Discovery of small-molecule inhibitors of tyrosinase

Juris P. Germanas, Shugauang Wang, Andrew Miner, Wayne Hao, Joseph M. Ready

Research output: Contribution to journalArticle

45 Citations (Scopus)

Abstract

To identify novel inhibitors of tyrosinase, a fluorescent assay was developed which is suitable for high-throughput screening. In the assay, oxidation of the substrate by tyrosinase leads to the release of a fluorescent coumarin. Several small molecules were identified that inhibited mushroom tyrosinase in vitro and human tyrosinase in cell culture. These compounds may represent lead structures for therapies targeted at disorders of hyperpigmentation.

Original languageEnglish (US)
Pages (from-to)6871-6875
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume17
Issue number24
DOIs
StatePublished - Dec 15 2007

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Monophenol Monooxygenase
Molecules
Assays
Hyperpigmentation
Agaricales
Cell culture
Screening
Cell Culture Techniques
Throughput
Oxidation
Substrates
Therapeutics

Keywords

  • Fluorescence
  • High-throughput screening
  • Pigmentation
  • Thiazoles
  • Tyrosinase inhibitors

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Biology
  • Organic Chemistry
  • Drug Discovery
  • Pharmaceutical Science

Cite this

Discovery of small-molecule inhibitors of tyrosinase. / Germanas, Juris P.; Wang, Shugauang; Miner, Andrew; Hao, Wayne; Ready, Joseph M.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 17, No. 24, 15.12.2007, p. 6871-6875.

Research output: Contribution to journalArticle

Germanas, Juris P. ; Wang, Shugauang ; Miner, Andrew ; Hao, Wayne ; Ready, Joseph M. / Discovery of small-molecule inhibitors of tyrosinase. In: Bioorganic and Medicinal Chemistry Letters. 2007 ; Vol. 17, No. 24. pp. 6871-6875.
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