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- W2789838539 abstract "Several combretastatin derivatives are currently undergoing clinical trials for various types of cancer. In this work, we elucidated the antiproliferative mechanism of action of a highly potentcombretastatin analogue, C12 (5-Quinolin-3-yl and 4-(3,4,5-trimethoxyphenyl) substituted imidazol-2-amine). The compound displayed much stronger activity than CA-4 against different types of cancer cells. Further, C12 inhibited the proliferation of different cancer cells more effectively compared to their non-cancerous counterparts. The binding of C12 to tubulin was examined using surface plasma resonance and the intrinsic fluorescence of C12. Using modified Dixon plot, C12 was found to competitively inhibit the binding of podophyllotoxin, a colchicine-site binding agent, to tubulin. A molecular docking analysis also supported the finding that C12 shares its binding site in tubulin with colchicine. C12 displayed preferential binding to GTP-tubulin than GDP-tubulin indicating that it may bind to the end of microtubules. Consistent with this idea, C12 inhibited the binding of a microtubule plus-end tracking protein, EB1, to microtubules. C12 depolymerized microtubules both in in-vitro and in cells. Using fluorescence recovery after photobleaching technique, C12 was found to strongly suppress the dynamics of spindle microtubules in live HeLa cells. C12 treatment induced multipolar spindle formation, increased the chromosome compactness index, activated mitotic checkpoint protein BubR1 and ultimately induced apoptotic cell death in HeLa cells." @default.
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- W2789838539 date "2018-02-01" @default.
- W2789838539 modified "2023-09-27" @default.
- W2789838539 title "A Combretastatin Analogue C12 Binds to Colchicine Site in Tubulin, Inhibits Spindle Microtubule Dynamics, Activates Mitotic Checkpoint and Induces Apoptosis in Cancer Cells" @default.
- W2789838539 doi "https://doi.org/10.1016/j.bpj.2017.11.2303" @default.
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