DNA methylation inhibitors in cancer: recent and future approaches

Christina Gros; Jacques Fahy; Ludovic Halby; Isabelle Dufau; Alexandre Erdmann; Jean-Marc Gregoire; Fréderic Ausseil; Stéphane Vispé; Paola B Arimondo

doi:10.1016/j.biochi.2012.07.025

DNA methylation inhibitors in cancer: recent and future approaches

Biochimie. 2012 Nov;94(11):2280-96. doi: 10.1016/j.biochi.2012.07.025. Epub 2012 Aug 11.

Authors

Christina Gros¹, Jacques Fahy, Ludovic Halby, Isabelle Dufau, Alexandre Erdmann, Jean-Marc Gregoire, Fréderic Ausseil, Stéphane Vispé, Paola B Arimondo

Affiliation

¹ USR CNRS-Pierre Fabre n° 3388-ETaC Epigenetic Targeting of Cancer, CRDPF 3 avenue Hubert Curien, 31035 Toulouse Cedex 01, France.

PMID: 22967704
DOI: 10.1016/j.biochi.2012.07.025

Abstract

This review presents the different human DNA methyltransferases (DNMTs), their biological roles, their mechanisms of action and their role in cancer. The description of assays for detecting DNMT inhibitors (DNMTi) follows. The different known DNMTi are reported along with their advantages, drawbacks and clinical trials. A discussion on the features of the future DNMT inhibitors will conclude this review.

Publication types

Review

MeSH terms

Animals
DNA (Cytosine-5-)-Methyltransferases / antagonists & inhibitors
DNA (Cytosine-5-)-Methyltransferases / metabolism
DNA Methylation / drug effects*
Enzyme Inhibitors / pharmacology
Enzyme Inhibitors / therapeutic use
Humans
Neoplasms / drug therapy
Neoplasms / enzymology
Neoplasms / genetics*

Substances

Enzyme Inhibitors
DNA (Cytosine-5-)-Methyltransferases