Medicinal Chemistry of Inhibiting RING-Type E3 Ubiquitin Ligases
| Autor: | Elisia Villemure, Nicole Blaquiere, Steven T. Staben |
|---|---|
| Rok vydání: | 2020 |
| Předmět: |
0303 health sciences
biology Chemistry Chemistry Pharmaceutical Ubiquitin-Protein Ligases 01 natural sciences Medicinal chemistry Protein Structure Secondary 0104 chemical sciences 010404 medicinal & biomolecular chemistry 03 medical and health sciences Proteasome Ubiquitin Drug Discovery biology.protein Animals Humans Molecular Medicine Ring type Enzyme Inhibitors Function (biology) 030304 developmental biology |
| Zdroj: | Journal of Medicinal Chemistry. 63:7957-7985 |
| ISSN: | 1520-4804 0022-2623 |
| DOI: | 10.1021/acs.jmedchem.9b01451 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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