JOURNAL ARTICLE

Epigenetic Regulation by Lysine Demethylase 5 (KDM5) Enzymes in Cancer

Lauren P Blair, Jian Cao, Mike Ran Zou, Joyce Sayegh, Qin Yan
Cancers 2011 March 1, 3 (1): 1383-404
21544224
Similar to genetic alterations, epigenetic aberrations contribute significantly to tumor initiation and progression. In many cases, these changes are caused by activation or inactivation of the regulators that maintain epigenetic states. Here we review our current knowledge on the KDM5/JARID1 family of histone demethylases. This family of enzymes contains a JmjC domain and is capable of removing tri- and di- methyl marks from lysine 4 on histone H3. Among these proteins, RBP2 mediates drug resistance while JARID1B is required for melanoma maintenance. Preclinical studies suggest inhibition of these enzymes can suppress tumorigenesis and provide strong rationale for development of their inhibitors for use in cancer therapy.

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