title: Fullerene derivatives as a new class of inhibitors of protein tyrosine phosphatases.
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.
authors.affiliation: Institute of Bioorganic Chemistry and Petrochemistry, National Academy of Sciences of Ukraine, Murmanska, 1, 02660 Kyiv-94, Ukraine.
authors.forename: Oleksandr L
authors.initials: OL
authors.lastname: Kobzar
authors.affiliation: Institute of Bioorganic Chemistry and Petrochemistry, National Academy of Sciences of Ukraine, Murmanska, 1, 02660 Kyiv-94, Ukraine.
authors.forename: Viacheslav V
authors.initials: VV
authors.lastname: Trush
authors.affiliation: Institute of Bioorganic Chemistry and Petrochemistry, National Academy of Sciences of Ukraine, Murmanska, 1, 02660 Kyiv-94, Ukraine.
authors.forename: Vsevolod Yu
authors.initials: VY
authors.lastname: Tanchuk
authors.affiliation: Institute for Problems of Chemical Physics of Russian Academy of Sciences, Semenov Prospect, 1, Chernogolovka, Moscow Region 142432, Russia.
authors.forename: Alexander V
authors.initials: AV
authors.lastname: Zhilenkov
authors.affiliation: Institute for Problems of Chemical Physics of Russian Academy of Sciences, Semenov Prospect, 1, Chernogolovka, Moscow Region 142432, Russia.
authors.forename: Pavel A
authors.initials: PA
authors.lastname: Troshin
authors.affiliation: Institute of Bioorganic Chemistry and Petrochemistry, National Academy of Sciences of Ukraine, Murmanska, 1, 02660 Kyiv-94, Ukraine. Electronic address: vovk@bpci.kiev.ua.
authors.forename: Andriy I
authors.initials: AI
authors.lastname: Vovk
mesh_terms: D004305:Dose-Response Relationship, Drug; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D037741:Fullerenes / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D008968:Molecular Conformation; D017027:Protein Tyrosine Phosphatases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D004791:Enzyme Inhibitors; D037741:Fullerenes; D017027:Protein Tyrosine Phosphatases
keywords: Fullerene; Inhibition; Molecular docking; Protein tyrosine phosphatase