Interaction of cryptophycin 1 with tubulin and microtubules

Kristen Kerksiek, Marisan R. Mejillano, Robert E. Schwartz, Gunda I. Georg, Richard H. Himes

Research output: Contribution to journalArticle

78 Scopus citations

Abstract

The cryptophycins are newly discovered antimitotic agents isolated from the cyanobacterium Nostoc. Previous studies using cultured cells demonstrated that microtubules are the target of these compounds. We have studied the interaction of cryptophycin 1 with tubulin and microtubules in vitro. Cryptophycin 1 is an effective inhibitor of tubulin polymerization, causes tubulin to aggregate, and depolymerizes microtubules to linear polymers somewhat similar to the spiral-like structures produced by the Vinca alkaloids. Cryptophycin 1 also inhibits vinblastine binding to tubulin but not colchicine binding. Thus, it appears that the cryptophycins may bind to the Vinca site in tubulin or to a site that overlaps with the Vinca site.

Original languageEnglish (US)
Pages (from-to)59-61
Number of pages3
JournalFEBS Letters
Volume377
Issue number1
DOIs
StatePublished - Dec 11 1995
Externally publishedYes

Keywords

  • Antimitotic drug
  • Cryptophycin
  • Tubulin
  • Vinblastine

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    Kerksiek, K., Mejillano, M. R., Schwartz, R. E., Georg, G. I., & Himes, R. H. (1995). Interaction of cryptophycin 1 with tubulin and microtubules. FEBS Letters, 377(1), 59-61. https://doi.org/10.1016/0014-5793(95)01271-0