Cellularly active N-hydroxyurea FEN1 inhibitors block substrate entry to the active site
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منابع مشابه
Cellular Active N-Hydroxyurea FEN1 Inhibitors Block Substrate Entry to the Active Site
The structure-specific nuclease human flap endonuclease-1 (hFEN1) plays a key role in DNA replication and repair and may be of interest as an oncology target. We present the crystal structure of inhibitor-bound hFEN1, which shows a cyclic N-hydroxyurea bound in the active site coordinated to two magnesium ions. Three such compounds had similar IC50 values but differed subtly in mode of action. ...
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ژورنال
عنوان ژورنال: Nature Chemical Biology
سال: 2016
ISSN: 1552-4450,1552-4469
DOI: 10.1038/nchembio.2148