Inhibition of microtubule assembly in vitro by TN-16, a synthetic antitumor drug.
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.
D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology*; D001665:Binding Sites / Q000187:drug effects; D001923:Brain Chemistry / Q000187:drug effects; D003078:Colchicine / Q000378:metabolism; D066298:In Vitro Techniques; D008870:Microtubules / Q000187:drug effects / Q000378:metabolism*; D011485:Protein Binding / Q000187:drug effects; D011760:Pyrrolidinones / Q000494:pharmacology*; D013552:Swine; D014404:Tubulin / Q000378:metabolism
D000970:Antineoplastic Agents; D011760:Pyrrolidinones; D014404:Tubulin; C038092:TN 16; D003078:Colchicine