Effects of HIF-1 inhibition by chetomin on hypoxia-related transcription and radiosensitivity in HT 1080 human fibrosarcoma cells
Open accessAbstract
BACKGROUND: Hypoxia-inducible factor-1 (HIF-1) overexpression has been linked to tumor progression and poor prognosis. We investigated whether targeting of HIF-1 using chetomin, a disrupter of the interaction of HIF-1 with the transcriptional coactivator p300, influences the radiosensitivity of hypoxic HT 1080 human fibrosarcoma cells. METHODS: Optimal dose of chetomin was determined by EGFP-HRE gene reporter assay in stably transfected HT 1080 cells. Cells were assayed for expression of the hypoxia-inducible genes carbonic anhydrase 9 (CA9) and vascular endothelial growth factor (VEGF) by RT-PCR and for clonogenic survival after irradiation with 2, 5 or 10 Gy, under normoxic or hypoxic (0.1% O2, 12 h) conditions in the presence or absence of chetomin (150 nM, 12 h, pre-treatment of 4 h). RESULTS: Chetomin treatment significantly reduced CA9 and VEGF mRNA expression in hypoxic cells to 44.4 +/- 7.2% and 39.6 +/- 16.0%, respectively, of untreated hypoxic controls. Chetomin clearly reduced the modified oxygen enhancement ratio (OER') compared to untreated cells, from 2.02 to 1.27, from 1.86 to 1.22 and from 1.49 to 1.06 at the 50%, 37% and 10% clonogenic survival levels, respectively. CONCLUSION: HIF-1 inhibition by chetomin effectively reduces hypoxia-dependent transcription and radiosensitizes hypoxic HT 1080 human fibrosarcoma cells in vitro.
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Chetomin HIF-1 inhibition attenuates expression of HIF-1 target genes and enhances radiotherapy efficacy in human HT1080 cells.
“While local toxicity of chetomin restricted its further development, an interesting study was carried out and demonstrated that chetomin HIF-1 inhibition attenuates the expression of HIF-1 target genes and enhances the radiotherapy efficacy in human HT 1080 cells77.”
From HIF-1α pathway: role, regulation and intervention for cancer therapy (2015) · cites this paper as [77]
The Discussion reports that chetomin downregulated the HIF-1-regulated genes CA9 and VEGF and enhanced radiation response in severely hypoxic HT 1080 cells. The claim omits that the radiosensitization was demonstrated in vitro under hypoxia; the Discussion says normoxic cells’ radiosensitivity was unchanged and that in vivo effects remain to be studied. (LLM, conf=0.86)
Experimental — accuracy not yet measuredChetomin destabilizes the CH1 domain of p300, a co-activator critical for optimal transcriptional activity of both HIF-1 and HIF-2.
“The fungal metabolite chetomin destabilizes the CH1 domain of p300, a co-activator critical for optimal transcriptional activity of both HIF-1 and HIF-2 [397,398].”
From HIF inhibition: Current strategies and clinical challenges (2026) · cites this paper as [398]
The Background (page unavailable) says chetomin disrupts p300’s CH1 domain, preventing its interaction with HIF and attenuating hypoxia-inducible transcription. The paper discusses HIF-1 but does not establish that p300 is critical for optimal transcriptional activity of both HIF-1 and HIF-2; the Discussion also says this study did not test the p300 mechanism. (LLM, conf=0.88)
Experimental — accuracy not yet measuredDisruption of HIF-p300 interactions by chetomin results in marked repression of HIF-dependent transcription in vitro and in murine xenograft models.
“Disruption of HIF–p300 interactions by chetomin results in marked repression of HIF-dependent transcription in vitro and in murine xenograft models [[397], [398], [399]].”
From HIF inhibition: Current strategies and clinical challenges (2026) · cites this paper as [398]
The Results section reports marked suppression of HIF-dependent reporter activity in HT 1080 cells in vitro. The Discussion reports that Kung et al. found inhibition of hypoxia-inducible transcription in tumors in vivo and mentions xenograft tumors, but it does not establish that repression in those tumors was marked or explicitly identify them as murine. This paper's own experiments were limited to an in-vitro model. (LLM, conf=0.81)
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- Authors
- Staab, A., Loeffler, J., Said, H. M., Diehlmann, D., Katzer, A., Beyer, M., Fleischer, M., Schwab, F., Baier, K., Einsele, H., Flentje, M., & Vordermark, D.
- Affiliations
- University of Würzburg (DE)
- Corresponding author
- Staab, Adrian
- Venue
- BMC Cancer
- Published
- 2007-11-13
- Volume
- 7
- Issue
- 1
- Pages
- 213-213
- ISSN
- 1471-2407 (ISSN-L)
- PMC
- PMC2200672
- OpenAlex
- W2021401984
- Cited by
- 89
- References
- 30
- Citations by year
- 2026: 2 · 2025: 3 · 2024: 4 · 2023: 3 · 2022: 6 · 2021: 12 · 2020: 5 · 2019: 4 · 2018: 2 · 2017: 4 · 2016: 6 · 2015: 10 · 2014: 5 · 2013: 4 · 2012: 4
- FWCI
- 0.94
- Type
- journal article
- Language
- en
- Open access
- gold
- doi.org
- Licence
- Locations
- BMC Cancer (publishedVersion, cc-by)
- Europe PMC (PubMed Central) (publishedVersion, cc-by)
- PubMed Central (publishedVersion, cc-by)
- PubMed (publishedVersion)
- DOAJ (DOAJ: Directory of Open Access Journals) (submittedVersion)
- Funders
- Deutsche Forschungsgemeinschaft
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Cancer Research › Cancer, Hypoxia, and Metabolism
- Health Sciences › Medicine › Pulmonary and Respiratory Medicine › Radiation Therapy and Dosimetry
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Angiogenesis and VEGF in Cancer
- Keywords
- HIF-1 inhibition, chetomin, hypoxia, radiosensitization, P300, carbonic anhydrase IX, vascular endothelial growth factor, fibrosarcoma, HT1080 cells, oxygen enhancement ratio, clonogenic survival
- MeSH terms
- Carbonic Anhydrases, Disulfides, Fibrosarcoma, Flow Cytometry, Humans, Radiation Tolerance, RNA, Messenger, Transcription, Genetic, Cell Hypoxia, Gene Expression, Reverse Transcriptase Polymerase Chain Reaction, Indole Alkaloids, Vascular Endothelial Growth Factor A, Cell Line, Tumor, Hypoxia-Inducible Factor 1, alpha Subunit
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