The DOI matches its Crossref record; 26 of the 26 references it cites were found in a registry or an index.
Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK
Open accessAbstract
Constitutive overexpression and activation of NPM-ALK fusion protein [t(2:5)(p23;q35)] is a key oncogenic event that drives the survival and proliferation of anaplastic large-cell lymphomas (ALCLs). We have identified a highly potent and selective small-molecule ALK inhibitor, NVP-TAE684, which blocked the growth of ALCL-derived and ALK-dependent cell lines with IC 50 values between 2 and 10 nM. NVP-TAE684 treatment resulted in a rapid and sustained inhibition of phosphorylation of NPM-ALK and its downstream effectors and subsequent induction of apoptosis and cell cycle arrest. In vivo , NVP-TAE684 suppressed lymphomagenesis in two independent models of ALK-positive ALCL and induced regression of established Karpas-299 lymphomas. NVP-TAE684 also induced down-regulation of CD30 expression, suggesting that CD30 may be used as a biomarker of therapeutic NPM-ALK kinase activity inhibition.
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Cites
Fusion of a Kinase Gene, ALK , to a Nucleolar Protein Gene, NPM , in Non-Hodgkin's Lymphoma
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Structural Mechanism for STI-571 Inhibition of Abelson Tyrosine Kinase
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Crystal structure of the tyrosine kinase domain of the human insulin receptor
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Structural Basis for the Autoinhibition and STI-571 Inhibition of c-Kit Tyrosine Kinase
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Garcı́a-Echeverrı́a, C., Pearson, M. A., Marti, A., Meyer, T., Mestan, J., Zimmermann, J., Gao, J., Brueggen, J., Capraro, H.-G., Cozens, R., et al. (2004) · Cancer Cell · doi:10.1016/s1535-6108(04)00051-0 · Cited by 542
Stat3 is required for ALK-mediated lymphomagenesis and provides a possible therapeutic target
Chiarle, R., Simmons, W. J., Cai, H., Dhall, G., Zamo, A., Raz, R., Karras, J. G., Levy, D. E., & Inghirami, G. (2005) · Nature Medicine · doi:10.1038/nm1249 · Cited by 442
Anaplastic lymphoma kinase (ALK) activates Stat3 and protects hematopoietic cells from cell death
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Cited by
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
Mechanisms of Acquired Crizotinib Resistance in ALK-Rearranged Lung Cancers
Katayama, R., Shaw, A. T., Khan, T. M., Mino-Kenudson, M., Solomon, B. J., Halmos, B., Jessop, N. A., Wain, J. C., Yeo, A. T., Benes, C., et al. (2012) · Science Translational Medicine · doi:10.1126/scitranslmed.3003316 · Cited by 1,309
Somatic and germline activating mutations of the ALK kinase receptor in neuroblastoma
Janoueix-Lerosey, I., Lequin, D., Brugières, L., Ribeiro, A., de Pontual, L., Combaret, V., Raynal, V., Puisieux, A., Schleiermacher, G., Pierron, G., et al. (2008) · Nature · doi:10.1038/nature07398 · Cited by 894
Activating mutations in ALK provide a therapeutic target in neuroblastoma
George, R. E., Sanda, T., Hanna, M., Fröhling, S., II, W. L., Zhang, J., Ahn, Y., Zhou, W., London, W. B., McGrady, P., et al. (2008) · Nature · doi:10.1038/nature07397 · Cited by 893
Self-citationHarnessing Connectivity in a Large-Scale Small-Molecule Sensitivity Dataset
Seashore-Ludlow, B., Rees, M. G., Cheah, J. H., Cokol, M., Price, E. V., Coletti, M. E., Jones, V., Bodycombe, N. E., Soule, C. K., Gould, J., et al. (2015) · Cancer Discovery · doi:10.1158/2159-8290.cd-15-0235 · Cited by 813
Metadata
- Authors
- Galkin, A. V., Melnick, J. S., Kim, S., Hood, T. L., Li, N., Li, L., Xia, G., Steensma, R., Chopiuk, G., Jiang, J., Wan, Y., Ding, P., Liu, Y., Sun, F., Schultz, P. G., Gray, N. S., & Warmuth, M.
- Venue
- Proceedings of the National Academy of Sciences
- Published
- 2007-01-02
- Volume
- 104
- Issue
- 1
- Pages
- 270-275
- ISSN
- 0027-8424 (ISSN-L)
- 1091-6490
- OpenAlex
- W2014639631
- Cited by
- 379
- References
- 26
- FWCI
- 8.33
- Type
- journal article
- Language
- en
- Open access
- green
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- Galkin, A. V., Melnick, J. S., Kim, S., Hood, T. L., Li, N., Li, L., Xia, G., Steensma, R., Chopiuk, G., Jiang, J., Wan, Y., Ding, P., Liu, Y., Sun, F., Schultz, P. G., Gray, N. S., & Warmuth, M. (2007). Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. Proceedings of the National Academy of Sciences. https://doi.org/10.1073/pnas.0609412103
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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.
