Medicinal Chemistry of Inhibiting RING-Type E3 Ubiquitin Ligases
- 6 March 2020
- journal article
- research article
- Published by American Chemical Society (ACS) in Journal of Medicinal Chemistry
- Vol. 63 (15), 7957-7985
- https://doi.org/10.1021/acs.jmedchem.9b01451
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 article highlights some of the dedicated medicinal chemistry efforts directed at inhibiting the function of specific single-protein and multi-component RING-type E3 ubiquitin ligases. We present opportunities and challenges associated with targeting this important class of enzymes.Keywords
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