DNA methyltransferase inhibitors and their emerging role in epigenetic therapy of cancer

A Gnyszka, Z JASTRZĘBSKI, S Flis - Anticancer research, 2013 - ar.iiarjournals.org
The DNA methyltransferase (DNMT) inhibitors azacytidine and decitabine are the most
successful epigenetic drugs to date and are still the most widely used as epigenetic …

DNA methyltransferase inhibitors: old and new drugs for an epigenetic cancer therapy

B Brueckner, F Lyko - Trends in pharmacological sciences, 2004 - cell.com
The pharmacological inhibition of DNA methyltransferases provides novel opportunities for
the therapy of human cancers. Several Phase III trials of DNA methyltransferase inhibitors …

DNA methyltransferase inhibitors in cancer: from pharmacology to translational studies

D Pechalrieu, C Etievant, PB Arimondo - Biochemical pharmacology, 2017 - Elsevier
DNA methylation is a mammalian epigenetic mark that participates to define where and
when genes are expressed, both in normal cells and in the context of diseases. Like other …

Development of DNA methyltransferase inhibitors for the treatment of neoplastic diseases

TE Fandy - Current medicinal chemistry, 2009 - ingentaconnect.com
Although chemotherapy is considered the mainstay of cancer therapy, unfortunate side
effects of chemotherapy create a continuous demand for developing other novel and specific …

DNA methyltransferase inhibitors and the development of epigenetic cancer therapies

F Lyko, R Brown - Journal of the National Cancer Institute, 2005 - academic.oup.com
Epimutations, such as the hypermethylation and epigenetic silencing of tumor suppressor
genes, play a role in the etiology of human cancers. In contrast to DNA mutations, which are …

[HTML][HTML] Nucleosidic DNA demethylating epigenetic drugs–a comprehensive review from discovery to clinic

K Agrawal, V Das, P Vyas, M Hajdúch - Pharmacology & therapeutics, 2018 - Elsevier
DNA methylation plays a pivotal role in the etiology of cancer by mediating epigenetic
silencing of cancer-related genes. Since the relationship between aberrant DNA methylation …

Modes of action of the DNA methyltransferase inhibitors azacytidine and decitabine

C Stresemann, F Lyko - International journal of cancer, 2008 - Wiley Online Library
The cytosine analogues 5‐azacytosine (azacytidine) and 2′‐deoxy‐5‐azacytidine
(decitabine) are the currently most advanced drugs for epigenetic cancer therapies. These …

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 …

DNA demethylation and invasive cancer: implications for therapeutics

D Cheishvili, L Boureau, M Szyf - British journal of …, 2015 - Wiley Online Library
One of the hallmarks of cancer is aberrant DNA methylation, which is associated with
abnormal gene expression. Both hypermethylation and silencing of tumour suppressor …

DNA methyltransferases as targets for cancer therapy.

K Ghoshal, S Bai - Drugs of Today (Barcelona, Spain: 1998), 2007 - europepmc.org
Methylation of DNA at 5-position of cytosine, catalyzed by DNA methyltransferases, is the
predominant epigenetic modification in mammals. Aberrations in methylation play a causal …