Vinblastine Sulfate is an antineoplastic agent with anti-mitotic properties and immunosuppressive activity. Vinblastine sulfate depolymerizes microtubules by binding tubulin and inducing self-association in spiral aggregates. This reaction that appears to be regulated by the C-terminus of β-Tubulin and is enhanced by GDP and GTP. Vinblastine sulfate has been observed to arrest the cell cycle in the G2/M-phase by blocking mitotic spindle formation. Vinblastine sulfate has also been documented to trigger Raf-1 activation and phosphorylation of Bcl-2 family proteins, to induce p53 expression, and to induce apoptosis in several tumor cell lines. The compound has also acted as a substrate of PGP and CYP3A4.
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