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EZH2: an emerging role in melanoma biology and strategies for targeted therapy.
- Source :
-
Pigment cell & melanoma research [Pigment Cell Melanoma Res] 2015 Jan; Vol. 28 (1), pp. 21-30. Date of Electronic Publication: 2014 Jun 27. - Publication Year :
- 2015
-
Abstract
- Histone modifications are increasingly being recognized as important epigenetic mechanisms that govern chromatin structure and gene expression. EZH2 is the catalytic subunit of the polycomb repressive complex 2 (PRC2), responsible for tri-methylation of lysine 27 on histone 3 (H3K27me3) that leads to gene silencing. This highly conserved histone methyltransferase is found to be overexpressed in many different types of cancers including melanoma, where it is postulated to abnormally repress tumor suppressor genes. Somatic mutations have been identified in approximately 3% of melanomas, and activating mutations described within the catalytic SET domain of EZH2 confer its oncogenic activity. In the following review, we discuss the evidence that EZH2 is an important driver of melanoma progression and we summarize the progress of EZH2 inhibitors against this promising therapeutic target.<br /> (© 2014 John Wiley & Sons A/S. Published by John Wiley & Sons Ltd.)
Details
- Language :
- English
- ISSN :
- 1755-148X
- Volume :
- 28
- Issue :
- 1
- Database :
- MEDLINE
- Journal :
- Pigment cell & melanoma research
- Publication Type :
- Academic Journal
- Accession number :
- 24912396
- Full Text :
- https://doi.org/10.1111/pcmr.12280