Docetaxel

Docetaxel is a clinically well-established anti-mitotic chemotherapy medication. Docetaxel binds to microtubules reversibly with high affinity and has a maximum stoichiometry of 1 mole docetaxel per mole tubulin in microtubules. It has also been found to lead to the phosphorylation of oncoprotein bcl-2, which is apoptosis-blocking in its oncoprotein form. Docetaxel exhibits cytotoxic activity on breast, colorectal, lung, ovarian, gastric, renal and prostate cancer cells. Docetaxel does not block disassembly of interphase microtubules and so does not prevent entry into the mitotic cycle, but does block mitosis by inhibiting mitotic spindle assembly. Docetaxel activity is significantly greater in ovarian and breast tumours than for lung tumours. Docetaxel prevents microtubule depolymerization and disassembly in the absence of GTP.