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

FEBS Letters

Arai, Takao¹ 

[1]Institute of Basic Medical Sciences, University of Tsukuba, Niihari-gun, Ibaraki 305, Japan

关键词: Antitumor drug;    TN-16;    Nocodazole;    Taxol;    Tubulin;    Microtubule assembly;    TN-16;    3-(1-anilinoethylidene)-5-benzylpyrrolidine-2;    4-dione;    MES;    2-(N-morpholino)ethane sulfonic acid;    EGTA;    ethyleneglycol-bis(2-aminoethylether)-N;    N;    N′;    N′-tetraacetic acids;    DMSO;    dimethylsulfoxide;   

DOI  :  10.1016/0014-5793(82)80619-4

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

An 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.

【 授权许可】

Unknown