DNA methylation and demethylation probed by small molecules

M Szyf - Biochimica et Biophysica Acta (BBA)-Gene Regulatory …, 2010 - Elsevier
DNA demethylation inhibitors has been lagging. This review will discuss DNA methylation
and demethylation machineries, and their therapeutic potentials as targets for small molecule

Targeting DNA methylation with small molecules: what's next? Miniperspective

A Erdmann, L Halby, J Fahy… - Journal of medicinal …, 2015 - ACS Publications
… of DNA methylation during the maintenance of DNA methylation; it must not be excluded
that these compounds may trigger active demethylation mechanisms that are not yet identified. …

Discovery of two novel, small-molecule inhibitors of DNA methylation

P Siedlecki, RG Boy, T Musch… - Journal of medicinal …, 2006 - ACS Publications
… effective in scanning small molecules for potential interactions … new insights into the DNA
methylation process. NSC401077, in … In addition, our data showed a substantial demethylating

Small molecules DNA methyltransferases inhibitors

N Martinet, BY Michel, P Bertrand, R Benhida - MedChemComm, 2012 - pubs.rsc.org
… We review here knowledge about DNA methylation to provide … Ideally, demethylation of
CmG islands and of repeat … are easily demethylated, but CmG islands are demethylated only …

Epigenetic small molecule modulators of histone and DNA methylation

AT Hauser, D Robaa, M Jung - Current Opinion in Chemical Biology, 2018 - Elsevier
… For a long time, histone methylation was considered as an irreversible modification. But
while the existence of an actual arginine demethylase still remains to be proven, two classes of …

DNA methylation and demethylation in mammals

Z Chen, AD Riggs - Journal of Biological Chemistry, 2011 - ASBMB
… , a wave of global de novo methylation re-establishes the DNA methylation patterns that will
be maintained, in large part, in somatic tissues. Genome-wide demethylation also occurs in …

Mechanisms of DNA methylation and demethylation in mammals

G Auclair, M Weber - Biochimie, 2012 - Elsevier
… of DNA methylation are highly dynamic between cell types. Here, we discuss the importance
of DNA methylation for genome regulation and the mechanisms that remodel the DNA

Epigenetic reactivation of tumor suppressor genes by a novel small-molecule inhibitor of human DNA methyltransferases

B Brueckner, R Garcia Boy, P Siedlecki, T Musch… - Cancer research, 2005 - AACR
… and maintenance of defined DNA methylation patterns that … demethylating activities for a
few other small molecules. For … anesthetic procaine induce demethylation at high micromolar …

Targeting DNA methylation

JPJ Issa, HM Kantarjian - Clinical Cancer Research, 2009 - AACR
… Any clinical effect of these weak “demethylating” drugs may require prolonged exposure
to … of small molecules targeting DNA methyltransferases (20). These small molecules have …

Target specificity of mammalian DNA methylation and demethylation machinery

M Ravichandran, RZ Jurkowska… - Organic & biomolecular …, 2018 - pubs.rsc.org
… maintenance of the methylation pattern, both generation of DNA methylation and its removal
… of ongoing DNA methylation and demethylation shapes the final epigenetic methylation