The DOI matches its Crossref record; 7 of the 7 references it cites were found in a registry or an index.
A Small-Molecule Probe of the Histone Methyltransferase G9a Induces Cellular Senescence in Pancreatic Adenocarcinoma
Open accessAbstract
Post-translational modifications of histones alter chromatin structure and play key roles in gene expression and specification of cell states. Small molecules that target chromatin-modifying enzymes selectively are useful as probes and have promise as therapeutics, although very few are currently available. G9a (also named euchromatin histone methyltransferase 2 (EHMT2)) catalyzes methylation of lysine 9 on histone H3 (H3K9), a modification linked to aberrant silencing of tumor-suppressor genes, among others. Here, we report the discovery of a novel histone methyltransferase inhibitor, BRD4770. This compound reduced cellular levels of di- and trimethylated H3K9 without inducing apoptosis, induced senescence, and inhibited both anchorage-dependent and -independent proliferation in the pancreatic cancer cell line PANC-1. ATM-pathway activation, caused by either genetic or small-molecule inhibition of G9a, may mediate BRD4770-induced cell senescence. BRD4770 may be a useful tool to study G9a and its role in senescence and cancer cell biology.
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Cites
DNA double-stranded breaks induce histone H2AX phosphorylation on serine 139
Rogakou, E. P., Pilch, D. R., Orr, A. H., Ivanova, V. S., & Bonner, W. M. (1998) · Journal of Biological Chemistry · doi:10.1074/jbc.273.10.5858 · Cited by 5,438
Cellular senescence: when bad things happen to good cells
Campisi, J., & d'Adda di Fagagna, F. (2007) · Nature Reviews Molecular Cell Biology · doi:10.1038/nrm2233 · Cited by 4,441
DNA damage activates ATM through intermolecular autophosphorylation and dimer dissociation
Bakkenist, C. J., & Kastan, M. B. (2003) · Nature · doi:10.1038/nature01368 · Cited by 3,466
Human cell senescence as a DNA damage response
Zglinicki, T. V., Saretzki, G., Ladhoff, J., Fagagna, F. D. D., & Jackson, S. P. (2005) · Mechanisms of Ageing and Development · doi:10.1016/j.mad.2004.09.034 · Cited by 419
Chen, M.-W., Hua, K.-T., Kao, H.-J., Chi, C.-C., Wei, L.-H., Johansson, G., Shiah, S.-G., Chen, P.-S., Jeng, Y.-M., Cheng, T.-Y., et al. (2010) · Cancer Research · doi:10.1158/0008-5472.can-10-0833 · Cited by 369
Activation of the Cellular DNA Damage Response in the Absence of DNA Lesions
Soutoglou, E., & Misteli, T. (2008) · Science · doi:10.1126/science.1159051 · Cited by 299
Bonilla, C. Y., Melo, J. A., & Toczyski, D. P. (2008) · Molecular Cell · doi:10.1016/j.molcel.2008.03.023 · Cited by 161
Cited by
Pan, M., Reid, M. A., Lowman, X. H., Kulkarni, R. P., Tran, T. Q., Liu, X., Yang, Y., Hernandez-Davies, J. E., Rosales, K. K., Li, H., et al. (2016) · Nature Cell Biology · doi:10.1038/ncb3410 · Cited by 368
Discovery of an in Vivo Chemical Probe of the Lysine Methyltransferases G9a and GLP
Liu, F., Barsyte-Lovejoy, D., Li, F., Xiong, Y., Korboukh, V., Huang, X.-P., Allali-Hassani, A., Janzen, W. P., Roth, B. L., Frye, S. V., et al. (2013) · Journal of Medicinal Chemistry · doi:10.1021/jm401480r · Cited by 268
Small molecule compounds that induce cellular senescence.
Petrova, N. V., Velichko, A. K., Razin, S. V., & Kantidze, O. L. (2016) · Aging Cell · doi:10.1111/acel.12518 · Cited by 240
Metadata
- Authors
- Yuan, Y., Wang, Q., Paulk, J., Kubicek, S., Kemp, M. M., Adams, D. J., Shamji, A. F., Wagner, B. K., & Schreiber, S. L.
- Venue
- ACS Chemical Biology
- Publisher
- American Chemical Society (ACS)
- Published
- 2012-04-30
- Volume
- 7
- Issue
- 7
- Pages
- 1152-1157
- ISSN
- 1554-8929 (ISSN-L)
- 1554-8937
- OpenAlex
- W2036777838
- Cited by
- 181
- References
- 7
- FWCI
- 5.34
- Type
- journal article
- Language
- en
- Open access
- hybrid
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