Article

Inhibition of demethylases by GSK-J1/J4

Nature, Springer Nature, ISSN 1476-4687

Volume 514, 7520, 2014

DOI:10.1038/nature13688, Dimensions: pub.1029300656, PMID: 25279926,

Affiliations

Organisations

  1. (1) EpiTherapeutics Aps, Ole Maal√łes Vej 3, 2200 Copenhagen, Denmark
  2. (2) University of Copenhagen, grid.5254.6, KU

Countries

Denmark

Continents

Europe

Description

Arising from L. Kruidenier et al.10.1038/nature11262 The recent publication1 of the first highly potent and specific inhibitor GSK-J1/J4 of the H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A provides a potential tool compound for this histone demethylase subfamily1. This inhibitor was used in tissue culture assays to conclude that the catalytic activities of the KDM6 proteins are required in inflammatory responses1; the generation of the inhibitor is intriguing, because it provides a strategy for generating sub-type-specific inhibitors of the 27-member Jumonji family and for the future treatment of various types of disease2,3,4,5,6. Here we show that the inhibitor is not specific for the H3K27me3/me2-demethylase subfamily in vitro and in tissue culture assays. Thus, the inhibitor cannot be used alone for drawing conclusions regarding the specific role of H3K27me3/me2-demethylase activity in biological processes or disease. There is a Reply to this Brief Communications Arising by Kruidenier et al. Nature514,10.1038/nature13689 (2014).

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University of Copenhagen

Danish Open Access Indicator

2014: Unused

Research area: Science & Technology

Danish Bibliometrics Indicator

2014: Level 2

Research area: Science & Technology

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Times Cited: 102

Field Citation Ratio (FCR): 12.67

Relative Citation ratio (RCR): 3.48