zheng,Matthew C. Trudeau
Handbook of Ion Channels Book PDF

Author : Jie Zheng,Matthew C. Trudeau
Publisher : CRC Press
Page : 682 pages
File Size : 54,7 Mb
Release : 2015-02-25
Category : Medical
ISBN : 9781466551428

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Handbook of Ion Channels by Jie Zheng,Matthew C. Trudeau Pdf

The New Benchmark for Understanding the Latest Developments of Ion ChannelsIon channels control the electrical properties of neurons and cardiac cells, mediate the detection and response to sensory stimuli, and regulate the response to physical stimuli. They can often interact with the cellular environment due to their location at the surface of ce

Ion channel screening: advances in technologies and analysis

Ralf F. Kettenhofen,Dermott W. O’Callaghan,Juha Kammonen,Marzia Martina,Geoff A. Mealing
Ion channel screening advances in technologies and analysis Book PDF

Author : Ralf F. Kettenhofen,Dermott W. O’Callaghan,Juha Kammonen,Marzia Martina,Geoff A. Mealing
Publisher : Frontiers E-books
Page : 103 pages
File Size : 55,9 Mb
Release : 2024-06-23
Category : Electronic
ISBN : 9782889190355

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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.