An antimitotic inhibitor of tubulin polymerization
Vincristine is an antimitotic vinca alkaloid, isolated from the plant V. rosea. It irreversibly blocks mitosis by binding to tubulin (Ki = 85 nM) and inhibiting tubulin polymerization.1,2 Vincristine is exported from cells via the ATP-
1.Jordan, M.A., Himes, R.H., and Wilson, L.Comparison of the effects of vinblastine, vincristine, vindesine, and vinepidine on microtubule dynamics and cell proliferation in vitroCancer Res.45(6)2741-2747(1985) 2.Towle, M.J., Salvato, K.A., Wels, B.F., et al.Eribulin induces irreversible mitotic blockade: Implications of cell-based pharmacodynamics for in vivo efficacy under intermittent dosing conditionsCancer Res.71(2)496-505(2011) 3.van Tellingen, O., Buckle, T., Jonker, J.W., et al.P-glycoprotein and Mrp1 collectively protect the bone marrow from vincristine-induced toxicity in vivoBr. J. Cancer89(9)1776-1782(2003) 4.Chan, H.S.L., Haddad, G., Thorner, P.S., et al.P-glycoprotein expression as a predictor of the outcome of therapy for neuroblastomaNew Engl. J. Med.325(23)1608-1614(1991)
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