Qualitative study of the interaction mechanism of estrogenic drugs with tubulin

Abstract Synthetic estrogenic drugs ( E -diethylstilbestrol, erythro-hexestrol and E , E -dienestrol) inhibit tubulin assembly and erythro-hexestrol and E , E -dienestrol lead to the formation of twisted ribbon structures. For the inhibitory effect on tubulin assembly, estrogenic drugs seem to interact directly with tubulin 6S on site(s) analogous to the colchicine-site, but independent of the GTP- and vinblastine-sites. This binding does not involve tubulin tryptophanyl residues or sulfhydryl groups. The influence of temperature, calcium and magnesium on the formation of twisted ribbon structures induced by the binding of estrogenic drugs to microtubular protein and tubulin has also been studied. This formation is strongly magnesium-dependent whereas preformed twisted ribbon structures are calcium- and chilling-insensitive.