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Modulating FOXO3 transcriptional activity by small, DBD-binding molecules

The result's identifiers

  • Result code in IS VaVaI

    <a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F67985823%3A_____%2F19%3A00518629" target="_blank" >RIV/67985823:_____/19:00518629 - isvavai.cz</a>

  • Alternative codes found

    RIV/00216208:11310/19:10402417

  • Result on the web

    <a href="https://elifesciences.org/articles/48876" target="_blank" >https://elifesciences.org/articles/48876</a>

  • DOI - Digital Object Identifier

    <a href="http://dx.doi.org/10.7554/eLife.48876" target="_blank" >10.7554/eLife.48876</a>

Alternative languages

  • Result language

    angličtina

  • Original language name

    Modulating FOXO3 transcriptional activity by small, DBD-binding molecules

  • Original language description

    FOXO transcription factors are critical regulators of cell homeostasis and steer cell death, differentiation and longevity in mammalian cells. By combined pharmacophore-modeling-based in silico and fluorescence polarization-based screening we identified small molecules that physically interact with the DNA-binding domain (DBD) of FOXO3 and modulate the FOXO3 transcriptional program in human cells. The mode of interaction between compounds and the FOXO3-DBD was assessed via NMR spectroscopy and docking studies. We demonstrate that compounds S9 and its oxalate salt S9OX interfere with FOXO3 target promoter binding, gene transcription and modulate the physiologic program activated by FOXO3 in cancer cells. These small molecules prove the druggability of the FOXO-DBD and provide a structural basis for modulating these important homeostasis regulators in normal and malignant cells.

  • Czech name

  • Czech description

Classification

  • Type

    J<sub>imp</sub> - Article in a specialist periodical, which is included in the Web of Science database

  • CEP classification

  • OECD FORD branch

    10608 - Biochemistry and molecular biology

Result continuities

  • Project

    <a href="/en/project/GF17-33854L" target="_blank" >GF17-33854L: Inhibition of FOXO3-DNA interaction by small molecule inhibitors</a><br>

  • Continuities

    I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Others

  • Publication year

    2019

  • Confidentiality

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

Data specific for result type

  • Name of the periodical

    eLife

  • ISSN

    2050-084X

  • e-ISSN

  • Volume of the periodical

    8

  • Issue of the periodical within the volume

    Dec 4

  • Country of publishing house

    GB - UNITED KINGDOM

  • Number of pages

    21

  • Pages from-to

    e48876

  • UT code for WoS article

    000503449700001

  • EID of the result in the Scopus database

    2-s2.0-85076876862