Fragment-Based Drug Discovery
Fragment-based drug discovery is a rapidly evolving area of research, which has recently seen new applications in areas such as epigenetics, GPCRs and the identification of novel allosteric binding pockets. The first fragment-derived drug was recently approved for the treatment of melanoma. It is hoped that this approval is just the beginning of the many drugs yet to be discovered using this fascinating technique.
This book is written from a Chemist's perspective and comprehensively assesses the impact of fragment-based drug discovery on a wide variety of areas of medicinal chemistry. It will prove to be an invaluable resource for medicinal chemists working in academia and industry, as well as anyone interested in novel drug discovery techniques.
Fragment-Based Drug Discovery, The Royal Society of Chemistry, 2015.
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Table of contents
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Personal Essay: Fragments in the BlogosphereByDaniel A. ErlansonDaniel A. ErlansonSearch for other works by this author on:
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Personal Essay: Adventures and Experiences in Fragment-Based Drug DiscoveryByMartin J. DrysdaleMartin J. DrysdaleBeatson Institute Drug Discovery Programme, Beatson Institute for Cancer ResearchGarscube Estate, Switchback Road, BearsdenGlasgow, G61 1BDUK[email protected]Search for other works by this author on:
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Different Flavours of Fragmentsp1-18ByClaudio DagostinClaudio DagostinSearch for other works by this author on:
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CHAPTER 2: Getting the Most Value from Your Screens: Advances in Hardware, Software, and Methodologies to Enhance Surface Plasmon Resonance Based Fragment Screening and Hit-to-Lead Supportp19-48ByAnthony M. Giannetti;Anthony M. GiannettiDepartment of Biochemical and Cellular Pharmacology, Genentech, Inc.1 DNA WaySouth San FranciscoCA 94080USA[email protected]Search for other works by this author on:Houston N. Gilbert;Houston N. GilbertDepartment of Biostatistics, Genentech, Inc.1 DNA WaySouth San FranciscoCA 94080USASearch for other works by this author on:Donald P. Huddler;Donald P. HuddlerMolecular Discovery Research, GlaxoSmithKline1250 South Collegeville Road, CollegevillePA 19426PhiladelphiaUSASearch for other works by this author on:Mac Reiter;Mac ReiterSensiQ Technologies Inc.800 Research Parkway, Suite 100Oklahoma CityOK 73104USASearch for other works by this author on:Chris Strande;Chris StrandeSensiQ Technologies Inc.800 Research Parkway, Suite 100Oklahoma CityOK 73104USASearch for other works by this author on:Keith E. Pitts;Keith E. PittsDepartment of Biochemical and Cellular Pharmacology, Genentech, Inc.1 DNA WaySouth San FranciscoCA 94080USA[email protected]Search for other works by this author on:Brandon J. BravoBrandon J. BravoDepartment of Biochemical and Cellular Pharmacology, Genentech, Inc.1 DNA WaySouth San FranciscoCA 94080USA[email protected]Search for other works by this author on:
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CHAPTER 3: Applications of NMR in Fragment-Based Drug Designp49-72ByIsabelle KrimmIsabelle KrimmInstitut des Sciences Analytiques, UMR CNRS 5280, Université Lyon5 rue de la Doua69100 VilleurbanneFrance[email protected]Search for other works by this author on:
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CHAPTER 4: Current Status and Future Direction of Fragment-Based Drug Discovery: A Computational Chemistry Perspectivep73-100ByStephen D. PickettStephen D. PickettSearch for other works by this author on:
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CHAPTER 5: Fragment Screening of G Protein-Coupled Receptorsp101-125ByMiles Congreve;Miles CongreveHeptares Therapeutics LtdBioPark, Broadwater RoadWelwyn Garden CityHertfordshire, AL7 3AXUK[email protected]Search for other works by this author on:Robert CookeRobert CookeHeptares Therapeutics LtdBioPark, Broadwater RoadWelwyn Garden CityHertfordshire, AL7 3AXUK[email protected]Search for other works by this author on:
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CHAPTER 6: Fragment-Based Lead Discovery Applied to Protein–Protein Interactionsp126-152ByRoderick E. HubbardRoderick E. HubbardYork Structural Biology Laboratory, University of YorkHeslingtonYork, YO10 5DDUKSearch for other works by this author on:
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CHAPTER 7: Fragment-Based Discovery of Allosteric Ligandsp153-176BySteven HowardSteven HowardDepartment of Medicinal Chemistry, Astex PharmaceuticalsCambridge Science ParkCambridge, CB4 0QAUK[email protected]Search for other works by this author on:
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CHAPTER 8: Fragment-Based Discovery of Antibacterialsp177-213ByChristina Spry;Christina SpryDepartment of Chemistry, University of CambridgeCambridge, CB2 1EWUKResearch School of Biology, The Australian National UniversityCanberra, ACT 2601Australia[email protected]Search for other works by this author on:Anthony G. CoyneAnthony G. CoyneDepartment of Chemistry, University of CambridgeCambridge, CB2 1EWUKSearch for other works by this author on:
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CHAPTER 9: Exploring Fragment Screening and Optimization Strategies Using Acetylcholine-Binding Proteinp214-237ByEwald Edink;Ewald EdinkVU University Amsterdam, Division of Medicinal ChemistryDe Boelelaan 10831081 HV, AmsterdamNetherlands[email protected]Search for other works by this author on:Gerdien E. de Kloe;Gerdien E. de KloeVU University Amsterdam, Division of Medicinal ChemistryDe Boelelaan 10831081 HV, AmsterdamNetherlands[email protected]Search for other works by this author on:Iwan J. P. de EschIwan J. P. de EschVU University Amsterdam, Division of Medicinal ChemistryDe Boelelaan 10831081 HV, AmsterdamNetherlands[email protected]Search for other works by this author on:
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CHAPTER 10: Fragment-Based Approaches to Epigenetic Targetsp238-258ByChun-wa Chung;Chun-wa ChungComputational and Structural Chemistry, Molecular Discovery Research, GlaxoSmithKline Medicines Research CentreGunnels Wood RoadStevenageHertfordshire, SG1 2NYUK[email protected][email protected]Search for other works by this author on:Paul BamboroughPaul BamboroughComputational and Structural Chemistry, Molecular Discovery Research, GlaxoSmithKline Medicines Research CentreGunnels Wood RoadStevenageHertfordshire, SG1 2NYUK[email protected][email protected]Search for other works by this author on:
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