Kinase Drug Discovery: Modern Approaches
Kinase inhibition remains an area of significant interest, and growing importance, across academia and the pharmaceutical industry. There are now many marketed drugs that target kinases and a significant number of compounds are currently in various stages of clinical development. This book is a forward-looking analysis of a number of key areas for kinase inhibition in the coming years and builds on the first volume. This includes topics such as screening approaches to target kinases along with different modes of inhibition such as allosteric and covalent. Novel approaches such as macrocyclisation are considered along with how the properties of kinase inhibitors have evolved, including the potential for brain penetration. Recent areas of great importance also covered include cutting edge molecular modelling approaches and the importance of kinase mutations. The evolving biology of kinases has also resulted in increased interest in the immuno-oncology area and also pseudokinases as a target family. As with the first volume the book finishes with a forward looking view of how research against this fascinating target class may evolve.
Kinase Drug Discovery: Modern Approaches, The Royal Society of Chemistry, 2018.
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Table of contents
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CHAPTER 1: Introduction to Kinase Drug Discovery – Modern Approachesp1-8ByFrederick W. GoldbergFrederick W. GoldbergSearch for other works by this author on:
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CHAPTER 2: New Screening Approaches for Kinasesp9-33ByD. H. Drewry;D. H. DrewryUNC Eshelman School of Pharmacy, University of North Carolina at Chapel HillChapel HillNC27599USA[email protected]Search for other works by this author on:B. W. King;B. W. KingPlatform Technology & Science, GlaxoSmithKlineCollegeville RoadCollegevillePennsylvania19426USASearch for other works by this author on:C. I. Wells;C. I. WellsUNC Eshelman School of Pharmacy, University of North Carolina at Chapel HillChapel HillNC27599USA[email protected]Search for other works by this author on:W. J. ZuercherW. J. ZuercherUNC Eshelman School of Pharmacy, University of North Carolina at Chapel HillChapel HillNC27599USA[email protected]Search for other works by this author on:
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CHAPTER 3: The Screening and Design of Allosteric Kinase Inhibitorsp34-60ByPeng Wu;Peng WuChemical Genomics Center of the Max Planck SocietyOtto-Hahn-Strasse 15DortmundDE44227GermanyChemical Biology and Therapeutics Science, Broad Institute of MIT and Harvard415 Main StreetCambridgeMA02142USA[email protected][email protected]Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of CopenhagenJagtvej 162CopenhagenDK2200DenmarkSearch for other works by this author on:Peter Dinér;Peter DinérDivision of Organic Chemistry, Department of Chemistry, KTH Royal Institute of TechnologyTeknikringen 30StockholmSE10044SwedenSearch for other works by this author on:Lennart BunchLennart BunchDepartment of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of CopenhagenJagtvej 162CopenhagenDK2200DenmarkSearch for other works by this author on:
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CHAPTER 4: Covalent Inhibition of Kinasesp61-96ByTjeerd BarfTjeerd BarfSearch for other works by this author on:
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CHAPTER 5: Small Molecule Macrocyclic Kinase Inhibitorsp97-127ByAnders Poulsen;Anders PoulsenExperimental Therapeutics Centre, A*STAR11 Biopolis Way, #03-10/11 The Helios138667Singapore[email protected]Department of Chemistry, National University of Singapore3 Science Drive 3117543SingaporeSearch for other works by this author on:Brian DymockBrian DymockQEDDI, Uniquest Pty Ltd, The University of Queensland306 Carmody RoadBrisbaneQueensland4072AustraliaSearch for other works by this author on:
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CHAPTER 6: The Design of Brain Penetrant Kinase Inhibitorsp128-180ByR. Ian StorerR. Ian StorerSearch for other works by this author on:
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CHAPTER 7: Cutting Edge Approaches to Structure-based Computational Modelling of Kinasesp181-215ByRobert AbelRobert AbelSearch for other works by this author on:
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CHAPTER 8: The Properties of Kinase Inhibitorsp216-236ByTed W. Johnson;Ted W. JohnsonPfizer La Jolla Oncology10770 Science Center DriveSan DiegoCA 92121USA[email protected][email protected]Search for other works by this author on:Robert L. HoffmanRobert L. HoffmanPfizer La Jolla Oncology10770 Science Center DriveSan DiegoCA 92121USA[email protected][email protected]Search for other works by this author on:
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CHAPTER 9: Assessment and Optimisation of Kinase Inhibitor Selectivity to Achieve Candidates with an Appropriate Safety Profilep237-252ByMikael Persson;Mikael PerssonDiscovery Safety, Drug Safety and Metabolism, IMED Biotech Unit, AstraZenecaGothenburgSweden[email protected]Search for other works by this author on:Mickael Mogemark;Mickael MogemarkDiscovery Safety, Drug Safety and Metabolism, IMED Biotech Unit, AstraZenecaGothenburgSweden[email protected]Search for other works by this author on:Lyn Rosenbrier-Ribeiro;Lyn Rosenbrier-RibeiroDiscovery Safety, Drug Safety and Metabolism, IMED Biotech Unit, AstraZenecaCambridgeUKSearch for other works by this author on:Jorrit J. HornbergJorrit J. HornbergDiscovery Safety, Drug Safety and Metabolism, IMED Biotech Unit, AstraZenecaGothenburgSweden[email protected]Search for other works by this author on:
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CHAPTER 10: Drugging the Kinomep253-280ByA. D. Axtman;A. D. AxtmanUNC Eshelman School of Pharmacy, University of North Carolina at Chapel HillChapel HillNC 27599USA[email protected]Search for other works by this author on:R. Couñago;R. CouñagoStructural Genomics Consortium, Universidade Estadual de Campinas – UNICAMPCampinasSP13083 BrazilSearch for other works by this author on:D. H. Drewry;D. H. DrewryUNC Eshelman School of Pharmacy, University of North Carolina at Chapel HillChapel HillNC 27599USA[email protected]Search for other works by this author on:M. B. Robers;M. B. RobersPromega Corporation2800 Woods Hollow RoadFitchburgWI 53711USASearch for other works by this author on:C. I. WellsC. I. WellsUNC Eshelman School of Pharmacy, University of North Carolina at Chapel HillChapel HillNC 27599USA[email protected]Search for other works by this author on:
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CHAPTER 11: The Importance of Kinase Mutations in Cancer Drug Discoveryp281-312ByRichard A. Ward;Richard A. WardMedicinal Chemistry, Oncology, IMED Biotech UnitAstraZenecaCambridgeCB4 0WGUK[email protected][email protected]Search for other works by this author on:Frederick W. GoldbergFrederick W. GoldbergMedicinal Chemistry, Oncology, IMED Biotech UnitAstraZenecaCambridgeCB4 0WGUK[email protected][email protected]Search for other works by this author on:
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CHAPTER 12: Kinase Inhibition for Immuno-oncologyp313-358ByK. J. Duffy;K. J. DuffyImmuno-oncology and Combinations DPU, GlaxoSmithKline1250 South Collegeville RoadCollegevillePA 19426USA[email protected]Search for other works by this author on:C. A. ParrishC. A. ParrishImmuno-oncology and Combinations DPU, GlaxoSmithKline1250 South Collegeville RoadCollegevillePA 19426USA[email protected]Search for other works by this author on:
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CHAPTER 13: A Structural Perspective of the Pseudokinome: Defining the Targetable Spacep359-380ByIsabelle S. Lucet;Isabelle S. LucetThe Walter and Eliza Hall Institute of Medical ResearchParkvilleVictoria3052Australia[email protected][email protected]Department of Medical Biology, University of MelbourneParkvilleVictoria3052AustraliaSearch for other works by this author on:James M. MurphyJames M. MurphyThe Walter and Eliza Hall Institute of Medical ResearchParkvilleVictoria3052Australia[email protected][email protected]Department of Medical Biology, University of MelbourneParkvilleVictoria3052AustraliaSearch for other works by this author on:
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CHAPTER 14: The Future of Kinase Therapeuticsp381-405ByBrion Murray;Brion MurrayPfizer Worldwide Research and Development, Oncology Research Unit10724 Science Center DriveSan DiegoCA 92121USASearch for other works by this author on:Matthew M. Hayward;Matthew M. HaywardPfizer Worldwide Research and Development, Discovery Sciences DepartmentEastern Point RoadGrotonCT 06340USA[email protected]Search for other works by this author on:Ravi G. KurumbailRavi G. KurumbailPfizer Worldwide Research and Development, Discovery Sciences DepartmentEastern Point RoadGrotonCT 06340USA[email protected]Search for other works by this author on:
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