Use of the main tyrosine protein kinase activity purified from HL-60 in the search for a new class of anticancer compounds

Anticancer Res. 1990 Jan-Feb;10(1):197-201.

Abstract

A tyrosine protein kinase (TPK) partially purified and two co-purified proteins (pp39 and pp44) from HL-60 cells were used as a basis for a SDS-PAGE electrophoresis screening test of inhibitors of the activity catalyzed by this enzyme. Such inhibitors may constitute a new class of anticancer agents. TPK is a protein of about 32 to 35 kDa as measured by gel-sizing exclusion. This enzyme is apparently the main tyrosine protein kinase from the cytosol of HL-60 cells. The test was assessed using known inhibitors of various types of protein kinases. Erbstatin and Cibcron Blue--a nucleotide analog--were shown to be potent inhibitors of TPK activity.

MeSH terms

  • Antineoplastic Agents / pharmacology*
  • Humans
  • Hydroquinones / pharmacology
  • Leukemia, Promyelocytic, Acute / enzymology*
  • Protein-Tyrosine Kinases / antagonists & inhibitors*
  • Protein-Tyrosine Kinases / isolation & purification
  • Triazines / pharmacology
  • Tumor Cells, Cultured

Substances

  • Antineoplastic Agents
  • Hydroquinones
  • Triazines
  • Cibacron Blue F 3GA
  • Protein-Tyrosine Kinases
  • erbstatin