A small molecule inhibitor that stabilizes the autoinhibited conformation of the oncogenic tyrosine phosphatase SHP2

Genetic mutations in the phosphatase PTPN11 (SHP2) are associated with childhood leukemias. These mutations cause hyperactivation of SHP2 due to the disruption of the auto-inhibitory conformation. By targeting the activation-associated protein conformational change, we have identified an SHP2 inhibi...

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Udgivet i:J Med Chem
Main Authors: Wu, Xiaoqin, Xu, Gang, Li, Xiaobo, Xu, Weiren, Li, Qianjin, Liu, Wei, Kirby, Karen A., Loh, Mignon L., Li, Jun, Sarafianos, Stefan G., Qu, Cheng-Kui
Format: Artigo
Sprog:Inglês
Udgivet: 2018
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Article
Online adgang:https://ncbi.nlm.nih.gov/pmc/articles/PMC6467801/
https://ncbi.nlm.nih.gov/pubmed/30457860
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acs.jmedchem.8b00513
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