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© Yang SI, Institut Pasteur
Publication : Future medicinal chemistry

Inhibition studies of DNA methyltransferases by maleimide derivatives of RG108 as non-nucleoside inhibitors

Scientific Fields
Diseases
Organisms
Applications
Technique

Published in Future medicinal chemistry - 10 Aug 2017

Rondelet G, Fleury L, Faux C, Masson V, Dubois J, Arimondo PB, Willems L, Wouters J

Link to Pubmed [PMID] – 28795598

Future Med Chem 2017 09;9(13):1465-1481

AIM: DNA methyltransferases (DNMTs) are important drug targets for epigenetic therapy of cancer. Nowadays, non-nucleoside DNMT inhibitors are in development to address high toxicity of nucleoside analogs. However, these compounds still have low activity in cancer cells and mode of action of these compounds remains unclear.

MATERIALS & METHODS: In this work, we studied maleimide derivatives of RG108 by biochemical, structural and computational approaches to highlight their inhibition mechanism on DNMTs.

RESULTS: Findings demonstrated a correlation between cytotoxicity on mesothelioma cells of these compounds and their inhibitory potency against DNMTs. Noncovalent and covalent docking studies, supported by crystallographic (apo structure of M.HhaI) and differential scanning fluorimetry assays, provided detailed insights into their mode of action and revealed essential residues for the stabilization of such compounds inside DNMTs. [Formula: see text].

https://www.ncbi.nlm.nih.gov/pubmed/28795598