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    DRUG:

    VNLG-152R

    i
    Other names: VNLG-152R
    Company:
    Isoprene Pharma
    Drug class:
    MNK1 degrader, MNK2 degrader
    1year
    VNLG-152R and its deuterated analogs potently inhibit/repress triple/quadruple negative breast cancer of diverse racial origins in vitro and in vivo by upregulating E3 Ligase Synoviolin 1 (SYVN1) and inducing proteasomal degradation of MNK1/2. (PubMed, Front Oncol)
    Importantly, in direct comparison, our compounds are more effective than enzalutamide and docetaxel in achieving tumor growth inhibition/repression in the AR+ MDA-MD-453 xenograft model in mice. Collectively, our study sheds light on the involvement of SYVN1 E3 ligase in the VNLG-152R-induced degradation of MNK1/2 and the therapeutic potential of VNLG-152R and its more potent deuterated analogs as promising agents for the treatment of TNBC across diverse patient populations.
    Preclinical • Journal
    |
    AR (Androgen receptor) • EIF4G1 (Eukaryotic translation initiation factor 4 gamma, 1)
    |
    AR expression
    |
    docetaxel • Xtandi (enzalutamide) • VNLG-152R