Abstract
Herbimycin A, a benzoquinonoid anasamycin antibiotic, preferentially inhibited the in vitro growth of Ph1-positive leukemia cell lines. On the other hand, genistein, which was developed as an inhibitor of receptor-type tyrosine kinase, and other protein kinase inhibitors showed no selective inhibition of Ph1-positive leukemia cell growth. Herbimycin A also displayed an abrogative effect on the transformation of murine hematopoietic cells by transfection with a bcr/abl oncoprotein-expressing retroviral vector. The antitumor action of herbimycin A on Ph1-positive leukemia cells is related to an inhibition of activity of bcr/abl protein tyrosine kinase and a subsequent reduction of the constitutive phosphotyrosyl proteins, however, the antibiotic has no effect on the expression of bcr/abl mRNA and oncoprotein. Therefore, herbimycin A may provide an important insight into the oncogenic action of bcr/abl oncoprotein and the future development of oncoprotein-targeted therapeutic agents.
Publication types
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Research Support, Non-U.S. Gov't
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Antibiotics, Antineoplastic / pharmacology*
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Benzoquinones
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Fusion Proteins, bcr-abl / metabolism
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Genistein
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Humans
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Isoflavones / pharmacology
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Lactams, Macrocyclic
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Leukemia, Myelogenous, Chronic, BCR-ABL Positive / enzymology
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Leukemia, Myelogenous, Chronic, BCR-ABL Positive / metabolism*
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Leukemia, Myelogenous, Chronic, BCR-ABL Positive / pathology
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Neoplasm Proteins / metabolism*
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Phosphotyrosine
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Protein-Tyrosine Kinases / antagonists & inhibitors*
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Quinones / pharmacology*
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Rifabutin / analogs & derivatives
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Tumor Cells, Cultured / drug effects
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Tumor Cells, Cultured / metabolism
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Tumor Cells, Cultured / pathology
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Tyrosine / analogs & derivatives*
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Tyrosine / metabolism
Substances
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Antibiotics, Antineoplastic
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Benzoquinones
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Isoflavones
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Lactams, Macrocyclic
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Neoplasm Proteins
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Quinones
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Rifabutin
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Phosphotyrosine
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Tyrosine
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herbimycin
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Genistein
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Protein-Tyrosine Kinases
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Fusion Proteins, bcr-abl