ArticleInternational journal of molecular sciences2017
Thiopurine Drugs Repositioned as Tyrosinase Inhibitors.
Article in International journal of molecular sciences, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.
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10 citing papers in PubMed, 19 citations in OpenAlex.
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- Study on the synthesis and biological activity of kojic acid-piperazine derivatives.RSC advances · 2026Article
- Effect of Chimpi, dried citrus peel, on aquaporin-3 expression in HaCaT human epidermal keratinocytes.Molecular biology reports · 2022Article
- Discovery of Kinase and Carbonic Anhydrase Dual Inhibitors by Machine Learning Classification and Experiments.Pharmaceuticals (Basel, Switzerland) · 2022Article
- Hydroxamic Acid as a Potent Metal-Binding Group for Inhibiting Tyrosinase.Antioxidants (Basel, Switzerland) · 2022Article
- New Inhibitors of Laccase and Tyrosinase by Examination of Cross-Inhibition between Copper-Containing Enzymes.International journal of molecular sciences · 2021Article
- Development of Pigmentation-Regulating Agents by Drug Repositioning.International journal of molecular sciences · 2021Review
- Diarylalkanoids as Potent Tyrosinase Inhibitors from the Stems ofEvidence-based complementary and alternative medicine : eCAM · 2021Article
- A medicinal chemistry perspective of drug repositioning: Recent advances and challenges in drug discovery.European journal of medicinal chemistry · 2020Review
- The Binding Affinity of Small Molecules with Yam Tyrosinase (Catechol Oxidase): A Biophysical Study.Biochemistry research international · 2019Article
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3 authors at 1 institution in 1 country.
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No grant is acknowledged in the PubMed record.
Abstract
Drug repositioning is the application of the existing drugs to new uses and has the potential to reduce the time and cost required for the typical drug discovery process. In this study, we repositioned thiopurine drugs used for the treatment of acute leukaemia as new tyrosinase inhibitors. Tyrosinase catalyses two successive oxidations in melanin biosynthesis: the conversions of tyrosine to dihydroxyphenylalanine (DOPA) and DOPA to dopaquinone. Continuous efforts are underway to discover small molecule inhibitors of tyrosinase for therapeutic and cosmetic purposes. Structure-based virtual screening predicted inhibitor candidates from the US Food and Drug Administration (FDA)-approved drugs. Enzyme assays confirmed the thiopurine leukaemia drug, thioguanine, as a tyrosinase inhibitor with the inhibitory constant of 52 μM. Two other thiopurine drugs, mercaptopurine and azathioprine, were also evaluated for their tyrosinase inhibition; mercaptopurine caused stronger inhibition than thioguanine did, whereas azathioprine was a poor inhibitor. The inhibitory constant of mercaptopurine (16 μM) was comparable to that of the well-known inhibitor kojic acid (13 μM). The cell-based assay using B16F10 melanoma cells confirmed that the compounds inhibit mammalian tyrosinase. Particularly, 50 μM thioguanine reduced the melanin content by 57%, without apparent cytotoxicity. Cheminformatics showed that the thiopurine drugs shared little chemical similarity with the known tyrosinase inhibitors.
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