DNA methylation and demethylation probed by small molecules

M Szyf - Biochimica et Biophysica Acta (BBA)-Gene Regulatory …, 2010 - Elsevier
DNA methylation is a covalent modification of DNA that plays an important role in setting
gene expression programs during development. Recent evidence suggests that changes in …

Regulation of the DNA methylation machinery and its role in cellular transformation

M Szyf, N Detich - 2001 - Elsevier
Publisher Summary Deoxyribonucleic acid (DNA) methylation, a covalent modification of the
genome, is emerging as an important player in the regulation of gene expression. This …

DNA hypermethylation as a chemotherapy target

J Ren, BN Singh, Q Huang, Z Li, Y Gao, P Mishra… - Cellular signalling, 2011 - Elsevier
Epigenetics refers to partially reversible, somatically inheritable, but DNA sequence-
independent traits that modulate gene expression, chromatin structure, and cell functions …

DNA methylation and cancer

PC Taberlay, PA Jones - Epigenetics and Disease: Pharmaceutical …, 2011 - Springer
DNA methylation acts in concert with other epigenetic mechanisms to regulate normal gene
expression and facilitate chromatin organization within cells. Aberrant DNA methylation …

DNA demethylases: a new epigenetic frontier in drug discovery

N Carey, CJ Marques, W Reik - Drug discovery today, 2011 - Elsevier
DNA methylation is one of the most extensively studied, and one of the most stable, of all
epigenetic modifications. Two drugs that target DNA methyltransferase enzymes are …

DNA demethylation: where genetics meets epigenetics

X Zhang, R Fu, J Yu, X Wu - Current Pharmaceutical Design, 2014 - ingentaconnect.com
Epigenetic regulation is essential to the well-being of developing as well as developed cells
by providing tissue-specific gene expression. DNA methylation on cytosine nucleotides is …

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

A Erdmann, L Halby, J Fahy… - Journal of medicinal …, 2015 - ACS Publications
DNA methylation is a mammalian epigenetic mark that is involved in defining where and
when genes are expressed, both in normal cells and in the context of diseases. Like other …

Therapeutic targeting of DNA methylation alterations in cancer

AV Lee, KA Nestler, KB Chiappinelli - Pharmacology & therapeutics, 2024 - Elsevier
DNA methylation is a critical component of gene regulation and plays an important role in
the development of cancer. Hypermethylation of tumor suppressor genes and silencing of …

Targeting DNA methylation in cancer

M Szyf - Ageing research reviews, 2003 - Elsevier
There is overwhelming evidence that DNA methylation patterns are altered in cancer.
Methylation of CG-rich islands in regulatory regions of genes marks them for transcriptional …

The role of DNA methylation in the pathogenesis and treatment of cancer

J Peedicayil - Current clinical pharmacology, 2012 - ingentaconnect.com
DNA methylation is a major epigenetic mechanism that leads to inhibition of gene
transcription and is known to be involved in the pathogenesis of cancer. The effectors of …