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Specific targeting of the deubiquitinase and E3 ligase families with engineered ubiquitin variants
| Content Provider | Semantic Scholar |
|---|---|
| Author | Gorelik, Maryna Sidhu, Sachdev S. |
| Copyright Year | 2017 |
| Abstract | The ubiquitin proteasome system (UPS) has garnered much attention due to its potential for the development of therapeutics. Following a successful clinical application of general proteasome inhibitors much effort has been devoted to targeting individual UPS components including E3 enzymes and deubiquitinases that control specificity of ubiquitination. Our group has developed a novel approach for targeting the UPS proteins using engineered ubiquitin variants (Ubvs). These drug-like proteins can serve as valuable tools to study biological function of UPS components and assist in the development of small molecules for clinical use. In this review, we summarize studies of Ubvs targeting members of three major families, including deubiquitinases, HECT E3 ligases, and CRL E3 ligases. In particular, we focus on Ubv binding mechanisms, structural studies, and effects on enzyme function. Furthermore, new insights gained from the Ubvs are discussed in the context of small molecule studies. |
| Starting Page | 31 |
| Ending Page | 42 |
| Page Count | 12 |
| File Format | PDF HTM / HTML |
| Alternate Webpage(s) | http://sites.utoronto.ca/sidhulab/pdf/Gorelik_2017_free_PMC.pdf |
| PubMed reference number | 28580429v1 |
| Alternate Webpage(s) | https://doi.org/10.1002/btm2.10044 |
| DOI | 10.1002/btm2.10044 |
| Journal | Bioengineering & translational medicine |
| Volume Number | 2 |
| Language | English |
| Access Restriction | Open |
| Subject Keyword | CNS disorder Deubiquitinating Enzymes Gain Proteasome inhibitor Small Molecule Therapeutic procedure Ubiquitination cellular targeting thiol-dependent ubiquitin-specific protease activity ubiquitin-protein ligase |
| Content Type | Text |
| Resource Type | Article |
