| Literature DB >> 25609585 |
Daniel Zingg1, Julien Debbache1, Simon M Schaefer1, Eylul Tuncer1, Sandra C Frommel2, Phil Cheng3, Natalia Arenas-Ramirez4, Jessica Haeusel1, Yudong Zhang1, Mario Bonalli1, Michael T McCabe5, Caretha L Creasy5, Mitchell P Levesque3, Onur Boyman4, Raffaella Santoro2, Olga Shakhova6, Reinhard Dummer3, Lukas Sommer1.
Abstract
Increased activity of the epigenetic modifier EZH2 has been associated with different cancers. However, evidence for a functional role of EZH2 in tumorigenesis in vivo remains poor, in particular in metastasizing solid cancers. Here we reveal central roles of EZH2 in promoting growth and metastasis of cutaneous melanoma. In a melanoma mouse model, conditional Ezh2 ablation as much as treatment with the preclinical EZH2 inhibitor GSK503 stabilizes the disease through inhibition of growth and virtually abolishes metastases formation without affecting normal melanocyte biology. Comparably, in human melanoma cells, EZH2 inactivation impairs proliferation and invasiveness, accompanied by re-expression of tumour suppressors connected to increased patient survival. These EZH2 target genes suppress either melanoma growth or metastasis in vivo, revealing the dual function of EZH2 in promoting tumour progression. Thus, EZH2-mediated epigenetic repression is highly relevant especially during advanced melanoma progression, which makes EZH2 a promising target for novel melanoma therapies.Entities:
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Year: 2015 PMID: 25609585 DOI: 10.1038/ncomms7051
Source DB: PubMed Journal: Nat Commun ISSN: 2041-1723 Impact factor: 14.919