Abstract
We employed a computational approach to design and synthesize a series of fluorescently labeled hPEPT1 substrates. Five Alexa Fluor-350-labeled peptides were assessed for their in vitro inhibitory activity in hPEPT1-transfected CHO cells. At least four labeled peptides show potent inhibitory activity toward hPEPT1-mediated uptake of [(3)H]-GlySar and three compounds displayed a significant cellular uptake specifically mediated by hPEPT1.
Publication types
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Research Support, N.I.H., Extramural
MeSH terms
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Animals
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CHO Cells
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Cricetinae
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Cricetulus
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Drug Design*
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Fluorescent Dyes / chemical synthesis*
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Fluorescent Dyes / chemistry
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Humans
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Models, Molecular
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Molecular Structure
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Peptide Transporter 1
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Peptides / chemistry*
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Symporters / chemistry
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Symporters / genetics
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Symporters / metabolism*
Substances
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Fluorescent Dyes
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Peptide Transporter 1
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Peptides
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SLC15A1 protein, human
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Symporters