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The Effect of TN-16 on the Alkylation of Tubulin

The Effect of TN-16 on the Alkylation of Tubulin

M C Roach, R F Luduena

Biochem Biophys Res Commun. 1985 May 31;129(1):200-5.

PMID: 4004874

Abstract:

The synthetic anti-tumor drug 3-(1-anilinoethylidene)-5-benzylpyrrolidine-2,4-dione (TN-16) is known to block microtubule assembly and colchicine binding to tubulin, although its structure does not resemble those of either colchicine, podophyllotoxin, or nocodazole (Arai, FEBS Lett. 155:273-276 (1983]. We have found that TN-16 affects the intra-chain cross-linking of beta-tubulin by N,N'-ethylene-bis(iodoacetamide) in a manner identical to that of colchicine, podophyllotoxin, and nocodazole, but different from that of vinblastine or maytansine. TN-16 also inhibits alkylation of tubulin by iodo[14C]acetamide, as do colchicine and its congeners. TN-16 appears to bind to tubulin at the colchicine binding site and one of its phenyl groups is likely to bind at the site on tubulin where colchicine's A ring binds.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP33016125	TN-16		33016-12-5	Price

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