IMR Press / FBE / Volume 8 / Issue 1 / DOI: 10.2741/E758

Frontiers in Bioscience-Elite (FBE) is published by IMR Press from Volume 13 Issue 2 (2021). Previous articles were published by another publisher on a subscription basis, and they are hosted by IMR Press on as a courtesy and upon agreement with Frontiers in Bioscience.

Open Access Review

Pharmacoepigenetics in gastrointestinal tumors: MGMT methylation and beyond

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1 Unit of Medical Oncology 2, Azienda Ospedaliero-Universitaria Pisana, Pisa, Italy
2 Unit of Oncology, Department of Oncology, Azienda USL2, Lucca, Italy

*Author to whom correspondence should be addressed.

Academic Editor: Francesco Crea

Front. Biosci. (Elite Ed) 2016, 8(1), 170–180;
Published: 1 January 2016
(This article belongs to the Special Issue Next-generation cancer biomarkers)

Epigenetic mechanisms are involved in gastrointestinal (GI) cancer pathogenesis. Insights into the molecular basis of GI carcinogenesis led to the identification of different epigenetic pathways and signatures that may play a role as therapeutic targets in metastatic colorectal cancer (mCRC) and non-colorectal GI tumors. Among these alterations, O6-methylguanine DNA methyltransferase (MGMT) gene promoter methylation is the most investigated biomarker and seems to be an early and frequent event, at least in CRC. Loss of expression of MGMT as a result of gene promoter methylation has been associated with interesting activity of alkylating agents in mCRC. However, the optimal methods for the definition of the MGMT status and additional predictive factors beyond MGMT in GI malignancies are lacking. Here we review the current role of MGMT methylation and other epigenetic alterations as potential treatment targets in GI tumors.

lkylating Agents
Cancer Epigenetics
Colorectal Cancer
Gastrointestinal Tumors
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