Fullerene derivatives as a new class of inhibitors of protein tyrosine phosphatases
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 de...
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| Veröffentlicht in: | Bioorganic & medicinal chemistry letters 2014-07, Vol.24 (14), p.3175-3179 |
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| container_end_page | 3179 |
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| container_issue | 14 |
| container_start_page | 3175 |
| container_title | Bioorganic & medicinal chemistry letters |
| container_volume | 24 |
| creator | Kobzar, Oleksandr L. Trush, Viacheslav V. Tanchuk, Vsevolod Yu Zhilenkov, Alexander V. Troshin, Pavel A. Vovk, Andriy I. |
| description | 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. |
| doi_str_mv | 10.1016/j.bmcl.2014.04.110 |
| format | Article |
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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.</description><identifier>ISSN: 0960-894X</identifier><identifier>EISSN: 1464-3405</identifier><identifier>DOI: 10.1016/j.bmcl.2014.04.110</identifier><identifier>PMID: 24856066</identifier><language>eng</language><publisher>England: Elsevier Ltd</publisher><subject>Dose-Response Relationship, Drug ; Enzyme Inhibitors - chemistry ; Enzyme Inhibitors - pharmacology ; Fullerene ; Fullerenes - chemistry ; Fullerenes - pharmacology ; Humans ; Inhibition ; Molecular Conformation ; Molecular docking ; Protein tyrosine phosphatase ; Protein Tyrosine Phosphatases - antagonists & inhibitors ; Protein Tyrosine Phosphatases - metabolism ; Structure-Activity Relationship</subject><ispartof>Bioorganic & medicinal chemistry letters, 2014-07, Vol.24 (14), p.3175-3179</ispartof><rights>2014 Elsevier Ltd</rights><rights>Copyright © 2014 Elsevier Ltd. 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These results demonstrate a new strategy for designing effective nanoscale protein tyrosine phosphatase inhibitors.</description><subject>Dose-Response Relationship, Drug</subject><subject>Enzyme Inhibitors - chemistry</subject><subject>Enzyme Inhibitors - pharmacology</subject><subject>Fullerene</subject><subject>Fullerenes - chemistry</subject><subject>Fullerenes - pharmacology</subject><subject>Humans</subject><subject>Inhibition</subject><subject>Molecular Conformation</subject><subject>Molecular docking</subject><subject>Protein tyrosine phosphatase</subject><subject>Protein Tyrosine Phosphatases - antagonists & inhibitors</subject><subject>Protein Tyrosine Phosphatases - metabolism</subject><subject>Structure-Activity Relationship</subject><issn>0960-894X</issn><issn>1464-3405</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2014</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqNkEFLwzAYhoMobk7_gAfp0UvrlzbJGvAiw6kw8KCCt5AmX1lG186km-zfm7npUYR8hA-e9yV5CLmkkFGg4maRVUvTZDlQlgHLKIUjMqRMsLRgwI_JEKSAtJTsfUDOQlhABIGxUzLIWckFCDEkL9N106DHFhOL3m107zYYEh1P0uJnYhodQtLViWvnrnJ957-3le96dG3Sb30XXAyv5l1YzXWvA4ZzclLrJuDF4R6Rt-n96-QxnT0_PE3uZqkpStmnnI-FGI81IBdoKTO5jMMrjhy4xbqiRoIpmNACBfBKVzVIo6uytmNLc1uMyPW-N77mY42hV0sXDDaNbrFbB0U5K6Qsc-D_QAshSiYLGdF8j5r4teCxVivvltpvFQW1864Waudd7bwrYCp6j6GrQ_-6WqL9jfyIjsDtHsAoZOPQq2Actgat82h6ZTv3V_8XqoGUuA</recordid><startdate>20140715</startdate><enddate>20140715</enddate><creator>Kobzar, Oleksandr L.</creator><creator>Trush, Viacheslav V.</creator><creator>Tanchuk, Vsevolod Yu</creator><creator>Zhilenkov, Alexander V.</creator><creator>Troshin, Pavel A.</creator><creator>Vovk, Andriy I.</creator><general>Elsevier Ltd</general><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7X8</scope><scope>7QO</scope><scope>8FD</scope><scope>FR3</scope><scope>P64</scope></search><sort><creationdate>20140715</creationdate><title>Fullerene derivatives as a new class of inhibitors of protein tyrosine phosphatases</title><author>Kobzar, Oleksandr L. ; Trush, Viacheslav V. ; Tanchuk, Vsevolod Yu ; Zhilenkov, Alexander V. ; Troshin, Pavel A. ; Vovk, Andriy I.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c389t-5576677a0e56ed14c294c25b5e505defb1c90c346a6e605babf09cab8fd7d12d3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2014</creationdate><topic>Dose-Response Relationship, Drug</topic><topic>Enzyme Inhibitors - chemistry</topic><topic>Enzyme Inhibitors - pharmacology</topic><topic>Fullerene</topic><topic>Fullerenes - chemistry</topic><topic>Fullerenes - pharmacology</topic><topic>Humans</topic><topic>Inhibition</topic><topic>Molecular Conformation</topic><topic>Molecular docking</topic><topic>Protein tyrosine phosphatase</topic><topic>Protein Tyrosine Phosphatases - antagonists & inhibitors</topic><topic>Protein Tyrosine Phosphatases - metabolism</topic><topic>Structure-Activity Relationship</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Kobzar, Oleksandr L.</creatorcontrib><creatorcontrib>Trush, Viacheslav V.</creatorcontrib><creatorcontrib>Tanchuk, Vsevolod Yu</creatorcontrib><creatorcontrib>Zhilenkov, Alexander V.</creatorcontrib><creatorcontrib>Troshin, Pavel A.</creatorcontrib><creatorcontrib>Vovk, Andriy I.</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><collection>Biotechnology Research Abstracts</collection><collection>Technology Research Database</collection><collection>Engineering Research Database</collection><collection>Biotechnology and BioEngineering Abstracts</collection><jtitle>Bioorganic & medicinal chemistry letters</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Kobzar, Oleksandr L.</au><au>Trush, Viacheslav V.</au><au>Tanchuk, Vsevolod Yu</au><au>Zhilenkov, Alexander V.</au><au>Troshin, Pavel A.</au><au>Vovk, Andriy I.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Fullerene derivatives as a new class of inhibitors of protein tyrosine phosphatases</atitle><jtitle>Bioorganic & medicinal chemistry letters</jtitle><addtitle>Bioorg Med Chem Lett</addtitle><date>2014-07-15</date><risdate>2014</risdate><volume>24</volume><issue>14</issue><spage>3175</spage><epage>3179</epage><pages>3175-3179</pages><issn>0960-894X</issn><eissn>1464-3405</eissn><abstract>In this study, we identified water-soluble C60 and C70 fullerene derivatives as a novel class of protein tyrosine phosphatase inhibitors. 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| fulltext | fulltext |
| identifier | ISSN: 0960-894X |
| ispartof | Bioorganic & medicinal chemistry letters, 2014-07, Vol.24 (14), p.3175-3179 |
| issn | 0960-894X 1464-3405 |
| language | eng |
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| source | MEDLINE; Access via ScienceDirect (Elsevier) |
| subjects | Dose-Response Relationship, Drug Enzyme Inhibitors - chemistry Enzyme Inhibitors - pharmacology Fullerene Fullerenes - chemistry Fullerenes - pharmacology Humans Inhibition Molecular Conformation Molecular docking Protein tyrosine phosphatase Protein Tyrosine Phosphatases - antagonists & inhibitors Protein Tyrosine Phosphatases - metabolism Structure-Activity Relationship |
| title | Fullerene derivatives as a new class of inhibitors of protein tyrosine phosphatases |
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