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Titel: Identification of catechols as histone–lysine demethylase inhibitors
Type: Journal articleJournal article
Person(er):
Forfatter:  Nielsen, Anders L.
Faculty of Health and Medical Sciences, University of Copenhagen

Forfatter:  Kristensen, Line H.
Faculty of Health and Medical Sciences, University of Copenhagen

Forfatter:  Stephansen, Karen (Cwisno: 72028)
Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, Universitetsparken 2, DK-2100 Copenhagen, Denmark
Email:

Forfatter:  Kristensen, Jan B.L.
Faculty of Health and Medical Sciences, University of Copenhagen

Forfatter:  Helgstrand, Charlotte
Faculty of Health and Medical Sciences, University of Copenhagen

Forfatter:  Lees, Michael
Biotech Research & Innovation Centre

Forfatter:  Cloos, Paul
Biotech Research & Innovation Centre

Forfatter:  Helin, Kristian
Biotech Research & Innovation Centre

Forfatter:  Gajhede, Michael
Faculty of Health and Medical Sciences, University of Copenhagen

Forfatter:  Olsen, Lars
Faculty of Health and Medical Sciences, University of Copenhagen

Uddrag: 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.
Publiceret: in journal: F E B S Letters (ISSN: 0014-5793) (DOI: http://dx.doi.org/10.1016/j.febslet.2012.03.001), vol: 586, issue: 8, pages: 1190-1194, 2012
DOI:
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