The effect of TN-16 on the alkylation of tubulin

Mary Carmen Roach, Richard F. Luduena

Research output: Contribution to journalArticle

13 Scopus citations

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 β-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.

Original languageEnglish (US)
Pages (from-to)200-205
Number of pages6
JournalBiochemical and Biophysical Research Communications
Volume129
Issue number1
DOIs
StatePublished - May 31 1985

ASJC Scopus subject areas

  • Biophysics
  • Biochemistry
  • Molecular Biology
  • Cell Biology

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