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Trisubstituted Pyrazolopyrimidines as Novel Angiogenesis Inhibitors

The result's identifiers

  • Result code in IS VaVaI

    <a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61989592%3A15310%2F13%3A33148299" target="_blank" >RIV/61989592:15310/13:33148299 - isvavai.cz</a>

  • Alternative codes found

    RIV/61389030:_____/13:00395043

  • Result on the web

    <a href="http://www.plosone.org/article/info%3Adoi%2F10.1371%2Fjournal.pone.0054607" target="_blank" >http://www.plosone.org/article/info%3Adoi%2F10.1371%2Fjournal.pone.0054607</a>

  • DOI - Digital Object Identifier

    <a href="http://dx.doi.org/10.1371/journal.pone.0054607" target="_blank" >10.1371/journal.pone.0054607</a>

Alternative languages

  • Result language

    angličtina

  • Original language name

    Trisubstituted Pyrazolopyrimidines as Novel Angiogenesis Inhibitors

  • Original language description

    Current inhibitors of angiogenesis comprise either therapeutic antibodies (e.g. bevacicumab binding to VEGF-A) or small molecular inhibitors of receptor tyrosin kinases like e.g. sunitinib, which inhibits PDGFR and VEGFR. We have recently identified cyclin-dependent kinase 5 (Cdk5) as novel alternative and pharmacologically accessible target in the context of angiogenesis. In the present work we demonstrate that trisubstituted pyrazolo[4,3-d]pyrimidines constitute a novel class of compounds which potently inhibit angiogenesis. All seven tested compounds inhibited endothelial cell proliferation with IC50 values between 1 and 18 mu M. Interestingly, this seems not to be due to cytotoxicity, since none of them showed acute cytotoxic effects on endothelialcells at a concentration of 10 mu M,. The three most potent compounds (LGR1404, LGR1406 and LGR1407) also inhibited cell migration (by 27, 51 and 31%, resp.), chemotaxis (by 50, 70 and 60% in accumulative distance, resp.), and tube forma

  • Czech name

  • Czech description

Classification

  • Type

    J<sub>x</sub> - Unclassified - Peer-reviewed scientific article (Jimp, Jsc and Jost)

  • CEP classification

    ED - Physiology

  • OECD FORD branch

Result continuities

  • Project

    Result was created during the realization of more than one project. More information in the Projects tab.

  • Continuities

    P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)

Others

  • Publication year

    2013

  • Confidentiality

    S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Data specific for result type

  • Name of the periodical

    PLoS One

  • ISSN

    1932-6203

  • e-ISSN

  • Volume of the periodical

    8

  • Issue of the periodical within the volume

    1

  • Country of publishing house

    US - UNITED STATES

  • Number of pages

    12

  • Pages from-to

    "e54607"

  • UT code for WoS article

    000314707700068

  • EID of the result in the Scopus database