Aberrant epigenetic reprogramming occurs frequently in the development
of tumors. Histone H3 lysine 27 trimethylation (H3K27me3) exerts
a repressive epigenetic mark on a large number of genes. UTX and
JMJD3 are the only two histone demethylases which activate gene expression
via demethylating H3K27me3 to H3K27me2 or H3K27me1. Current
studies show that dysregulation of these two proteins are heavily linked to
oncogenesis in various tissue types. Accumulating evidence suggested that
there is remarkable therapeutic potential of targeting JMJD3 or UTX in different
types of cancer. Herein, we shall give a brief review on the functional
roles of JMJD3 and UTX in cancers and evaluate the available compounds
and agents targeting UTX and JMJD3. Finally, we also discuss the several modalities that
target UTX and JMJD3 for cancer therapy. This review will help to develop novel strategies
to abolish or restore effects of UTX and JMJD3 in the pathogenesis of cancer.
Keywords: UTX, JMJD3, H3K27, cancer, therapeutic target.
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