Docetaxel, from Taxus brevifoia. Docetaxel (DTX) is a semi-synthetic taxane, derived from Paclitaxel, which was originally isolated from the inner bark of the Pacific Yew tree (Taxus brevifolia). Docetaxel is prepared by estertification of Paclitaxel (Taxol) side chain to 10-deacetyl baccatin III (10-DAB). On the basis of photoaffinity labeling and crystallographic analyses, Docetaxel was shown to inhibit the function of tubulin by binding to a similar, highly defined region within ????beta-tubulin. Docetaxel disturbs the dynamic equilibrium of microtubules by inhibiting the net removal of tubulin dimers from the polymer end. The resulting microtubule/docetaxel complex does not have the ability to disassemble. At stoichiometric concentrations, Docetaxel enhances microtubule assembly.
Because of Docetaxel's ability to act as a microtubule stabilizer, it was shown to be an anti-mitotic, apoptosis inducer and anti-neoplastic agent. Some studies indicate that this activity of taxanes in general and Docetaxel in particular, may originate in part, from the induction of genetic encoding of transcription factors with tumor suppressant effects as well as enzymes governing proliferation, apoptosis, inflammation and other anti-proliferative factors.Cell Signaling Activators and Inhibitors; Anticancer Compounds, Apoptosis Inducers.