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

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

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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...

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Bibliografske podrobnosti
Main Authors: Rose, N, Ng, S, Mecinović, J, Liénard, B, Bello, S, Sun, Z, McDonough, M, Oppermann, U, Schofield, C
Format: Journal article
Jezik:English
Izdano: 2008
Teme:
Enzyme Inhibitors
chemistry
Crystallography, X-Ray
Stereoisomerism
Models, Molecular
Dose-Response Relationship, Drug
pharmacology
Oxidoreductases, N-Demethylating
antagonists and inhibitors
chemical synthesis
metabolism
Protein Structure, Tertiary
Ketoglutaric Acids
Molecular Structure
Structure-Activity Relationship

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