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Drug Discovery
Epigenetic Drug Discovery
Edited by
Cheryl Arrowsmith
Cheryl Arrowsmith
University of Toronto, Canada
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Volume
83
Hardback ISBN:
978-1-83767-110-6
PDF ISBN:
978-1-83767-491-6
EPUB ISBN:
978-1-83767-492-3
Special Collection:
2024 eBook Collection
Series:
Drug Discovery
No. of Pages:
696
Publication date:
30 Sep 2024
About this book
Epigenetics is one of the fastest moving fields in drug discovery, with almost every large pharmaceutical company, and a substantial number of biotechnology companies, targeting epigenetic processes to treat diseases ranging from cancer to Huntington’s disease and from inflammation to sickle cell anaemia. This book aims to provide an overview of the key topics adopted in current epigenetic drug discovery programmes with a focus on major developments and new technologies. Importantly, the book incorporates case studies and outlines the key challenges and techniques employed to overcome them. The book is an ideal resource for researchers in both industry and academia with an interest in epigenetic and genetic factors involved in drug discovery, target ID and validation. The book is also an excellent introduction for postgraduates interested in the interface between epigenetics and pharmaceuticals.
Epigenetic Drug Discovery, Royal Society of Chemistry, 2024.
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Digital access
$275.00
Print format
Epigenetic Drug Discovery
$275.00
Table of contents
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Section 1: Introduction to Epigenetic Drug Discovery
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Chapter 1: Introduction to Drug Discovery in Epigeneticsp1-16ByPeter A. Jones;Peter A. JonesDepartment of Epigenetics, Van Andel Institute, 333 Bostwick Ave. NE, Grand Rapids, MI 49503, USA [email protected]Search for other works by this author on:Minmin LiuMinmin LiuDepartment of Epigenetics, Van Andel Institute, 333 Bostwick Ave. NE, Grand Rapids, MI 49503, USASearch for other works by this author on:
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Section II: Emerging Technologies for Epigenetic Drug Discovery
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Chapter 2: Assay Development and Screening Strategies for Epigenetic Targetsp17-49ByPeter J. BrownPeter J. BrownEshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA [email protected]Search for other works by this author on:
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Chapter 3: Mass Spectrometry and Chemical Biology Approaches for Deconvoluting Epigenetic Targetsp50-83ByAntony J. Burton;Antony J. Burtona Dunad Therapeutics, The Officers’ Mess, Duxford, Cambridge, CB22 4QH, UK†Search for other works by this author on:Ghaith M. Hamza;Ghaith M. Hamzab Discovery Biology, Discovery Sciences, R&D, AstraZeneca, Waltham, MA 02451, USA †Search for other works by this author on:Anthony A. Iannetta;Anthony A. Iannettab Discovery Biology, Discovery Sciences, R&D, AstraZeneca, Waltham, MA 02451, USA †Search for other works by this author on:Eric Miele;Eric Mieleb Discovery Biology, Discovery Sciences, R&D, AstraZeneca, Waltham, MA 02451, USA †Search for other works by this author on:Andrew X. ZhangAndrew X. Zhangb Discovery Biology, Discovery Sciences, R&D, AstraZeneca, Waltham, MA 02451, USA [email protected]†Search for other works by this author on:
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Chapter 4: Recent Developments in the Structural Mechanism of Protein Methyltransferase Inhibitionp84-108ByRachel Leung;Rachel LeungaStructural Genomics Consortium, University of Toronto, 101 College Street, MaRS South Tower, Suite 700, Toronto, Ontario, M5G 1L7, CanadaSearch for other works by this author on:Matthieu SchapiraMatthieu SchapiraaStructural Genomics Consortium, University of Toronto, 101 College Street, MaRS South Tower, Suite 700, Toronto, Ontario, M5G 1L7, CanadabDepartment of Pharmacology and Toxicology, University of Toronto, 1 King’s College Circle, Toronto, Ontario, M5S 1A8, Canada[email protected]Search for other works by this author on:
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Chapter 5: Epigenomic Sequencing Technologiesp109-157ByJocelyn Chen;Jocelyn ChenaPrincess Margaret Cancer Centre, University Health Network, Toronto, Ontario, M5G 1L7, Canada†bDepartment of Medical Biophysics, University of Toronto, Toronto, Ontario, M5G 1L7, CanadaSearch for other works by this author on:Tina Keshavarzian;Tina KeshavarzianaPrincess Margaret Cancer Centre, University Health Network, Toronto, Ontario, M5G 1L7, Canada†bDepartment of Medical Biophysics, University of Toronto, Toronto, Ontario, M5G 1L7, CanadaSearch for other works by this author on:Mathieu LupienMathieu LupienaPrincess Margaret Cancer Centre, University Health Network, Toronto, Ontario, M5G 1L7, Canada[email protected]bDepartment of Medical Biophysics, University of Toronto, Toronto, Ontario, M5G 1L7, CanadacOntario Institute for Cancer Research, Toronto, Ontario, M5G 0A3, CanadaSearch for other works by this author on:
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Chapter 6: Safety Considerations of Targeting Epigenetic Mechanismsp158-192ByC. A. Lovatt;C. A. LovattaAstraZeneca, The Discovery Centre, Cambridge Biomedical Campus, 1 Francis Crick Avenue, Cambridge, UK, CB2 0AA[email protected]Search for other works by this author on:S. Liu;S. LiubAstraZeneca, 35 Gatehouse Drive, Waltham MA, USA, 02451Search for other works by this author on:C. W. ScottC. W. ScottbAstraZeneca, 35 Gatehouse Drive, Waltham MA, USA, 02451Search for other works by this author on:
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Section III: Drug Discovery for Chromatin Readers, Writers, Erasers, Remodelers and Epitranscriptomic Targets
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Chapter 7: Toward Understanding Pharmacological Modulation of DNA Methylationp193-227ByJohn R. HortonJohn R. HortonDepartment of Epigenetics and Molecular Carcinogenesis, University of Texas MD Anderson Cancer Center, Houston, TX 77030, USA[email protected]Search for other works by this author on:
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Chapter 8: Histone Deacetylasesp228-265ByShunsheng Zheng;Shunsheng ZhengaLaboratory of Cancer Biology, Department of Oncology, University of Oxford, Old Road Campus Research Building, Old Road Campus, Roosevelt Drive, Oxford, OX3 7DQ, United KingdombIngenOx Therapeutics Limited, Magdalen Centre, Oxford Science Park, Robert Robinson Ave, Oxford, OX4 4GA, UKSearch for other works by this author on:Wojciech Barczak;Wojciech BarczakaLaboratory of Cancer Biology, Department of Oncology, University of Oxford, Old Road Campus Research Building, Old Road Campus, Roosevelt Drive, Oxford, OX3 7DQ, United KingdomSearch for other works by this author on:Geng Liu;Geng LiuaLaboratory of Cancer Biology, Department of Oncology, University of Oxford, Old Road Campus Research Building, Old Road Campus, Roosevelt Drive, Oxford, OX3 7DQ, United KingdomSearch for other works by this author on:Nicholas La ThangueNicholas La ThangueaLaboratory of Cancer Biology, Department of Oncology, University of Oxford, Old Road Campus Research Building, Old Road Campus, Roosevelt Drive, Oxford, OX3 7DQ, United Kingdom[email protected]bIngenOx Therapeutics Limited, Magdalen Centre, Oxford Science Park, Robert Robinson Ave, Oxford, OX4 4GA, UKSearch for other works by this author on:
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Chapter 9: Chemical Targeting of Histone Acetyltransferasesp266-306ByQi Liu;Qi LiuaDana-Farber Cancer Institute, Harvard Medical School, Boston, MA, USASearch for other works by this author on:Aimee L. Qi;Aimee L. QibPhillips Academy Andover, Andover, MA, USASearch for other works by this author on:Adam D. Durbin;Adam D. DurbincSt. Jude Children’s Research Hospital, Memphis, TN, USA[email protected]Search for other works by this author on:Jun QiJun QiaDana-Farber Cancer Institute, Harvard Medical School, Boston, MA, USA[email protected]Search for other works by this author on:
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Chapter 10: Histone Lysine Methyltransferasesp307-342ByDaniel H. O Donovan;Daniel H. O DonovanaOncology R&D, AstraZeneca, Cambridge, UK[email protected]Search for other works by this author on:Jessie Hsu;Jessie HsubOncology R&D, AstraZeneca, Waltham, USASearch for other works by this author on:Huayang Liu;Huayang LiubOncology R&D, AstraZeneca, Waltham, USASearch for other works by this author on:Jon A. ReadJon A. ReadcDiscovery Sciences R&D, AstraZeneca, Cambridge, UK[email protected]Search for other works by this author on:
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Chapter 11: Inhibiting Arginine Methylationp343-382ByGianluca Sbardella;Gianluca SbardellaaDipartimento di Farmacia, Epigenetic Med Chem Lab, Università degli Studi di Salerno, Fisciano, Italy[email protected]Search for other works by this author on:Mark T. BedfordMark T. BedfordbDepartment of Epigenetics and Molecular Carcinogenesis, University of Texas MD Anderson Cancer Center, Houston, Texas, USA[email protected]Search for other works by this author on:
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Chapter 12: Histone Demethylasesp383-403ByStephen C. Kales;Stephen C. KalesNational Center for Advancing Translational Sciences, National Institutes of Health, Rockville, Maryland 20850, USASearch for other works by this author on:Anton SimeonovAnton SimeonovNational Center for Advancing Translational Sciences, National Institutes of Health, Rockville, Maryland 20850, USA[email protected]Search for other works by this author on:
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Chapter 13: Targeting the Acetylation Reader Family: Bromodomain Proteinsp404-439ByMartin P. Schwalm;Martin P. SchwalmbInstitut für Pharmazeutische Chemie, Goethe-University Frankfurt, Biozentrum, Max-von-Laue-Str. 9, 60438 Frankfurt am Main, GermanycStructural Genomics Consortium, Goethe-University Frankfurt, Buchmann Institute for Life Sciences, Max-von-Laue-Str. 15, 60438 Frankfurt am Main, GermanydGerman Cancer Consortium (DKTK)/German Cancer Research Center (DKFZ), DKTK site Frankfurt-Mainz, 69120 Heidelberg, GermanySearch for other works by this author on:Atoosa Karimi Babaahmadi;Atoosa Karimi BabaahmadiaDepartment of Toxicology and Pharmacology, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, IranbInstitut für Pharmazeutische Chemie, Goethe-University Frankfurt, Biozentrum, Max-von-Laue-Str. 9, 60438 Frankfurt am Main, GermanySearch for other works by this author on:Suzanne Ackloo;Suzanne AcklooeStructural Genomics Consortium, University of Toronto, Toronto, Ontario M5G 1L7, CanadaSearch for other works by this author on:Stefan KnappStefan KnappbInstitut für Pharmazeutische Chemie, Goethe-University Frankfurt, Biozentrum, Max-von-Laue-Str. 9, 60438 Frankfurt am Main, Germany[email protected]cStructural Genomics Consortium, Goethe-University Frankfurt, Buchmann Institute for Life Sciences, Max-von-Laue-Str. 15, 60438 Frankfurt am Main, GermanydGerman Cancer Consortium (DKTK)/German Cancer Research Center (DKFZ), DKTK site Frankfurt-Mainz, 69120 Heidelberg, GermanySearch for other works by this author on:
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Chapter 14: Targeting Histone Readers: Non-bromodomain Readersp440-472ByXiaolei Huang;Xiaolei HuangJiangsu Key Laboratory of Neuropsychiatric Diseases and College of Pharmaceutical Sciences, Jiangsu Province Engineering Research Center of Precision Diagnostics and Therapeutics Development, Soochow University, Suzhou, Jiangsu 215123, Republic of ChinaSearch for other works by this author on:Yichang Chen;Yichang ChenJiangsu Key Laboratory of Neuropsychiatric Diseases and College of Pharmaceutical Sciences, Jiangsu Province Engineering Research Center of Precision Diagnostics and Therapeutics Development, Soochow University, Suzhou, Jiangsu 215123, Republic of ChinaSearch for other works by this author on:Qin Xiao;Qin XiaoJiangsu Key Laboratory of Neuropsychiatric Diseases and College of Pharmaceutical Sciences, Jiangsu Province Engineering Research Center of Precision Diagnostics and Therapeutics Development, Soochow University, Suzhou, Jiangsu 215123, Republic of ChinaSearch for other works by this author on:Xinci Shang;Xinci ShangJiangsu Key Laboratory of Neuropsychiatric Diseases and College of Pharmaceutical Sciences, Jiangsu Province Engineering Research Center of Precision Diagnostics and Therapeutics Development, Soochow University, Suzhou, Jiangsu 215123, Republic of ChinaSearch for other works by this author on:Yanli LiuYanli LiuJiangsu Key Laboratory of Neuropsychiatric Diseases and College of Pharmaceutical Sciences, Jiangsu Province Engineering Research Center of Precision Diagnostics and Therapeutics Development, Soochow University, Suzhou, Jiangsu 215123, Republic of China[email protected]Search for other works by this author on:
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Chapter 15: Chromatin Remodeling Complexes: Arising Opportunities and Challenges of Targeting Chromatin Remodelersp473-499ByGabriel J. Sandoval;Gabriel J. SandovalFoghorn Therapeutics, 500 Technology Square Suite 700, Cambridge, MA 02139, USASearch for other works by this author on:Nathan Gioacchini;Nathan GioacchiniFoghorn Therapeutics, 500 Technology Square Suite 700, Cambridge, MA 02139, USASearch for other works by this author on:Liguo Wu;Liguo WuFoghorn Therapeutics, 500 Technology Square Suite 700, Cambridge, MA 02139, USASearch for other works by this author on:Alexia F. Kalogeropulou;Alexia F. KalogeropulouFoghorn Therapeutics, 500 Technology Square Suite 700, Cambridge, MA 02139, USASearch for other works by this author on:Stephen Hesler;Stephen HeslerFoghorn Therapeutics, 500 Technology Square Suite 700, Cambridge, MA 02139, USASearch for other works by this author on:Asad M. Taherbhoy;Asad M. TaherbhoyFoghorn Therapeutics, 500 Technology Square Suite 700, Cambridge, MA 02139, USASearch for other works by this author on:Matthew R. Netherton;Matthew R. NethertonFoghorn Therapeutics, 500 Technology Square Suite 700, Cambridge, MA 02139, USASearch for other works by this author on:Steven F. Bellon;Steven F. BellonFoghorn Therapeutics, 500 Technology Square Suite 700, Cambridge, MA 02139, USA[email protected]Search for other works by this author on:Danette L. DanielsDanette L. DanielsFoghorn Therapeutics, 500 Technology Square Suite 700, Cambridge, MA 02139, USA[email protected]Search for other works by this author on:
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Chapter 16: RNA Modifying Proteins: Emerging Targets for Drug Discoveryp500-528ByP. Ann Boriack-Sjodin;P. Ann Boriack-SjodinAccent Therapeutics, 1050 Waltham Street, Lexington, MA 02421, USASearch for other works by this author on:Serena J. SilverSerena J. SilverAccent Therapeutics, 1050 Waltham Street, Lexington, MA 02421, USA[email protected]Search for other works by this author on:
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Chapter 17: Directly Targeting RNA with Drug-like Small Moleculesp529-560ByHao Wu;Hao WuOncology Chemistry, AstraZeneca, 35 Gatehouse Dr, Waltham, MA 02451, USASearch for other works by this author on:Sharan K. Bagal;Sharan K. BagalOncology Chemistry, AstraZeneca, 35 Gatehouse Dr, Waltham, MA 02451, USASearch for other works by this author on:Meizhong JinMeizhong JinOncology Chemistry, AstraZeneca, 35 Gatehouse Dr, Waltham, MA 02451, USA[email protected]Search for other works by this author on:
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Section IV: Case Studies
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Chapter 18: Discovery and Development of Tazemetostatp561-595ByPeter T. C. Ho;Peter T. C. HoaPhase One Advisors, LLC, 6 Paul Street, Newton Centre, MA 02459, USASearch for other works by this author on:Robert A. CopelandRobert A. CopelandbAccent Therapeutics, Inc., 1050 Waltham Street, Lexington, MA 02421, USA[email protected]Search for other works by this author on:
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Chapter 19: Menin Inhibitors: Discovery, Development and Clinical Translationp596-622ByDong Chen;Dong ChenDepartment of Pathology, University of Michigan, Ann Arbor, MI, USASearch for other works by this author on:Joshua Ray;Joshua RayDepartment of Pathology, University of Michigan, Ann Arbor, MI, USASearch for other works by this author on:Tomasz Cierpicki;Tomasz CierpickiDepartment of Pathology, University of Michigan, Ann Arbor, MI, USA[email protected]Search for other works by this author on:Jolanta GrembeckaJolanta GrembeckaDepartment of Pathology, University of Michigan, Ann Arbor, MI, USA[email protected]Search for other works by this author on:
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Chapter 20: Discovery of MTA-cooperative PRMT5 Inhibitorsp623-650ByJ. Maxwell;J. MaxwellTango Therapeutics, Inc., 201 Brookline Avenue, Suite 901, Boston, MA 02215, USA[email protected]Search for other works by this author on:K. Cottrell;K. CottrellTango Therapeutics, Inc., 201 Brookline Avenue, Suite 901, Boston, MA 02215, USASearch for other works by this author on:K. BriggsK. BriggsTango Therapeutics, Inc., 201 Brookline Avenue, Suite 901, Boston, MA 02215, USASearch for other works by this author on:
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