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Dodaro, A.

Publications and source records attributed to Dodaro, A..

2 recordsLinked to original sources

A novel dual-chimeric surrogate virus to select, test and characterize mutants of protease and glycoprotein inhibitors.

Antivirals are life-saving medications. However, pathogens develop resistances, mitigating their effect. Resistance studies (gain-of-function, GOF) are therefore paramount before and while antivirals are used clinically to characterize resistances and ideally study how to counteract them with other antivirals. The ability to switch from one antiviral, against which the virus is resistant, to another, depends on the availability of alternative drugs. Furthermore, targeting different parts of the virus synergistically with multiple drugs decreases the odds of simultaneous resistance. However, studying resistance, cross-resistance and remaining susceptibility requires working with the actual pathogen. Especially when introducing resistances into dangerous viruses, performing GOF studies would raise safety concerns and require firm biological containment. In this study we developed a novel dual-chimeric virus encoding both SARS-CoV-2 spike glycoprotein and main protease (Mpro) based on the model virus, vesicular stomatitis virus (VSV). We applied selection pressure with spike and Mpro inhibitors, generated mutants of these viruses and determined their resistance and cross-resistance profiles by performing dose-response experiments with live and pseudotyped viruses. Additionally, we conducted in silico calculations to determine the impact of spike substitutions to the observed resistance phenotype. With the new technology presented here, we demonstrate that it is possible to carry out GOF studies more safely and highlight their importance in the future challenges of virological research.

microbiology↗

A comprehensive study of SARS-CoV-2 main protease (Mpro) inhibitor-resistant mutants selected in a VSV-based system

Nirmatrelvir was the first protease inhibitor (PI) specifically developed against the SARS-CoV-2 main protease (3CLpro/Mpro) and licensed for clinical use. As SARS-CoV-2 continues to spread, variants resistant to nirmatrelvir and other currently available treatments are likely to arise. This study aimed to identify and characterize mutations that confer resistance to nirmatrelvir. To safely generate Mpro resistance mutations, we passaged a previously developed, chimeric vesicular stomatitis virus (VSV-Mpro) with increasing, yet suboptimal concentrations of nirmatrelvir. Using Wuhan-1 and Omicron Mpro variants, we selected a large set of mutants. Some mutations are frequently present in GISAID, suggesting their relevance in SARS-CoV-2. The resistance phenotype of a subset of mutations was characterized against clinically available PIs (nirmatrelvir and ensitrelvir) with cell-based and biochemical assays. Moreover, we showed the putative molecular mechanism of resistance based on in silico molecular modelling. These findings have implications on the development of future generation Mpro inhibitors, will help to understand SARS-CoV-2 protease-inhibitor-resistance mechanisms and show the relevance of specific mutations in the clinic, thereby informing treatment decisions. TeaserUnderstanding how SARS-CoV-2 could counter the antiviral drug nirmatrelvir and what it means for the future of COVID-19 treatment.

microbiology↗