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Discovery of Bisubstrate Inhibitors for Protein N‑Terminal Methyltransferase 1

Protein N-terminal methyltransferase 1 (NTMT1) plays an important role in regulating mitosis and DNA repair. Here, we describe the discovery of a potent NTMT1 bisubstrate inhibitor 4 (IC(50) = 35 ± 2 nM) that exhibits greater than 100-fold selectivity against a panel of methyltransferases. We also r...

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Vydáno v:J Med Chem
Hlavní autoři: Chen, Dongxing, Dong, Guangping, Noinaj, Nicholas, Huang, Rong
Médium: Artigo
Jazyk:Inglês
Vydáno: 2019
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On-line přístup:https://ncbi.nlm.nih.gov/pmc/articles/PMC6760264/
https://ncbi.nlm.nih.gov/pubmed/30883119
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acs.jmedchem.9b00206
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