Glycine hydroxamate inhibits tyrosinase activity and melanin contents through downregulating cAMP/PKA signaling pathways.

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.
AuthorsYin-Shiou Lin, Wen-Chung Wu, Shyr-Yi Lin, Wen-Chi Hou
JournalAmino acids (Amino Acids) Vol. 47 Issue 3 Pg. 617-25 (Mar 2015) ISSN: 1438-2199 [Electronic] Austria
PMID25501504 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • Enzyme Inhibitors
  • Hydroxamic Acids
  • MITF protein, human
  • Melanins
  • Microphthalmia-Associated Transcription Factor
  • alpha-MSH
  • Cyclic AMP
  • Monophenol Monooxygenase
  • Cyclic AMP-Dependent Protein Kinases
  • PRSS1 protein, human
  • Trypsin
  • Intramolecular Oxidoreductases
  • dopachrome isomerase
  • Glycine
  • Cell Line, Tumor
  • Cyclic AMP (metabolism)
  • Cyclic AMP-Dependent Protein Kinases (metabolism)
  • Enzyme Inhibitors (pharmacology)
  • Glycine (pharmacology)
  • Humans
  • Hydroxamic Acids (pharmacology)
  • Intramolecular Oxidoreductases (metabolism)
  • Melanins (biosynthesis)
  • Microphthalmia-Associated Transcription Factor (metabolism)
  • Monophenol Monooxygenase (antagonists & inhibitors, metabolism)
  • Second Messenger Systems (drug effects)
  • Trypsin (metabolism)
  • alpha-MSH (pharmacology)

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