<scp>EZH</scp>2: an emerging role in melanoma biology and strategies for targeted therapy
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- Jessamy Tiffen
- Melanoma Research Group Kolling Institute of Medical Research University of Sydney St Leonards NSW Australia
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- Stuart J. Gallagher
- Melanoma Research Group Kolling Institute of Medical Research University of Sydney St Leonards NSW Australia
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- Peter Hersey
- Melanoma Research Group Kolling Institute of Medical Research University of Sydney St Leonards NSW Australia
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説明
<jats:title>Summary</jats:title><jats:p>Histone modifications are increasingly being recognized as important epigenetic mechanisms that govern chromatin structure and gene expression. <jats:styled-content style="fixed-case">EZH</jats:styled-content>2 is the catalytic subunit of the polycomb repressive complex 2 (<jats:styled-content style="fixed-case">PRC</jats:styled-content>2), 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 <jats:styled-content style="fixed-case">SET</jats:styled-content> domain of <jats:styled-content style="fixed-case">EZH</jats:styled-content>2 confer its oncogenic activity. In the following review, we discuss the evidence that <jats:styled-content style="fixed-case">EZH</jats:styled-content>2 is an important driver of melanoma progression and we summarize the progress of <jats:styled-content style="fixed-case">EZH</jats:styled-content>2 inhibitors against this promising therapeutic target.</jats:p>
収録刊行物
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- Pigment Cell & Melanoma Research
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Pigment Cell & Melanoma Research 28 (1), 21-30, 2014-06-27
Wiley
