Discovery of Bisubstrate Inhibitors for Protein N‑Terminal Methyltransferase 1
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https://figshare.com/articles/dataset/Discovery_of_Bisubstrate_Inhibitors_for_Protein_N_Terminal_Methyltransferase_1/7904951
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资源简介：
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 (IC50 = 35 ± 2 nM) that exhibits greater than 100-fold selectivity
against a panel of methyltransferases. We also report the first crystal
structure of NTMT1 in complex with an inhibitor, which revealed that 4 occupies substrate and cofactor binding sites of NTMT1.
创建时间：
2019-03-27
