bims-p53act Biomed News
on p53 mutations and anti-cancer therapy response
Issue of 2025–11–23
two papers selected by
Toni Martinez-Bernabe, Universitat de les Illes Balears



  1. Cancer Sci. 2025 Nov 17.
      Tumor suppressor p53 is the most frequently mutated gene in cancers. Mutations in p53 not only result in the loss of its classical tumor-suppressive functions but also confer new oncogenic properties. The protein stabilization of mutant p53 (mutp53) is a prerequisite for gain-of-function manifestation. Here, we report the novel mechanism that pyruvate dehydrogenase kinase1 (PDK1) modulates both wild-type and mutant p53, and facilitates proliferation and migration of TP53 mutant breast cancer. On the one hand, we identified PDK1 as a direct transcriptional repression target of wild-type p53, whereas transcriptional activation of PDK1 in mutp53 cells is initiated by the EGR1 axis. On the other hand, PDK1 promoted mutp53 protein accumulation by binding to mutp53 and inhibiting its degradation. Taken together, mutp53 activated a positive feedback loop by upregulating PDK1 to enhance p53 protein stability and promote the malignancy of breast cancer. Moreover, PDK1 inhibition increased the therapeutic effect of APR-246 on TP53 mutant breast cancer in xenograft tumors. Our results suggested that intervention of PDK1 could potentially emerge as a new therapeutic strategy to impede the progression of TP53 mutant breast cancer.
    Keywords:  APR‐246; breast cancer; mutant p53; pyruvate dehydrogenase kinase 1; ubiquitination
    DOI:  https://doi.org/10.1111/cas.70252
  2. Cell Death Dis. 2025 Nov 17. 16(1): 837
      Ovarian cancer (OC) is a highly aggressive malignancy in women, and platinum resistance remains a major clinical obstacle. p53 mutations are prevalent in OC and exhibit functional heterogeneity that is associated with therapeutic response and disease progression. However, the roles and mechanisms underlying the functional heterogeneity of p53 mutations in platinum-resistant OC remain elusive. This investigation delineated that p53 mutations within the Loop 2, Loop 3, and β-strand S10 regions were closely linked to platinum resistance. In particular, functional assays unveiled that p53R175H and p53R175G mutations at Arg175 revealed distinct roles in tumor cell migration and drug resistance, with p53R175G conferring resistance to agents targeting p53R175H. Through multi-omics sequencing analysis, it was discerned that p53R175H and p53R175G promoted tumor progression through distinct cofactors and regulatory networks. p53R175H mediated upregulation of extracellular matrix-related genes, whereas p53R175G activated pathways associated with cytokine receptor interaction and membrane trafficking. Notably, the chromatin remodeling protein CHD1 selectively interacted with p53R175G, but not p53R175H, and regulated the transcriptional activity of p53R175G, including target genes such as IL7R. Moreover, CHD1 knockdown or pharmacological inhibition of IL7R synergistically enhanced platinum sensitivity, suggesting promising combination therapies specifically targeting the R175G mutation. The findings revealed that p53 mutations at the same residue exhibited distinct functional properties and relied on unique cofactors, offering valuable insights for precision therapy in OC.
    DOI:  https://doi.org/10.1038/s41419-025-08172-0