This study showed that MER proto-oncogene tyrosine kinase (MERTK) — which is often overexpressed or activated in several malignancies — is a new potential therapeutic target for melanoma. MERTK was overexpressed in >50% of melanoma cell lines and its expression correlated with disease progression. In a mouse xenograft model of melanoma, RNA-based MERTK inhibition reduced tumour volume by 60%. Moreover, treatment of melanoma cells with a novel MERTK-selective inhibitor (UNC1062) reduced activation of MERTK-mediated downstream signalling, induced apoptosis and also reduced migration and invasion of melanoma cells.
References
Schlegel, J. et al. MERTK receptor tyrosine kinase is a therapeutic target in melanoma. J. Clin. Invest. 123, 2257–2267 (2013)
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Harrison, C. A new target for melanoma. Nat Rev Drug Discov 12, 424 (2013). https://doi.org/10.1038/nrd4040
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DOI: https://doi.org/10.1038/nrd4040
