The DOI matches its Crossref record; 3 of the 3 references it cites were found in a registry or an index.
Salicylic Acid Based Small Molecule Inhibitor for the Oncogenic Src Homology-2 Domain Containing Protein Tyrosine Phosphatase-2 (SHP2)
Open accessAbstract
The Src homology-2 domain containing protein tyrosine phosphatase-2 (SHP2) plays a pivotal role in growth factor and cytokine signaling. Gain-of-function SHP2 mutations are associated with Noonan syndrome, various kinds of leukemias, and solid tumors. Thus, there is considerable interest in SHP2 as a potential target for anticancer and antileukemia therapy. We report a salicylic acid based combinatorial library approach aimed at binding both active site and unique nearby subpockets for enhanced affinity and selectivity. Screening of the library led to the identification of a SHP2 inhibitor II-B08 (compound 9) with highly efficacious cellular activity. Compound 9 blocks growth factor stimulated ERK1/2 activation and hematopoietic progenitor proliferation, providing supporting evidence that chemical inhibition of SHP2 may be therapeutically useful for anticancer and antileukemia treatment. X-ray crystallographic analysis of the structure of SHP2 in complex with 9 reveals molecular determinants that can be exploited for the acquisition of more potent and selective SHP2 inhibitors.
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Citations
Cites
The ‘Shp'ing news: SH2 domain-containing tyrosine phosphatases in cell signaling
Neel, B. G., Gu, H., & Pao, L. (2003) · Trends in Biochemical Sciences · doi:10.1016/s0968-0004(03)00091-4 · Cited by 1,249
Coactivation of receptor tyrosine kinases affects the response of tumor cells to targeted therapies
Stommel, J. M., Kimmelman, A. C., Ying, H., Nabioullin, R., Ponugoti, A. H., Wiedemeyer, R., Stegh, A. H., Bradner, J. E., Ligon, K. L., Brennan, C., et al. (2007) · Science · doi:10.1126/science.1142946 · Cited by 938
Chan, R. J., Leedy, M. B., Munugalavadla, V., Voorhorst, C. S., Li, Y., Yu, M., & Kapur, R. (2005) · Blood · doi:10.1182/blood-2004-10-4002 · Cited by 156
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Cited by
Garcia Fortanet, J., Chen, C. H.-T., Chen, Y.-N. P., Chen, Z., Deng, Z., Firestone, B., Fekkes, P., Fodor, M., Fortin, P. D., Fridrich, C., et al. (2016) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.6b00680 · Cited by 298
Self-citationInhibition of SHP2-mediated dephosphorylation of Ras suppresses oncogenesis
Bunda, S., Burrell, K., Heir, P., Zeng, L., Alamsahebpour, A., Kano, Y., Raught, B., Zhang, Z.-Y., Zadeh, G., & Ohh, M. (2015) · Nature Communications · doi:10.1038/ncomms9859 · Cited by 249
Self-citationIdentification of TNO155, an Allosteric SHP2 Inhibitor for the Treatment of Cancer
LaMarche, M. J., Acker, M., Argintaru, A., Bauer, D., Boisclair, J., Chan, H., Chen, C. H.-T., Chen, Y.-N., Chen, Z., Deng, Z., et al. (2020) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.0c01170 · Cited by 231
Self-citationTherapeutic targeting of oncogenic tyrosine phosphatases
Frankson, R., Yu, Z.-H., Bai, Y., Li, Q., Zhang, R.-Y., & Zhang, Z.-Y. (2017) · Cancer Research · doi:10.1158/0008-5472.can-17-1510 · Cited by 189
Self-citationDiscovery of SHP2-D26 as a First, Potent, and Effective PROTAC Degrader of SHP2 Protein
Wang, M., Lu, J., Wang, M., Yang, C.-Y., & Wang, S. (2020) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.0c00471 · Cited by 172
Metadata
- Authors
- Zhang, X., He, Y., Liu, S., Yu, Z., Jiang, Z.-X., Yang, Z., Dong, Y., Nabinger, S. C., Wu, L., Gunawan, A. M., Wang, L., Chan, R. J., & Zhang, Z.-Y.
- Venue
- Journal of Medicinal Chemistry
- Publisher
- American Chemical Society (ACS)
- Published
- 2010-02-19
- Volume
- 53
- Issue
- 6
- Pages
- 2482-2493
- ISSN
- 0022-2623 (ISSN-L)
- 1520-4804
- OpenAlex
- W2024352432
- Cited by
- 199
- References
- 3
- FWCI
- 5.67
- Type
- journal article
- Language
- en
- Open access
- green
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- Zhang, X., He, Y., Liu, S., Yu, Z., Jiang, Z.-X., Yang, Z., Dong, Y., Nabinger, S. C., Wu, L., Gunawan, A. M., Wang, L., Chan, R. J., & Zhang, Z.-Y. (2010). Salicylic Acid Based Small Molecule Inhibitor for the Oncogenic Src Homology-2 Domain Containing Protein Tyrosine Phosphatase-2 (SHP2). Journal of Medicinal Chemistry. https://doi.org/10.1021/jm901645u
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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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