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Updated: Dec 26, 2025

Functional Characterization of RING-Type E3 Ubiquitin Ligases In Vitro and In Planta
Published on: December 5, 2019
Medicinal Chemistry of Inhibiting RING-Type E3 Ubiquitin Ligases
Nicole Blaquiere1, Elisia Villemure1, Steven T Staben1
1Discovery Chemistry, Genentech Inc., 1 DNA Way, South San Francisco, California 94080, United States.
Abstract:
The ubiquitin proteasome system (UPS) presents many opportunities for pharmacological intervention. Key players in the UPS are E3 ubiquitin ligases, responsible for conjugation of ubiquitin to specific cognate substrates. Numbering more than 600 members, these ligases represent the most selective way to intervene within this physiologically important system. This Perspective highlights some of the dedicated medicinal chemistry efforts directed at inhibiting the function of specific single-protein and multicomponent RING-type E3 ubiquitin ligases. We present opportunities and challenges associated with targeting this important class of enzymes.
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