Abstract
We evaluated the effect of the human immunodeficiency virus (HIV) protease inhibitor saquinavir on the imatinib-sensitive and imatinib-resistant chronic myelogenous leukemia cell lines. Saquinavir, which is also a proteasome blocker, showed dose- and time-related anti-proliferative activity, particularly on the imatinib-resistant lines and a pro-apoptotic effect. Association with imatinib caused a significant increase of activity.
MeSH terms
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Adolescent
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Apoptosis / drug effects
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Benzamides
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Blast Crisis / drug therapy
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Blast Crisis / pathology
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Cell Line, Tumor / drug effects
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Cell Line, Tumor / enzymology
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Dose-Response Relationship, Drug
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Drug Resistance, Neoplasm
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Drug Screening Assays, Antitumor
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Drug Synergism
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Humans
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Imatinib Mesylate
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Interferons / therapeutic use
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K562 Cells / drug effects
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K562 Cells / enzymology
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Leukemia, Myelogenous, Chronic, BCR-ABL Positive / drug therapy
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Leukemia, Myelogenous, Chronic, BCR-ABL Positive / pathology*
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Leukemia, Myeloid, Chronic-Phase / drug therapy
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Leukemia, Myeloid, Chronic-Phase / pathology
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Male
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Middle Aged
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Piperazines / pharmacology*
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Protease Inhibitors / pharmacology*
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Proteasome Inhibitors
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Pyrimidines / pharmacology*
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Saquinavir / pharmacology*
Substances
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Benzamides
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Piperazines
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Protease Inhibitors
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Proteasome Inhibitors
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Pyrimidines
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Imatinib Mesylate
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Interferons
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Saquinavir