Identification of catechols as histone–lysine demethylase inhibitors

Publication: Research - peer-reviewJournal article – Annual report year: 2012

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  • Author: Nielsen, Anders L., Denmark

    Faculty of Health and Medical Sciences, University of Copenhagen, Denmark

  • Author: Kristensen, Line H., Denmark

    Faculty of Health and Medical Sciences, University of Copenhagen, Denmark

  • Author: Stephansen, Karen B.

    Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, Universitetsparken 2, DK-2100 Copenhagen, Denmark

  • Author: Kristensen, Jan B.L., Denmark

    Faculty of Health and Medical Sciences, University of Copenhagen, Denmark

  • Author: Helgstrand, Charlotte, Denmark

    Faculty of Health and Medical Sciences, University of Copenhagen, Denmark

  • Author: Lees, Michael, Denmark

    Biotech Research & Innovation Centre, Denmark

  • Author: Cloos, Paul, Denmark

    Biotech Research & Innovation Centre, Denmark

  • Author: Helin, Kristian, Denmark

    Biotech Research & Innovation Centre, Denmark

  • Author: Gajhede, Michael, Denmark

    Faculty of Health and Medical Sciences, University of Copenhagen, Denmark

  • Author: Olsen, Lars, Denmark

    Faculty of Health and Medical Sciences, University of Copenhagen, Denmark

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Identification of inhibitors of histone–lysine demethylase (HDM) enzymes is important because of their involvement in the development of cancer. An ELISA-based assay was developed for identification of inhibitors of the HDM KDM4C in a natural products library. Based on one of the hits with affinity in the low μM range (1, a catechol), a subset of structurally related compounds was selected and tested against a panel of HDMs. In this subset, two inhibitors (2 and 10) had comparable affinities towards KDM4C and KDM6A but no effect on PHF8. One inhibitor restored H3K9me3 levels in KDM4C transfected U2-OS cells.
Original languageEnglish
JournalF E B S Letters
Publication date2012
Volume586
Journal number8
Pages1190-1194
ISSN0014-5793
DOIs
StatePublished
CitationsWeb of Science® Times Cited: 4
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