A Novel Dual HDAC6 and Tubulin Inhibitor, MPT0B451, Displays Anti-tumor Ability in Human Cancer Cells in Vitro and in Vivo

A Novel Dual HDAC6 and Tubulin Inhibitor, MPT0B451, Displays Anti-tumor Ability in Human Cancer Cells in Vitro and in Vivo

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The combination cancer therapy is a new strategy to circumvent drug resistance for the treatment ivoryjinelle.com of high metastasis and advanced malignancies.Herein, we developed a synthesized compound MPT0B451 that display inhibitory effect against histone deacetylase (HDAC) 6 and tubulin assembly.Our data demonstrated that MPT0B451 significantly inhibited cancer cell growths in HL-60 and PC-3 cells due to inhibition of HDAC activity.

MPT0B451 also markedly increased caspase-mediated apoptosis in these cells.The cell cycle analysis showed mitotic arrest induced by MPT0B451 with enhanced expression of G2/M transition proteins.Moreover, molecular docking analysis supported MPT0B451 as a dual HDAC6 and tubulin inhibitor.

Finally, rumchata proof MPT0B451 led to tumor growth inhibition (TGI) in HL-60 and PC-3 xenograft models.These findings indicated that MPT0B451 has dual inhibition effects for HDAC6 and tubulin, and also contributed to G2/M arrest followed by apoptotic induction.Together, our results suggested that MPT0B451 may serve as a potent anti-cancer treatment regimen in human prostate cancer and acute myeloid leukemia.