SARS-CoV-2 Protease Assays for Testing of new COVID-19 Therapeutics
In today’s global COVID-19 pandemic crisis, protease studies are more important than ever, since proteases are essential for virus replication. Existing protease inhibitors are now being added to clinical trials for treating COVID-19, and more specific proteases have been under special investigation as new strategical targets to prevent and cure COVID-19 infections. These targets include ACE2, TMPRSS2, and Main Protease (Mpro) which are indispensable for virus replication and the infection process.
To support the drug discovery community in the challenge to identify efficacious COVID-19 drugs, we have developed specific assays targeting proteases that are essential for SARS-CoV-2 virus entry and replication.
- Fluorescence-based activity assays
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Low and large scale screening, as well as high-throughput screening options, are available
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Full protease panel screening is available for off-target analysis.
Reaction Biology supports the global quest for relief from COVID-19 through offering SARS-CoV-2-Related Protease Assays accurately determining the potency of potential therapeutics to inhibit host and viral proteases.
Our research organization has two facilities: one in the United States and another in Germany. With a strong presence in both sides of the Atlantic, we’re easily accessible by pharmaceutical companies and drug discovery researchers around the world in need for COVID-19-related protease studies.
Proteases as Targets against SARS-CoV-2
Host proteases furin and TMPRSS2 play a vital role in the pathogenesis and replication of SARS-CoV-2 by cleaving the spike protein to enable membrane fusion for virus entry. Cathepsin L further primes the spike protein in the acidic environment of endosomes. PLpro and Mpro are viral proteases required for virus replication. They proteolytically process the polyprotein, which is a prerequisite for virus assembly. PLpro is also known to interfere with the anti-viral immune response of the host cell.
List of Targets
| Target | Synonyms | Data |
|---|---|---|
| ACE2 | angiotensin I converting enzyme 2 | Please inquire |
| Cathepsin B | APP secretase, Cathepsin B1, CATB, CTSB, CPSB | Data sheet |
| Cathepsin L | CTSL, CTSL1 | Data sheet |
| Furin | FUR, PACE, PCSK3 | Data sheet |
| Mpro | 3CLpro, main protease | Data sheet |
| PLpro | NSP3, Papain-Like cysteine protease | Data sheet |
| TMPRSS2 | Transmembrane protease serine 2, PRSS10 | Data sheet |
| TMPRSS6 | Transmembrane protease serine 6, matriptase 2 | Data sheet |
See our full portfolio on our Protease Assay webpage.
Assay Details
The papain-like protease (PLpro) is responsible for cleavage of the coronavirus polyprotein necessary for virus assembly. PLpro also suppresses the host innate immune through the reversal of ubiquitination and ISGylation events. We offer the investigation of the proteolytic activity of PLpro for deubiquitination and for proteolysis of a peptide.
The PLpro assay allows for screening compounds using a fluorogenic substrate, either Z-RLRGG-AMC or Ubiquitin-AMC. PLpro cleaves the substrate for the release of AMC and the resulting fluorescence can be quantified with a luminometer for readout of PLpro enzymatic activity.
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