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Communication dans un congrès

Potent, Selective, and Cell-active Chemical Probe of Protein Lysine Methyltransferases G9a and GLP: Cell-Based Assays

Abstract : Histone lysine methylation is important epigenetic mark that regulates chromatin structure and gene expression. G9a and GLP lysine methyltransferases dimethylate lysine 9 on histone H3 and repress gene transcription playing roles in development, cancer, pluripotency and other biological processes. We report the development of UNC0638 as a chemical probe of G9a/GLP, active in a cellular system at nM concentrations, with excellent toxicity/potency ratio and low nM in vitro potency and selectivity for G9a/GLP over a wide range of targets. Cell immunofluorescence assay/ Incell Western as fast, reproducible and high throughput cellular assay measuring the levels of dimethylated histone H3 lysine 9 was developed and validated using G9a and GLP knockdowns. High G9a/GLP selectivity for lysine 9 dimethyl modification on histone H3 was also established by the mass spectrometry. In mouse ES cells, UNC0638 reactivated silenced GFP reporter
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Communication dans un congrès
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https://hal.inrae.fr/hal-02823689
Déposant : Migration Prodinra <>
Soumis le : samedi 6 juin 2020 - 21:46:21
Dernière modification le : vendredi 19 février 2021 - 09:12:32

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  • HAL Id : hal-02823689, version 1
  • PRODINRA : 40822

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Dalia Baryste-Lovejoy, Sylvie Rival-Gervier, Feng Liu, Abdellah Allali-Hassani, Tim J. Wigle, et al.. Potent, Selective, and Cell-active Chemical Probe of Protein Lysine Methyltransferases G9a and GLP: Cell-Based Assays. 2. Oxford Symposium on "Epigenetic Mechanisms in Health and Disease" - "Role of chromatin modifications in inflammation", Dec 2010, Oxford, United Kingdom. ⟨hal-02823689⟩

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