ArticleCancer research2017
Modulation of Bax and mTOR for Cancer Therapeutics.
Article in Cancer research, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
17 citing papers in PubMed, 33 citations in OpenAlex.
- Article
- Lapatinib Promotes Apoptosis in Hepatoma Cells by Regulating SPP1 Expression.Anti-cancer agents in medicinal chemistry · 2026Article
- Phytochemical Characterization and Anticancer Activity ofInternational journal of molecular sciences · 2025Article
- Directly targeting BAX for drug discovery: Therapeutic opportunities and challenges.Acta pharmaceutica Sinica. B · 2024Review
- Targeting regulated cell death pathways in cancers for effective treatment: a comprehensive review.Frontiers in cell and developmental biology · 2024Review
- Advances in the Application of Apoptotic Proteins and Alternative Splicing in Tumor Therapy: A Narrative Review.Iranian journal of public health · 2023Review
- Mcl-1 levels critically impact the sensitivities of human colorectal cancer cells to APG-1252-M1, a novel Bcl-2/Bcl-XNeoplasia (New York, N.Y.) · 2022Article
- Review
- Adapted to Survive: Targeting Cancer Cells with BH3 Mimetics.Cancer discovery · 2022Review
- Physiological and pharmacological modulation of BAX.Trends in pharmacological sciences · 2022Review
- Non-phosphorylatable mutants of Ser184 lead to incomplete activation of Bax.Frontiers in oncology · 2022Article
- LncRNA XIST acts as a MicroRNA-520 sponge to regulate the Cisplatin resistance in NSCLC cells by mediating BAX through CeRNA network.International journal of medical sciences · 2021Article
- Discovery of Small Molecule Bak Activator for Lung Cancer Therapy.Theranostics · 2021Article
- Targeting apoptosis in cancer therapy.Nature reviews. Clinical oncology · 2020Review
- miRNA Modulation and Antitumor Activity by the Extra-Virgin Olive Oil Polyphenol Oleacein in Human Melanoma Cells.Frontiers in pharmacology · 2020Article
- Shisa3 brakes resistance to EGFR-TKIs in lung adenocarcinoma by suppressing cancer stem cell properties.Journal of experimental & clinical cancer research : CR · 2019Article
- Small Molecule KRAS Agonist for Mutant KRAS Cancer Therapy.Molecular cancer · 2019Article
Corrections and comments
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Authors and funding
23 authors at 3 institutions in 1 country.
Funding
Abstract
A rationale exists for pharmacologic manipulation of the serine (S)184 phosphorylation site of the proapoptotic Bcl2 family member Bax as an anticancer strategy. Here, we report the refinement of the Bax agonist SMBA1 to generate CYD-2-11, which has characteristics of a suitable clinical lead compound. CYD-2-11 targeted the structural pocket proximal to S184 in the C-terminal region of Bax, directly activating its proapoptotic activity by inducing a conformational change enabling formation of Bax homooligomers in mitochondrial membranes. In murine models of small-cell and non-small cell lung cancers, including patient-derived xenograft and the genetically engineered mutant KRAS-driven lung cancer models, CYD-2-11 suppressed malignant growth without evident significant toxicity to normal tissues. In lung cancer patients treated with mTOR inhibitor RAD001, we observed enhanced S184 Bax phosphorylation in lung cancer cells and tissues that inactivates the propaoptotic function of Bax, contributing to rapalog resistance. Combined treatment of CYD-2-11 and RAD001 in murine lung cancer models displayed strong synergistic activity and overcame rapalog resistance
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.