Use of the main tyrosine protein kinase activity purified from HL-60 in the search for a new class of anticancer compounds.
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.
Ernould
A P
AP
Institut de Recherches Servier, Suresnes, France.
Ferry
G
G
Genton
A
A
Cudennec
C A
CA
Boutin
J A
JA
D000970:Antineoplastic Agents / Q000494:pharmacology*; D006801:Humans; D006873:Hydroquinones / Q000494:pharmacology; D015473:Leukemia, Promyelocytic, Acute / Q000201:enzymology*; D011505:Protein-Tyrosine Kinases / Q000037:antagonists & inhibitors* / Q000302:isolation & purification; D014227:Triazines / Q000494:pharmacology; D014407:Tumor Cells, Cultured
D000970:Antineoplastic Agents; D006873:Hydroquinones; D014227:Triazines; C012842:Cibacron Blue F 3GA; D011505:Protein-Tyrosine Kinases; C048212:erbstatin