The DOI matches its Crossref record; 56 of the 56 references it cites were found in a registry or an index.
Antitumor Activity of a Small-Molecule Inhibitor of Human Silent Information Regulator 2 Enzymes
Abstract
SIRT1 and other NAD-dependent deacetylases have been implicated in control of cellular responses to stress and in tumorigenesis through deacetylation of important regulatory proteins, including p53 and the BCL6 oncoprotein. Hereby, we describe the identification of a compound we named cambinol that inhibits NAD-dependent deacetylase activity of human SIRT1 and SIRT2. Consistent with the role of SIRT1 in promoting cell survival during stress, inhibition of SIRT1 activity with cambinol during genotoxic stress leads to hyperacetylation of key stress response proteins and promotes cell cycle arrest. Treatment of BCL6-expressing Burkitt lymphoma cells with cambinol as a single agent induced apoptosis, which was accompanied by hyperacetylation of BCL6 and p53. Because acetylation inactivates BCL6 and has the opposite effect on the function of p53 and other checkpoint pathways, the antitumor activity of cambinol in Burkitt lymphoma cells may be accomplished through a combined effect of BCL6 inactivation and checkpoint activation. Cambinol was well tolerated in mice and inhibited growth of Burkitt lymphoma xenografts. Inhibitors of NAD-dependent deacetylases may constitute novel anticancer agents. (Cancer Res 2006; 66(8): 4368-77)
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Cites
Transcriptional silencing and longevity protein Sir2 is an NAD-dependent histone deacetylase
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Stress-dependent regulation of FOXO transcription factors by the SIRT1 deacetylase
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InfluentialNegative Control of p53 by Sir2α Promotes Cell Survival under Stress
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Cited by
Mammalian Sirtuins: Biological Insights and Disease Relevance
Haigis, M. C., & Sinclair, D. A. (2010) · Annual Review of Pathology: Mechanisms of Disease · doi:10.1146/annurev.pathol.4.110807.092250 · Cited by 2,085
Cellular Senescence: Aging, Cancer, and Injury
Calcinotto, A., Kohli, J., Zagato, E., Pellegrini, L., Demaria, M., & Alimonti, A. (2019) · Physiological Reviews · doi:10.1152/physrev.00020.2018 · Cited by 1,270
Cancer epigenetics reaches mainstream oncology
Rodríguez-Paredes, M., & Esteller, M. (2011) · Nature Medicine · doi:10.1038/nm.2305 · Cited by 1,205
Stressing the role of FoxO proteins in lifespan and disease
van der Horst, A., & Burgering, B. M. T. (2007) · Nature Reviews Molecular Cell Biology · doi:10.1038/nrm2190 · Cited by 759
SIRT2 Maintains Genome Integrity and Suppresses Tumorigenesis through Regulating APC/C Activity
Kim, H.-S., Vassilopoulos, A., Wang, R.-H., Lahusen, T., Xiao, Z., Xu, X., Li, C., Veenstra, T. D., Li, B., Yu, H., et al. (2011) · Cancer Cell · doi:10.1016/j.ccr.2011.09.004 · Cited by 537
Metadata
- Authors
- Heltweg, B., Gatbonton, T., Schuler, A. D., Posakony, J., Li, H., Goehle, S., Kollipara, R., DePinho, R. A., Gu, Y., Simon, J. A., & Bedalov, A.
- Venue
- Cancer Research
- Published
- 2006-04-15
- Volume
- 66
- Issue
- 8
- Pages
- 4368-4377
- ISSN
- 0008-5472 (ISSN-L)
- 1538-7445
- OpenAlex
- W2101690600
- Cited by
- 469
- References
- 56
- FWCI
- 13.81
- Type
- journal article
- Language
- en
- Open access
- closed
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- Heltweg, B., Gatbonton, T., Schuler, A. D., Posakony, J., Li, H., Goehle, S., Kollipara, R., DePinho, R. A., Gu, Y., Simon, J. A., & Bedalov, A. (2006). Antitumor Activity of a Small-Molecule Inhibitor of Human Silent Information Regulator 2 Enzymes. Cancer Research. https://doi.org/10.1158/0008-5472.can-05-3617
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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
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