Abstract
Non-peptide, small-molecular, non-competitive inhibitors of puromycin-sensitive aminopeptidase (PSA), that is, 3-(2,6-diethylphenyl)-2,4(1H,3H)-quinazolinedione (PAQ-22, 3) and its 1N-methyl analogue (MPAQ-22 4), were structurally modified to afford fluorescent bioprobes, ANTAQ (5) and DAMPAQ-22 (6). The cellular localization of PSA could be visualized by the use of these fluorescent bioprobes.
Publication types
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Research Support, Non-U.S. Gov't
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Validation Study
MeSH terms
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Aminopeptidases / analysis*
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Aminopeptidases / antagonists & inhibitors
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Fluorescent Dyes / chemical synthesis*
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Fluorescent Dyes / chemistry
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Humans
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Inhibitory Concentration 50
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Kinetics
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Microscopy, Fluorescence
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Puromycin / pharmacology
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Quinazolines / chemical synthesis
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Quinazolines / pharmacology
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Tumor Cells, Cultured
Substances
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Fluorescent Dyes
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Quinazolines
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Puromycin
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Aminopeptidases