ArticleCancer science2021
Targeting the mutant PIK3CA gene by DNA-alkylating pyrrole-imidazole polyamide in cervical cancer.
Article in Cancer science, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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Who cites it
13 citing papers in PubMed, 26 citations in OpenAlex.
- Novel therapeutic strategy targeting STMN1 using chlorambucil-conjugated pyrrole-imidazole polyamide in small cell lung cancer.International journal of cancer · 2026Article
- PIK3CA Polymorphisms in Cervical Cancer: Differential Impact of rs6443624 and rs141178472.Asian Pacific journal of cancer prevention : APJCP · 2026Article
- Targeting Wnt/β-Catenin Pathway by DNA Alkylating Pyrrole-Imidazole Polyamide in Colon Cancer.Cancer science · 2026Article
- DNA hypomethylation modification promotes BST2 expression in cervical cancer by facilitating STAT1 binding to the promoter of BST2.Infectious agents and cancer · 2025Article
- Article
- Circular RNA circ0001955 promotes cervical cancer tumorigenesis and metastasis via the miR-188-3p/NCAPG2 axis.Journal of translational medicine · 2023Article
- Therapeutic potential of pyrrole and pyrrolidine analogs: an update.Molecular diversity · 2022Review
- Suppression of non-small-cell lung cancer A549 tumor growth by an mtDNA mutation-targeting pyrrole-imidazole polyamide-triphenylphosphonium and a senolytic drug.Cancer science · 2022Article
- RNA polymerase II trapped on a molecular treadmill: Structural basis of persistent transcriptional arrest by a minor groove DNA binder.Proceedings of the National Academy of Sciences of the United States of America · 2022Article
- The role of PI3K/AKT signaling pathway in gallbladder carcinoma.American journal of translational research · 2022Review
- Mitochondria: Endosymbiont bacteria DNA sequence as a target against cancer.Cancer science · 2021Review
- Effects of miR-202-5p silencing PIK3CA gene expression on proliferation, invasion, and epithelial-mesenchymal transition of cervical cancer SiHa cells through inhibiting PI3K/Akt/mTOR signaling pathway activation.Molecular and cellular biochemistry · 2021Article
- Targeting the mutant PIK3CA gene by DNA-alkylating pyrrole-imidazole polyamide in cervical cancer.Cancer science · 2021Article
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Authors and funding
10 authors at 2 institutions in 1 country.
Funding
Abstract
PIK3CA is the most frequently mutated oncogene in cervical cancer, and somatic mutations in the PIK3CA gene result in increased activity of PI3K. In cervical cancer, the E545K mutation in PIK3CA leads to elevated cell proliferation and reduced apoptosis. In the present study, we designed and synthesized a novel pyrrole-imidazole polyamide-seco-CBI conjugate, P3AE5K, to target the PIK3CA gene bearing the E545K mutation, rendered possible by nuclear access and the unique sequence specificity of pyrrole-imidazole polyamides. P3AE5K interacted with double-stranded DNA of the coding region containing the E545K mutation. When compared with conventional PI3K inhibitors, P3AE5K demonstrated strong cytotoxicity in E545K-positive cervical cancer cells at lower concentrations. PIK3CA mutant cells exposed to P3AE5K exhibited reduced expression levels of PIK3CA mRNA and protein, and subsequent apoptotic cell death. Moreover, P3AE5K significantly decreased the tumor growth in mouse xenograft models derived from PIK3CA mutant cells. Overall, the present data strongly suggest that the alkylating pyrrole-imidazole polyamide P3AE5K should be a promising new drug candidate targeting a constitutively activating mutation of PIK3CA in cervical cancer.
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