The DOI matches its Crossref record; 9 of the 9 references it cites were found in a registry or an index.
Development of covalent inhibitors that can overcome resistance to first-generation FGFR kinase inhibitors
Open accessAbstract
Significance: Inhibitors of the FGF receptors (FGFRs) are currently under clinical investigation for the treatment of various cancers. All currently approved kinase inhibitors eventually are rendered useless by the emergence of drug-resistant tumors. We used structure-based drug design to develop the first, to our knowledge, selective, next-generation covalent FGFR inhibitors that can overcome the most common form of kinase inhibitor resistance, the mutation of the so-called “gatekeeper” residue located in the ATP-binding pocket. We also describe a novel kinase inhibitor design strategy that uses a single electrophile to target covalently cysteines that are located in different positions within the ATP-binding pocket. These results have important implications for the design of covalent FGFR inhibitors that can overcome clinical resistance.
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Citations
Cites
The T790M mutation in EGFR kinase causes drug resistance by increasing the affinity for ATP
Yun, C.-H., Mengwasser, K. E., Toms, A. V., Woo, M. S., Greulich, H., Wong, K.-K., Meyerson, M., & Eck, M. J. (2008) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.0709662105 · Cited by 2,118 · cited 2×
“FRIN-3 also lost potency against EGFR, suggesting that covalence is required to achieve potency against EGFR, as is consistent with reports for other covalent inhibitors such as WZ4002 (4, 46).”
ResultSelf-citationYun, C.-H., Boggon, T. J., Li, Y., Woo, M. S., Greulich, H., Meyerson, M., & Eck, M. J. (2007) · Cancer Cell · doi:10.1016/j.ccr.2006.12.017 · Cited by 1,192 · cited 3×
“The structure was solved by the difference Fourier method using the previously reported EGFR/AMP-PnP structure (PDB ID code 2ITV) (61) with PHENIX software (88) and then was refined using Coot (90) and PHENIX.”
BackgroundMethodSelf-citationNovel mutant-selective EGFR kinase inhibitors against EGFR T790M
Zhou, W., Ercan, D., Chen, L., Yun, C.-H., Li, D., Capelletti, M., Cortot, A. B., Chirieac, L., Iacob, R. E., Padera, R., et al. (2009) · Nature · doi:10.1038/nature08622 · Cited by 1,013
Self-citationSolca, F., Dahl, G., Zoephel, A., Bader, G., Sanderson, M., Klein, C., Kraemer, O., Himmelsbach, F., Haaksma, E., & Adolf, G. R. (2012) · The Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.112.197756 · Cited by 865 · cited 1×
“Breast Cancer Res Treat 140(3):587–601.”
Drug resistance via feedback activation of Stat3 in oncogene-addicted cancer cells
Lee, H.-J., Zhuang, G., Cao, Y., Du, P., Kim, H.-J., & Settleman, J. (2014) · Cancer Cell · doi:10.1016/j.ccr.2014.05.019 · Cited by 555
Shimizu, T., Tolcher, A. W., Papadopoulos, K. P., Beeram, M., Rasco, D. W., Smith, L. S., Gunn, S., Smetzer, L., Mays, T. A., Kaiser, B., et al. (2012) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-11-2381 · Cited by 431
Ba/F3 cells and their use in kinase drug discovery
Warmuth, M., Kim, S., Gu, X.-J., Xia, G., & Adrián, F. (2007) · Current Opinion in Oncology · doi:10.1097/cco.0b013e328011a25f · Cited by 240
Miura, S., Mitsuhashi, N., Shimizu, H., Kimura, F., Yoshidome, H., Otsuka, M., Kato, A., Shida, T., Okamura, D., & Miyazaki, M. (2012) · BMC Cancer · doi:10.1186/1471-2407-12-56 · Cited by 193
Turkington, R. C., Longley, D. B., Allen, W. L., Stevenson, L., McLaughlin, K., Dunne, P. D., Blayney, J. K., Salto-Tellez, M., Van Schaeybroeck, S., & Johnston, P. G. (2014) · Cell Death & Disease · doi:10.1038/cddis.2014.10 · Cited by 98
Cited by
Advances 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
Advances and challenges in targeting FGFR signalling in cancer
Babina, I. S., & Turner, N. C. (2017) · Nature Reviews Cancer · doi:10.1038/nrc.2017.8 · Cited by 799
Parikh, A. R., Leshchiner, I., Elagina, L., Goyal, L., Levovitz, C., Siravegna, G., Livitz, D., Rhrissorrakrai, K., Martin, E. E., Van Seventer, E. E., et al. (2019) · Nature Medicine · doi:10.1038/s41591-019-0561-9 · Cited by 518
Advances in covalent kinase inhibitors
Abdeldayem, A., Raouf, Y. S., Constantinescu, S. N., Moriggl, R., & Gunning, P. T. (2020) · Chemical Society Reviews · doi:10.1039/c9cs00720b · Cited by 317
Colchicine-Binding Site Inhibitors from Chemistry to Clinic: A Review
McLoughlin, E. C., & O’Boyle, N. M. (2020) · Pharmaceuticals · doi:10.3390/ph13010008 · Cited by 316
Metadata
- Authors
- Tan, L., Wang, J., Tanizaki, J., Huang, Z., Aref, A. R., Rusan, M., Zhu, S.-J., Zhang, Y., Ercan, D., Liao, R. G., Capelletti, M., Zhou, W., Hur, W., Kim, N., Sim, T., Gaudet, S., Barbie, D. A., Yeh, J.-R. J., Yun, C.-H., Hammerman, P. S., Mohammadi, M., Jänne, P. A., & Gray, N. S.
- Venue
- Proceedings of the National Academy of Sciences
- Published
- 2014-10-27
- Volume
- 111
- Issue
- 45
- Pages
- E4869-77
- ISSN
- 0027-8424 (ISSN-L)
- 1091-6490
- OpenAlex
- W2096258722
- Cited by
- 174
- References
- 9
- FWCI
- 6.08
- Type
- journal article
- Language
- en
- Open access
- green
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- Tan, L., Wang, J., Tanizaki, J., Huang, Z., Aref, A. R., Rusan, M., Zhu, S.-J., Zhang, Y., Ercan, D., Liao, R. G., Capelletti, M., Zhou, W., Hur, W., Kim, N., Sim, T., Gaudet, S., Barbie, D. A., Yeh, J.-R. J., Yun, C.-H., . . . Gray, N. S. (2014). Development of covalent inhibitors that can overcome resistance to first-generation FGFR kinase inhibitors. Proceedings of the National Academy of Sciences. https://doi.org/10.1073/pnas.1403438111
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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.
