The DOI matches its Crossref record; 6 of the 6 references it cites were found in a registry or an index.
A Targeting Modality for Destruction of RNA Polymerase I that Possesses Anticancer Activity
Open accessAbstract
SUMMARY We define here the activity and mechanisms of action of a small molecule lead compound for cancer targeting. We show that the compound, BMH-21, has wide and potent antitumorigenic activity across NCI60 cancer cell lines and represses tumor growth in vivo. BMH-21 binds GC-rich sequences, which is present at high frequency in ribosomal DNA genes, and potently and rapidly represses RNA polymerase I (Pol I) transcription. Strikingly, we find that BMH-21 causes proteasome-dependent destruction of RPA194, the large catalytic subunit protein of Pol I holocomplex, and this correlates with cancer cell killing. Our results show that Pol I activity is under proteasome-mediated control, which reveals an unexpected therapeutic opportunity.
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Trott, O., & Olson, A. J. (2010) · Journal of Computational Chemistry · doi:10.1002/jcc.21334 · Cited by 38,412
Vogelstein, B., Papadopoulos, N., Velculescu, V. E., Zhou, S., Diaz, L. A., & Kinzler, K. W. (2013) · Science · doi:10.1126/science.1235122 · Cited by 7,863
Boulon, S., Westman, B. J., Hutten, S., Boisvert, F.-M., & Lamond, A. I. (2010) · Molecular Cell · doi:10.1016/j.molcel.2010.09.024 · Cited by 1,103
Pederson, T. (2011) · Cold Spring Harbor Perspectives in Biology · doi:10.1101/cshperspect.a000638 · Cited by 455
Repression of RNA Polymerase I Transcription by the Tumor Suppressor p53
Zhai, W., & Comai, L. (2000) · Molecular and Cellular Biology · doi:10.1128/mcb.20.16.5930-5938.2000 · Cited by 289
p53 represses ribosomal gene transcription
Budde, A., & Grummt, I. (1999) · Oncogene · doi:10.1038/sj.onc.1202402 · Cited by 157
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CX-5461 is a DNA G-quadruplex stabilizer with selective lethality in BRCA1/2 deficient tumours
Xu, H., Di Antonio, M., McKinney, S., Mathew, V., Ho, B., O’Neil, N. J., Santos, N. D., Silvester, J., Wei, V., Garcia, J., et al. (2017) · Nature Communications · doi:10.1038/ncomms14432 · Cited by 580
The Ribosome Biogenesis—Cancer Connection
Penzo, M., Montanaro, L., Treré, D., & Derenzini, M. (2019) · Cells · doi:10.3390/cells8010055 · Cited by 242
Pharmacological reactivation of p53 as a strategy to treat cancer
Zawacka‐Pankau, J., & Selivanova, G. (2015) · Journal of Internal Medicine · doi:10.1111/joim.12336 · Cited by 82
The Role of Translation Control in Tumorigenesis and Its Therapeutic Implications
Xu, Y., & Ruggero, D. (2020) · Annual Review of Cancer Biology · doi:10.1146/annurev-cancerbio-030419-033420 · Cited by 67
Dark force rising: Reawakening and targeting of fetal-like stem cells in colorectal cancer
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Metadata
- Authors
- Peltonen, K., Colis, L., Liu, H., Trivedi, R., Moubarek, M. S., Moore, H. M., Bai, B., Rudek, M. A., Bieberich, C. J., & Laiho, M.
- Venue
- Cancer Cell
- Publisher
- Elsevier BV
- Published
- 2014-01
- Volume
- 25
- Issue
- 1
- Pages
- 77-90
- ISSN
- 1535-6108 (ISSN-L)
- OpenAlex
- W2033742799
- Cited by
- 314
- References
- 6
- FWCI
- 8.64
- Type
- journal article
- Language
- en
- Open access
- bronze
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- Peltonen, K., Colis, L., Liu, H., Trivedi, R., Moubarek, M. S., Moore, H. M., Bai, B., Rudek, M. A., Bieberich, C. J., & Laiho, M. (2014). A Targeting Modality for Destruction of RNA Polymerase I that Possesses Anticancer Activity. Cancer Cell. https://doi.org/10.1016/j.ccr.2013.12.009
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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.
