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Substituted 2-(2-aminopyrimidin-4-yl)pyridine-4-carboxylates as potent inhibitors of JumonjiC domain-containing histone demethylases

DOI: 10.4155/fmc.15.188 DOI Help

Authors: Martin Roatsch (Albert-Ludwigs-University Freiburg) , Dina Robaa (Martin-Luther-University Halle-Wittenberg) , Martin Pippel (Martin-Luther-University Halle-Wittenberg) , Joanne E Nettleship (Oxford Protein Production Facility UK) , Yamini Reddivari (Oxford Protein Production Facility UK) , Louise Bird (Oxford Protein Production Facility UK) , Inga Hoffmann (Albert-Ludwigs-University Freiburg) , Henriette Franz (University Medical Center Freiburg) , Ray Owens (University of Oxford) , Roland Schüle (University Medical Center Freiburg) , Ralf Flaig (Diamond Light Source) , Wolfgang Sippl (Martin-Luther-University Halle-Wittenberg) , Manfred Jung (Albert-Ludwigs-University Freiburg)
Co-authored by industrial partner: No

Type: Journal Paper
Journal: Future Medicinal Chemistry

State: Published (Approved)
Published: March 2016

Open Access Open Access

Abstract: Aberrant expression of iron(II)- and 2-oxoglutarate-dependent JumonjiC histone demethylases has been linked to cancer. Potent demethylase inhibitors are drug candidates and biochemical tools to elucidate the functional impact of demethylase inhibition.

Keywords: JumonjiC domain; aminopyrimidylpyridines; epigenetics; histone demethylase; metal chelators; prodrugs; virtual screening

Subject Areas: Biology and Bio-materials


Beamlines: I04-Macromolecular Crystallography

Documents:
fmc.15.pdf