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  • Title: Antimicrotubular effect of calvatic acid and of some related compounds.
    Author: Gadoni E, Gabriel L, Olivero A, Bocca C, Miglietta A.
    Journal: Cell Biochem Funct; 1995 Dec; 13(4):231-8. PubMed ID: 10232925.
    Abstract:
    A structure-activity relationship has been established between calvatic acid and some related synthetic compounds, and their ability to inhibit GTP-induced microtubular protein polymerization in vitro. These compounds were effective in a dose- and a time-dependent manner. The most active drug was the p-chloro substituted compound, which showed its inhibitory activity without any preincubation period, which the others needed. Since if cysteine was present, polymerization was no longer affected, an involvement of titratable -SH groups of tubulin could be suggested. In contrast, taxol-induced polymerization was only slightly inhibited by these compounds, and colchicine-binding activity was not generally impaired.
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