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 …

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 …

[HTML][HTML] DNA methyltransferase inhibitors—state of the art

J Goffin, E Eisenhauer - Annals of Oncology, 2002 - Elsevier
Background DNA methylation is the addition of a methyl group to the 5 position of cytosine. It
is an epigenetic process with several effects, including chromatin structure modulation …

Targeting DNA methylation

JPJ Issa, HM Kantarjian - Clinical Cancer Research, 2009 - AACR
Two nucleoside inhibitors of DNA methylation, azacitidine and decitabine, are now standard
of care for the treatment of the myelodysplastic syndrome, a deadly form of leukemia. These …

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 …

Epigenetic therapy of cancer with 5-aza-2′-deoxycytidine (decitabine)

RL Momparler - Seminars in oncology, 2005 - Elsevier
Epigenetic events, such as aberrant DNA methylation, have been demonstrated to silence
the expression of many genes that suppress malignancy. Since the event is reversible, it is …

[PDF][PDF] Phase I and pharmacodynamic trial of the DNA methyltransferase inhibitor decitabine and carboplatin in solid tumors

K Appleton, HJ Mackay, I Judson… - Journal of Clinical …, 2007 - researchgate.net
Purpose The DNA methyltransferase inhibitor 5-aza-2-deoxycytidine (decitabine) induces
DNA demethylation and re-expression of epigenetically silenced genes, and increases …

[PDF][PDF] Evaluation of a 7-day continuous intravenous infusion of decitabine: inhibition of promoter-specific and global genomic DNA methylation

WE Samlowski, SA Leachman, M Wade, P Cassidy… - J Clin …, 2005 - researchgate.net
Purpose The nucleoside analog 5-aza-2#-deoxycytidine (5-aza-CdR, decitabine) is a potent
inhibitor of DNA methylation in vitro. Cellular treatment with this agent induces the re …

Mechanism of inhibition of DNA methyltransferases by cytidine analogs in cancer therapy

H Gowher, A Jeltsch - Cancer biology & therapy, 2004 - Taylor & Francis
Hypermethylation of tumor suppressor genes caused by aberrant activity of DNA
methyltransferases is an important mechanism that contributes to cancer. The reaction …

5-Azacytidine and 5-aza-2′-deoxycytidine as inhibitors of DNA methylation: mechanistic studies and their implications for cancer therapy

JK Christman - Oncogene, 2002 - nature.com
Azacytidine was first synthesized almost 40 years ago. It was demonstrated to have a wide
range of anti-metabolic activities when tested against cultured cancer cells and to be an …