In vitro Characterization of Peptidomimetic Proteolysis Targeting Chimera (PROTAC) as a Degrader of 3-Chymotrypsin-Like Protease (Mpro/3CLpro) against SARS-CoV-2
Liturri, M. G.; Bergna, A.; Lai, A.; Della Ventura, C.; Gabrieli, A.; Seravalli, I.; Ciofi-Baffoni, S.; Lenci, E.; Trabocchi, A.; Rusconi, S.
Show abstract
The SARS-CoV-2 main protease (3CLpro) is a key target for antiviral development. We investigated FT235, a peptidomimetic PROTAC linking a GC-376 warhead to pomalidomide for targeted degradation. FT235 bound 3CLpro, inhibiting activity (IC50 = 21.2 {micro}M), and reducing protease levels in cells. In vitro data showed no cytotoxicity up to 100 {micro}M and variant-dependent antiviral activity, with increased potency in the presence of a P-gp inhibitor. These results support PROTAC-based antivirals as promising therapeutic candidates.
Matching journals
The top 4 journals account for 50% of the predicted probability mass.
Similar papers in this journal
- A highly sensitive cell-based luciferase assay for high-throughput automated screening of SARS-CoV-2 nsp5/3CLpro inhibitors 95%
- Combined in silico docking and in vitro antiviral testing for drug repurposing identified lurasidone and elbasvir as SARS-CoV-2 and HCoV-OC43 inhibitors 95%
- Identification of novel Ebola virus inhibitors using biologically contained virus 95%
Similar papers in this journal
Similar papers in this journal
- Boceprevir, calpain inhibitors II and XII, and GC-376 have broad-spectrum antiviral activity against coronaviruses in cell culture 96%
- Screening a library of FDA-approved and bioactive compounds for antiviral activity against SARS-CoV-2 95%
- The SARS-CoV-2 cytopathic effect is blocked with autophagy modulators 93%
Similar papers in this journal
- Host-directed FDA-approved drugs with antiviral activity against SARS-CoV-2 identified by hierarchical in silico/in vitro screening methods 96%
- Discovery of Potent Triple Inhibitors of Both SARS-CoV-2 Proteases and Human Cathepsin L 95%
- Methylene Blue Is a Nonspecific Protein-Protein Interaction Inhibitor with Potential for Repurposing as an Antiviral for COVID-19 95%
"Similar papers" are the closest papers from that journal in the model's embedding space. They show what the match is built on, but the ranking comes mostly from a classifier over the whole training set, not from these examples alone.