Identification of catechols as histone-lysine demethylase inhibitors

Research output: Contribution to journalJournal articleResearchpeer-review

Anders L Nielsen, Line H Kristensen, Karen B Stephansen, Jan B L Kristensen, Charlotte Helgstrand, Michael Lees, Paul Cloos, Kristian Helin, Michael Gajhede, Lars Olsen

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
Volume586
Issue number8
Pages (from-to)1190-4
Number of pages5
ISSN0014-5793
DOIs
Publication statusPublished - 2012

ID: 38187819