DNA methylation inhibitors in cancer: Recent and future approaches

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...

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Published inBiochimie Vol. 94; no. 11; pp. 2280 - 2296
Main Authors Gros, Christina, Fahy, Jacques, Halby, Ludovic, Dufau, Isabelle, Erdmann, Alexandre, Gregoire, Jean-Marc, Ausseil, Fréderic, Vispé, Stéphane, Arimondo, Paola B.
Format Journal Article
LanguageEnglish
Published France Elsevier B.V 01.11.2012
Subjects
Animals
DNA (Cytosine-5-)-Methyltransferases - antagonists & inhibitors
DNA (Cytosine-5-)-Methyltransferases - metabolism
DNA methylation
DNA Methylation - drug effects
DNMT inhibitors
Enzyme Inhibitors - pharmacology
Enzyme Inhibitors - therapeutic use
Epigenetics
Humans
Neoplasms - drug therapy
Neoplasms - enzymology
Neoplasms - genetics
Screening tests
DNA methylation
Epigenetics
Screening tests
DNMT inhibitors
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Summary: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. ► The advantage of designing selective inhibitors is analyzed. ► DNMT inhibitors are reviewed and future approaches are described. ► The existing screening test are summarized.
Bibliography:ObjectType-Article-2
SourceType-Scholarly Journals-1
ObjectType-Feature-3
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ObjectType-Review-1
ISSN:0300-9084
1638-6183
DOI:10.1016/j.biochi.2012.07.025