Activation of the p53 DNA damage response pathway after inhibition of DNA methyltransferase by 5-aza-2′-deoxycytidine

AR Karpf, BC Moore, TO Ririe, DA Jones - Molecular pharmacology, 2001 - ASPET
Transcriptional silencing of tumor suppressor genes by DNA methylation occurs in cancer
cell lines and in human tumors. This has led to the pursuit of DNA methyltransferase …

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 …

Pharmacological inhibition of DNA methylation induces proinvasive and prometastatic genes in vitro and in vivo

B Ateeq, A Unterberger, M Szyf, SA Rabbani - Neoplasia, 2008 - Elsevier
The mechanism of action of DNA methylation inhibitor 5-aza-2′-deoxycytidine (5-aza-
CdR), a potential anticancer agent is believed to be activated by the demethylation of tumor …

DNA methylation inhibitor 5-Aza-2′-deoxycytidine induces reversible genome-wide DNA damage that is distinctly influenced by DNA methyltransferases 1 and 3B

SS Palii, BO Van Emburgh, UT Sankpal… - … and cellular biology, 2008 - Taylor & Francis
Genome-wide DNA methylation patterns are frequently deregulated in cancer. There is
considerable interest in targeting the methylation machinery in tumor cells using nucleoside …

Differential induction of apoptosis and senescence by the DNA methyltransferase inhibitors 5-azacytidine and 5-aza-2′-deoxycytidine in solid tumor cells

S Venturelli, A Berger, T Weiland, F Essmann… - Molecular cancer …, 2013 - AACR
Epigenetic alterations are a hallmark of cancer that govern the silencing of genes. Up to
now, 5-azacytidine (5-aza-CR, Vidaza) and 5-aza-2′-deoxycytidine (5-aza-dC, Dacogen) …

Comparison of biological effects of non-nucleoside DNA methylation inhibitors versus 5-aza-2′-deoxycytidine

JC Chuang, CB Yoo, JM Kwan, TWH Li, G Liang… - Molecular cancer …, 2005 - AACR
DNA cytosine methylation plays a considerable role in normal development, gene
regulation, and carcinogenesis. Hypermethylation of the promoters of some tumor …

Importance of dose-schedule of 5-aza-2'-deoxycytidine for epigenetic therapy of cancer

M Lemaire, GG Chabot, NJM Raynal, LF Momparler… - BMC cancer, 2008 - Springer
Background The inactivation of tumor suppressor genes (TSGs) by aberrant DNA
methylation plays an important role in the development of malignancy. Since this epigenetic …

Role of estrogen receptor gene demethylation and DNA methyltransferase· DNA adduct formation in 5-Aza-2′ deoxycytidine-induced cytotoxicity in human breast …

AT Ferguson, PM Vertino, JR Spitzner, SB Baylin… - Journal of Biological …, 1997 - ASBMB
The cytosine analog 5-aza-2′-deoxycytidine is a potent inhibitor of DNA methyltransferase.
Its cytotoxicity has been attributed to several possible mechanisms including reexpression of …

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 …

Synergistic anti-breast cancer effect of a combined treatment with the methyl donor S-adenosyl methionine and the DNA methylation inhibitor 5-aza-2 …

F Chik, Z Machnes, M Szyf - Carcinogenesis, 2014 - academic.oup.com
DNA-demethylating agents activate tumor suppressor genes that are silenced by DNA
methylation in cancer and are therefore emerging as a novel approach to cancer therapy. 5 …