The DOI matches its Crossref record; 5 of the 5 references it cites were found in a registry or an index.
Targeting RNA Polymerase I with an Oral Small Molecule CX-5461 Inhibits Ribosomal RNA Synthesis and Solid Tumor Growth
Abstract
Deregulated ribosomal RNA synthesis is associated with uncontrolled cancer cell proliferation. RNA polymerase (Pol) I, the multiprotein complex that synthesizes rRNA, is activated widely in cancer. Thus, selective inhibitors of Pol I may offer a general therapeutic strategy to block cancer cell proliferation. Coupling medicinal chemistry efforts to tandem cell- and molecular-based screening led to the design of CX-5461, a potent small-molecule inhibitor of rRNA synthesis in cancer cells. CX-5461 selectively inhibits Pol I–driven transcription relative to Pol II–driven transcription, DNA replication, and protein translation. Molecular studies demonstrate that CX-5461 inhibits the initiation stage of rRNA synthesis and induces both senescence and autophagy, but not apoptosis, through a p53-independent process in solid tumor cell lines. CX-5461 is orally bioavailable and demonstrates in vivo antitumor activity against human solid tumors in murine xenograft models. Our findings position CX-5461 for investigational clinical trials as a potent, selective, and orally administered agent for cancer treatment. Cancer Res; 71(4); 1418–30. ©2010 AACR.
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LC3, a mammalian homologue of yeast Apg8p, is localized in autophagosome membranes after processing.
Kabeya, Y., Mizushima, N., Ueno, T., Yamamoto, A., Kirisako, T., Noda, T., Kominami, E., Ohsumi, Y., & Yoshimori, T. (2000) · The EMBO Journal · doi:10.1093/emboj/19.21.5720 · Cited by 6,605
Creation of human tumour cells with defined genetic elements
Hahn, W. C., Counter, C. M., Lundberg, A. S., Beijersbergen, R. L., Brooks, M. W., & Weinberg, R. A. (1999) · Nature · doi:10.1038/22780 · Cited by 2,345
Autophagy mediates the mitotic senescence transition
Young, A. R. J., Narita, M., Ferreira, M., Kirschner, K., Sadaie, M., Darot, J. F. J., Tavaré, S., Arakawa, S., Shimizu, S., Watt, F. M., et al. (2009) · Genes & Development · doi:10.1101/gad.519709 · Cited by 1,078
Life on a planet of its own: Regulation of RNA polymerase I transcription in the nucleolus
Grummt, I. (2003) · Genes & Development · doi:10.1101/gad.1098503r · Cited by 540
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
Cited by
Targeting the translation machinery in cancer
Bhat, M., Robichaud, N., Hulea, L., Sonenberg, N., Pelletier, J., & Topisirovic, I. (2015) · Nature Reviews Drug Discovery · doi:10.1038/nrd4505 · Cited by 799
Ribosomal proteins: functions beyond the ribosome
Zhou, X., Liao, W.-J., Liao, J.-M., Liao, P., & Lu, H. (2015) · Journal of Molecular Cell Biology · doi:10.1093/jmcb/mjv014 · Cited by 743
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
New frontiers in translational control of the cancer genome
Truitt, M. L., & Ruggero, D. (2016) · Nature Reviews Cancer · doi:10.1038/nrc.2016.27 · Cited by 378
Translational Control in Cancer Etiology
Ruggero, D. (2013) · Cold Spring Harbor Perspectives in Biology · doi:10.1101/cshperspect.a012336 · Cited by 367
Metadata
- Authors
- Drygin, D., Lin, A., Bliesath, J., Ho, C. B., O'Brien, S. E., Proffitt, C., Omori, M., Haddach, M., Schwaebe, M. K., Siddiqui-Jain, A., Streiner, N., Quin, J. E., Sanij, E., Bywater, M. J., Hannan, R. D., Ryckman, D., Anderes, K., & Rice, W. G.
- Venue
- Cancer Research
- Published
- 2011-02-14
- Volume
- 71
- Issue
- 4
- Pages
- 1418-1430
- ISSN
- 0008-5472 (ISSN-L)
- 1538-7445
- OpenAlex
- W2100893053
- Cited by
- 618
- References
- 5
- FWCI
- 5.79
- Type
- journal article
- Language
- en
- Open access
- closed
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- Drygin, D., Lin, A., Bliesath, J., Ho, C. B., O'Brien, S. E., Proffitt, C., Omori, M., Haddach, M., Schwaebe, M. K., Siddiqui-Jain, A., Streiner, N., Quin, J. E., Sanij, E., Bywater, M. J., Hannan, R. D., Ryckman, D., Anderes, K., & Rice, W. G. (2011). Targeting RNA Polymerase I with an Oral Small Molecule CX-5461 Inhibits Ribosomal RNA Synthesis and Solid Tumor Growth. Cancer Research. https://doi.org/10.1158/0008-5472.can-10-1728
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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.
