Rational Design of Bisubstrate-Type Analogues as Inhibitors of DNA Methyltransferases in Cancer Cells.

@article{Halby2017RationalDO,
  title={Rational Design of Bisubstrate-Type Analogues as Inhibitors of DNA Methyltransferases in Cancer Cells.},
  author={Ludovic Halby and Yoann Menon and Elodie Rilova and Dany Pechalrieu and V{\'e}ronique Masson and C{\'e}line Faux and Mohamed Amine Bouhlel and Marie-H{\'e}l{\`e}ne David-Cordonnier and Natacha Novosad and Yannick Aussagues and Arnaud Samson and Laurent Lacroix and Fr{\'e}d{\'e}ric Ausseil and Laurence Fleury and Dominique Guianvarc'h and Clotilde Ferroud and Paola B. Arimondo},
  journal={Journal of medicinal chemistry},
  year={2017},
  volume={60 11},
  pages={4665-4679}
}
Aberrant DNA hypermethylation of promoter of tumor suppressor genes is commonly observed in cancer, and its inhibition by small molecules is promising for their reactivation. Here we designed bisubstrate analogues-based inhibitors, by mimicking each substrate, the S-adenosyl-l-methionine and the deoxycytidine, and linking them together. This approach… CONTINUE READING