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2017 (English)In: Expert Opinion on Drug Discovery, ISSN 1746-0441, E-ISSN 1746-045X, Vol. 12, no 4, p. 345-362Article, review/survey (Refereed) Published
Abstract [en]
Introduction: 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.
Place, publisher, year, edition, pages
TAYLOR & FRANCIS LTD, 2017
Keywords
Epigenomics, epigenetics, drug discovery, drugs, bioinformatics, cheminformatics, chemogenomics, proteochemometrics
National Category
Pharmacology and Toxicology
Identifiers
urn:nbn:se:uu:diva-321031 (URN)10.1080/17460441.2017.1295954 (DOI)000396838300004 ()28276705 (PubMedID)
Funder
Swedish Research Council, C0610701
2017-04-282017-04-282018-01-13Bibliographically approved