Cellular analysis of the action of epigenetics drugs and probes

Hau, Mirjam, Zenk, Fides, Ganesan, A. ORCID: https://orcid.org/0000-0003-4862-7999, Iovino, Nicola and Jung, Manfred (2017) Cellular analysis of the action of epigenetics drugs and probes. Epigenetics, 12 (5). pp. 308-322. ISSN 1559-2294

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Small molecule drugs and probes are important tools in drug discovery, pharmacology, and cell biology. This is of course also true for epigenetic inhibitors. Important examples for the use of established epigenetic inhibitors are the study of the mechanistic role of a certain target in a cellular setting or the modulation of a certain phenotype in an approach that aims towards therapeutic application. Alternatively, cellular testing may aim at the validation of a new epigenetic inhibitor in drug discovery approaches. Cellular and eventually animal models provide powerful tools for these different approaches but certain caveats have to be recognized and taken into account. This involves both the selectivity of the pharmacological tool as well as the specificity and the robustness of the cellular system. In this article, we present an overview of different methods that are used to profile and screen for epigenetic agents and comment on their limitations. We describe not only diverse successful case studies of screening approaches using different assay formats, but also some problematic cases, critically discussing selected applications of these systems.

Item Type: Article
Uncontrolled Keywords: epigenetics,cellular models,screening,chemical probes,epigenetic drugs,chip-seq,chem-seq
Faculty \ School: Faculty of Science > School of Pharmacy
UEA Research Groups: Faculty of Science > Research Groups > Medicinal Chemistry (former - to 2017)
Faculty of Science > Research Groups > Chemical Biology and Medicinal Chemistry (former - to 2021)
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Depositing User: Pure Connector
Date Deposited: 03 Feb 2017 03:29
Last Modified: 22 Oct 2022 02:12
URI: https://ueaeprints.uea.ac.uk/id/eprint/62286
DOI: 10.1080/15592294.2016.1274472


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