Abstract
Recently, we developed a series of novel and potent aminopeptidase inhibitors with a homophthalimide skeleton. Among them, N-(2,6-diethylphenyl)homophthalimide (PIQ-22) possesses a specific aminopeptidase-inhibiting activity more potent than that of bestatin or actinonin, as assayed in terms of hydrolysis of L-alanine 4-methylcoumaryl-7-amide (Ala-AMC) by human acute lymphoblastic leukemia MOLT-4 cells. We show here that PIQ-22 and its 2,6-dimethylphenyl derivative (PIQ-11) are more potent inhibitors of tumor cell invasion than bestatin and actinonin in a Matrigel assay using mouse melanoma B16F10/L5 cells.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Aminopeptidases / antagonists & inhibitors*
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Animals
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Antineoplastic Agents / pharmacology*
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Enzyme Inhibitors / pharmacology*
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Enzyme Inhibitors / therapeutic use
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Humans
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Hydroxamic Acids / pharmacology
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Isoquinolines / pharmacology*
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Isoquinolines / therapeutic use
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Leucine / analogs & derivatives
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Leucine / pharmacology
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Melanoma, Experimental
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Mice
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Neoplasm Invasiveness / prevention & control
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Tumor Cells, Cultured
Substances
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Antineoplastic Agents
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Enzyme Inhibitors
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Hydroxamic Acids
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Isoquinolines
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N-(2,6-diethylphenyl)homophthalimide
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N-(2,6-dimethylphenyl)homophthalimide
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Aminopeptidases
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Leucine
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ubenimex
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actinonin