The DOI matches its Crossref record; 3 of the 3 references it cites were found in a registry or an index.
Structure Based Drug Design of Crizotinib (PF-02341066), a Potent and Selective Dual Inhibitor of Mesenchymal–Epithelial Transition Factor (c-MET) Kinase and Anaplastic Lymphoma Kinase (ALK)
Open accessAbstract
Because of the critical roles of aberrant signaling in cancer, both c-MET and ALK receptor tyrosine kinases are attractive oncology targets for therapeutic intervention. The cocrystal structure of 3 (PHA-665752), bound to c-MET kinase domain, revealed a novel ATP site environment, which served as the target to guide parallel, multiattribute drug design. A novel 2-amino-5-aryl-3-benzyloxypyridine series was created to more effectively make the key interactions achieved with 3. In the novel series, the 2-aminopyridine core allowed a 3-benzyloxy group to reach into the same pocket as the 2,6-dichlorophenyl group of 3 via a more direct vector and thus with a better ligand efficiency (LE). Further optimization of the lead series generated the clinical candidate crizotinib (PF-02341066), which demonstrated potent in vitro and in vivo c-MET kinase and ALK inhibition, effective tumor growth inhibition, and good pharmaceutical properties.
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Cites
Identification of the transforming EML4–ALK fusion gene in non-small-cell lung cancer
Soda, M., Choi, Y. L., Enomoto, M., Takada, S., Yamashita, Y., Ishikawa, S., Fujiwara, S.-I., Watanabe, H., Kurashina, K., Hatanaka, H., et al. (2007) · Nature · doi:10.1038/nature05945 · Cited by 5,439
MET Amplification Leads to Gefitinib Resistance in Lung Cancer by Activating ERBB3 Signaling
Engelman, J. A., Zejnullahu, K., Mitsudomi, T., Song, Y., Hyland, C., Park, J. O., Lindeman, N., Gale, C.-M., Zhao, X., Christensen, J., et al. (2007) · Science · doi:10.1126/science.1141478 · Cited by 4,496
Self-citationIdentification of ALK as a major familial neuroblastoma predisposition gene
Mossé, Y. P., Laudenslager, M., Longo, L., Cole, K. A., Wood, A., Attiyeh, E. F., Laquaglia, M. J., Sennett, R., Lynch, J. E., Perri, P., et al. (2008) · Nature · doi:10.1038/nature07261 · Cited by 1,407
Cited by
Roskoski, R. (2016) · Pharmacological Research · doi:10.1016/j.phrs.2015.10.021 · Cited by 886
Frampton, G. M., Ali, S. M., Rosenzweig, M., Chmielecki, J., Lu, X., Bauer, T. M., Akimov, M., Bufill, J. A., Lee, C., Jentz, D., et al. (2015) · Cancer Discovery · doi:10.1158/2159-8290.cd-15-0285 · Cited by 796
Sun, H., Li, Y., Tian, S., Xu, L., & Hou, T. (2014) · Phys. Chem. Chem. Phys. · doi:10.1039/c4cp01388c · Cited by 738
Targeted therapy for non-small cell lung cancer: current standards and the promise of the future.
(2015) · Europe PMC (PubMed Central) · doi:10.3978/j.issn.2218-6751.2014.05.01 · Cited by 716
Johnson, T. W., Richardson, P. F., Bailey, S., Brooun, A., Burke, B. J., Collins, M. R., Cui, J. J., Deal, J. G., Deng, Y.-L., Dinh, D., et al. (2014) · Journal of Medicinal Chemistry · doi:10.1021/jm500261q · Cited by 594
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Metadata
- Authors
- Cui, J. J., Tran-Dubé, M., Shen, H., Nambu, M., Kung, P.-P., Pairish, M., Jia, L., Meng, J., Funk, L., Botrous, I., McTigue, M., Grodsky, N., Ryan, K., Padrique, E., Alton, G., Timofeevski, S., Yamazaki, S., Li, Q., Zou, H., Christensen, J., Mroczkowski, B., Bender, S., Kania, R. S., & Edwards, M. P.
- Venue
- Journal of Medicinal Chemistry
- Publisher
- American Chemical Society (ACS)
- Published
- 2011-08-18
- Volume
- 54
- Issue
- 18
- Pages
- 6342-6363
- ISSN
- 0022-2623 (ISSN-L)
- 1520-4804
- OpenAlex
- W2111254482
- Cited by
- 932
- References
- 3
- FWCI
- 51.13
- Type
- journal article
- Language
- en
- Open access
- green
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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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