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  1. Article ; Online: Correction

    Jeroen Overman / Frank Fontaine / Mehdi Moustaqil / Deepak Mittal / Emma Sierecki / Natalia Sacilotto / Johannes Zuegg / Avril AB Robertson / Kelly Holmes / Angela A Salim / Sreeman Mamidyala / Mark S Butler / Ashley S Robinson / Emmanuelle Lesieur / Wayne Johnston / Kirill Alexandrov / Brian L Black / Benjamin M Hogan / Sarah De Val /
    Robert J Capon / Jason S Carroll / Timothy L Bailey / Peter Koopman / Ralf Jauch / Matthew A Cooper / Yann Gambin / Mathias Francois

    eLife, Vol

    Pharmacological targeting of the transcription factor SOX18 delays breast cancer in mice

    2023  Volume 12

    Keywords Medicine ; R ; Science ; Q ; Biology (General) ; QH301-705.5
    Language English
    Publishing date 2023-08-01T00:00:00Z
    Publisher eLife Sciences Publications Ltd
    Document type Article ; Online
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

    Full text online

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  2. Article ; Online: Pharmacological targeting of the transcription factor SOX18 delays breast cancer in mice

    Jeroen Overman / Frank Fontaine / Mehdi Moustaqil / Deepak Mittal / Emma Sierecki / Natalia Sacilotto / Johannes Zuegg / Avril AB Robertson / Kelly Holmes / Angela A Salim / Sreeman Mamidyala / Mark S Butler / Ashley S Robinson / Emmanuelle Lesieur / Wayne Johnston / Kirill Alexandrov / Brian L Black / Benjamin M Hogan / Sarah De Val /
    Robert J Capon / Jason S Carroll / Timothy L Bailey / Peter Koopman / Ralf Jauch / Mark J Smyth / Matthew A Cooper / Yann Gambin / Mathias Francois

    eLife, Vol

    2017  Volume 6

    Abstract: Pharmacological targeting of transcription factors holds great promise for the development of new therapeutics, but strategies based on blockade of DNA binding, nuclear shuttling, or individual protein partner recruitment have yielded limited success to ... ...

    Abstract Pharmacological targeting of transcription factors holds great promise for the development of new therapeutics, but strategies based on blockade of DNA binding, nuclear shuttling, or individual protein partner recruitment have yielded limited success to date. Transcription factors typically engage in complex interaction networks, likely masking the effects of specifically inhibiting single protein-protein interactions. Here, we used a combination of genomic, proteomic and biophysical methods to discover a suite of protein-protein interactions involving the SOX18 transcription factor, a known regulator of vascular development and disease. We describe a small-molecule that is able to disrupt a discrete subset of SOX18-dependent interactions. This compound selectively suppressed SOX18 transcriptional outputs in vitro and interfered with vascular development in zebrafish larvae. In a mouse pre-clinical model of breast cancer, treatment with this inhibitor significantly improved survival by reducing tumour vascular density and metastatic spread. Our studies validate an interactome-based molecular strategy to interfere with transcription factor activity, for the development of novel disease therapeutics.
    Keywords small molecules ; transcription factors ; protein protein interactions ; tumour angiogenesis ; gene expression ; Medicine ; R ; Science ; Q ; Biology (General) ; QH301-705.5
    Subject code 570
    Language English
    Publishing date 2017-01-01T00:00:00Z
    Publisher eLife Sciences Publications Ltd
    Document type Article ; Online
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

    Full text online

    More links

    Kategorien

    Inter-library loan at ZB MED

    Your chosen title can be delivered directly to ZB MED Cologne location if you are registered as a user at ZB MED Cologne.

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