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• W2890427385 abstract "e14578 Background: The management of pancreatic cancer (PanCa) is exceptionally difficult due to poor response to available therapeutic approaches. Tubulins play a major role in cell dynamics and are important molecular targets for cancer therapy. Among various tubulins, βIII and βIV-tubulin isoforms have been primarily implicated in PanCa progression, metastasis and chemo-resistance. However, specific inhibitors of these isoforms that have potent anti-cancer activity with low toxicity are not readily available. In this study, we evaluated the therapeutic efficacy of VERU-111, a potent inhibitor of β-tubulin isotypes, in PanCa in vitro, and in vivo model systems. Methods: Effect of VERU-111 on proliferation, migration and invasion of human PanCa cells was performed using in vitro functional assays (MTS, wound healing, and Boyden chamber migrations). Effect of VERU-111 on the expression of β-tubulin isoforms was determined and compared with other clinical inhibitors of β-tubulin by Western blot, and qRT-PCR. Therapeutic efficacy of VERU-111 against PanCa was evaluated in an ectopic xenograft mouse model. Results: An orally bioavailable, small molecule inhibitor VERU-111, preferentially represses βIII and βIV tubulin isoforms via restoring the expression of miR-200c that directly targets these isoforms. Primarily, VERU-111 bind to cholchine binding sites and inhibit tubulin polymerization. As a result, VERU-111 efficiently inhibited tumorigenic and metastatic characteristics of PanCa cells in nanomolar range concentrations. VERU-111 arrested the cell cycle in the G2/M phase and induced apoptosis in PanCa cell lines via modulation of cell cycle regulatory (Cdc2, Cdc25c, and Cyclin B1) and apoptosis associated (Bax, Bad, Bcl-2, and Bcl-xl) proteins. VERU-111 treatment also showed significant (P < 0.01) inhibition of xenograft tumors in athymic nude mouse model. Excised xenograft tumors tissues were also analyzed for oncogenic signaling components, which showed potent inhibition of aforementioned oncogenic signaling compared to control. Conclusions: VERU-111 is an orally bioavailable, novel small molecule inhibitor of βIII/βIV tubulin isoforms with apparent efficacy in models of pancreatic cancer." @default.
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• W2890427385 date "2018-05-20" @default.
• W2890427385 modified "2023-10-06" @default.
• W2890427385 title "Therapeutic efficacy of a novel βIII/βIV-tubulin inhibitor (VERU-111) in pancreatic cancer." @default.
• W2890427385 doi "https://doi.org/10.1200/jco.2018.36.15_suppl.e14578" @default.
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