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    DRUG:

    maprotiline

    Company:
    Generic mfg.
    Drug class:
    Norepinephrine reuptake inhibitor, Noradrenaline uptake inhibitor, α2 adrenergic receptor antagonist
    Related drugs:
    25d
    O-GlcNAcylation of SPOP regulates colorectal cancer progression and ferroptosis by mediating β-catenin degradation. (PubMed, Cell Death Discov)
    Combined treatment with the SPOP-targeted drug maprotiline and a ferroptosis inducer has synergistic antitumor efficacy in CRC cells and xenografts. Our study reveals the multifaceted function of SPOP in CRC, and the activation of SPOP may be a feasible strategy to increase the sensitivity of CRC to ferroptosis inducers.
    Journal
    |
    CTNNB1 (Catenin (cadherin-associated protein), beta 1) • SPOP (Speckle Type BTB/POZ Protein) • SLC7A11 (Solute Carrier Family 7 Member 11)
    |
    maprotiline
    1year
    Network Medicine-Based Strategy Identifies Maprotiline as a Repurposable Drug by Inhibiting PD-L1 Expression via Targeting SPOP in Cancer. (PubMed, Adv Sci (Weinh))
    By applying Mnet-DRI to PD-L1, maprotiline (MAP), an antidepressant drug is repurposed, as a potential PD-L1 modifier for colorectal and lung cancers. Experimental validation revealed that MAP reduced PD-L1 expression by targeting E3 ubiquitin ligase speckle-type zinc finger structural protein (SPOP), and the combination of MAP and anti-CTLA4 in vivo significantly enhanced the antitumor effect, providing a new alternative for the clinical treatment of colorectal and lung cancer.
    Journal • PD(L)-1 Biomarker • IO biomarker
    |
    PD-L1 (Programmed death ligand 1) • SPOP (Speckle Type BTB/POZ Protein)
    |
    PD-L1 expression
    |
    maprotiline