The DOI matches its Crossref record; 43 of the 43 references it cites were found in a registry or an index.
Selective targeting of BD1 and BD2 of the BET proteins in cancer and immunoinflammation
Open accessAbstract
Bromodomain inhibitors revisited: Bromodomain and extraterminal domain (BET) proteins contribute to the pathogenesis of cancer and immune diseases through their effects on transcriptional regulation. BET proteins contain two nearly identical bromodomains, BD1 and BD2, structural modules that have attracted great interest as targets for drug development. First-generation drugs that inhibited both BD1 and BD2 showed promising therapeutic activity in preclinical models but proved to be less efficacious in clinical trials. Gilan et al. took a different approach and designed drugs that selectively inhibited BD1 or BD2 (see the Perspective by Filippakopoulos and Knapp). They found that BD1 and BD2 inhibitors altered gene expression in different ways and that BD2 inhibitors had greater therapeutic activity than BD1 inhibitors in preclinical models of inflammation and autoimmune disease. Science , this issue p. 387 ; see also p. 367
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Overview of the CCP 4 suite and current developments
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Selective inhibition of BET bromodomains
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Data processing and analysis with the autoPROC toolbox
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Self-citationInhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemia
Dawson, M. A., Prinjha, R. K., Dittmann, A., Giotopoulos, G., Bantscheff, M., Chan, W.-I., Robson, S. C., Chung, C.-W., Hopf, C., Savitski, M. M., et al. (2011) · Nature · doi:10.1038/nature10509 · Cited by 1,503
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Trivalent PROTACs enhance protein degradation via combined avidity and cooperativity
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Self-citationDragovich, P. S., Pillow, T. H., Blake, R. A., Sadowsky, J. D., Adaligil, E., Adhikari, P., Chen, J., Corr, N., dela Cruz-Chuh, J., Del Rosario, G., et al. (2021) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.0c01846 · Cited by 174
Dragovich, P. S., Pillow, T. H., Blake, R. A., Sadowsky, J. D., Adaligil, E., Adhikari, P., Bhakta, S., Blaquiere, N., Chen, J., dela Cruz-Chuh, J., et al. (2021) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.0c01845 · Cited by 152
Metadata
- Authors
- Gilan, O., Rioja, I., Knezevic, K., Bell, M. J., Yeung, M. M., Harker, N. R., Lam, E. Y. N., Chung, C.-W., Bamborough, P., Petretich, M., Urh, M., Atkinson, S. J., Bassil, A. K., Roberts, E. J., Vassiliadis, D., Burr, M. L., Preston, A. G. S., Wellaway, C., Werner, T., Gray, J. R., Michon, A.-M., Gobbetti, T., Kumar, V., Soden, P. E., Haynes, A., Vappiani, J., Tough, D. F., Taylor, S., Dawson, S.-J., Bantscheff, M., Lindon, M., Drewes, G., Demont, E. H., Daniels, D. L., Grandi, P., Prinjha, R. K., & Dawson, M. A.
- Venue
- Science
- Published
- 2020-04-24
- Volume
- 368
- Issue
- 6489
- Pages
- 387-394
- ISSN
- 0036-8075 (ISSN-L)
- 1095-9203
- OpenAlex
- W3011089475
- Cited by
- 422
- References
- 43
- FWCI
- 18.39
- Type
- journal article
- Language
- en
- Open access
- green
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- Gilan, O., Rioja, I., Knezevic, K., Bell, M. J., Yeung, M. M., Harker, N. R., Lam, E. Y. N., Chung, C.-W., Bamborough, P., Petretich, M., Urh, M., Atkinson, S. J., Bassil, A. K., Roberts, E. J., Vassiliadis, D., Burr, M. L., Preston, A. G. S., Wellaway, C., Werner, T., . . . Dawson, M. A. (2020). Selective targeting of BD1 and BD2 of the BET proteins in cancer and immunoinflammation. Science. https://doi.org/10.1126/science.aaz8455
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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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