The clinical relevance of NEDDylation has in recent years been demonstrated by the use of MLN4924, a small molecule inhibitor that targets NEDD8‐activating enzyme by forming an adduct with NEDD8, ...

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 ...

we provided functional evidence of neddylation in mammalian embryo quality and blastocyst hatching. Treatment with MLN4924, a specific neddylation inhibitor, lowered the embryo quality and ...

为了在 MPM 中识别出可替代的蛋白质抑制和 ICD 有效诱导剂，作者专注于 neddylation 抑制剂（MLN4924）进行研究。在患者源性MPM培养和同基因小鼠模型中，MLN4924和顺铂显示出抗肿瘤作用（图1），能增加DNA损伤，诱导S-和G2/ M-细胞周期阻滞和凋亡（图2）。从机制上讲 ...

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 ...

“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 ...

Neuronal precursor cell-expressed developmentally downregulated protein 8 (NEDD8) is a ubiquitin-like protein that is involved in protein neddylation. The first-in-class anticancer agent called ...

The dysregulation of neddylation may provide a better understanding of CLD pathology and even a novel therapeutic strategy. Correspondingly, inhibiting neddylation via MLN4924, a small molecule ...

相关发现促进了针对Neddylation修饰通路靶向新药的研发进程。MLN4924是NEDD8活化酶的小分子抑制剂，它可以灭活Neddylation-CRL通路，并通过诱导肿瘤细胞发生凋亡和衰老等杀伤肿瘤细胞。鉴于其高效低毒的特点，MLN4924 已经进入多种恶性肿瘤的 II/III 期临床试验阶段 ...

In vivo, deficiency of UBC12 also greatly suppressed tumour growth and metastasis. Together, these results confirm a critical role of UBC12 in controlling neddylation and are reminiscent of those ...