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Synthesis, Activity and Metabolic Stability of Non-Ribose Containing Inhibitors of Histone Methyltransferase DOT1L
Histone methyltransferase DOT1L is a drug target for MLL leukemia. We report an efficient synthesis of a cyclopentane-containing compound that potently and selectively inhibits DOT1L (K(i) = 1.1 nM) as well as H3K79 methylation (IC(50) ~ 200 nM). Importantly, this compound exhibits a high stability...
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| Main Authors: | , , , , , , |
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| Format: | Artigo |
| Sprog: | Inglês |
| Udgivet: |
2013
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| Fag: | |
| Online adgang: | https://ncbi.nlm.nih.gov/pmc/articles/PMC3686528/ https://ncbi.nlm.nih.gov/pubmed/23795283 https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1039/C3MD00021D |
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