#C1209N 3CLPro L50F + E166V Expression Kit

3CL^pro (M^pro) L50F + E166V mutation Expression Kit

In a recombinant SARS-COV-2 assay conducted in huh7-ACE2 cells, the E166V mutation alone displayed a 100-fold IC50 resistance to nirmatrelvir, although it led to reduced fitness (Iketani et al. 2023). However, when combined with the mutation L50F, virus replication was restored, resulting in a 53-fold increase in IC₅₀ to nirmatrelvir (Iketani et al. 2023). The L50F, E166V mutation has been detected in patients and reported to the GISAID database (Shu and McCauley 2017; Iketani et al. 2023). Pfizer also reported a 34 to 175-fold increase in EC₅₀ to nirmatrelvir using a biochemical assay (Pfizer Laboratories 2022).

• Identify protease inhibitors that maintain efficacy against the L50F + E166V mutation
• Easy co-expression with our 3CLglow and 3CLglowUp sensors
• Cost effective screening with minimal safety requirements (BSL-1)

Materials in the Kit:

• 3CL^pro L50F + E166V in BacMam
• Sodium Butyrate, 500 mM in H₂O

References:

Iketani, S., Mohri, H., Culbertson, B., Hong, S. J., Duan, Y., Luck, M. I., Annavajhala, M. K., Guo, Y., Sheng, Z., Uhlemann, A.-C., Goff, S. P., Sabo, Y., Yang, H., Chavez, A., & Ho, D. D. (2023). Multiple pathways for SARS-COV-2 resistance to Nirmatrelvir. Nature, 613(7944), 558–564. https://doi.org/10.1038/s41586-022-05514-2

Pfizer Laboratories. (2022). (rep.). FACT SHEET FOR HEALTHCARE PROVIDERS:  EMERGENCY USE AUTHORIZATION FOR PAXLOVID. Retrieved from https://labeling.pfizer.com/ShowLabeling.aspx?id=16474.

Shu, Y., & McCauley, J. (2017). GISAID: Global initiative on sharing all influenza data – from vision to reality. Eurosurveillance, 22(13). https://doi.org/10.2807/1560-7917.es.2017.22.13.30494