The effect of 2-(4-methyl-1-piperazinylmethyl) acrylophenone dihydrochloride on the alkylation of tubulin

Richard F. Luduena, Mary Carmen Roach, Phyllis P. Trcka, M. L. Mallevais, Thomas MacRae

Research output: Contribution to journalArticlepeer-review

12 Scopus citations

Abstract

2-(4-Methyl-1-piperazinylmethyl) acrylophenone dihydrochloride (MPMAP) is a novel inhibitor of microtubule assembly in vitro and in vivo whose molecular mechanism of action has not been investigated (M. L. Mallevais, A. Delacourte, I. Lesieur, D. Lesieur, M. Cazin, C. Brunet, and M. Luyckx (1984) Biochimie 66, 477-482). We have examined the effect of MPMAP on the alkylation of tubulin by iodo[14C]acetamide and N,N′-ethylenebis (iodoacetamide) (EBI). MPMAP is a very potent inhibitor of tubulin alkylation by iodo[14C]acetamide. MPMAP gives half-maximal inhibition at a concentration of 15 μm. MPMAP also inhibits the alkylation of denatured tubulin and of aldolase, implying that it reacts strongly with sulfhydryl groups. MPMAP does not, however, interfere with formation by EBI of a crosslink between cysteines 239 and 354 in the β subunit of tubulin, suggesting that these sulfhydryls are located in a cleft in the tubulin molecule.

Original languageEnglish (US)
Pages (from-to)453-459
Number of pages7
JournalArchives of Biochemistry and Biophysics
Volume255
Issue number2
DOIs
StatePublished - Jun 1987

ASJC Scopus subject areas

  • Biophysics
  • Biochemistry
  • Molecular Biology

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