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

Published: 2024-06-07

Total Pages: 153

ISBN-13: 2832550169

DOWNLOAD EBOOK

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.


Book Synopsis Targeting Ion Channels for Drug Discovery: Emerging Challenges for High Throughput Screening Technologies by : Ciria Hernandez

Download or read book Targeting Ion Channels for Drug Discovery: Emerging Challenges for High Throughput Screening Technologies written by Ciria Hernandez and published by Frontiers Media SA. This book was released on 2024-06-07 with total page 153 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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

Ion Channel Drug Discovery

Author: Brian Cox

Publisher: Royal Society of Chemistry

Published: 2014-09-24

Total Pages: 384

ISBN-13: 1849731861

DOWNLOAD EBOOK

A rapidly growing field, this book covers the recent advances in screening technology, ion channel structure and modelling, with up-to-date case histories.


Book Synopsis Ion Channel Drug Discovery by : Brian Cox

Download or read book Ion Channel Drug Discovery written by Brian Cox and published by Royal Society of Chemistry. This book was released on 2014-09-24 with total page 384 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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 in Health and Sickness

Ion Channels in Health and Sickness

Author: Fatima Shad Kaneez

Publisher: BoD – Books on Demand

Published: 2018-10-10

Total Pages: 204

ISBN-13: 1789842271

DOWNLOAD EBOOK

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.


Book Synopsis Ion Channels in Health and Sickness by : Fatima Shad Kaneez

Download or read book Ion Channels in Health and Sickness written by Fatima Shad Kaneez and published by BoD – Books on Demand. This book was released on 2018-10-10 with total page 204 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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.


Voltage-Gated Ion Channels as Drug Targets

Voltage-Gated Ion Channels as Drug Targets

Author: David J. Triggle

Publisher: John Wiley & Sons

Published: 2006-08-21

Total Pages: 492

ISBN-13: 3527607749

DOWNLOAD EBOOK

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.


Book Synopsis Voltage-Gated Ion Channels as Drug Targets by : David J. Triggle

Download or read book Voltage-Gated Ion Channels as Drug Targets written by David J. Triggle and published by John Wiley & Sons. This book was released on 2006-08-21 with total page 492 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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 in Drug Discovery

High-Throughput Screening in Drug Discovery

Author: Jörg Hüser

Publisher: John Wiley & Sons

Published: 2006-12-13

Total Pages: 362

ISBN-13: 3527609369

DOWNLOAD EBOOK

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.


Book Synopsis High-Throughput Screening in Drug Discovery by : Jörg Hüser

Download or read book High-Throughput Screening in Drug Discovery written by Jörg Hüser and published by John Wiley & Sons. This book was released on 2006-12-13 with total page 362 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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.


High Throughput Screening

High Throughput Screening

Author: William P. Janzen

Publisher: Methods in Molecular Biology

Published: 2009-07-09

Total Pages: 290

ISBN-13:

DOWNLOAD EBOOK

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.


Book Synopsis High Throughput Screening by : William P. Janzen

Download or read book High Throughput Screening written by William P. Janzen and published by Methods in Molecular Biology. This book was released on 2009-07-09 with total page 290 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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

Ion Channels and Disease

Author: Frances M. Ashcroft

Publisher: Academic Press

Published: 1999-10-20

Total Pages: 505

ISBN-13: 0080535216

DOWNLOAD EBOOK

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


Book Synopsis Ion Channels and Disease by : Frances M. Ashcroft

Download or read book Ion Channels and Disease written by Frances M. Ashcroft and published by Academic Press. This book was released on 1999-10-20 with total page 505 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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


Basic Principles of Drug Discovery and Development

Basic Principles of Drug Discovery and Development

Author: Benjamin E. Blass

Publisher: Academic Press

Published: 2021-03-30

Total Pages: 712

ISBN-13: 0128172150

DOWNLOAD EBOOK

Basic Principles of Drug Discovery and Development presents the multifaceted process of identifying a new drug in the modern era, which requires a multidisciplinary team approach with input from medicinal chemists, biologists, pharmacologists, drug metabolism experts, toxicologists, clinicians, and a host of experts from numerous additional fields. Enabling technologies such as high throughput screening, structure-based drug design, molecular modeling, pharmaceutical profiling, and translational medicine are critical to the successful development of marketable therapeutics. Given the wide range of disciplines and techniques that are required for cutting edge drug discovery and development, a scientist must master their own fields as well as have a fundamental understanding of their collaborator’s fields. This book bridges the knowledge gaps that invariably lead to communication issues in a new scientist’s early career, providing a fundamental understanding of the various techniques and disciplines required for the multifaceted endeavor of drug research and development. It provides students, new industrial scientists, and academics with a basic understanding of the drug discovery and development process. The fully updated text provides an excellent overview of the process and includes chapters on important drug targets by class, in vitro screening methods, medicinal chemistry strategies in drug design, principles of in vivo pharmacokinetics and pharmacodynamics, animal models of disease states, clinical trial basics, and selected business aspects of the drug discovery process. Provides a clear explanation of how the pharmaceutical industry works, as well as the complete drug discovery and development process, from obtaining a lead, to testing the bioactivity, to producing the drug, and protecting the intellectual property Includes a new chapter on the discovery and development of biologics (antibodies proteins, antibody/receptor complexes, antibody drug conjugates), a growing and important area of the pharmaceutical industry landscape Features a new section on formulations, including a discussion of IV formulations suitable for human clinical trials, as well as the application of nanotechnology and the use of transdermal patch technology for drug delivery Updated chapter with new case studies includes additional modern examples of drug discovery through high through-put screening, fragment-based drug design, and computational chemistry


Book Synopsis Basic Principles of Drug Discovery and Development by : Benjamin E. Blass

Download or read book Basic Principles of Drug Discovery and Development written by Benjamin E. Blass and published by Academic Press. This book was released on 2021-03-30 with total page 712 pages. Available in PDF, EPUB and Kindle. Book excerpt: Basic Principles of Drug Discovery and Development presents the multifaceted process of identifying a new drug in the modern era, which requires a multidisciplinary team approach with input from medicinal chemists, biologists, pharmacologists, drug metabolism experts, toxicologists, clinicians, and a host of experts from numerous additional fields. Enabling technologies such as high throughput screening, structure-based drug design, molecular modeling, pharmaceutical profiling, and translational medicine are critical to the successful development of marketable therapeutics. Given the wide range of disciplines and techniques that are required for cutting edge drug discovery and development, a scientist must master their own fields as well as have a fundamental understanding of their collaborator’s fields. This book bridges the knowledge gaps that invariably lead to communication issues in a new scientist’s early career, providing a fundamental understanding of the various techniques and disciplines required for the multifaceted endeavor of drug research and development. It provides students, new industrial scientists, and academics with a basic understanding of the drug discovery and development process. The fully updated text provides an excellent overview of the process and includes chapters on important drug targets by class, in vitro screening methods, medicinal chemistry strategies in drug design, principles of in vivo pharmacokinetics and pharmacodynamics, animal models of disease states, clinical trial basics, and selected business aspects of the drug discovery process. Provides a clear explanation of how the pharmaceutical industry works, as well as the complete drug discovery and development process, from obtaining a lead, to testing the bioactivity, to producing the drug, and protecting the intellectual property Includes a new chapter on the discovery and development of biologics (antibodies proteins, antibody/receptor complexes, antibody drug conjugates), a growing and important area of the pharmaceutical industry landscape Features a new section on formulations, including a discussion of IV formulations suitable for human clinical trials, as well as the application of nanotechnology and the use of transdermal patch technology for drug delivery Updated chapter with new case studies includes additional modern examples of drug discovery through high through-put screening, fragment-based drug design, and computational chemistry


Ionic Channels of Excitable Membranes

Ionic Channels of Excitable Membranes

Author: Bertil Hille

Publisher: Sinauer Associates, Incorporated

Published: 1992

Total Pages: 632

ISBN-13:

DOWNLOAD EBOOK

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.


Book Synopsis Ionic Channels of Excitable Membranes by : Bertil Hille

Download or read book Ionic Channels of Excitable Membranes written by Bertil Hille and published by Sinauer Associates, Incorporated. This book was released on 1992 with total page 632 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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.


Handbook of Drug Screening

Handbook of Drug Screening

Author: Ramakrishna Seethala

Publisher: CRC Press

Published: 2001-07-24

Total Pages: 619

ISBN-13: 0824741447

DOWNLOAD EBOOK

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.


Book Synopsis Handbook of Drug Screening by : Ramakrishna Seethala

Download or read book Handbook of Drug Screening written by Ramakrishna Seethala and published by CRC Press. This book was released on 2001-07-24 with total page 619 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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.