The DOI matches its Crossref record; 37 of the 37 references it cites were found in a registry or an index.
Dasatinib, a small-molecule protein tyrosine kinase inhibitor, inhibits T-cell activation and proliferation
Open accessAbstract
Dasatinib is an oral small molecule inhibitor of Abl and Src family tyrosine kinases (SFK), including p56Lck (Lck). Given the central importance of Lck in transmitting signals from the T-cell receptor (TCR) signaling complex and the potent ability of dasatinib to inhibit Lck activity, we hypothesized this agent could provide a novel route of immunomodulation via targeted inhibition of antigen-induced signaling. Herein, we show that dasatinib inhibits TCR-mediated signal transduction, cellular proliferation, cytokine production, and in vivo T-cell responses. However, dasatinib-mediated inhibition does not induce apoptosis because the effect is reversible or may be overcome by signals bypassing the TCR, such as phorbol ester. Signal transduction and proliferative responses via IL-2 remain essentially unperturbed, suggesting that dasatinib displays specificity for TCR signaling. In addition, dasatinib combined with cyclosporine A or rapamycin led to a much more potent inhibition of T-cell activation, suggesting that targeted inhibition of Lck could be a useful adjunct for enhanced immunomodulation. In combination with currently available immunomodulatory agents, SFK inhibition could potentially increase immunomodulatory efficacy while minimizing toxicity of individual agents.
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1 retracted
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Cytokine Pathways and Joint Inflammation in Rheumatoid Arthritis
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Dasatinib in imatinib-resistant Philadelphia chromosome-positive leukemias
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Mechanisms of Disease: oncogene addiction—a rationale for molecular targeting in cancer therapy
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Hochhaus, A., Kantarjian, H. M., Baccarani, M., Lipton, J. H., Apperley, J. F., Druker, B. J., Facon, T., Goldberg, S. L., Cervantes, F., Niederwieser, D., et al. (2007) · Blood · doi:10.1182/blood-2006-09-047266 · Cited by 609
New fluorescent dyes for lymphocyte migration studies
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Cited by
Bendall, S. C., Simonds, E. F., Qiu, P., Amir, E.-A. D., Krutzik, P. O., Finck, R., Bruggner, R. V., Melamed, R., Trejo, A., Ornatsky, O. I., et al. (2011) · Science · doi:10.1126/science.1198704 · Cited by 2,279
Transient rest restores functionality in exhausted CAR-T cells through epigenetic remodeling
Weber, E. W., Parker, K. R., Sotillo, E., Lynn, R. C., Anbunathan, H., Lattin, J., Good, Z., Belk, J. A., Daniel, B., Klysz, D., et al. (2021) · Science · doi:10.1126/science.aba1786 · Cited by 607
Cruz, C. R. Y., Micklethwaite, K. P., Savoldo, B., Ramos, C. A., Lam, S., Ku, S., Diouf, O., Liu, E., Barrett, A. J., Ito, S., et al. (2013) · Blood · doi:10.1182/blood-2013-06-506741 · Cited by 508
Broad-Spectrum Kinase Profiling in Live Cells with Lysine-Targeted Sulfonyl Fluoride Probes
Zhao, Q., Ouyang, X., Wan, X., Gajiwala, K. S., Kath, J. C., Jones, L. H., Burlingame, A. L., & Taunton, J. (2017) · Journal of the American Chemical Society · doi:10.1021/jacs.6b08536 · Cited by 388
Wilgenburg, B. V., Browne, C., Vowles, J., & Cowley, S. A. (2013) · PLoS ONE · doi:10.1371/journal.pone.0071098 · Cited by 353
Metadata
- Authors
- Schade, A. E., Schieven, G. L., Townsend, R., Jankowska, A. M., Susulic, V., Zhang, R., Szpurka, H., & Maciejewski, J. P.
- Venue
- Blood
- Publisher
- American Society of Hematology
- Published
- 2008-02-01
- Volume
- 111
- Issue
- 3
- Pages
- 1366-1377
- ISSN
- 0006-4971 (ISSN-L)
- 1528-0020
- OpenAlex
- W2036118441
- Cited by
- 296
- References
- 37
- FWCI
- 4.50
- Type
- journal article
- Language
- en
- Open access
- green
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- CoChat. (2026). Citation check: Dasatinib, a small-molecule protein tyrosine kinase inhibitor, inhibits T-cell activation and proliferation. https://app.cochat.ai/papers/10.1182/blood-2007-04-084814
- The paper
- Schade, A. E., Schieven, G. L., Townsend, R., Jankowska, A. M., Susulic, V., Zhang, R., Szpurka, H., & Maciejewski, J. P. (2008). Dasatinib, a small-molecule protein tyrosine kinase inhibitor, inhibits T-cell activation and proliferation. Blood. https://doi.org/10.1182/blood-2007-04-084814
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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.
