2-Methoxyestradiol, an endogenous mammalian metabolite, inhibits tubulin polymerization by interacting at the colchicine site.

@article{DAmato19942MethoxyestradiolAE,
  title={2-Methoxyestradiol, an endogenous mammalian metabolite, inhibits tubulin polymerization by interacting at the colchicine site.},
  author={Robert J D'Amato and Chii Mei Lin and Evelyn A. Flynn and Judah M Folkman and Ernest Hamel},
  journal={Proceedings of the National Academy of Sciences of the United States of America},
  year={1994},
  volume={91 9},
  pages={3964-8}
}
A metabolite of estradiol, 2-methoxyestradiol (2ME), inhibits angiogenesis in the chicken embryo chorioallantoic membrane assay. Since 2ME causes mitotic perturbations, we examined its interactions with tubulin. In our standard 1.0 M glutamate system (plus 1.0 mM MgCl2 at 37 degrees C), superstoichiometric concentrations (relative to tubulin) of 2ME inhibited the nucleation and propagation phases of tubulin assembly but did not affect the reaction extent. Although polymer formed in the presence… CONTINUE READING