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Fullerene derivatives as a new class of inhibitors of protein tyrosine phosphatases
Affiliation:1. Institute of Bioorganic Chemistry and Petrochemistry, National Academy of Sciences of Ukraine, Murmanska, 1, 02660 Kyiv-94, Ukraine;2. Institute for Problems of Chemical Physics of Russian Academy of Sciences, Semenov Prospect, 1, Chernogolovka, Moscow Region 142432, Russia;1. Central Tehran Branch, Islamic Azad University, Tehran, Iran;2. Materials and Energy Research Center, Semiconductors Department, P.O. Box 31787-316, Karaj, Iran;1. Department of Physics, Hong Kong University of Science and Technology, Clear Water Bay, Kowloon, Hong Kong;2. Department of Chemistry, National Taiwan University, Taipei, Taiwan;1. Department of Biochemistry, Albert Einstein College of Medicine, Bronx, NY 10461, USA;2. Department of Microbiology and Immunology, Albert Einstein College of Medicine, Bronx, NY 10461, USA;3. Graduate School of Medicine, Graduate School of Pharmaceutical Sciences, Osaka University, Suita, Osaka 565-0871;4. Laboratories of Nuclear Transport Dynamics, Health and Nutrition, Ibaraki, Osaka 567-0085;5. Bioinformatics, Health and Nutrition, Ibaraki, Osaka 567-0085;12. National Institutes of Biomedical Innovation, Health and Nutrition, Ibaraki, Osaka 567-0085;6. Graduate School of Life Science, Hokkaido University, Sapporo, Hokkaido 001-0021, Japan
Abstract:In this study, we identified water-soluble C60 and C70 fullerene derivatives as a novel class of protein tyrosine phosphatase inhibitors. The evaluated compounds were found to inhibit CD45, PTP1B, TC-PTP, SHP2, and PTPβ with IC50 values in the low micromolar to high nanomolar range. These results demonstrate a new strategy for designing effective nanoscale protein tyrosine phosphatase inhibitors.
Keywords:Protein tyrosine phosphatase  Fullerene  Inhibition  Molecular docking
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