Extracellular stress and mitogens activate mitogen activated protein kinase (MAPK) pathways that mediate various intracellular events including cell differentiation, cell proliferation, and cell death. The MEK-5/ERK-5 pathway is up-regulated in breast and prostate cancer and is involved in tumor progression and development of resistance. While screening a series of compounds for inhibition of MEK5 activity and proliferation/viability, we observed a concomitant reversal of the epithelial-to-mesenchymal transition (EMT) by one of our compounds. Consistent with the acquisition of a more epithelial morphology, qPCR analysis confirmed an increased in E-Cadherin gene expression and altered expression of associated EMT related genes. We will present how structural variations on anthranillic amides modify this transition.

Structural variations on anthranillic amides and their effect on mesenchymal transition

246th National Meeting (2013)

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