4.7 Review

Epigenetics and therapeutic targets in gastrointestinal malignancies

Journal

DRUG DISCOVERY TODAY
Volume 26, Issue 10, Pages 2303-2314

Publisher

ELSEVIER SCI LTD
DOI: 10.1016/j.drudis.2021.04.013

Keywords

Gastrointestinal cancers; Epigenetics; DNA methyltransferases; Histone deacetylases; Therapy; Clinical outcomes

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Gastrointestinal malignancies are heavily influenced by dysregulated signal transduction and epigenetic pathways, with HDACs and DNMTs playing crucial roles in these processes. Understanding the enzyme targets and functional mechanisms involved can aid in the development of therapeutic strategies for gastrointestinal malignancies.
Gastrointestinal (GI) malignancies account for substantial mortality and morbidity worldwide. They are generally promoted by dysregu-lated signal transduction and epigenetic pathways, which are con -trolled by specific enzymes. Recent studies demonstrated that histone deacetylases (HDACs) together with DNA methyltransferases (DNMTs) have crucial roles in the signal transduction/epigenetic pathways in GI regulation. In this review, we discuss various enzyme targets and their functional mechanisms responsible for the regula-tory processes of GI malignancies. We also discuss the epigenetic therapeutic targets that are mainly facilitated by DNMT and HDAC inhibitors, which have functional consequences and clinical out-comes for GI malignancies.

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