Cell-based assays to support the profiling of small molecules with histone methyltransferase and demethylase modulatory activity

Histone methylation is a prevalent and dynamic chromatin modification, executed by the action of histone methyltransferases (HMTs) and demethylases (HDMs). Aberrant activity of many of these enzymes is associated with human disease, hence, there is a growing interest in identifying corresponding sma...

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Publicado no:Drug Discov Today Technol
Main Authors: Martinez, Natalia J., Simeonov, Anton
Formato: Artigo
Idioma:Inglês
Publicado em: 2015
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Article
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC4698313/
https://ncbi.nlm.nih.gov/pubmed/26723887
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.ddtec.2015.10.004
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spelling pubmed-46983132016-11-03 Cell-based assays to support the profiling of small molecules with histone methyltransferase and demethylase modulatory activity Martinez, Natalia J. Simeonov, Anton Drug Discov Today Technol Article Histone methylation is a prevalent and dynamic chromatin modification, executed by the action of histone methyltransferases (HMTs) and demethylases (HDMs). Aberrant activity of many of these enzymes is associated with human disease, hence, there is a growing interest in identifying corresponding small molecule inhibitors with therapeutic potential. To date, most of the technologies supporting the identification of these inhibitors constitute in vitro biochemical assays which, although robust and sensitive, do not study HMTs and HDMs in their native cellular state nor provide information of inhibitor’s cell permeability and toxicity. The evident need for complementary cellular approaches has recently propelled the development of cell-based assays that enable screening of HMT and HDM enzymes in a more relevant environment. Here, we highlight current cellular methodologies for HMT and HDM drug discovery support. We anticipate that implementation of these cell-based assays will positively impact the discovery of pharmacologically potent HMT and HDM inhibitors. 2015-11-03 2015-11 /pmc/articles/PMC4698313/ /pubmed/26723887 http://dx.doi.org/10.1016/j.ddtec.2015.10.004 Text en
institution US NLM
collection PubMed Central
language Inglês
format Artigo
topic Article
spellingShingle Article
Martinez, Natalia J.
Simeonov, Anton
Cell-based assays to support the profiling of small molecules with histone methyltransferase and demethylase modulatory activity
description Histone methylation is a prevalent and dynamic chromatin modification, executed by the action of histone methyltransferases (HMTs) and demethylases (HDMs). Aberrant activity of many of these enzymes is associated with human disease, hence, there is a growing interest in identifying corresponding small molecule inhibitors with therapeutic potential. To date, most of the technologies supporting the identification of these inhibitors constitute in vitro biochemical assays which, although robust and sensitive, do not study HMTs and HDMs in their native cellular state nor provide information of inhibitor’s cell permeability and toxicity. The evident need for complementary cellular approaches has recently propelled the development of cell-based assays that enable screening of HMT and HDM enzymes in a more relevant environment. Here, we highlight current cellular methodologies for HMT and HDM drug discovery support. We anticipate that implementation of these cell-based assays will positively impact the discovery of pharmacologically potent HMT and HDM inhibitors.
author Martinez, Natalia J.
Simeonov, Anton
author_facet Martinez, Natalia J.
Simeonov, Anton
author_sort Martinez, Natalia J.
title Cell-based assays to support the profiling of small molecules with histone methyltransferase and demethylase modulatory activity
title_short Cell-based assays to support the profiling of small molecules with histone methyltransferase and demethylase modulatory activity
title_full Cell-based assays to support the profiling of small molecules with histone methyltransferase and demethylase modulatory activity
title_fullStr Cell-based assays to support the profiling of small molecules with histone methyltransferase and demethylase modulatory activity
title_full_unstemmed Cell-based assays to support the profiling of small molecules with histone methyltransferase and demethylase modulatory activity
title_sort cell-based assays to support the profiling of small molecules with histone methyltransferase and demethylase modulatory activity
container_title Drug Discov Today Technol
publishDate 2015
url https://ncbi.nlm.nih.gov/pmc/articles/PMC4698313/
https://ncbi.nlm.nih.gov/pubmed/26723887
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.ddtec.2015.10.004
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