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Selective Inhibitors of Histone Methyltransferase DOT1L: Design, Synthesis and Crystallographic Studies
Histone H3-lysine79 (H3K79) methyl transferase DOT1L plays critical roles in normal cell differentiation as well as initiation of acute leukemia. We used structure and mechanism based design to discover several potent inhibitors of DOT1L with IC(50) values as low as 38 nM. These inhibitors exhibit o...
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| Autori principali: | , , , , , , , |
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| Natura: | Artigo |
| Lingua: | Inglês |
| Pubblicazione: |
2011
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| Soggetti: | |
| Accesso online: | https://ncbi.nlm.nih.gov/pmc/articles/PMC3492951/ https://ncbi.nlm.nih.gov/pubmed/21936531 https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/ja206312b |
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