Inhibition of proliferation and invasion in 2D and 3D models by 2-methoxyestradiol in human melanoma cells

• DOI: 10.1016/j.phrs.2017.02.013
• Publication Date: 2017-02-14T20:17:00Z
• Authors: R.R. Massaro; F. Faião-Flores; V.W. Rebecca; S. Sandri; D.K. Alves-Fernandes; P.C. Pennacchi; K.S.M. Smalley; S.S. Maria-Engler
• Keywords: 2-Methoxyestradiol

Despite the recent advances in clinical management of melanoma, there remains a need for new pharmacological approaches to treat this cancer. 2-methoxyestradiol (2ME) is metabolite estrogen that has shown anti-tumor effects many cancer types. In study we show 2ME treatment leads growth inhibition melanoma cells, an effect associated with entry into senescence, decreased pRb and Cyclin B1 expression, increased p21/Cip1 expression G2/M cell cycle arrest. also inhibits colony formation assay, including lines acquired resistance BRAF + MEK inhibitors. We further effective against different NRAS mutational status. Moreover, induced retraction cytoplasmic projections 3D spheroid model significantly proliferation skin reconstruct model. Together our studies bring insights mechanism action allowing targeted therapy be refined. Continued progress area expected lead improved anti-cancer treatments development more analogues.