Methods for identifying compounds that inhibit ubiquitin-mediated proteolysis of ikappab

摘要

Compounds that inhibit ubiquitin-mediated proteolysis of phosphorylated IkappaB by interfering, directly or indirectly, with the ability of beta-TrCP/E3RS to engage in protein-protein association involving hnRNP-U, are useful as drugs for treating conditions associated with NF-kappaB activation. Cellular and non-cellular screening methods for identifying such compounds are based on monitoring the association/dissociation of beta-TrCP/E3RS.