Antitumor agent
Dolastatin 10 trifluoroacetate is an antitumor agent [1].
Dolastatin 10 trifluoroacetate is a potent antimitotic polypeptide isolated from a marine animal and is developed as a potential antitumor agent. Dolastatin 10 is found to have activity to inhibit tubulin polymerization with IC50 value of 1.2 μM. Besides that, it potently inhibits vincristine binding to tubulin with a Ki value of 1.4 μM in a noncompetitive manner. Dolastatin 10 also shows moderate effect on enhancing the binding of colchicines to tubulin. In addition, Dolastatin 10 has the inhibitory activity in tubulin-dependent GTP binding [1].
In the cellular assay, Dolastatin 10 shows activity against some human leukaemia, lymphoma and solid tumour cell lines (such as OVCAR-3 and NSCLC) with IC50 values ranging from 0.1nM to 10nM. It is currently tested in the clinical trials [2].
参考文献:
[1] Bai R L, Pettit G R, Hamel E.? Binding of dolastatin 10 to tubulin at a distinct site for peptide antimitotic agents near the exchangeable nucleotide and vinca alkaloid sites. Journal of Biological Chemistry, 1990, 265(28): 17141-17149.
[2] Schwartsmann G.? Marine organisms and other novel natural sources of new cancer drugs. Annals of Oncology, 2000, 11(suppl 3): 235-243.
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