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Showing results 1 to 5 of 5

Journal article

A novel conformational state for SARS-CoV-2 main protease

Authors : Fornasier, Emanuele (2021)

The SARS-CoV-2 main protease (Mpro) has a pivotal role in mediating viral genome replication and transcription of coronavirus, making it a promising target for drugs against Covid-19 pandemic. Here we present a crystal structure of Mpro disclosing new structural features of key regions of the enzyme. We show that the oxyanion loop, involved in substrate recognition and enzymatic activity, can adopt a new conformation, which is stable&#...

Journal article

An expanded 2-pyridinecarboxaldehyde (2PCA)-based chemoproteomics toolbox for probing protease specificity

Authors : Bridge, Haley N. (2023)

Proteomic profiling of protease-generated N termini, or N terminomics, provides key insights into protease function and specificity. However, current N terminomics technologies have sequence limitations or require specialized synthetic reagents for N-terminal peptide isolation. Here, we introduce an expanded N terminomics toolbox that is based on 2-pyridinecarboxaldehyde (2PCA) reagents. These tools enable efficient enrichment of protein N termini by combining sele...

Journal article

Design of a mucin-selective protease for targeted degradation of cancer-associated mucins

Authors : Pedram, Kayvon (2023)

Targeted protein degradation is an emerging strategy for the elimination of classically undruggable proteins. Here, to expand the landscape of substrates that can be selectively degraded, we designed degraders which are dependent on both peptide sequence and glycosylation status of the target protein. We applied this approach to mucins, O-glycosylated proteins that drive cancer progression through biophysical and immunological mechanisms. Engineering of&...

Journal article

Production of a functionally active recombinant SARS-CoV-2 (COVID-19) 3C-Like protease and a soluble inactive 3C-like protease-RBD chimeric in a prokaryotic expression system

Authors : Verissimo, Carolina De Marco (2023)

During the SARS-CoV-2 intracellular life-cycle, two large polyproteins, pp1a and pp1ab, are 29 produced. Processing of these by viral cysteine proteases, the papain-like protease (PLpro) and 30 the chymotrypsin-like 3C-like protease (3CL-pro) release non-structural proteins necessary for 31 the establishment of the viral replication and transcription complex (RTC), crucial for viral 32 replication. Hence, these proteases are considered prime targets against which anti-COVID-19&#...

Journal article

Tau protein aggregation associated with SARS-CoV-2 main protease

Authors : Eberle, Raphael Josef (2023)

The primary function of virus proteases is the proteolytic processing of the viral polyprotein. These 16 enzymes can also cleave host cell proteins, which is important for viral pathogenicity, modulation of 17 cellular processes, viral replication, the defeat of antiviral responses and modulation of the immune 18 response. It is known that COVID-19 can influence multiple tissues or organs and that infection can 19 damage the functionality of the...