E3 Ligase Family
Protein degradation is a regulated, multistep process. Ubiquitin is loaded onto E1-activating enzymes in an ATP-dependent manner and then transferred to E2-binding enzymes. Thesame E2 can bind to many E3 ligases, which in turn can ubiquitinate multiple targetsubstrate proteins. E3 ligases bind specific substrate proteins based onsubstrate degron motifs.
E3 ubiquitin ligases play crucial roles ineukaryotic biology by promoting protein ubiquitination and degradation. Humangenome encodes over 600 E3 ubiquitin ligases which could function in distinctcellular contexts, respond to different cellular signals, and process diverseprotein targets. In recent years, various E3 ligases became pharmacologicaltargets for developing drugs. Two novel strategies, proteolysis-targetingchimeras (PROTAC) and molecular glue make E3 ligase protein productionnecessary for structure-based drug design.
The Biortus Protein Catalogue currently offersover 100 of E3 ubiquitin ligases expressed in multiple expression systems, withseveral structurally resolved and assay developments ready.
