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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Pubblicato in:J Med Chem
Autori principali: 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
Natura: Artigo
Lingua:Inglês
Pubblicazione: 2018
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Article
Accesso online: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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