Bazuin, Mel (2024) CRBN based Nsp13 degrading PROTAC for SARS-CoV-2. Master's Thesis / Essay, Medical Pharmaceutical Sciences.
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Abstract
In the aftermath of the COVID-19 pandemic, the global medical need for effective antivirals that combat SARS-CoV-2 and its new drug-resistant variants is ever important. Proteolysis-targeting chimeras (PROTACs) are an exciting new heterobifunctional drug modality that induces targeted protein degradation of proteins involved in pathology, by exploitation of the ubiquitin-proteasome system (UPS). Using PROTACs as antivirals is a relatively unexplored field in drug discovery. SARS-CoV-2 expresses 16 non-structural proteins (nsps) which facilitate its RNA transcription and replication, virus-host interactions, and host immune modulation functions. Nsp13 helicase is a multi-functional enzyme with the main function being the nucleotide triphosphate (NTP)-dependent unwinding double-stranded RNA (dsRNA) in the 5’ to 3’ direction. Nsp13 helicase is a highly conserved, essential enzyme needed for SARS-CoV-2 transcription, replication, and ultimately its survival. This essay presents the theoretical design of a nsp13 helicase degrading PROTAC based on CRBN and the non-competitive inhibitor of nsp13, SSYA010-001.
| Item Type: | Thesis (Master's Thesis / Essay) |
|---|---|
| Supervisor name: | Rafie, K. |
| Degree programme: | Medical Pharmaceutical Sciences |
| Thesis type: | Master's Thesis / Essay |
| Language: | English |
| Date Deposited: | 10 Dec 2024 07:45 |
| Last Modified: | 10 Dec 2024 07:45 |
| URI: | https://fse.studenttheses.ub.rug.nl/id/eprint/34484 |
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