title: Exploring the epigenetic drug discovery landscape.
abstract: Epigenetic modification has been implicated in a wide range of diseases and the ability to modulate such systems is a lucrative therapeutic strategy in drug discovery. Areas covered: This article focuses on the concepts and drug discovery aspects of epigenomics. This is achieved by providing a survey of the following concepts: (i) factors influencing epigenetics, (ii) diseases arising from epigenetics, (iii) epigenetic enzymes as druggable targets along with coverage of existing FDA-approved drugs and pharmacological agents, and (iv) drug repurposing/repositioning as a means for rapid discovery of pharmacological agents targeting epigenetics. Expert opinion: Despite significant interests in targeting epigenetic modifiers as a therapeutic route, certain classes of target proteins are heavily studied while some are less characterized. Thus, such orphan target proteins are not yet druggable with limited report of active modulators. Current research points towards a great future with novel drugs directed to the many complex multifactorial diseases of humans, which are still often poorly understood and difficult to treat.
authors.affiliation: a Center of Data Mining and Biomedical Informatics, Faculty of Medical Technology , Mahidol University , Bangkok , Thailand.
authors.forename: Veda
authors.initials: V
authors.lastname: Prachayasittikul
authors.affiliation: b National Institutes of Biomedical Innovation, Health and Nutrition , Osaka , Japan.
authors.forename: Philip
authors.initials: P
authors.lastname: Prathipati
authors.affiliation: a Center of Data Mining and Biomedical Informatics, Faculty of Medical Technology , Mahidol University , Bangkok , Thailand.
authors.forename: Reny
authors.initials: R
authors.lastname: Pratiwi
authors.affiliation: a Center of Data Mining and Biomedical Informatics, Faculty of Medical Technology , Mahidol University , Bangkok , Thailand.
authors.forename: Chuleeporn
authors.initials: C
authors.lastname: Phanus-Umporn
authors.affiliation: a Center of Data Mining and Biomedical Informatics, Faculty of Medical Technology , Mahidol University , Bangkok , Thailand.
authors.forename: Aijaz Ahmad
authors.initials: AA
authors.lastname: Malik
authors.affiliation: a Center of Data Mining and Biomedical Informatics, Faculty of Medical Technology , Mahidol University , Bangkok , Thailand.
authors.forename: Nalini
authors.initials: N
authors.lastname: Schaduangrat
authors.affiliation: c Department of Clinical Microscopy, Faculty of Medical Technology , Mahidol University , Bangkok , Thailand.
authors.forename: Kanokwan
authors.initials: K
authors.lastname: Seenprachawong
authors.affiliation: d Center for Research and Innovation, Faculty of Medical Technology , Mahidol University , Bangkok , Thailand.
authors.forename: Prapimpun
authors.initials: P
authors.lastname: Wongchitrat
authors.affiliation: c Department of Clinical Microscopy, Faculty of Medical Technology , Mahidol University , Bangkok , Thailand.
authors.forename: Aungkura
authors.initials: A
authors.lastname: Supokawej
authors.affiliation: e Department of Clinical Microbiology and Applied Technology, Faculty of Medical Technology , Mahidol University , Bangkok , Thailand.
authors.forename: Virapong
authors.initials: V
authors.lastname: Prachayasittikul
authors.affiliation: f Department of Pharmaceutical Biosciences , Uppsala University , Uppsala , Sweden.
authors.forename: Jarl E S
authors.initials: JE
authors.lastname: Wikberg
authors.affiliation: a Center of Data Mining and Biomedical Informatics, Faculty of Medical Technology , Mahidol University , Bangkok , Thailand.
authors.forename: Chanin
authors.initials: C
authors.lastname: Nantasenamat
mesh_terms: D000818:Animals; D015195:Drug Design; D055808:Drug Discovery / Q000379:methods*; D058492:Drug Repositioning; D044127:Epigenesis, Genetic; D057890:Epigenomics / Q000379:methods; D006801:Humans; D058990:Molecular Targeted Therapy
keywords: Epigenomics; bioinformatics; cheminformatics; chemogenomics; drug discovery; drugs; epigenetics; proteochemometrics