Abstract
Among the eight amino acid hydroxamates tested, Glycine hydroxamate (GH) was the best inhibitor of mushroom tyrosinase (TYR). With L-tyrosine as substrate, the GH inhibition of the monophenolase activity of the mushroom TYR was noncompetitive. GH decreased not only TYR protein expression, but also melanin content, tyrosinase-related protein (TRP)-1, TRP-2, and microphthalmia-associated transcription factor (MITF) expression in B16F10 melanoma cells while in the presence of α-melanocyte-stimulating hormone (α-MSH). GH also significantly decreased the isobutylmethylxanthine (IBMX)-induced increase in melanin content, which was not prevented by the ERK inhibitor PD98059. These results suggest GH has the potential for use in cosmetic hypopigmentation.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Cell Line, Tumor
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Cyclic AMP / metabolism*
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Cyclic AMP-Dependent Protein Kinases / metabolism*
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Enzyme Inhibitors / pharmacology*
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Glycine / pharmacology
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Humans
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Hydroxamic Acids / pharmacology
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Intramolecular Oxidoreductases / metabolism
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Melanins / biosynthesis*
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Microphthalmia-Associated Transcription Factor / metabolism
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Monophenol Monooxygenase / antagonists & inhibitors*
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Monophenol Monooxygenase / metabolism
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Second Messenger Systems / drug effects*
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Trypsin / metabolism
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alpha-MSH / pharmacology
Substances
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Enzyme Inhibitors
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Hydroxamic Acids
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MITF protein, human
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Melanins
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Microphthalmia-Associated Transcription Factor
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alpha-MSH
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Cyclic AMP
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Monophenol Monooxygenase
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Cyclic AMP-Dependent Protein Kinases
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PRSS1 protein, human
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Trypsin
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Intramolecular Oxidoreductases
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dopachrome isomerase
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Glycine