APE1 Redox Products

Description

E3330 represents a novel class of inhibitor. Unlike other compounds that target APE1, it has been recently reported that E3330 recognizes an alternate, redox active conformation of APE1, and that it potentially inhibits APE1's redox activity by inducing disulfide bond formation. No other compound has been reported to selectively recognize an alternate conformation of APE1 or work through this type of mechanism. Thus, E3330 represents a novel class of inhibitor. E3330 was originally developed as an NFkB inhibitor, but subsequently APE1 was found to bind to E3330 through affinity pull-down experiments using immobilized E3330. In light of later work demonstrating that APE1 regulates the transcriptional activity of NFkB, we now know that E3330 actually works upstream of NFkB by inhibiting APE1. Although many quinone compounds have undesirable properties including susceptibility to Michael additions by nucleophiles, E3330 does not form covalent adducts with APE1 because there is no substituent that can serve as an effective leaving group.

Bioinformatics

Alternate Names

(2E)-2-[(4,5-Dimethoxy-2-methyl-3,6-dioxo-1,4-cyclohexadien-1-yl)methylene]-undecanoic acid 3330 AP endonuclease 1 Inhibitor APE-1 Inhibitor APEX 1 Inhibitor Apurinic Endonuclase Factor 1 Inhibitor APX3330 E-3330 REF1 Inhibitor REF-1 Inhibitor