The DOI matches its Crossref record; 2 of the 2 references it cites were found in a registry or an index.
HATs off
Open accessAbstract
Histone acetyltransferases (HATs) play important roles in the regulation of gene expression. In this report, we describe the design, synthesis, and application of peptide CoA conjugates as selective HAT inhibitors for the transcriptional coactivators p300 and PCAF. Two inhibitors (Lys-CoA for p300 and H3-CoA-20 for PCAF) were found to be potent (IC(50) approximately = 0.5 microM) and selective (approximately 200-fold) in blocking p300 and PCAF HAT activities. These inhibitors were used to probe enzymatic and transcriptional features of HAT function in several assay systems. These compounds should be broadly useful as biological tools for evaluating the roles of HATs in transcriptional studies and may serve as lead agents for the development of novel antineoplastic therapeutics.
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Cites
A Mammalian Histone Deacetylase Related to the Yeast Transcriptional Regulator Rpd3p
Taunton, J., Hassig, C. A., & Schreiber, S. L. (1996) · Science · doi:10.1126/science.272.5260.408 · Cited by 1,829
Histone acetylation and transcriptional regulatory mechanisms
Struhl, K. (1998) · Genes & Development · doi:10.1101/gad.12.5.599 · Cited by 1,815
Cited by
Epigenetic protein families: a new frontier for drug discovery
Arrowsmith, C. H., Bountra, C., Fish, P. V., Lee, K., & Schapira, M. (2012) · Nature Reviews Drug Discovery · doi:10.1038/nrd3674 · Cited by 1,327
Targeting epigenetic regulators for cancer therapy: mechanisms and advances in clinical trials
Cheng, Y., He, C., Wang, M., Ma, X., Mo, F., Yang, S., Han, J., & Wei, X. (2019) · Signal Transduction and Targeted Therapy · doi:10.1038/s41392-019-0095-0 · Cited by 1,097
CREB-binding Protein and p300 in Transcriptional Regulation
Vo, N., & Goodman, R. H. (2001) · Journal of Biological Chemistry · doi:10.1074/jbc.r000025200 · Cited by 866
Discovery of a selective catalytic p300/CBP inhibitor that targets lineage-specific tumours
Lasko, L. M., Jakob, C. G., Edalji, R. P., Qiu, W., Montgomery, D., Digiammarino, E. L., Hansen, T. M., Risi, R. M., Frey, R., Manaves, V., et al. (2017) · Nature · doi:10.1038/nature24028 · Cited by 858
Self-citationBalasubramanyam, K., Varier, R. A., Altaf, M., Swaminathan, V., Siddappa, N. B., Ranga, U., & Kundu, T. K. (2004) · Journal of Biological Chemistry · doi:10.1074/jbc.m409024200 · Cited by 832
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Metadata
- Authors
- Lau, O. D., Kundu, T. K., Soccio, R. E., Ait-Si-Ali, S., Khalil, E. M., Vassilev, A., Wolffe, A. P., Nakatani, Y., Roeder, R. G., & Cole, P. A.
- Venue
- Molecular Cell
- Publisher
- Elsevier BV
- Published
- 2000-03
- Volume
- 5
- Issue
- 3
- Pages
- 589-595
- ISSN
- 1097-2765 (ISSN-L)
- OpenAlex
- W56939234
- Cited by
- 394
- References
- 2
- FWCI
- 5.75
- Type
- journal article
- Language
- en
- Open access
- hybrid
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- Lau, O. D., Kundu, T. K., Soccio, R. E., Ait-Si-Ali, S., Khalil, E. M., Vassilev, A., Wolffe, A. P., Nakatani, Y., Roeder, R. G., & Cole, P. A. (2000). HATs off. Molecular Cell. https://doi.org/10.1016/s1097-2765(00)80452-9
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