Gemcitabine reactivates epigenetically silenced genes and functions as a DNA methyltransferase inhibitor

SG Gray, AM Baird, F O'Kelly… - International …, 2012 - spandidos-publications.com
Gemcitabine is indicated in combination with cisplatin as first-line therapy for solid tumours
including non-small cell lung cancer (NSCLC), bladder cancer and mesothelioma …

Demethylation of DNA by decitabine in cancer chemotherapy

R Brown, JA Plumb - Expert review of anticancer therapy, 2004 - Taylor & Francis
Genes involved in all aspects of tumor development and growth can become aberrantly
methylated in tumor cells, including genes involved in apoptosis and cell cycle regulation …

Gemcitabine functions epigenetically by inhibiting repair mediated DNA demethylation

A Schäfer, L Schomacher, G Barreto, G Döderlein… - PLoS …, 2010 - journals.plos.org
Gemcitabine is a cytotoxic cytidine analog, which is widely used in anti-cancer therapy. One
mechanism by which gemcitabine acts is by inhibiting nucleotide excision repair (NER) …

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… - Journal of Clinical …, 2005 - ascopubs.org
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 …

Azacytidine and decitabine induce gene-specific and non-random DNA demethylation in human cancer cell lines

S Hagemann, O Heil, F Lyko, B Brueckner - PloS one, 2011 - journals.plos.org
The DNA methyltransferase inhibitors azacytidine and decitabine represent archetypal
drugs for epigenetic cancer therapy. To characterize the demethylating activity of azacytidine …

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

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

Potential of 5-aza-2′-deoxycytidine (Decitabine) a potent inhibitor of DNA methylation for therapy of advanced non-small cell lung cancer

RL Momparler, J Ayoub - Lung cancer, 2001 - Elsevier
Although new agents and drug combinations have increased the response rate in advanced
non-small cell lung cancer (NSCLC), long-term survivors are rare. There is an urgent need …

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 …

Identification of novel DNA methylation inhibitors via a two-component reporter gene system

YS Lin, AY Shaw, SG Wang, CC Hsu, IW Teng… - Journal of biomedical …, 2011 - Springer
Background Targeting abnormal DNA methylation represents a therapeutically relevant
strategy for cancer treatment as demonstrated by the US Food and Drug Administration …

Decitabine effect on tumor global DNA methylation and other parameters in a phase I trial in refractory solid tumors and lymphomas

DJ Stewart, JP Issa, R Kurzrock, MI Nunez… - Clinical Cancer …, 2009 - AACR
Purpose: By hypomethylating genes, decitabine may up-regulate factors required for
chemotherapeutic cytotoxicity. Platinum-resistant cells may have reduced expression of the …