Voltage-Gated Ion Channels as Drug Targets PDF Download
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Author: David J. Triggle
Publisher: John Wiley & Sons
ISBN: 3527607749
Category : Science
Languages : en
Pages : 492
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Book Description
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.
Author: David J. Triggle
Publisher: John Wiley & Sons
ISBN: 3527607749
Category : Science
Languages : en
Pages : 492
Get Book Here
Book Description
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.
Author:
Publisher:
ISBN:
Category : Drug targeting
Languages : en
Pages :
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Book Description
This program specifically deals with the basic concept of a ligand-gated ion channel embedded in the cell membrane. An attached screen shows further details of the gross structure of this type of receptor and that often, two agonist molecules must be bound for receptor activation. Some of the various sorts of ligand-gated ion channel channels found in the body are listed together with their major gating ligands and their speed of response is illustrated. The skeletal neuromuscular junction is used as an example of an excitatory ligand-gated ion channel and the GABAA receptor as an example of an inhibitory channel. The processes involved in the transmission of an impulse through junctions are explored, together with the transmembrane signal transduction mechanisms and their effects on current flow across the cell membrane. The effects of competitive and depolarising neuromuscular blockers are shown at the neuromuscular junction. A summary screen highlights the main points in the program and allows users to jump directly to any appropriate part of the program.
Author: Gary Stephens
Publisher: Springer Nature
ISBN: 3031521978
Category :
Languages : en
Pages : 540
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Book Description
Author: César Mattei
Publisher: Frontiers Media SA
ISBN: 2889747964
Category : Science
Languages : en
Pages : 245
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Book Description
Author: Ciria Hernandez
Publisher: Frontiers Media SA
ISBN: 2832550169
Category : Science
Languages : en
Pages : 153
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Book Description
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.
Author: Valentin K. Gribkoff
Publisher: John Wiley & Sons
ISBN: 0470429895
Category : Science
Languages : en
Pages : 505
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Book Description
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.
Author: Brian Cox
Publisher: Royal Society of Chemistry
ISBN: 1849735085
Category : Science
Languages : en
Pages : 385
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Book Description
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.
Author: Jean-Marc Sabatier
Publisher: MDPI
ISBN: 3039437976
Category : Medical
Languages : en
Pages : 134
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Book Description
Marine Drugs is glad to announce its first Special Issue book on “ion channels” related research: Under the great stewardship of the Guest Editor, Dr. Jean-Marc Sabatier, four advanced research articles and three comprehensive review papers were collected in the Special Issue “Ion Channels as Marine Drug Targets”. Join us to explore the advanced research outcomes in this field: α-Conotoxin RgIA and a potent analog, RgIA4, in treatment of pain; botulinum toxin-chitosan nanoparticles in treatment of atrial fibrillation; 27-amino acid (aa)-long δ-conotoxin TxVIA that modulates mammalian CaV3.x; first venomics study of Conus tulipa venom; review on marine toxins targeting Kv1 channels; review on synthetic approaches to zetekitoxin AB; and review on marine natural products and drug resistance in latent tuberculosis. The second edition of this Special Issue is open for submissions, we look forward to your contribution.
Author: Jie Zheng
Publisher: CRC Press
ISBN: 1000857751
Category : Medical
Languages : en
Pages : 331
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Book Description
The Textbook of Ion Channels is a set of three volumes providing a wide-ranging reference source on ion channels for students, instructors and researchers. Ion channels are membrane proteins that control the electrical properties of neurons and cardiac cells; mediate the detection and response to sensory stimuli like light, sound, odor, and taste; and regulate the response to physical stimuli like temperature and pressure. In non-excitable tissues, ion channels are instrumental for the regulation of basic salt balance that is critical for homeostasis. Ion channels are located at the surface membrane of cells, giving them the unique ability to communicate with the environment, as well as the membrane of intracellular organelles, allowing them to regulate internal homeostasis. Ion channels are fundamentally important for human health and diseases, and are important targets for pharmaceuticals in mental illness, heart disease, anesthesia, pain and other clinical applications. The modern methods used in their study are powerful and diverse, ranging from single ion-channel measurement techniques to models of ion channel diseases in animals, and human clinical trials for ion channel drugs. Volume I, Part 1 covers fundamental topics such as the basic principles of ion permeation and selectivity, voltage-dependent, ligand-dependent, and mechano-dependent ion channel activation mechanisms, the mechanisms for ion channel desensitization and inactivation, and basic ion channel pharmacology and inhibition. Volume I, Part 2 offers a practical guide of cardinal methods for researching ion channels, including heterologous expression and voltage-clamp and patch-clamp electrophysiology; isolation of native currents using patch clamping; modeling ion channel gating, structures, and its dynamics; crystallography and cryo-electron microscopy; fluorescence and paramagnetic resonance spectroscopy methods; and genetics approaches in model organisms. All three volumes give the reader an introduction to fundamental concepts needed to understand the mechanism of ion channels; a guide to the technical aspects of ion channel research; a modern guide to the properties of major ion channel families; and includes coverage of key examples of regulatory, physiological and disease roles for ion channels.
Author: Satya Prakash Gupta
Publisher: Springer Science & Business Media
ISBN: 3642199224
Category : Science
Languages : en
Pages : 358
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Book Description
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.
