Article
Dissecting the Specificity of Adenosyl Sulfamate Inhibitors Targeting the Ubiquitin-Activating Enzyme.
Structure (London, England : 1993) - 5 Jul 2017
Misra Mohit, Kuhn Maximilian, Löbel Mark, An Heeseon, Statsyuk Alexander V, Sotriffer Christoph, Schindelin Hermann
Abstract excerpt
Targeting the activating enzymes (E1) of ubiquitin (Ub) and ubiquitin-like modifiers (Ubls) has emerged as a promising anti-cancer strategy, possibly overcoming the ineffectiveness of proteasome inhibitors against solid tumors. Here, we report crystal structures of the yeast ubiquitin E1 (Uba1) with three adenosyl sulfamate inhibitors exhibiting different E1 specificities, which are all covalently linked to...
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