Abstract:
:DNA hypomethylating drugs that act on DNA methyltransferase (DNMT) isoforms are promising anticancer agents. By using a well-characterized live-cell system to measure DNA methylation revisions (imprints), we characterize olsalazine, an approved anti-inflammatory drug, as a novel DNA hypomethylating agent. The cell-based screen used in this work is highly tractable, internally controlled, and well-suited for a drug repurposing strategy in epigenetics. Olsalazine very closely mimics the action of 5-aza-2'-deoxycytidine, a known hypomethylating drug, with minimal cytotoxicity at the concentrations tested. Olsalazine was identified by a rapid computer-guided similarity search of a database of approved drugs to a previously identified inhibitor of DNMTs.
journal_name
ChemMedChemjournal_title
ChemMedChemauthors
Méndez-Lucio O,Tran J,Medina-Franco JL,Meurice N,Muller Mdoi
10.1002/cmdc.201300555subject
Has Abstractpub_date
2014-03-01 00:00:00pages
560-5issue
3eissn
1860-7179issn
1860-7187journal_volume
9pub_type
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