catalysis, structure, ubiquitination, ubiquitin ligaseThe RBR (RING-BetweenRING-RING) or TRIAD [two RING fingers and a DRIL (double RING finger linked)] E3 ubiquitin ligases comprise a group of 12 complex multidomain enzymes. This unique family of E3 ligases includes parkin, whose dysfunction is...
2024年2月28日,复旦大学张英梅、葛均波及中国科学院分子细胞科学卓越创新中心胡荣贵共同通讯在Cell Discovery(IF=34)在线发表题为“The E3 ubiquitin ligase MARCH2 protects against myocardial ischemia-reperfusion injury through inhibiting pyro...
surface ligases, we treated HT29 gD–ligase–Flag cells with gD*IGF1R PROTABs and monitored IGF1R levels. Western blot analysis confirmed that colocalizing validated cell-surface E3 ubiquitin ligases to IGF1R drives degradation (Fig.4d). Conversely, ligases that could not be detected on the cel...
L.;Epemolu, O.; Rocha, S.; Read, K. D.; Ciulli, A. Group-Based Optimization of Potent and Cell-Active Inhibitors of the von Hippel−Lindau (VHL) E3 Ubiquitin Ligase: Structure−Activity Relationships Leading to the Chemical Probe (2S,4R)-1-((S)-2-(1-Cyanocyclopro-panecarboxami...
某些E2在体外能直接把泛素转移到底物.但在大多数情况下是泛素连接酶(ubiquitin ligase.E3参与底物的识别,它在凋节泛素与底物连接的特异性上起着中心作用L4-s]。 26S蛋白酶体是一个由70多个亚 基所组成的巨大的复合分子,分子量接近2000000。它由两部分组成:20S核心蛋白酶体及19S调节复合物或1IS调节复合物。已...
近日,北京大学基础医学院系统生物医学研究所尹玉新教授团队在The EMBO Journal上发表了题为“Structural Insights into the Ubiquitylation Strategy of the Oligomeric CRL2FEM1B E3 Ubiquitin Ligase”的文章,报道了多聚形态E3泛素连接酶CRL2FEM1B在NEDD8修饰激活前,NEDD8修饰激活后与小分子量底物BEX2(约15kDa)结合...
Ubiquitin ligase (e3) is the key factor of the eukaryotic protein selective degradation in vivo system (ups) to regulate a variety of physiological and biochemical reactions in eukaryotic cells. 翻译结果2复制译文编辑译文朗读译文返回顶部 With the aggravation day by day of the energy crisis of the...
在该过程中,起决定性作用的E3泛素化连接酶能介导泛素蛋白连接到靶蛋白上,因此针对E3进行PROTAC药物的弹头及分子胶降解剂(Molecular glue degrader, MGD)正逐渐被人们所关注和深入探究。最近,来自阿斯利康的两位研究者联合在JMC上发表综述文章,总结近年来基于结构的先导化合物发现策略(Fragment-based lead discovery, FB...
The molecular structure and the E3 ligase(s) recruited by ARV-110 and ARV-471 have not been disclosed. The speed at which targeted molecular degraders are progressing toward clinical development is tremendous. It has been estimated that up to 15 molecules will be in human testing by end of ...
Ubiquitin E3 ligases catalyze the final step of the ubiquitination cascade, promoting the transfer of ubiquitin from the E2 to the substrate target. Recent structural and biochemical studies have given insights in the catalytic mechanisms of all three E3