Histone Methylation and Demethylation

Our current knowledge regarding histone methylation stems in large part from the study of histone methyltransferases. Several of these enzymes are essential for development, vdth deregulated expression being linked to human disorders such as cancer [4]. Whereas proteins responsible for methylation of histones have been knovm for almost a decade, enzymes with histone demethylase activity (HDM) have only recently been discovered. Here we summarize our current knowledge regarding histone demethylases with a focus on the demethylation mechanisms, potential roles 

Interestingly, since the expression levels of several of these demethylases are increased in primary tumors (Table 13.1) and it is speculated that the demethylases contribute to tumor formation and maintenance, they present strong candidate drug targets. 

LSDl Overexpressed in prostate cancers correlating with relapse during therapy. 

JMJD2A JMJD2C is amplified in esophageal squamous carcinomas and in desmoblastic JMJD2B medulloblastomas. 

JMJD2C Depletion of JMJD2C inhibits proliferation of various cancer cell lines. 

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