Accumulating evidence
suggests that aberrant regulation of chromatin modification is important to
tumorigenesis.Histone methylation is the posttranslational modification of
histone amino acids by addition of methyl groups that regulates chromatin
structure, transcription, and cellular epigenetic status. The jumonji (jmj)
domain containing gene family of proteins has been discovered to play a
role in chromatin regulation by influencing transcriptional activation,
suppression, and demethylation. Some recently characterized members of the
jmj family of histone demethylases include JARID1A/RBP2, JARID1C, JMJD1A,
JMJD1B, JMJD1C, JMJD2A, JMJD2C and JMJD2D. Two members of this protein
family, JARID1A/RBP2 and JMJD2A, have been found to bind the tumor
suppressor protein pRb further strengthening the role of these proteins in
transcriptional regulation. Additionally, JMJD2C, a lso known as GASC1
(gene amplified in squamous cell carcinoma), has been found to be amplified
in several espophageal squaumous carcinomas and inhibition of JMJD2C/GASC1
expression results in decreased cellular proliferation. Therefore, histone
demethylases can be viewed as an up and coming target of research for
anti-cancer therapies.