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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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| Pubblicato in: | Oncotarget |
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| Autori principali: | , , , , , , , , , , , , , , , , , , , , |
| Natura: | Artigo |
| Lingua: | Inglês |
| Pubblicazione: |
Impact Journals LLC
2017
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| Soggetti: | |
| Accesso online: | 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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