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Synthetic Tubulysin derivative, Tubugi-1, against invasive melanoma cells: The cell death triangle
Tubugi-1 is a more stable and accessible synthetic counterpart of natural tubulysins. This study aimed to evaluate its cytotoxic potential against anaplastic human melanoma cells. Results: Tubugi-1 reduced the viability of A-375 cells, inducing massive micronucleation, followed by augmented expression of inhibitor of nuclear factor-κB and caspase-2, typical of a mitotic catastrophe. Specific inhibition of autophagy by chloroquine resulted in conversion from mitotic catastrophe to rapid apoptosis. Conclusion: Multilevel anticancer action of tubugi-1 is extended by co-application of an autophagy inhibitor, giving a new dimension in further preclinical advancement of this potential agent.
DIJANA DRAČA, SANJA MIJATOVIĆ, TAMARA KRAJNOVIĆ, GORAN N. KALUĐEROVIĆ, LUDGER A. WESSJOHANN & DANIJELA MAKSIMOVIĆ-IVANIĆ. Synthetic Tubulysin derivative, Tubugi-1, against invasive melanoma cells: The cell death triangle. Anticancer Research, 2019