NCIt definition : A small molecule inhibitor of ubiquitin-activating enzyme (UAE), with potential antineoplastic
activity. UAE inhibitor TAK-243 binds to and inhibits UAE, which prevents both protein
ubiquitination and subsequent protein degradation by the proteasome. This results
in an excess of proteins in the cells and may lead to endoplasmic reticulum (ER) stress-mediated
apoptosis. This inhibits tumor cell proliferation and survival. UAE, also called ubiquitin
E1 enzyme (UBA1; E1), is more active in cancer cells than in normal, healthy cells.;
Semantic type(s)