Intratumoral hypoxia followed by stabilization/activation of hypoxia-inducible factor 1 (HIF-1) and its downstream
transcriptional factors, is one of the most important mechanisms inducing epithelial-mesenchymal transition (EMT),
which has been widely accepted as a crucial step to generate early stage of tumor metastasis. Accumulating evidence suggests
that epigenetic mechanisms play important roles in hypoxia-induced EMT and metastasis. These epigenetic regulations
are mediated by various players including chromatin modifiers, transcriptional co-regulators, microRNAs, etc. In this
review, we discuss how his tone-modifying enzymes and transcriptional co-regulators regulate EMT under hypoxic conditions. Developed
or potential anticancer agents targeting epigenetic molecules regulating hypoxia-induced EMT are also discussed.
Keywords: Epigenetic regulation, hypoxia, epithelial-mesenchymal transition, HIF-1α, chromatin modifier, co-regulator, target.
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