Interaction of dolastatin 10 with bovine brain tubulin

Biochem Pharmacol. 1992 Feb 4;43(3):539-43. doi: 10.1016/0006-2952(92)90576-5.

Abstract

Dolastatin 10 is an unusual peptide of marine origin which binds to tubulin in the vinblastine/maytansine/phomopsin-binding region and potently inhibits mitosis. Using N,N'-ethylenebis(iodoacetamide) (EBI) and iodo[14C]acetamide as probes for the effects of ligands on the thiol groups of tubulin, we found that dolastatin 10 has effects on the sulfhydryls indistinguishable from those of phomopsin A but quite different from those of vinblastine and maytansine. Using the binding of bis-5,5'-[8-(N-phenyl)aminonaphthalene-1-sulfonic acid] (BisANS) as a measure of tubulin decay, we found that dolastatin 10 resembled phomopsin A in that decay was not detectable by this assay in its presence. Interestingly, both otherwise very different peptides are among the most effective inhibitors of tubulin decay yet discovered.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Alkylation
  • Anilino Naphthalenesulfonates
  • Animals
  • Antineoplastic Agents / pharmacology*
  • Brain Chemistry*
  • Cattle
  • Cross-Linking Reagents
  • Cystine / chemistry
  • Depsipeptides
  • Ethylenediamines
  • Microtubules / chemistry
  • Mycotoxins / pharmacology
  • Oligopeptides / pharmacology*
  • Protein Conformation
  • Sulfhydryl Compounds / chemistry
  • Tubulin / chemistry*
  • Vinblastine / pharmacology

Substances

  • Anilino Naphthalenesulfonates
  • Antineoplastic Agents
  • Cross-Linking Reagents
  • Depsipeptides
  • Ethylenediamines
  • Mycotoxins
  • Oligopeptides
  • Sulfhydryl Compounds
  • Tubulin
  • Cystine
  • Vinblastine
  • 5,5'-bis(8-(phenylamino)-1-naphthalenesulfonate)
  • phomopsin
  • N,N'-ethylenebis(iodoacetamide)
  • dolastatin 10