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Inhibition of microtubule assembly in vitro by TN-16, a synthetic antitumor drug

By Takao Arai

Abstract

AbstractAn antitumor drug, 3-(1-anilinoethylidene)-5-benzylpyrrolidine-2,4-dione (TN-16) inhibited the assembly of porcine brain microtubules in vitro. The assembly induced by taxol was also suppressed by the drug. However, the latter required much higher concentration of TN-16 than the former. Binding studies by means of the fluorometric method and the spun-column procedure indicate that the inhibition was caused by the reversible binding of the drug to the colchicine-sensitive site of tubulin. The affinity of TN-16 to tubulin was almost equal to that of nocodazole

Publisher: Published by Elsevier B.V.
Year: 1983
DOI identifier: 10.1016/0014-5793(82)80619-4
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