Selective inhibitors of the JMJD2 histone demethylases: combined nondenaturing mass spectrometric screening and crystallographic approaches.

Selective inhibitors of the JMJD2 histone demethylases: combined nondenaturing mass spectrometric screening and crystallographic approaches.

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Ferrous ion and 2-oxoglutarate (2OG) oxygenases catalyze the demethylation of N(epsilon)-methylated lysine residues in histones. Here we report studies on the inhibition of the JMJD2 subfamily of histone demethylases, employing binding analyses by nondenaturing mass spectrometry (MS), dynamic combin...

Ausführliche Beschreibung

Bibliographische Detailangaben
Hauptverfasser: Rose, N, Woon, E, Kingham, G, King, O, Mecinović, J, Clifton, I, Ng, S, Talib-Hardy, J, Oppermann, U, McDonough, M, Schofield, C
Format: Journal article
Sprache:English
Veröffentlicht: 2010
Schlagworte:
Binding, Competitive
Spectrometry, Mass, Electrospray Ionization
Binding Sites
analogs and derivatives
chemistry
Tyrosine
Structure-Activity Relationship
Crystallography, X-Ray
chemical synthesis
Models, Molecular
Combinatorial Chemistry Techniques
Oxalic Acids
antagonists and inhibitors
Jumonji Domain-Containing Histone Demethylases
Spectrometry, Mass, Matrix-Assisted Laser Desorption-Ionization

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