Protein Degradation with New Chemical Modalities
Targeting protein degradation using small molecules is one of the most exciting small-molecule therapeutic strategies in decades and a rapidly growing area of research. In particular, the development of proteolysis targeting chimera (PROTACs) as potential drugs capable of recruiting target proteins to the cellular quality control machinery for elimination has opened new avenues to address traditionally ‘difficult to target’ proteins. This book provides a comprehensive overview from the leading academic and industrial experts on recent developments, scope and limitations in this dynamically growing research area; an ideal reference work for researchers in drug discovery and chemical biology as well as advanced students.
Protein Degradation with New Chemical Modalities, The Royal Society of Chemistry, 2020.
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PROTAC-mediated Target Degradation: A Paradigm Changer in Drug Discovery?p1-13ByPhilipp M. Cromm;Philipp M. CrommResearch and DevelopmentPharmaceuticalsBayer AG13353BerlinGermanySearch for other works by this author on:Craig M. Crews;Craig M. CrewsDepartment of Molecular, Cellular & Developmental BiologyYale UniversityNew HavenCT06511USADepartment of ChemistryYale UniversityNew HavenCT06511USADepartment of PharmacologyYale UniversityNew HavenCT06511USASearch for other works by this author on:Hilmar WeinmannHilmar WeinmannSearch for other works by this author on:
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Chapter 2: Structural and Biophysical Principles of Degrader Ternary Complexesp14-54ByDavid Zollman;David ZollmanDivision of Biological Chemistry and Drug Discovery, School of Life Sciences, University of DundeeDow StreetDundee DD1 5EHScotlandUnited Kingdom[email protected]Search for other works by this author on:Alessio CiulliAlessio CiulliDivision of Biological Chemistry and Drug Discovery, School of Life Sciences, University of DundeeDow StreetDundee DD1 5EHScotlandUnited Kingdom[email protected]Search for other works by this author on:
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Chapter 3: Immediate and Selective Control of Protein Abundance Using the dTAG Systemp55-74ByBehnam Nabet;Behnam NabetDepartment of Cancer BiologyDana-Farber Cancer InstituteBostonMassachusettsUSADepartment of Biological Chemistry and Molecular PharmacologyHarvard Medical SchoolBostonMassachusettsUSA[email protected][email protected]Search for other works by this author on:Nathanael S. GrayNathanael S. GrayDepartment of Cancer BiologyDana-Farber Cancer InstituteBostonMassachusettsUSADepartment of Biological Chemistry and Molecular PharmacologyHarvard Medical SchoolBostonMassachusettsUSA[email protected][email protected]Search for other works by this author on:
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Chapter 4: Developing Pharmacokinetic/Pharmacodynamic Relationships With PROTACsp75-93ByJohn D. Harling;John D. HarlingMedicinal Chemistry, Medicines Design, GlaxoSmithKline, Medicines Research CentreGunnels Wood RoadStevenageHertfordshireSG1 2NYUnited Kingdom[email protected]Search for other works by this author on:Paul Scott-Stevens;Paul Scott-StevensDMPK, In Vitro–In Vivo Translation, GlaxoSmithKline, Medicines Research CentreGunnels Wood RoadStevenageHertfordshireSG1 2NYUnited KingdomSearch for other works by this author on:Lu GaohuaLu GaohuaSystems Modelling & Translational Biology, Data and Computational Sciences, GlaxoSmithKline, Medicines Research CentreGunnels Wood RoadStevenageHertfordshireSG1 2NYUnited KingdomSearch for other works by this author on:
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Chapter 5: New Activities of CELMoDs, Cereblon E3 Ligase-modulating Drugsp94-114ByPhilip P. ChamberlainPhilip P. ChamberlainSearch for other works by this author on:
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Chapter 6: Structure-based PROTAC Designp115-134ByDarryl B. McConnellDarryl B. McConnellSearch for other works by this author on:
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Chapter 7: Plate-based High-throughput Cellular Degradation Assays to Identify PROTAC Molecules and Protein Degradersp135-146ByNikki CarterNikki CarterSearch for other works by this author on:
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Chapter 8: PROTAC Targeting BTK for the Treatment of Ibrutinib-resistant B-cell Malignanciesp147-166ByYonghui Sun;Yonghui SunMOE Key Laboratory of Protein Sciences, School of Pharmaceutical Sciences, MOE Key Laboratory of Bioorganic Phosphorus Chemistry & Chemical BiologyTsinghua UniversityBeijing100084P.R. China[email protected]Search for other works by this author on:Yu RaoYu RaoMOE Key Laboratory of Protein Sciences, School of Pharmaceutical Sciences, MOE Key Laboratory of Bioorganic Phosphorus Chemistry & Chemical BiologyTsinghua UniversityBeijing100084P.R. China[email protected]Search for other works by this author on:
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Chapter 9: An Efficient Approach Toward Drugging Undruggable Targetsp167-183ByNaomi Kitamoto;Naomi KitamotoDepartment of Chromosome Science, National Institute of Genetics, Research Organization of Information and Systems (ROIS)Yata 1111MishimaShizuoka 411–8540JapanSearch for other works by this author on:Masato T. Kanemaki;Masato T. KanemakiDepartment of Chromosome Science, National Institute of Genetics, Research Organization of Information and Systems (ROIS)Yata 1111MishimaShizuoka 411–8540JapanDepartment of Genetics, The Graduate University for Advanced Studies (SOKENDAI)Yata 1111MishimaShizuoka 411–8540JapanSearch for other works by this author on:Yusuke TominariYusuke TominariSearch for other works by this author on:
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Chapter 10: E3-mediated Ubiquitin and Ubiquitin-like Protein Ligation: Mechanisms and Chemical Probesp184-211ByBrenda A. SchulmanBrenda A. SchulmanDepartment of Molecule Machines and SignalingMax Planck Institute of BiochemistryMartinsried82152GermanySearch for other works by this author on:
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Chapter 11: Plant E3 Ligases as Versatile Tools for Novel Drug Development and Plant Bioengineeringp212-233ByHanjo HellmannHanjo HellmannSearch for other works by this author on:
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Chapter 12: Deubiquitinase Inhibitors: An Emerging Therapeutic Classp234-253ByRobert S. Magin;Robert S. MaginDepartment of Cancer BiologyDana-Farber Cancer InstituteBostonMA02215USADepartment of Biological Chemistry and Molecular PharmacologyHarvard Medical SchoolBostonMA02115USA[email protected]Search for other works by this author on:Laura M. Doherty;Laura M. DohertyDepartment of Cancer BiologyDana-Farber Cancer InstituteBostonMA02215USADepartment of Biological Chemistry and Molecular PharmacologyHarvard Medical SchoolBostonMA02115USA[email protected]Department of Systems Biology and Laboratory of Systems PharmacologyHarvard Medical SchoolBostonMA02115USASearch for other works by this author on:Sara J. BuhrlageSara J. BuhrlageDepartment of Cancer BiologyDana-Farber Cancer InstituteBostonMA02215USADepartment of Biological Chemistry and Molecular PharmacologyHarvard Medical SchoolBostonMA02115USA[email protected]Search for other works by this author on:
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Chapter 13: Targeting Translation Regulation for the Development of Novel Drugsp254-276ByWissam Mansour;Wissam MansourAnima Biotech, Ltd.10 Hanechoshet St.Tel-AvivIsrael6971072Search for other works by this author on:Yoni SheinbergerYoni SheinbergerAnima Biotech, Ltd.10 Hanechoshet St.Tel-AvivIsrael6971072Search for other works by this author on:
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Chapter 14: Classes, Modes of Action and Selection of New Modalities in Drug Discoveryp277-316ByEric ValeurEric ValeurSearch for other works by this author on:
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Chapter 15: Small-molecule Targeted Degradation of RNAp317-336ByAndrei Ursu;Andrei UrsuDepartment of ChemistryThe Scripps Research Institute130 Scripps WayJupiter, FL33458USA[email protected]Search for other works by this author on:Matthew G. Costales;Matthew G. CostalesDepartment of ChemistryThe Scripps Research Institute130 Scripps WayJupiter, FL33458USA[email protected]Search for other works by this author on:Jessica L. Childs-Disney;Jessica L. Childs-DisneyDepartment of ChemistryThe Scripps Research Institute130 Scripps WayJupiter, FL33458USA[email protected]Search for other works by this author on:Matthew D. DisneyMatthew D. DisneyDepartment of ChemistryThe Scripps Research Institute130 Scripps WayJupiter, FL33458USA[email protected]Search for other works by this author on:
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