The DOI matches its Crossref record; 3 of the 3 references it cites were found in a registry or an index.
Discovery of a Potent, Selective Protein Tyrosine Phosphatase 1B Inhibitor Using a Linked-Fragment Strategy
Open accessAbstract
Protein tyrosine phosphatase 1B (PTP1B) is an enzyme that downregulates the insulin receptor. Inhibition of PTP1B is expected to improve insulin action, and the design of small molecule PTP1B inhibitors to treat type II diabetes has received considerable attention. In this work, NMR-based screening identified a nonselective competitive inhibitor of PTP1B. A second site ligand was also identified by NMR-based screening and then linked to the catalytic site ligand by rational design. X-ray data confirmed that the inhibitor bound with the catalytic site in the native, "open" conformation. The final compound displayed excellent potency and good selectivity over many other phosphatases. The modular approach to drug design described in this work should be applicable for the design of potent and selective inhibitors of other therapeutically relevant protein tyrosine phosphatases.
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Cites
Global and societal implications of the diabetes epidemic
Zimmet, P., Alberti, K. G. M. M., & Shaw, J. (2001) · Nature · doi:10.1038/414782a · Cited by 5,883
Klaman, L. D., Boss, O., Peroni, O. D., Kim, J. K., Martino, J. L., Zabolotny, J. M., Moghal, N., Lubkin, M., Kim, Y.-B., Sharpe, A. H., et al. (2000) · Molecular and Cellular Biology · doi:10.1128/mcb.20.15.5479-5489.2000 · Cited by 1,235
The T-cell protein tyrosine phosphatase
Ibarra-Sánchez, M. D. J., Simoncic, P. D., Nestel, F. R., Duplay, P., Lapp, W. S., & Tremblay, M. L. (2000) · Seminars in Immunology · doi:10.1006/smim.2000.0220 · Cited by 110
Cited by
Allosteric inhibition of SHP2 phosphatase inhibits cancers driven by receptor tyrosine kinases
Chen, Y.-N. P., LaMarche, M. J., Chan, H. M., Fekkes, P., Garcia-Fortanet, J., Acker, M. G., Antonakos, B., Chen, C. H.-T., Chen, Z., Cooke, V. G., et al. (2016) · Nature · doi:10.1038/nature18621 · Cited by 925
Self-citationPTP1B as a drug target: recent developments in PTP1B inhibitor discovery
Zhang, S., & Zhang, Z.-Y. (2007) · Drug Discovery Today · doi:10.1016/j.drudis.2007.03.011 · Cited by 558
Ligand efficiency indices as guideposts for drug discovery
Abad-Zapatero, C., & Metz, J. T. (2005) · Drug Discovery Today · doi:10.1016/s1359-6446(05)03386-6 · Cited by 527
Self-citationOvercoming mTOR resistance mutations with a new-generation mTOR inhibitor
Rodrik-Outmezguine, V. S., Okaniwa, M., Yao, Z., Novotny, C. J., McWhirter, C., Banaji, A., Won, H., Wong, W., Berger, M., de Stanchina, E., et al. (2016) · Nature · doi:10.1038/nature17963 · Cited by 479
Inhibitors of Protein Tyrosine Phosphatases: Next‐Generation Drugs?
Bialy, L., & Waldmann, H. (2005) · Angewandte Chemie International Edition · doi:10.1002/anie.200461517 · Cited by 420
Metadata
- Authors
- Szczepankiewicz, B. G., Liu, G., Hajduk, P. J., Abad-Zapatero, C., Pei, Z., Xin, Z., Lubben, T. H., Trevillyan, J. M., Stashko, M. A., Ballaron, S. J., Liang, H., Huang, F., Hutchins, C. W., Fesik, S. W., & Jirousek, M. R.
- Venue
- Journal of the American Chemical Society
- Publisher
- American Chemical Society (ACS)
- Published
- 2003-03-12
- Volume
- 125
- Issue
- 14
- Pages
- 4087-4096
- ISSN
- 0002-7863 (ISSN-L)
- 1520-5126
- OpenAlex
- W2134486592
- Cited by
- 231
- References
- 3
- FWCI
- 6.33
- Type
- journal article
- Language
- en
- Open access
- green
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