Discovery of a highly selective KIT kinase primary V559D mutant inhibitor for gastrointestinal stromal tumors (GISTs)

KIT kinase V559D mutation is the most prevalent primary gain-of-function mutation in Gastrointestinal Stromal Tumors (GISTs). Here we reported a highly selective KIT V559D inhibitor CHMFL-KIT-031, which displayed about 10-20 fold selectivity over KIT wt in the biochemical assay (IC(50): 28 nM over 1...

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Vydáno v:Oncotarget
Hlavní autoři: Yu, Kailin, Liu, Xuesong, Jiang, Zongru, Hu, Chen, Zou, Fengming, Chen, Cheng, Ge, Juan, Wu, Jiaxin, Liu, Xiaochuan, Wang, Aoli, Wang, Wenliang, Wang, Wenchao, Qi, Ziping, Wang, Beilei, Wang, Li, Yan, Hezhong, Wang, Jiaoxue, Ren, Tao, Tang, Jun, Liu, Qingsong, Liu, Jing
Médium: Artigo
Jazyk:Inglês
Vydáno: Impact Journals LLC 2017
Témata:
Research Paper
On-line přístup:https://ncbi.nlm.nih.gov/pmc/articles/PMC5762309/
https://ncbi.nlm.nih.gov/pubmed/29340041
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.18632/oncotarget.22624
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