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    DRUG CLASS:

    PIK3C3 inhibitor

    Related drugs:
    over2years
    Heterogeneity of Platelet Derived Growth Factor Pathway Gene Expression Profile Defines Three Distinct Subgroups of Renal Cell Carcinomas. (PubMed, Cancer Genomics Proteomics)
    Three ccRCC subgroups were defined: 1) PIK3C3 (VSP34)/SLC9A3 which may be proper for anti PIK3C3 inhibitors; 2) VEGF subgroup where association of anti VEGF may be a benefit and 3) JAK2/STAT1 subgroup, potentially being eligible for anti JAK/STAT therapy associated with IKK inhibitors.
    Journal • Gene Expression Profile
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    JAK2 (Janus kinase 2) • STAT3 (Signal Transducer And Activator Of Transcription 3) • STAT1 (Signal Transducer And Activator Of Transcription 1) • PIK3C3 (Phosphatidylinositol 3-Kinase Catalytic Subunit Type 3)
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    STAT3 expression
    over2years
    Clinical considerations for the design of PROTACs in cancer. (PubMed, Mol Cancer)
    MDM2 ligase coupled with inhibitors of the targets BCL2, BRD4, CDK9, PLK1 and MCL1 in stomach tumor, and MDM2 with PIK3C3 inhibitors in breast cancer, seems to be the best therapeutic strategy. Our results suggest potential options for the design of PROTACS in specific medical indications.
    Review • Journal • IO biomarker
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    BCL2 (B-cell CLL/lymphoma 2) • MDM2 (E3 ubiquitin protein ligase) • CDK4 (Cyclin-dependent kinase 4) • PTPN11 (Protein Tyrosine Phosphatase Non-Receptor Type 11) • CRBN (Cereblon) • AURKA (Aurora kinase A) • PLK1 (Polo Like Kinase 1) • BRD4 (Bromodomain Containing 4) • CDK9 (Cyclin Dependent Kinase 9) • XIAP (X-Linked Inhibitor Of Apoptosis) • PIK3C3 (Phosphatidylinositol 3-Kinase Catalytic Subunit Type 3) • PTK2 (Protein Tyrosine Kinase 2)
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    MCL1 expression
    3years
    The Role of Phosphatidylinositol 3-Kinase Catalytic Subunit Type 3 in the Pathogenesis of Human Cancer. (PubMed, Int J Mol Sci)
    The implications in cancer biology, patient prognosis prediction, and cancer therapy are discussed. Altogether, the discovery of pharmacological inhibitors of PIK3C3 could reveal novel strategies for improving treatment outcomes for PIK3C3-mediated human diseases.
    Review • Journal
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    PIK3C3 (Phosphatidylinositol 3-Kinase Catalytic Subunit Type 3)
    3years
    Combining an Autophagy Inhibitor, MPT0L145, with Abemaciclib Is a New Therapeutic Strategy in GBM Treatment. (PubMed, Cancers (Basel))
    Combined MPT0L145 with abemaciclib significantly reduced cell proliferation, suppressed RB phosphorylation, and increased ROS production. In conclusion, the data suggested that blocking autophagy by MPT0L145 synergistically sensitized GBM cancer cells to abemaciclib and represents a potential therapeutic strategy for treating GBM in the future.
    Journal
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    HER-2 (Human epidermal growth factor receptor 2)
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    HR positive • HER-2 negative
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    Verzenio (abemaciclib) • MPT0L145