研究团队首先用neddylation抑制剂MLN4924联合不同代际TKIs（伊马替尼、尼洛替尼、普纳替尼）处理K562细胞，意外发现MLN4924竟使TKIs的细胞毒性"功亏一篑"。这种"帮倒忙"现象在KU812细胞系和小鼠移植瘤模型中均得到验证，而neddylation激活剂VII-31则展现协同效应。

此项研究旨在评估 Cullin3 neddylation 对 DR 的影响及其潜在机制，研究人员利用 neddylation 抑制剂 MLN4924 展开实验。 在研究方法上，研究人员选用雄性 Sprague–Dawley 大鼠构建糖尿病大鼠模型，将其随机分为糖尿病（Diabetes Mellitus，DM）组和 DM + MLN4924 组，对大鼠进行 ...

Neddylation的底物蛋白参与诸如细胞 ... Millennium公司研究的首个进入临床研究的NAE抑制剂Pevonedistat（MLN4924），在急性髓系白血病(AML)或骨髓增生异常 ...

研究团队首先发现利用拟泛素化（Neddylation）通路特异性抑制剂MLN4924处理可以显著降低狼疮小鼠死亡率、缓解小鼠狼疮表型并伴随着DN T细胞的积累 ...

NEDD8激活酶抑制剂“MLN4924”是近年研发的小分子抗癌药物。赵冰樵团队发现，缺血性脑卒中引起NEDD8类泛素化修饰通路在中性粒细胞中异常激活 ...

However, the impacts of neddylation inhibition on VSMCs and neointimal hyperplasia have not been studied. In our present study, we have shown that MLN4924, a selective inhibitor of NEDD8 ...

“The existence of a novel neddylation inhibitor in early-stage clinical trials further intrigued us to this pathway,” said Dr. Norton. MLN4924 (Pevonedistat) is a small molecule that inhibits ...

Inhibition of neddylation is already being investigated in other tumor types in clinical trials. In pancreatic cancer MLN4924 has also been shown to have an additive effect with cisplatin," says Prof.

Inhibition of neddylation is already being investigated in other tumor types in clinical trials. In pancreatic cancer MLN4924 has also been shown to have an additive effect with cisplatin," says Prof.

The potential utility of blocking NEDDylation has not passed the pharma industry by. Takeda Pharmaceutical already has a NEDD8 activating enzyme inhibitor, MLN4924, in Phase I trials against ...