Abstract
We report the discovery of an inhibitor of NEDD8-activating enzyme (NAE) by an integrated virtual screening approach. Piperacillin 1 inhibited NAE activity in cell-free and cell-based systems with high selectivity. Furthermore, piperacillin 1 was able to inhibit the degradation of the NAE downstream protein substrate p27kip1. Our molecular modeling and kinetic studies suggested that this compound may act as a non-covalent ATP-competitive inhibitor of NAE
Original language | English |
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Pages (from-to) | 211 - 215 |
Number of pages | 5 |
Journal | Biochimie |
Volume | 102 |
Issue number | 1 |
DOIs | |
Publication status | Published - 2014 |
Externally published | Yes |
Keywords
- Ubiquitin-Protein Ligases
- ligases CRLs
- Cullin Proteins