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Discovery of Selective Irreversible Inhibitors for Bruton’s Tyrosine Kinase
Abstract
A series of highly selective irreversible inhibitors for Bruton's tyrosine kinase (Btk) was developed using a structural bioinformatics approach. Their capabilities to modulate Btk's activity were characterized both in vitro and in vivo. Oral treatment with once-a-day dosing of compound 4 greatly inhibited disease development in a rodent rheumatoid arthritis (RA) model.
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Cited by
Chronic active B-cell-receptor signalling in diffuse large B-cell lymphoma
Davis, R. E., Ngo, V. N., Lenz, G., Tolar, P., Young, R. M., Romesser, P. B., Kohlhammer, H., Lamy, L., Zhao, H., Yang, Y., et al. (2010) · Nature · doi:10.1038/nature08638 · Cited by 1,643
Honigberg, L. A., Smith, A. M., Sirisawad, M., Verner, E., Loury, D., Chang, B., Li, S., Pan, Z., Thamm, D. H., Miller, R. A., et al. (2010) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.1004594107 · Cited by 1,561
Self-citationAdvances in covalent drug discovery
Boike, L., Henning, N. J., & Nomura, D. K. (2022) · Nature Reviews Drug Discovery · doi:10.1038/s41573-022-00542-z · Cited by 823
Role of Bruton’s tyrosine kinase in B cells and malignancies
Pal Singh, S., Dammeijer, F., & Hendriks, R. W. (2018) · Molecular Cancer · doi:10.1186/s12943-018-0779-z · Cited by 726
Ponader, S., Chen, S.-S., Buggy, J. J., Balakrishnan, K., Gandhi, V., Wierda, W. G., Keating, M. J., O'Brien, S., Chiorazzi, N., & Burger, J. A. (2012) · Blood · doi:10.1182/blood-2011-10-386417 · Cited by 640
Metadata
- Authors
- Pan, Z., Scheerens, H., Li, S., Schultz, B. E., Sprengeler, P. A., Burrill, L. C., Mendonca, R. V., Sweeney, M. D., Scott, K. C. K., Grothaus, P. G., Jeffery, D. A., Spoerke, J. M., Honigberg, L. A., Young, P. R., Dalrymple, S. A., & Palmer, J. T.
- Venue
- ChemMedChem
- Publisher
- Wiley
- Published
- 2006-12-27
- Volume
- 2
- Issue
- 1
- Pages
- 58-61
- ISSN
- 1860-7179 (ISSN-L)
- 1860-7187
- OpenAlex
- W2019216438
- Cited by
- 674
- References
- 0
- FWCI
- 5.13
- Type
- journal article
- Language
- en
- Open access
- closed
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- CoChat. (2026). Citation check: Discovery of Selective Irreversible Inhibitors for Bruton’s Tyrosine Kinase. https://app.cochat.ai/papers/10.1002/cmdc.200600221
- The paper
- Pan, Z., Scheerens, H., Li, S., Schultz, B. E., Sprengeler, P. A., Burrill, L. C., Mendonca, R. V., Sweeney, M. D., Scott, K. C. K., Grothaus, P. G., Jeffery, D. A., Spoerke, J. M., Honigberg, L. A., Young, P. R., Dalrymple, S. A., & Palmer, J. T. (2007). Discovery of Selective Irreversible Inhibitors for Bruton’s Tyrosine Kinase. ChemMedChem. https://doi.org/10.1002/cmdc.200600221
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Bibliographic data: Semantic Scholar, OpenAlex, Crossref.
Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.
