Pevonedistat (MLN4924, MLN-4924)是一种有效的和选择性的Nedd8激活酶(NAE)的小分子抑制剂，IC₅₀为4 nM。MLN4924与AMP竞争性结合NAE的核苷酸结合位点。MLN4924对NAE的选择性高于UAE、SAE、UBA6和ATG7（IC₅₀值分别为1.5、8.2、1.8和10 μM）等酶，并且对其它利用ATP的酶没有明显作用。

参考文献

1. Soucy TA, et al. An inhibitor of NEDD8-activating enzyme as a new approach to treat cancer. Nature. 2009 Apr 9;458(7239):732-6.
2. Milhollen MA, et al. MLN4924, a NEDD8-activating enzyme inhibitor, is active in diffuse large B-cell lymphoma models: rationale for treatment of NF-{kappa}B-dependent lymphoma. Blood, 2010 Sep 2; 116(9), 1515-1523.
3. Lin JJ, et al. NEDD8-targeting drug MLN4924 elicits DNA rereplication by stabilizing Cdt1 in S phase, triggering checkpoint activation, apoptosis, and senescence in cancer cells. 2010 Dec 15;70(24):10310-20.

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