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...

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Hlavní autoři: Rose, N, Woon, E, Kingham, G, King, O, Mecinović, J, Clifton, I, Ng, S, Talib-Hardy, J, Oppermann, U, McDonough, M, Schofield, C
Médium: Journal article
Jazyk:English
Vydáno: 2010
Témata:
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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