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Gemcitabine is indicated in combination with cisplatin as first-line therapyfor solid tumours including non-small cell lung cancer (NSCLC), bladder cancerand mesothelioma. Gemcitabine is an analogue of pyrimidine cytosine and functionsas an anti-metabolite. Structurally, however, gemcitabine has similarities to5-aza-2-deoxycytidine (decitabine/Dacogen®), a DNA methyltransferase inhibitor(DNMTi). NSCLC, mesothelioma and prostate cancer cell lines were treated withdecitabine and gemcitabine. Reactivation of epigenetically silenced genes wasexamined by RT-PCR/qPCR. DNA methyltransferase activity in nuclear extracts andrecombinant proteins was measured using a DNA methyl-transferase assay, and alterationsin DNA methylation status were examined using methylation-specific PCR (MS-PCR)and pyrosequencing. We observe a reactivation of several epigenetically silencedgenes including GSTP1, IGFBP3 and RASSF1A. Gemcitabine functionally inhibitedDNA methyltransferase activity in both nuclear extracts and recombinant proteins.Gemcitabine dramatically destabilised DNMT1 protein. However, DNA CpG methylationwas for the most part unaffected by gemcitabine. In conclusion, gemcitabine bothinhibits and destabilises DNA methyltransferases and reactivates epigeneticallysilenced genes having activity equivalent to decitabine at concentrations significantlylower than those achieved in the treatment of patients with solid tumours. Thisproperty may contribute to the anticancer activity of gemcitabine.

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