ArticleCancer research2014
HO-3867, a safe STAT3 inhibitor, is selectively cytotoxic to ovarian cancer.
Article in Cancer research, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 54 papers, 1 of them a synthesis that pooled it.
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The trial behind it
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
54 citing papers in PubMed, 1 synthesis or guideline pooled it, 97 citations in OpenAlex.
- Pooled it
- Targeting oral cancer with curcumin and its structural analogs: molecular mechanisms, pharmacokinetic optimization, and clinical translation.Archives of pharmacal research · 2026Review
- TP53-mutated myelodysplastic syndromes and acute myeloid leukemia: a comprehensive overview of targeted approaches.Frontiers in oncology · 2026Review
- Curcumin Analogues Trigger HMOX1-Mediated Ferroptosis to Halt Endometrial Cancer Growth.bioRxiv : the preprint server for biology · 2025Article
- Novel p53 reactivators that are synergistic with olaparib for the treatment of gynecologic cancers with mutant p53.Translational oncology · 2025Article
- Synergistic effects of the curcumin analog HO-3867 and olaparib in transforming fallopian tube epithelial cells.Investigational new drugs · 2025Article
- Review
- STAT3 mediates CAF-induced osimertinib resistance via regulating protein secretion in non-small cell lung cancer.Frontiers in pharmacology · 2025Article
- Article
- pSTAT3 activation ofProceedings of the National Academy of Sciences of the United States of America · 2024Article
- TTI-101 targets STAT3/c-Myc signaling pathway to suppress cervical cancer progression: an integrated experimental and computational analysis.Cancer cell international · 2024Article
- Longevity and anti-aging effects of curcumin supplementation.GeroScience · 2024Review
- Effect and potential mechanism of oncometabolite succinate promotes distant metastasis of colorectal cancer by activating STAT3.BMC gastroenterology · 2024Article
- Review
- Eupalinolide J Inhibits Cancer Metastasis by Promoting STAT3 Ubiquitin-Dependent Degradation.Molecules (Basel, Switzerland) · 2023Article
- BRCA2 Status Alters the Effect of the P53 Reactivator HO-3867 in Ovarian Cancer Cells.Journal of cancer science and clinical therapeutics · 2023Article
- Curcumin and its Analogs and Carriers: Potential Therapeutic Strategies for Human Osteosarcoma.International journal of biological sciences · 2023Review
- Curcumin Analog, HO-3867, Induces Both Apoptosis and Ferroptosis via Multiple Mechanisms in NSCLC Cells with Wild-Type p53.Evidence-based complementary and alternative medicine : eCAM · 2023Article
- HO-3867 Induces Apoptosis via the JNK Signaling Pathway in Human Osteosarcoma Cells.Pharmaceutics · 2022Article
- Curcumin analog HO-3867 triggers apoptotic pathways through activating JNK1/2 signalling in human oral squamous cell carcinoma cells.Journal of cellular and molecular medicine · 2022Article
Corrections and comments
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Authors and funding
15 authors at 5 institutions in 2 countries.
Funding
Abstract
STAT3 is well corroborated preclinically as a cancer therapeutic target, but tractable translational strategies for its blockade by small molecule inhibitors have remained elusive. In this study, we report the development of a novel class of bifunctional STAT3 inhibitors, based on conjugation of a diarylidenyl-piperidone (DAP) backbone to an N-hydroxypyrroline (-NOH) group, which exhibits minimal toxicity against normal cells and good oral bioavailability. Molecular modeling studies of this class suggested direct interaction with the STAT3 DNA binding domain. In particular, the DAP compound HO-3867 selectively inhibited STAT3 phosphorylation, transcription, and DNA binding without affecting the expression of other active STATs. HO-3867 exhibited minimal toxicity toward noncancerous cells and tissues but induced apoptosis in ovarian cancer cells. Pharmacologic analysis revealed greater bioabsorption and bioavailability of the active (cytotoxic) metabolites in cancer cells compared with normal cells. The selective cytotoxicity of HO-3867 seemed to be multifaceted, eliciting differential activation of the Akt pathway in normal versus cancer cells. RNAi attenuation experiments confirmed the requirement of STAT3 for HO-3867-mediated apoptosis in ovarian cancer cells. In vivo testing showed that HO-3867 could block xenograft tumor growth without toxic side effects. Furthermore, in primary human ovarian cancer cells isolated from patient ascites, HO-3867 inhibited cell migration/invasion and survival. Our results offer preclinical proof-of-concept for HO-3867 as a selective STAT3 inhibitor to treat ovarian cancer and other solid tumors where STAT3 is widely upregulated.
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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.