细胞凋亡抑制剂(cIAP1/2)和X-连锁凋亡抑制剂(XIAP)是两种抗凋亡蛋白(Inhibitor of apoptosis, IAPs),是UPS降解底物,受到Neddylation修饰的调控。激活Neddylation过程,降解抗凋亡蛋白,诱导细胞死亡,理论上也能发挥抗肿瘤作用。研究人员合理设计了化合物VII-31,在MGC803细胞中VII-31能够
Recent studies have found that MLN4924, small molecule inhibitor of Neddylation modification, has a significant anti-tumor effect, which can inhibit the tumor growth by inducing cell cycle arrest, senescence and apoptosis, and inhibiting tumor angiogenesis. This paper reviews the related mechanism ...
患者的总体生存率较低;体内外实验均表明下调NEDD8可显著抑制肿瘤的生长;下调NEDD8能够诱导DNA损伤,并激活死亡受体5(death receptor 5,DR5)依赖的外源性细胞凋亡途径,进而杀伤肿瘤;除此之外,敲低NEDD8使CRL失活,导致其底物细胞周期抑制蛋白...
Neddylation修饰是新近发现的一种类泛素化蛋白翻译后修饰方式,类泛素分子神经前体细胞表达发育下调蛋白8(neural precursor cell expressed, developmentally downregulated 8, NEDD8)在NEDD8活化酶1(NEDD8-activating enzyme 1,NAE1)、NEDD8结...
JJ, Gaulin JL, Gershman RE, Lublinsky AR, McDonald A, Mizutani H, Narayanan U, Olhava EJ, Peluso S, Rezaei M, Sintchak MD, Talreja T, Thomas MP, Traore T, Vyskocil S, Weatherhead GS, Yu J, Zhang J, Dick LR, Claiborne CF, Rolfe M, Bolen JB, Langston SP. An inhibitor of ...
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Neddylation在病毒感染性疾病中的作用
sotherelationshipbetweenNeddylationandcancerhasarousedmuchconcern.Ned-dylationhasbeenconsideredtobeanovelanticancertarget.Neddylationinactivationbyafirst-in-classsmallmolecularinhibitor,MLN4924,inducescellcyclearrest,apoptosis,senescenceandautophagyindifferenttumorcells.MLN4924alsoexertssignificantanticancereffectsbyinhibiting...
Olhava EJ, Peluso S, Rezaei M, Sintchak MD, Talreja T, Thomas MP, Traore T, Vyskocil S, Weatherhead GS, Yu J, Zhang J, Dick LR, Claiborne CF, Rolfe M, Bolen JB, Langston SP. An inhibitor of NEDD8-activating...