The DOI matches its Crossref record; 45 of the 45 references it cites were found in a registry or an index.
Discovery of Entrectinib: A New 3-Aminoindazole As a Potent Anaplastic Lymphoma Kinase (ALK), c-ros Oncogene 1 Kinase (ROS1), and Pan-Tropomyosin Receptor Kinases (Pan-TRKs) inhibitor
Open accessAbstract
Anaplastic lymphoma kinase (ALK) is a receptor tyrosine kinase responsible for the development of different tumor types. Despite the remarkable clinical activity of crizotinib (Xalkori), the first ALK inhibitor approved in 2011, the emergence of resistance mutations and of brain metastases frequently causes relapse in patients. Within our ALK drug discovery program, we identified compound 1, a novel 3-aminoindazole active on ALK in biochemical and in cellular assays. Its optimization led to compound 2 (entrectinib), a potent orally available ALK inhibitor active on ALK-dependent cell lines, efficiently penetrant the blood-brain barrier (BBB) in different animal species and highly efficacious in in vivo xenograft models. Moreover, entrectinib resulted to be strictly potent on the closely related tyrosine kinases ROS1 and TRKs recently found constitutively activated in several tumor types. Entrectinib is currently undergoing phase I/II clinical trial for the treatment of patients affected by ALK-, ROS1-, and TRK-positive tumors.
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Cites
Coot : model-building tools for molecular graphics
Emsley, P., & Cowtan, K. (2004) · Acta Crystallographica Section D Biological Crystallography · doi:10.1107/s0907444904019158 · Cited by 30,571
Phaser crystallographic software
McCoy, A. J., Grosse-Kunstleve, R. W., Adams, P. D., Winn, M. D., Storoni, L. C., & Read, R. J. (2007) · Journal of Applied Crystallography · doi:10.1107/s0021889807021206 · Cited by 20,612
Refinement of Macromolecular Structures by the Maximum-Likelihood Method
Murshudov, G. N., Vagin, A. A., & Dodson, E. J. (1997) · Acta Crystallographica Section D Biological Crystallography · doi:10.1107/s0907444996012255 · Cited by 14,742
Overview of the CCP 4 suite and current developments
Winn, M. D., Ballard, C. C., Cowtan, K. D., Dodson, E. J., Emsley, P., Evans, P. R., Keegan, R. M., Krissinel, E. B., Leslie, A. G. W., McCoy, A., et al. (2011) · Acta Crystallographica Section D Biological Crystallography · doi:10.1107/s0907444910045749 · Cited by 12,353
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
Fusion of a Kinase Gene, ALK , to a Nucleolar Protein Gene, NPM , in Non-Hodgkin's Lymphoma
Morris, S. W., Kirstein, M. N., Valentine, M. B., Dittmer, K. G., Shapiro, D. N., Saltman, D. L., & Look, A. T. (1994) · Science · doi:10.1126/science.8122112 · Cited by 2,409
Global Survey of Phosphotyrosine Signaling Identifies Oncogenic Kinases in Lung Cancer
Rikova, K., Guo, A., Zeng, Q., Possemato, A., Yu, J., Haack, H., Nardone, J., Lee, K., Reeves, C., Li, Y., et al. (2007) · Cell · doi:10.1016/j.cell.2007.11.025 · Cited by 2,317
Erlotinib in Lung Cancer — Molecular and Clinical Predictors of Outcome
Tsao, M.-S., Sakurada, A., Cutz, J.-C., Zhu, C.-Q., Kamel-Reid, S., Squire, J., Lorimer, I., Zhang, T., Liu, N., Daneshmand, M., et al. (2005) · New England Journal of Medicine · doi:10.1056/nejmoa050736 · Cited by 1,830
ROS1 Rearrangements Define a Unique Molecular Class of Lung Cancers
Bergethon, K., Shaw, A. T., Ignatius Ou, S.-H., Katayama, R., Lovly, C. M., McDonald, N. T., Massion, P. P., Siwak-Tapp, C., Gonzalez, A., Fang, R., et al. (2012) · Journal of Clinical Oncology · doi:10.1200/jco.2011.35.6345 · Cited by 1,555
Identification 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
Doebele, R. C., Drilon, A., Paz-Ares, L., Siena, S., Shaw, A. T., Farago, A. F., Blakely, C. M., Seto, T., Cho, B. C., Tosi, D., et al. (2020) · The Lancet Oncology · doi:10.1016/s1470-2045(19)30691-6 · Cited by 1,790
Drilon, A., Siena, S., Dziadziuszko, R., Barlesi, F., Krebs, M. G., Shaw, A. T., de Braud, F., Rolfo, C., Ahn, M.-J., Wolf, J., et al. (2020) · The Lancet Oncology · doi:10.1016/s1470-2045(19)30690-4 · Cited by 528
Targeting ALK: Precision Medicine Takes on Drug Resistance
Lin, J. J., Riely, G. J., & Shaw, A. T. (2017) · Cancer Discovery · doi:10.1158/2159-8290.cd-16-1123 · Cited by 522
Molecular characterization of cancers with NTRK gene fusions
Gatalica, Z., Xiu, J., Swensen, J., & Vranic, S. (2019) · Modern Pathology · doi:10.1038/s41379-018-0118-3 · Cited by 486
Development of small-molecule tropomyosin receptor kinase (TRK) inhibitors for NTRK fusion cancers
Jiang, T., Wang, G., Liu, Y., Feng, L., Wang, M., Liu, J., Chen, Y., & Ouyang, L. (2021) · Acta Pharmaceutica Sinica B · doi:10.1016/j.apsb.2020.05.004 · Cited by 157
Metadata
- Authors
- Menichincheri, M., Ardini, E., Magnaghi, P., Avanzi, N., Banfi, P., Bossi, R., Buffa, L., Canevari, G., Ceriani, L., Colombo, M., Corti, L., Donati, D., Fasolini, M., Felder, E., Fiorelli, C., Fiorentini, F., Galvani, A., Isacchi, A., Borgia, A. L., Marchionni, C., Nesi, M., Orrenius, C., Panzeri, A., Pesenti, E., Rusconi, L., Saccardo, M. B., Vanotti, E., Perrone, E., & Orsini, P.
- Venue
- Journal of Medicinal Chemistry
- Publisher
- American Chemical Society (ACS)
- Published
- 2016-03-30
- Volume
- 59
- Issue
- 7
- Pages
- 3392-3408
- ISSN
- 0022-2623 (ISSN-L)
- 1520-4804
- OpenAlex
- W2304533799
- Cited by
- 299
- References
- 45
- FWCI
- 19.07
- Type
- journal article
- Language
- en
- Open access
- green
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- CoChat. (2026). Citation check: Discovery of Entrectinib: A New 3-Aminoindazole As a Potent Anaplastic Lymphoma Kinase (ALK), c-ros Oncogene 1 Kinase (ROS1), and Pan-Tropomyosin Receptor Kinases (Pan-TRKs) inhibitor. https://app.cochat.ai/papers/10.1021/acs.jmedchem.6b00064
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- Menichincheri, M., Ardini, E., Magnaghi, P., Avanzi, N., Banfi, P., Bossi, R., Buffa, L., Canevari, G., Ceriani, L., Colombo, M., Corti, L., Donati, D., Fasolini, M., Felder, E., Fiorelli, C., Fiorentini, F., Galvani, A., Isacchi, A., Borgia, A. L., . . . Orsini, P. (2016). Discovery of Entrectinib: A New 3-Aminoindazole As a Potent Anaplastic Lymphoma Kinase (ALK), c-ros Oncogene 1 Kinase (ROS1), and Pan-Tropomyosin Receptor Kinases (Pan-TRKs) inhibitor. Journal of Medicinal Chemistry. https://doi.org/10.1021/acs.jmedchem.6b00064
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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.
