Use of Erbstatin as Protein-Tyrosine Kinase Inhibitor

Kazuo Umezawa, Masaya Imoto

Research output: Contribution to journalArticle

52 Citations (Scopus)

Abstract

This chapter discusses the use of erbstatin as protein-tyrosine kinase inhibitor. Streptomyces and other microorganisms produce antibiotics, anticancer agents, and enzyme inhibitors as secondary metabolites. Isolation of specific bioactive products in culture broths depends on the assay system. Erbstatin is easily inactivated in calf serum, and more stable analogs of erbstatin have been looked for. Various erbstatin analogs have been synthesized and tested for their inhibitory activity against tyrosine kinase. This analog inhibits tyrosine kinase in vitro, but are not active in vivo, because, being a polar molecule, it would penetrate the cells poorly.

Original languageEnglish
Pages (from-to)379-385
Number of pages7
JournalMethods in Enzymology
Volume201
Issue numberC
DOIs
Publication statusPublished - 1991 Jan
Externally publishedYes

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Biology

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