Inhibition of the histone lysine demethylase JMJD2A by ejection of structural Zn(II).

نویسندگان

  • Rok Sekirnik
  • Nathan R Rose
  • Armin Thalhammer
  • Peter T Seden
  • Jasmin Mecinović
  • Christopher J Schofield
چکیده

JMJD2A, a 2-oxoglutarate dependent N(epsilon)-methyl lysine histone demethylase, is inhibited by disruption of its Zn-binding site by Zn-ejecting compounds including disulfiram and ebselen; this observation may enable the development of inhibitors selective for this subfamily of 2OG dependent oxygenases that do not rely on binding to the highly-conserved Fe(ii)-containing active site.

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عنوان ژورنال:
  • Chemical communications

دوره 42  شماره 

صفحات  -

تاریخ انتشار 2009