Ion Channel Drug Discovery
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 Channel Drug Discovery, The Royal Society of Chemistry, 2014.
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Table of contents
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CHAPTER 1: Ion Channel Drug Discovery: a Historical Perspectivep1-15ByBrian CoxBrian CoxGlobal Discovery Chemistry, Novartis Institutes for Biomedical ResearchWimblehurst RoadHorsham, West SussexRH12 5ABUK[email protected]Search for other works by this author on:
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CHAPTER 2: High-Throughput Screeningp16-41ByStephen D. HessStephen D. HessSearch for other works by this author on:
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CHAPTER 3: Automated Electrophysiology in Ion Channel Drug Discoveryp42-55ByJohn DunlopJohn DunlopNeuroscience Innovative Medicine Unit, AstraZeneca141 Portland StCambridge, MA02139USA[email protected]Search for other works by this author on:
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CHAPTER 4: Structural Understanding of Ion Channels in Atomic Detailp56-82ByPhillip J. StansfeldPhillip J. StansfeldSearch for other works by this author on:
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CHAPTER 5: Voltage-gated Sodium Channels: Structure, Function, and Molecular Pharmacologyp83-104ByWilliam A. CatterallWilliam A. CatterallDepartment of Pharmacology, University of WashingtonCampus Mailstop 357280Seattle, WA98195-7280[email protected]Search for other works by this author on:
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CHAPTER 6: AMPA Receptor Positive Allosteric Modulators – a Case Historyp105-134BySimon E WardSimon E WardProfessor of Medicinal Chemistry, Translational Drug Discovery Group, School of Life Sciences, University of SussexBrightonUnited KingdomBN1 9RB[email protected]Search for other works by this author on:
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CHAPTER 7: The Discovery of Novel Inhaled ENaC Blockers for the Treatment of Cystic Fibrosis Lung Diseasep135-155ByCatherine Howsham;Catherine HowshamGlobal Discovery Chemistry, Novartis Institutes for Biomedical ResearchHorsham, West SussexRH12 5ABUKSearch for other works by this author on:Henry DanahayHenry DanahayRespiratory Disease Area, Novartis Institutes for Biomedical ResearchHorsham, West SussexRH12 5ABUK[email protected]Search for other works by this author on:
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CHAPTER 8: The Therapeutic Potential of Small-molecule Modulators of the Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) Cl− Channelp156-185ByJia Liu;Jia LiuSchool of Physiology and Pharmacology, University of BristolMedical Sciences Building, University WalkBristolBS8 1TDUKSearch for other works by this author on:Gerta Cami-Kobeci;Gerta Cami-KobeciDepartment of Pharmacy and Pharmacology, University of BathClaverton DownBathBA2 7AYUK[email protected]Search for other works by this author on:Yiting Wang;Yiting WangSchool of Physiology and Pharmacology, University of BristolMedical Sciences Building, University WalkBristolBS8 1TDUKSearch for other works by this author on:Pissared Khuituan;Pissared KhuituanSchool of Physiology and Pharmacology, University of BristolMedical Sciences Building, University WalkBristolBS8 1TDUKCenter of Calcium and Bone Research, Department of Physiology, Faculty of Science, Mahidol UniversityBangkok10400ThailandSearch for other works by this author on:Zhiwei Cai;Zhiwei CaiSchool of Physiology and Pharmacology, University of BristolMedical Sciences Building, University WalkBristolBS8 1TDUKSearch for other works by this author on:Hongyu Li;Hongyu LiSchool of Physiology and Pharmacology, University of BristolMedical Sciences Building, University WalkBristolBS8 1TDUKDepartment of Applied Sciences, London South Bank UniversityLondonSE1 0AAUKSearch for other works by this author on:Stephen M. Husbands;Stephen M. HusbandsDepartment of Pharmacy and Pharmacology, University of BathClaverton DownBathBA2 7AYUK[email protected]Search for other works by this author on:David N. SheppardDavid N. SheppardSchool of Physiology and Pharmacology, University of BristolMedical Sciences Building, University WalkBristolBS8 1TDUKSearch for other works by this author on:
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CHAPTER 9: TRPV1 Antagonism: From Research to Clinicp186-237ByMark S. Nash;Mark S. NashNovartis Institutes for Biomedical ResearchForum 1, Novartis CampusCH-4056BaselSwitzerland[email protected]Search for other works by this author on:J. Martin Verkuyl;J. Martin VerkuylNovartis Institutes for Biomedical ResearchWimblehurst RoadHorsham, West SussexRH12 5ABUK[email protected][email protected]Search for other works by this author on:Gurdip BhalayGurdip BhalayNovartis Institutes for Biomedical ResearchWimblehurst RoadHorsham, West SussexRH12 5ABUK[email protected][email protected]Search for other works by this author on:
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CHAPTER 10: Open Access to the KCNQ Channel: Retigabine and Second Generation M-current Openersp238-257ByJohannes Krupp;Johannes KruppAstraZeneca R&DSödertäljeSwedenSearch for other works by this author on:Anthony M. Rush;Anthony M. RushAstraZeneca R&DSödertäljeSwedenSearch for other works by this author on:Britt-Marie Swahn;Britt-Marie SwahnAstraZeneca R&DSödertäljeSwedenSearch for other works by this author on:Martin MainMartin MainSearch for other works by this author on:
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CHAPTER 11: The Therapeutic Potential of hERG1 K+ Channels for Treating Cancer and Cardiac Arrhythmiasp258-296ByJohn Mitcheson;John MitchesonUniversity of Leicester, Department of Cell Physiology and Pharmacology, Medical Sciences BuildingUniversity RoadLeicesterLE1 9HNUK[email protected]Search for other works by this author on:Annarosa ArcangeliAnnarosa ArcangeliDepartment of Experimental Pathology and Oncology, University of FlorenceViale GB Morgagni, 5050134FirenzeItaly[email protected]Search for other works by this author on:
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CHAPTER 12: Does Nature do Ion Channel Drug Discovery Better than Us?p297-319ByRichard J. Lewis;Richard J. LewisInstitute for Molecular Bioscience, The University of QueenslandBrisbane4072Australia[email protected]Search for other works by this author on:Irina Vetter;Irina VetterInstitute for Molecular Bioscience, The University of QueenslandBrisbane4072Australia[email protected]Search for other works by this author on:Fernanda C. Cardoso;Fernanda C. CardosoInstitute for Molecular Bioscience, The University of QueenslandBrisbane4072Australia[email protected]Search for other works by this author on:Marco Inserra;Marco InserraInstitute for Molecular Bioscience, The University of QueenslandBrisbane4072Australia[email protected]Search for other works by this author on:Glenn KingGlenn KingInstitute for Molecular Bioscience, The University of QueenslandBrisbane4072Australia[email protected]Search for other works by this author on:
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CHAPTER 13: Antibodies as Ion Channel Modulatorsp320-340ByWilson Edwards;Wilson EdwardsBiotechnology Center of Excellence, Janssen Research & Development, L. L. C.3210 Merryfield RowSan DiegoCA 92121USASearch for other works by this author on:Alan D. WickendenAlan D. WickendenNeuroscience Discovery, Janssen Research & Development, L. L. C.3210 Merryfield RowSan DiegoCA 92121USA[email protected]Search for other works by this author on:
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CHAPTER 14: Ion Channel Drug Discovery: Future Perspectivesp341-354ByMartin GoslingMartin GoslingSearch for other works by this author on:
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