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Discovery of a Potent, Selective Protein Tyrosine Phosphatase 1B Inhibitor Using a Linked-Fragment Strategy

✍ Scribed by Szczepankiewicz, Bruce G.; Liu, Gang; Hajduk, Philip J.; Abad-Zapatero, Cele; Pei, Zhonghua; Xin, Zhili; Lubben, Thomas H.; Trevillyan, James M.; Stashko, Michael A.; Ballaron, Stephen J.; Liang, Heng; Huang, Flora; Hutchins, Charles W.; Fesik, Stephen W.; Jirousek, Michael R.


Book ID
120040018
Publisher
American Chemical Society
Year
2003
Tongue
English
Weight
375 KB
Volume
125
Category
Article
ISSN
0002-7863

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Discovery and SAR of novel, potent and s
✍ Zhonghua Pei; Xiaofeng Li; Gang Liu; Cele Abad-Zapatero; Tom Lubben; Tianyuan Zh πŸ“‚ Article πŸ“… 2003 πŸ› Elsevier Science 🌐 English βš– 211 KB

A salicylate second site binder was linked to three classes of phosphotyrosine mimetics to produce potent protein tyrosine phosphatase 1B (PTP1B) inhibitors which exhibit significant selectivity against other phosphatases including the most homologous member, TCPTP.