Inhibitor scaffolds for 2-oxoglutarate-dependent histone lysine demethylases.

Inhibitor scaffolds for 2-oxoglutarate-dependent histone lysine demethylases.

Show other versions (1)

The dynamic methylation of histone lysyl residues plays an important role in biology by regulating transcription, maintaining genomic integrity, and by contributing to epigenetic effects. Here we describe a variety of inhibitor scaffolds that inhibit the human 2-oxoglutarate-dependent JMJD2 subfamil...

Full description

Bibliographic Details
Main Authors:	Rose, N, Ng, S, Mecinović, J, Liénard, B, Bello, S, Sun, Z, McDonough, M, Oppermann, U, Schofield, C
Format:	Journal article
Language:	English
Published:	2008

Similar Items

Inhibitor scaffolds for 2-oxoglutarate-dependent histone lysine demethylases.
by: Rose, N, et al.
Published: (2008)

Investigations on the oxygen dependence of a 2-oxoglutarate histone demethylase.
by: Sánchez-Fernández, E, et al.
Published: (2013)

The oncometabolite 2-hydroxyglutarate inhibits histone lysine demethylases.
by: Chowdhury, R, et al.
Published: (2011)

The oncometabolite 2-hydroxyglutarate inhibits histone lysine demethylases
by: Chowdhury, R, et al.
Published: (2011)

The oncometabolite 2-hydroxyglutarate inhibits histone lysine demethylases
by: Chowdhury, R, et al.
Published: (2011)

Selective inhibitors of the JMJD2 histone demethylases: combined nondenaturing mass spectrometric screening and crystallographic approaches.
by: Rose, N, et al.
Published: (2010)

Selective inhibitors of the JMJD2 histone demethylases: combined nondenaturing mass spectrometric screening and crystallographic approaches.
by: Rose, N, et al.
Published: (2010)

Inhibition of the histone lysine demethylase JMJD2A by ejection of structural Zn(II).
by: Sekirnik, R, et al.
Published: (2009)

Monitoring the activity of 2-oxoglutarate dependent histone demethylases by NMR spectroscopy: direct observation of formaldehyde.
by: Hopkinson, R, et al.
Published: (2010)

Linking of 2-oxoglutarate and substrate binding sites enables potent and highly selective inhibition of JmjC histone demethylases.
by: Woon, E, et al.
Published: (2012)

A miniaturized screen for inhibitors of Jumonji histone demethylases.
by: Sakurai, M, et al.
Published: (2010)

A miniaturized screen for inhibitors of Jumonji histone demethylases.
by: Sakurai, M, et al.
Published: (2010)

Kinetic investigations on the reaction of a 2-oxoglutarate dependent histone demethylase with oxygen
by: Sanchez-Fernandez, E, et al.
Published: (2012)

Chemical probes for histone lysine demethylases
by: Gerken, P
Published: (2016)

Targeting histone lysine demethylases - Progress, challenges, and the future.
by: Thinnes, C, et al.
Published: (2014)

Dynamic combinatorial mass spectrometry leads to inhibitors of a 2-oxoglutarate-dependent nucleic acid demethylase.
by: Woon, E, et al.
Published: (2012)

Pan-histone demethylase inhibitors simultaneously targeting Jumonji C and lysine-specific demethylases display high anticancer activities.
by: Rotili, D, et al.
Published: (2014)

Inhibition of 2-oxoglutarate dependent oxygenases.
by: Rose, N, et al.
Published: (2011)

Recent progress in histone demethylase inhibitors
by: McAllister, T, et al.
Published: (2016)

Identification of the KDM2/7 histone lysine demethylase subfamily inhibitor and its antiproliferative activity.
by: Suzuki, T, et al.
Published: (2013)

Crystal structure of the PHF8 Jumonji domain, an Nepsilon-methyl lysine demethylase
by: Yue, W, et al.
Published: (2010)

Crystal structure of the PHF8 Jumonji domain, an Nepsilon-methyl lysine demethylase.
by: Yue, W, et al.
Published: (2010)

Crystal structures of histone demethylase JMJD2A reveal basis for substrate specificity.
by: Ng, S, et al.
Published: (2007)

Structure and mechanism guided identification of histone demethylase inhibitors
by: Schofield, C
Published: (2010)

Zn-ejection for the selective inhibition of JMJD2 histone demethylases
by: Sekirnik, R, et al.
Published: (2012)

Oxygen-dependent histone lysine demethylase 4 restricts hepatitis B virus replication
by: Harris, JM, et al.
Published: (2024)

Structure-activity studies of a macrocyclic peptide inhibitor of histone lysine demethylase 4A
by: Passioura, T, et al.
Published: (2018)

Arginine demethylation is catalysed by a subset of JmjC histone lysine demethylases.
by: Walport, L, et al.
Published: (2016)

Inhibition of histone demethylases by 4-carboxy-2,2'-bipyridyl compounds.
by: Chang, K, et al.
Published: (2011)

Assessing histone demethylase inhibitors in cells: lessons learned
by: Hatch, S, et al.
Published: (2017)

Discovery of a highly selective cell‐active inhibitor of the histone lysine demethylases KDM2/7
by: Gerken, P, et al.
Published: (2017)

Discovery of a highly selective cell-active inhibitor of the histone lysine demethylases KDM2/7
by: Gerken, PA, et al.
Published: (2017)

Autocatalysed oxidative modifications to 2-oxoglutarate dependent oxygenases
by: Mantri, M, et al.
Published: (2012)

Autocatalysed oxidative modifications to 2-oxoglutarate dependent oxygenases
by: Mantri, M, et al.
Published: (2012)

Autocatalysed oxidative modifications to 2-oxoglutarate dependent oxygenases.
by: Mantri, M, et al.
Published: (2012)

Structural and evolutionary basis for the dual substrate selectivity of human KDM4 histone demethylase family.
by: Hillringhaus, L, et al.
Published: (2011)

Investigating the substrate selectivity and the inhibitor of the human KDM7 sub-family of JmjC histone lysine demethylases
by: Zhang, Y
Published: (2019)

Development of homogeneous luminescence assays for histone demethylase catalysis and binding.
by: Kawamura, A, et al.
Published: (2010)

Development of homogeneous luminescence assays for histone demethylase catalysis and binding.
by: Kawamura, A, et al.
Published: (2010)

Structural studies on human 2-oxoglutarate dependent oxygenases.
by: McDonough, M, et al.
Published: (2010)