期刊
ACS MEDICINAL CHEMISTRY LETTERS
卷 11, 期 6, 页码 1175-1184出版社
AMER CHEMICAL SOC
DOI: 10.1021/acsmedchemlett.0c00029
关键词
Naa50; N-alpha-acetyltransferase; acetyl-CoA; DEL
资金
- NATIONAL CANCER INSTITUTE [ZIABC011488] Funding Source: NIH RePORTER
Two novel compounds were identified as Naa50 binders/inhibitors using DNA-encoded technology screening. Biophysical and biochemical data as well as cocrystal structures were obtained for both compounds (3a and 4a) to understand their mechanism of action. These data were also used to rationalize the binding affinity differences observed between the two compounds and a MLGP peptide-containing substrate. Cellular target engagement experiments further confirm the Naa50 binding of 4a and demonstrate its selectivity toward related enzymes (Naa10 and Naa60). Additional analogs of inhibitor 4a were also evaluated to study the binding mode observed in the cocrystal structures.
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