Drug Discovery in Cancer Epigenetics PDF
Preview Drug Discovery in Cancer Epigenetics
Drug Discovery in Cancer Epigenetics Translational Epigenetics Series Trygve O. Tollefsbol, Series Editor TransgenerationalEpigenetics Edited by Trygve O.Tollefsbol, 2014 Personalized Epigenetics Edited by Trygve O.Tollefsbol, 2015 Epigenetic Technological Applications Edited by Y.George Zheng, 2015 Epigenetic Cancer Therapy Edited bySteven G.Gray, 2015 DNA Methylation andComplex Human Disease By Michel Neidhart,2015 Epigenomics inHealth and Disease Editedby Mario F. Fraga and Agustin F. Ferna´ndez, 2016 DNA Biomarkers and Diagnostics Edited by Jose´ Luis Garc´ıa-Gime´nez, 2016 Drug Discovery in Cancer Epigenetics Edited by Gerda Egger and Paola Arimondo, 2016 Drug Discovery in Cancer Epigenetics Edited by Gerda Egger and Paola Arimondo AMSTERDAM(cid:129)BOSTON(cid:129)HEIDELBERG(cid:129)LONDON NEWYORK(cid:129)OXFORD(cid:129)PARIS(cid:129)SANDIEGO SANFRANCISCO(cid:129)SINGAPORE(cid:129)SYDNEY(cid:129)TOKYO AcademicPressisanimprintofElsevier AcademicPressisanimprintofElsevier TheBoulevard,LangfordLane,Kidlington,OxfordOX51GB 225WymanStreet,WalthamMA02451 Copyrightr2016ElsevierInc.Allrightsreserved Nopartofthispublicationmaybereproducedortransmittedinanyformorbyanymeans,electronicormechanical, includingphotocopying,recording,oranyinformationstorageandretrievalsystem,withoutpermissioninwritingfrom thepublisher.Detailsonhowtoseekpermission,furtherinformationaboutthePublisher’spermissionspoliciesandour arrangementswithorganizationssuchastheCopyrightClearanceCenterandtheCopyrightLicensingAgency,canbe foundatourwebsite:www.elsevier.com/permissions. ThisbookandtheindividualcontributionscontainedinitareprotectedundercopyrightbythePublisher(otherthanasmay benotedherein). Notices Knowledgeandbestpracticeinthisfieldareconstantlychanging.Asnewresearchandexperiencebroadenour understanding,changesinresearchmethods,professionalpractices,ormedicaltreatmentmaybecomenecessary. Practitionersandresearchersmayalwaysrelyontheirownexperienceandknowledgeinevaluatingandusingany information,methods,compounds,orexperimentsdescribedherein.Inusingsuchinformationormethodstheyshouldbe mindfuloftheirownsafetyandthesafetyofothers,includingpartiesforwhomtheyhaveaprofessionalresponsibility. Tothefullestextentofthelaw,neitherthePublishernortheauthors,contributors,oreditors,assumeanyliabilityforany injuryand/ordamagetopersonsorpropertyasamatterofproductsliability,negligenceorotherwise,orfromanyuseor operationofanymethods,products,instructions,orideascontainedinthematerialherein. LibraryofCongressCataloging-in-PublicationData AcatalogrecordforthisbookisavailablefromtheLibraryofCongress BritishLibraryCataloguing-in-PublicationData AcataloguerecordforthisbookisavailablefromtheBritishLibrary ISBN:978-0-12-802208-5 ForinformationonallAcademicPresspublications visitourwebsiteathttp://store.elsevier.com PrintedandboundintheUnitedStatesofAmerica Publisher:MicaHaley AcquisitionEditor:CatherineVanDerLaan EditorialProjectManager:LisaEppich ProductionProjectManager:MelissaRead Designer:MarkRogers List of Contributors Paola Arimondo Unite´ deService etde Recherche, CRDPF,Toulouse, France Dina Arvanitis INSERM, UMR1048, Institute ofCardiovascularand Metabolic Diseases, University-Paul Sabatier, Toulouse,France Fre´deric Ausseil Unite´ deService etde Recherche, CRDPF,Toulouse, France Mina Bekheet Laboratory ofCancerBiology,Department ofOncology, University ofOxford,Oxford,UK ChristopherG. Bell Department ofTwin Research & Genetic Epidemiology,St Thomas’Hospital, King’sCollege London,London,UK; MRC Lifecourse Epidemiology Unit, University ofSouthampton, Southampton, UK; Academic Unit ofHuman Development and Health,University of Southampton, Southampton, UK; EpigenomicMedicine, Centrefor Biological Sciences, Faculty ofEnvironmentaland Natural Sciences, University ofSouthampton, Southampton, UK Magdalena Benetkiewicz GroupeCoope´rateur Multidisciplinaire en Oncologie, Paris, France Kate H.Brettingham-Moore SchoolofMedicine, University ofTasmania,Hobart, TAS, Australia Peter J. Brown StructuralGenomics Consortium, University of Toronto,Toronto, ON, Canada Corey Carter John P.Murtha Cancer Center, WalterReed NationalMilitary Medical Center/National Cancer Institute,Bethesda, MD, USA Christophe Cisarovsky Research Laboratory inOncology,University ofLausanne, Centre Hospitalier Universitaire Vaudois,Lausanne, Switzerland Pierre Cordelier INSERM, UMR1037, Cancer ResearchCenter ofToulouse,University ofToulouse-Paul Sabatier, Toulouse,France Armandde Gramont New Drug Evaluation Laboratory,Centre ofExperimental TherapeuticsandMedical Oncology, Department ofOncology,University ofLausanne, Centre HospitalierUniversitaire Vaudois, Lausanne,Switzerland xv xvi List of Contributors Frank J. Dekker Pharmaceutical Gene Modulation, Groningen ResearchInstitute ofPharmacy, University of Groningen, Groningen,The Netherlands Yannick Delpu Skirball Instituteof Biomolecular Medicine, New York University LangoneMedical Center, New York, NY,USA Helmut Dolznig InstituteofMedical Genetics, Medical University ofVienna, Vienna, Austria Marle`ne Dufresne INSERM, UMR1037, Cancer Research Center ofToulouse,University ofToulouse-Paul Sabatier,Toulouse, France GerdaEgger Clinical Institute of Pathology,Medical University ofVienna, Vienna, Austria ChantalEtievant Unite´ de Service etde Recherche, CRDPF,Toulouse,France Sandrine Faivre Medical Oncology, Department ofOncology,University ofLausanne,CentreHospitalier Universitaire Vaudois, Lausanne, Switzerland Gary R.Fanger EpicentRx, Mountain View,CA, USA Panagis Filippakopoulos Structural GenomicsConsortium, Nuffield Department of Clinical Medicine,University of Oxford,Oxford,UK; LudwigInstitutefor Cancer Research,Nuffield Department ofClinical Medicine, University ofOxford,Oxford,UK Alexandre Gagnon De´partementde Chimie, Universite´ duQue´bec a` Montre´al, Montre´al, QC, Canada MarionGayral INSERM, UMR1037, Cancer Research Center ofToulouse,University ofToulouse-Paul Sabatier,Toulouse, France MelanieR.Hassler Clinical Institute of Pathology,Medical University ofVienna, Vienna, Austria MarkusHengstschla¨ger InstituteofMedical Genetics, Medical University ofVienna, Vienna, Austria QuanahJ. Hudson CeMM Research Center for Molecular Medicine oftheAustrian Academy ofSciences, Vienna, Austria List of Contributors xvii Jean-PierreJ. Issa Fels Institutefor Cancer Research and Molecular Biology,Temple University School of Medicine, Philadelphia,PA,USA Manfred Jung Institute ofPharmaceutical Sciences, Albert-Ludwigs-Universita¨tFreiburg, Freiburg, Germany Stefan Knapp StructuralGenomics Consortium, Nuffield Department ofClinicalMedicine, University of Oxford,Oxford,UK; Institutefor Pharmaceutical Chemistry,Johann WolfgangGoethe-University, Frankfurt amMain,Germany Nina Kramer Institute ofMedical Genetics, Medical University ofVienna, Vienna,Austria Stefan Kubicek CeMM ResearchCenter for MolecularMedicine of theAustrianAcademy ofSciences, Vienna, Austria; Christian DopplerLaboratory for ChemicalEpigenetics and Antiinfectives, CeMM ResearchCenter for MolecularMedicine of theAustrianAcademy ofSciences, Vienna, Austria Nicholas B.La Thangue Laboratory ofCancerBiology,Department ofOncology, University ofOxford,Oxford,UK Dorian Larrieu INSERM, UMR1037, Cancer ResearchCenter ofToulouse,University ofToulouse-Paul Sabatier, Toulouse,France MaximeLeroy De´partement de Chimie,Universite´ du Que´bec a` Montre´al,Montre´al,QC, Canada Niek G.J.Leus Pharmaceutical Gene Modulation, Groningen Research Institute ofPharmacy,University of Groningen, Groningen,The Netherlands Marco P. Licciardello CeMM ResearchCenter for MolecularMedicine of theAustrianAcademy ofSciences, Vienna, Austria Marie Lopez Unite´ deService etde Recherche, CRDPF,Toulouse, France MichelleLybeck EpicentRx, MountainView, CA,USA Wolfgang J. Miller Laboratoriesof Genome Dynamics, Department ofCell and DevelopmentalBiology,Center of AnatomyandCellBiology,Medical University of Vienna, Vienna, Austria xviii List of Contributors HeidiOlzscha Laboratory ofCancerBiology,Department of Oncology,University of Oxford, Oxford, UK Arnold L. Oronsky InterWestPartners, Menlo Park, CA, USA Bryan T.Oronsky EpicentRx, Mountain View,CA, USA NeilC. Oronsky CFLS,San Jose, CA, USA Thomas Prebet Departement d’Hematologie etUnite d’EvaluationTherapeutique en Oncologie/Hematologie, InstitutPaoli Calmettes, Marseille, France; Hematology Department,Smilow CancerCenter at Yale University, New Haven,CT,USA EricRaymond Medical Oncology, Department ofOncology,University ofLausanne,CentreHospitalier Universitaire Vaudois, Lausanne, Switzerland Noe¨lJ.-M. Raynal De´partementde Pharmacologie, Universite´ de Montre´al and Sainte-Justine University Hospital ResearchCenter,Montre´al,QC, Canada Elisa Redl Clinical Institute of Pathology,Medical University ofVienna, Vienna, Austria Tony R.Reid MooresCancerInstitute, University ofCalifornia, San Diego, CA, USA Dina Robaa Institutfu¨rPharmazie, Martin-Luther-Universita¨tHalle-Wittenberg,Halle,Germany MartinScherzer InstituteofMedical Genetics, Medical University ofVienna, Vienna, Austria Jan J. Scicinski EpicentRx, Mountain View,CA, USA Semira Sheikh Laboratory ofCancerBiology,Department of Oncology,University of Oxford, Oxford, UK Wolfgang Sippl Institutfu¨rPharmazie, Martin-Luther-Universita¨tHalle-Wittenberg,Halle,Germany Mira Stadler InstituteofMedical Genetics, Medical University ofVienna, Vienna, Austria List of Contributors xix Phillippa C. Taberlay Chromatin DynamicGroup,Genomics and Epigenetics Division,Garvan Instituteof Medical Research, Darlinghurst, NSW,Australia; Epigenetics Program, Genomicsand Epigenetics Division,Garvan Institute ofMedical Research,Darlinghurst, NSW,Australia; St. Vincent’s Clinical School, Faculty ofMedicine,University ofNew South Wales,Darlinghurst, NSW, Australia Tirza Timmerman, Pharmaceutical Gene Modulation, Groningen Research Institute ofPharmacy,University of Groningen, Groningen,The Netherlands Je´roˆme Torrisani INSERM, UMR1037, Cancer ResearchCenter ofToulouse,University ofToulouse-Paul Sabatier, Toulouse,France Christine Unger Institute ofMedical Genetics, Medical University ofVienna, Vienna,Austria Thea van denBosch Pharmaceutical Gene Modulation, Groningen Research Institute ofPharmacy,University of Groningen, Groningen,The Netherlands NorbertVey Departement d’Hematologie etUnite d’Evaluation Therapeutique en Oncologie/Hematologie, Institut Paoli Calmettes, Marseille, France;Aix-Marseille Universite´,Marseille, France TobiasWagner Institute ofPharmaceutical Sciences, Albert-Ludwigs-Universita¨tFreiburg, Freiburg, Germany Stefanie Walter Institute ofMedical Genetics, Medical University ofVienna, Vienna,Austria Angelika Walzl Institute ofMedical Genetics, Medical University ofVienna, Vienna,Austria Daniel J. Weisenberger USC/Norris Comprehensive Cancer Center,University of Southern California, LosAngeles, CA, USA Preface The causal involvement of epigenetic pathways in tumor development and progression has been widely accepted and recent findings have nourished our knowledge of tumor biology and opened potential clinical applications dependent on epigenetic aberrations. Deregulation and mutation of epigenetic enzymes as well as global and local changes of epigenetic chromatin modifications are implicated in a variety of malignancies and provide novel therapeutic and diagnostic targets for oncology. There is great interest in developing novel epigenetic drugs targeting chromatin modifiers as well as chromatin reader proteins and some successful recent studies have confirmed the validityofthesedrugs for cancer therapy. We were fortunate to gather many experts and renowned authors to contribute to this book and are very thankful for their efforts and valuable contributions. This book intends to provide (i) an introduction into cancer epigenetics and to give a comprehensive overview on, (ii) methods and tools for epigenetic drug development, (iii) classes of epigenetic drugs, (iv) development of diag- nostic tools, and (v) clinical implications of epigenetic therapy. Emerging concepts, such as “epi- sensitization,” are also presentedalongside with indications beyond cancer. The intended audience includes both basic scientists as well as clinicians. The book is directed toward scientists of the academic and industrial sector, who are aiming to test and develop epige- netic cancer drugs. Importantly, the book will increase the awareness level of epigenetic drugs for oncologists. We envision that this might foster increased and more rapid translation of epigenetic drugs into the clinics. Gerda Egger and Paola Arimondo xxi
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