The DOI matches its Crossref record; 7 of the 7 references it cites were found in a registry or an index.
CBP30, a selective CBP/p300 bromodomain inhibitor, suppresses human Th17 responses
Open accessAbstract
Significance: Epigenetic inhibitors have shown considerable promise for the treatment of malignant and inflammatory diseases. We present here the detailed characterization of a potent and highly selective inhibitor of the bromodomains of CBP (CREB binding protein)/p300. Functional preclinical data studying cells derived from patients with ankylosing spondylitis and psoriatic arthritis (two human Th17-driven diseases) show that selective inhibition of the CBP/p300 bromodomain with CBP30 strongly reduces secretion of IL-17A, without having the broader and potentially deleterious effects on cytokine production and gene transcription of the pan-BET (bromo and extraterminal domain protein family) inhibitor JQ1. CBP/p300 play a significant role in IL-17A production, and CBP/p300 inhibition is a promising therapeutic strategy in human type-17–mediated diseases such as ankylosing spondylitis and psoriatic arthritis.
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Coot : model-building tools for molecular graphics
Emsley, P., & Cowtan, K. (2004) · Acta Crystallographica Section D Biological Crystallography · doi:10.1107/s0907444904019158 · Cited by 30,571
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MolProbity : all-atom structure validation for macromolecular crystallography
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Selective inhibition of BET bromodomains
Filippakopoulos, P., Qi, J., Picaud, S., Shen, Y., Smith, W. B., Fedorov, O., Morse, E. M., Keates, T., Hickman, T. T., Felletar, I., et al. (2010) · Nature · doi:10.1038/nature09504 · Cited by 4,262
Self-citationPhenotypic and functional features of human Th17 cells
Annunziato, F., Cosmi, L., Santarlasci, V., Maggi, L., Liotta, F., Mazzinghi, B., Parente, E., Filì, L., Ferri, S., Frosali, F., et al. (2007) · The Journal of Experimental Medicine · doi:10.1084/jem.20070663 · Cited by 1,861
Suppression of inflammation by a synthetic histone mimic
Nicodeme, E., Jeffrey, K. L., Schaefer, U., Beinke, S., Dewell, S., Chung, C.-W., Chandwani, R., Marazzi, I., Wilson, P., Coste, H., et al. (2010) · Nature · doi:10.1038/nature09589 · Cited by 1,563
Cited by
Bromodomain inhibitors and cancer therapy: From structures to applications
Pérez-Salvia, M., & Esteller, M. (2017) · Epigenetics · doi:10.1080/15592294.2016.1265710 · Cited by 292
Prostaglandin‐cytokine crosstalk in chronic inflammation
Yao, C., & Narumiya, S. (2019) · British Journal of Pharmacology · doi:10.1111/bph.14530 · Cited by 283
Targeted degradation of the enhancer lysine acetyltransferases CBP and p300
Vannam, R., Sayilgan, J., Ojeda, S., Karakyriakou, B., Hu, E., Kreuzer, J., Morris, R., Herrera Lopez, X. I., Rai, S., Haas, W., et al. (2021) · Cell Chemical Biology · doi:10.1016/j.chembiol.2020.12.004 · Cited by 177
Targeting the acetylation signaling pathway in cancer therapy
Dang, F., & Wei, W. (2022) · Seminars in Cancer Biology · doi:10.1016/j.semcancer.2021.03.001 · Cited by 109
Structural insights into p300 regulation and acetylation-dependent genome organisation
Ibrahim, Z., Wang, T., Destaing, O., Salvi, N., Hoghoughi, N., Chabert, C., Rusu, A., Gao, J., Feletto, L., Reynoird, N., et al. (2022) · Nature Communications · doi:10.1038/s41467-022-35375-2 · Cited by 64
Metadata
- Authors
- Hammitzsch, A., Tallant, C., Fedorov, O., O’Mahony, A., Brennan, P. E., Hay, D. A., Martinez, F. O., Al-Mossawi, M. H., de Wit, J., Vecellio, M., Wells, C., Wordsworth, P., Müller, S., Knapp, S., & Bowness, P.
- Venue
- Proceedings of the National Academy of Sciences
- Published
- 2015-08-10
- Volume
- 112
- Issue
- 34
- Pages
- 10768-10773
- ISSN
- 0027-8424 (ISSN-L)
- 1091-6490
- OpenAlex
- W1945410182
- Cited by
- 254
- References
- 7
- FWCI
- 10.58
- Type
- journal article
- Language
- en
- Open access
- green
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- Hammitzsch, A., Tallant, C., Fedorov, O., O’Mahony, A., Brennan, P. E., Hay, D. A., Martinez, F. O., Al-Mossawi, M. H., de Wit, J., Vecellio, M., Wells, C., Wordsworth, P., Müller, S., Knapp, S., & Bowness, P. (2015). CBP30, a selective CBP/p300 bromodomain inhibitor, suppresses human Th17 responses. Proceedings of the National Academy of Sciences. https://doi.org/10.1073/pnas.1501956112
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