Fullerene derivatives as a new class of inhibitors of protein tyrosine phosphatases

Oleksandr L Kobzar; Viacheslav V Trush; Vsevolod Yu Tanchuk; Alexander V Zhilenkov; Pavel A Troshin; Andriy I Vovk

doi:10.1016/j.bmcl.2014.04.110

Fullerene derivatives as a new class of inhibitors of protein tyrosine phosphatases

Bioorg Med Chem Lett. 2014 Jul 15;24(14):3175-9. doi: 10.1016/j.bmcl.2014.04.110. Epub 2014 May 5.

Authors

Oleksandr L Kobzar¹, Viacheslav V Trush¹, Vsevolod Yu Tanchuk¹, Alexander V Zhilenkov², Pavel A Troshin², Andriy I Vovk³

Affiliations

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.
³ Institute of Bioorganic Chemistry and Petrochemistry, National Academy of Sciences of Ukraine, Murmanska, 1, 02660 Kyiv-94, Ukraine. Electronic address: [email protected].

PMID: 24856066
DOI: 10.1016/j.bmcl.2014.04.110

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: Fullerene; Inhibition; Molecular docking; Protein tyrosine phosphatase.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Dose-Response Relationship, Drug
Enzyme Inhibitors / chemistry
Enzyme Inhibitors / pharmacology*
Fullerenes / chemistry
Fullerenes / pharmacology*
Humans
Molecular Conformation
Protein Tyrosine Phosphatases / antagonists & inhibitors*
Protein Tyrosine Phosphatases / metabolism
Structure-Activity Relationship

Substances

Enzyme Inhibitors
Fullerenes
Protein Tyrosine Phosphatases