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    DRUG:

    6RK73

    i
    Other names: 6RK73
    Company:
    Mission Therap
    Drug class:
    UCHL1 inhibitor
    7ms
    Deubiquitinase UCHL1 stabilizes KDM4B to augment VEGF signaling and confer bevacizumab resistance in clear cell renal cell carcinoma. (PubMed, Transl Oncol)
    Overall, this study defined an epigenetic mechanism of UCHL1/KDM4B in activating VEGF signaling. The UCHL1-KDM4B axis represents a novel target for treating ccRCC and improving the efficacy of anti-angiogenesis therapy.
    Journal
    |
    EPAS1 (Endothelial PAS domain protein 1) • KDM4B (Lysine Demethylase 4B)
    |
    Avastin (bevacizumab) • 6RK73
    over2years
    Both SUMOylation and ubiquitination of TFE3 fusion protein regulated by androgen receptor are the potential target in the therapy of Xp11.2 translocation renal cell carcinoma. (PubMed, Clin Transl Med)
    Androgen and AR function as facilitators in Xp11.2 tRCC progression and may be a novel therapeutic target for Xp11.2 tRCC. The combined use of AR antagonist MDV3100 and UCHL1 inhibitor 6RK73 increased both the SUMOylation and ubiquitination of the PRCC-TFE3 fusion protein.
    Journal
    |
    AR (Androgen receptor) • TFE3 (Transcription Factor Binding To IGHM Enhancer 3) • PRCC (Proline Rich Mitotic Checkpoint Control Factor)
    |
    PRCC-TFE3 fusion • TFE3 translocation • TFE3 fusion
    |
    Xtandi (enzalutamide) • 6RK73