Ubiquitin-activating Enzyme (E1) Inhibitors Small Molecules and Peptides

Ubiquitin-activating enzyme E1 catalyzes the first stage of the multistep enzymatic cascade of ubiquitination. The E1 enzyme binds to a ubiquitin molecule which is subsequently transferred to E2 enzymes, E3 enzymes, and then finally the target protein. Unlike the remainder of the ubiquitin-proteasome system, this enzymatic step is dependent on ATP.

There are currently two recognized E1 enzymes that catalyze the first stage of ubiquitination - UBA1 and UBA6 - with a further six related E1 ...