Premium
Inhibition of microtubule assembly in vitro by TN‐16, a synthetic antitumor drug
Author(s) -
Arai Takao
Publication year - 1983
Publication title -
febs letters
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.593
H-Index - 257
eISSN - 1873-3468
pISSN - 0014-5793
DOI - 10.1016/0014-5793(82)80619-4
Subject(s) - nocodazole , tubulin , microtubule , colchicine , in vitro , chemistry , drug , anticancer drug , paclitaxel , biophysics , biochemistry , microbiology and biotechnology , biology , pharmacology , cytoskeleton , cell , genetics , chemotherapy
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.