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Antimicrotubular effect of calvatic acid and of some related compounds
Author(s) -
Gadoni Elena,
Gabriel Ludovica,
Olivero Antonella,
Bocca Claudia,
Miglietta Antonella
Publication year - 1995
Publication title -
cell biochemistry and function
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.933
H-Index - 61
eISSN - 1099-0844
pISSN - 0263-6484
DOI - 10.1002/cbf.290130403
Subject(s) - polymerization , chemistry , in vitro , colchicine , gtp' , cysteine , tubulin , titratable acid , biochemistry , drug , microtubule , stereochemistry , pharmacology , organic chemistry , biology , enzyme , medicine , microbiology and biotechnology , polymer
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.