The DOI matches its Crossref record; 2 of the 2 references it cites were found in a registry or an index.
Crenolanib is a selective type I pan-FLT3 inhibitor
Open accessAbstract
Significance: Rapid evolution of drug resistance associated with secondary kinase domain (KD) mutations is the best characterized mechanism of acquired resistance to effective tyrosine kinase inhibitor (TKI) therapy. Medicinal chemistry efforts have largely been devoted toward synthesizing type II TKIs that, by targeting an inactive kinase conformation, are believed to afford greater selectivity than type I TKIs that bind an active kinase conformation. The only previously described TKI with the ability to successfully suppress all resistance-conferring KD mutants (i.e. “pan-kinase” inhibitor) is the type II multikinase TKI ponatinib. Here, we demonstrate that a type I TKI can be potent, selective, and invulnerable to resistance-conferring KD mutation as a mechanism of resistance. Efforts to develop potent, selective type I pan-kinase inhibitors are warranted.
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Cites
Ponatinib in Refractory Philadelphia Chromosome–Positive Leukemias
Cortes, J. E., Kantarjian, H., Shah, N. P., Bixby, D., Mauro, M. J., Flinn, I., O'Hare, T., Hu, S., Narasimhan, N. I., Rivera, V. M., et al. (2012) · New England Journal of Medicine · doi:10.1056/nejmoa1205127 · Cited by 769
Self-citationBradeen, H. A., Eide, C. A., O'Hare, T., Johnson, K. J., Willis, S. G., Lee, F. Y., Druker, B. J., & Deininger, M. W. (2006) · Blood · doi:10.1182/blood-2006-02-004580 · Cited by 393
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‘Acute myeloid leukemia: a comprehensive review and 2016 update’
De Kouchkovsky, I., & Abdul-Hay, M. (2016) · Blood Cancer Journal · doi:10.1038/bcj.2016.50 · Cited by 1,317
McMahon, C. M., Ferng, T., Canaani, J., Wang, E. S., Morrissette, J. J. D., Eastburn, D. J., Pellegrino, M., Durruthy-Durruthy, R., Watt, C. D., Asthana, S., et al. (2019) · Cancer Discovery · doi:10.1158/2159-8290.cd-18-1453 · Cited by 446
Self-citationFLT3 mutations in acute myeloid leukemia: Therapeutic paradigm beyond inhibitor development
Kiyoi, H., Kawashima, N., & Ishikawa, Y. (2020) · Cancer Science · doi:10.1111/cas.14274 · Cited by 298
A human multi-lineage hepatic organoid model for liver fibrosis
Guan, Y., Enejder, A., Wang, M., Fang, Z., Cui, L., Chen, S.-Y., Wang, J., Tan, Y., Wu, M., Chen, X., et al. (2021) · Nature Communications · doi:10.1038/s41467-021-26410-9 · Cited by 149
Metadata
- Authors
- Smith, C. C., Lasater, E. A., Lin, K. C., Wang, Q., McCreery, M. Q., Stewart, W. K., Damon, L. E., Perl, A. E., Jeschke, G. R., Sugita, M., Carroll, M., Kogan, S. C., Kuriyan, J., & Shah, N. P.
- Venue
- Proceedings of the National Academy of Sciences
- Published
- 2014-03-12
- Volume
- 111
- Issue
- 14
- Pages
- 5319-5324
- ISSN
- 0027-8424 (ISSN-L)
- 1091-6490
- OpenAlex
- W2029056941
- Cited by
- 211
- References
- 2
- FWCI
- 13.88
- Type
- journal article
- Language
- en
- Open access
- bronze
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- Smith, C. C., Lasater, E. A., Lin, K. C., Wang, Q., McCreery, M. Q., Stewart, W. K., Damon, L. E., Perl, A. E., Jeschke, G. R., Sugita, M., Carroll, M., Kogan, S. C., Kuriyan, J., & Shah, N. P. (2014). Crenolanib is a selective type I pan-FLT3 inhibitor. Proceedings of the National Academy of Sciences. https://doi.org/10.1073/pnas.1320661111
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