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© Yang SI, Institut Pasteur
Publication : Expert opinion on therapeutic patents

DNA methyltransferase inhibitors in cancer: a chemical and therapeutic patent overview and selected clinical studies

Scientific Fields
Diseases
Organisms
Applications
Technique

Published in Expert opinion on therapeutic patents - 03 Oct 2012

Fahy J, Jeltsch A, Arimondo PB

Link to Pubmed [PMID] – 23033952

Expert Opin Ther Pat 2012 Dec;22(12):1427-42

INTRODUCTION: DNA methylation is an epigenetic modification that modulates gene expression without altering the DNA base sequence. It plays a crucial role in cancer by silencing tumor suppressor genes (TSG). The DNA methyltransferases (DNMT) are the enzymes that catalyze DNA methylation and they are interesting therapeutical targets since DNA methylation is reversible such that an aberrant hypermethylation of DNA can be reverted by inhibition of DNMTs. Today, two drugs are on the market for the treatment of myelodysplastic syndrome, azacitidine and decitabine.

AREAS COVERED: Here, we present a review of the patents describing the chemistry and biological activities of novel DNMT inhibitors and discuss select clinical studies.

EXPERT OPINION: DNMT inhibitors have shown efficacy in clinics. However, highly efficient and specific DNMT inhibitors have not yet been identified. Improving methods will certainly lead to the prediction of novel directly binding inhibitors in the future.

https://www.ncbi.nlm.nih.gov/pubmed/23033952