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    BIOMARKER:

    TP53 273H

    i
    Other names: TP53, Tumor Protein P53, Cellular Tumor Antigen P53, Phosphoprotein P53, Tumor Protein P53, Antigen NY-CO-13, Transformation-Related Protein 53, Mutant Tumor Protein 53, P53 Tumor Suppressor, Tumor Suppressor P53, Tumor Protein 53, BMFS5, TRP53, BCC7, LFS1
    Entrez ID:
    7157
    Related biomarkers:
    Expression
    Mutation
    CNA
    Fusion
    Others
    2years
    Kras Co-mutations lead to resistance to mutant TP53 targeted therapy in mouse models of spontaneous non-small cell lung cancer (AACR 2022)
    Recently, the FDA granted breakthrough therapy designation to the PRIMA-1 methylated analog, APR-246 in combination with azacytidine for the treatment of patients with myelodysplastic syndromes and a TP53 mutation. PRIMA 1 therapy results in antitumor activity against P53 mutant lung tumors. However, the presence of K-ras co-mutation is a significant resistance factor. Combination of APR-246 and K-ras inhibitor therapy would be needed to overcome this resistance.
    Preclinical
    |
    KRAS (KRAS proto-oncogene GTPase) • TP53 (Tumor protein P53)
    |
    TP53 mutation • KRAS mutation • KRAS G12D • KRAS G12V • KRAS G12 • TP53 expression • KRAS Q61L • TP53 273H
    |
    azacitidine • eprenetapopt (APR-246)
    2years
    MicroRNA expression in murine spontaneous non-small cell lung cancer and human cell lines post-treatment of PRIMA-1 (AACR 2022)
    PRIMA-1 methylated analog, PRIMA-1Met (APR-246, Eprenetapopt) have been used in clinical trials to target cancers containing mutant TP53...This difference is due to model specific expression. Further investigation is needed to better understand the effects of PRIMA-1 in regulation of micro-RNA expression in the treatment of lung cancers containing mutant p53.
    Preclinical
    |
    TP53 (Tumor protein P53) • MIR200C (MicroRNA 200c) • MIR181C (MicroRNA 181c) • MIR183 (MicroRNA 183)
    |
    TP53 mutation • TP53 expression • TP53 R248Q • TP53 273H • TP53 R273H
    |
    eprenetapopt (APR-246)
    3years
    [VIRTUAL] Targeting mutant p53 protein in spontaneous non-small cell lung cancers in transgenic mice (AACR 2021)
    The results of the study indicated a significant reduction in tumor size in the mice treated with PRIMA-1, based on micro-CT images. Contrary to this finding, an increased average fold change was seen in the control group, indicating an overall average increase in tumor volume. The results indicate the activity of PRIMA-1 in lung tumor-bearing P53 mutant transgenics and suggest the potential feasibility of using PRIMA-1 (APR-246) to treat lung cancer.
    Preclinical
    |
    TP53 (Tumor protein P53)
    |
    TP53 mutation • TP53 273H
    |
    eprenetapopt (APR-246)