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

Cancers

Lauren P. Blair¹  Jian Cao¹  Mike Ran Zou¹  Joyce Sayegh¹ 

[1] Department of Pathology, Yale University School of Medicine, New Haven, CT, USA;

关键词: KDM5;    JARID1;    RBP2;    PLU1;    SMCX;    SMCY;    Lid;    histone demethylase;    cancer stem cell;    drug resistance;   

DOI  :  10.3390/cancers3011383

来源: mdpi

【 摘 要 】

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.

【 授权许可】

CC BY   
© 2011 by the authors; licensee MDPI, Basel, Switzerland.