There is an extremely urgent need for the development of specific antiviral therapeutics and vaccines against SARS-CoV-2. The coronavirus main protease, which plays a pivotal role in viral gene expression and replication through the proteolytic processing of replicase polyproteins, is an attractive target for anti-CoV drug design.
The inhibition of viral proteases necessary for proteolytic processing of polyproteins has been a successful strategy in the treatment of human immunodeficiency virus (HIV) and hepatitis C respectively, proving the potential of protease inhibitors for the treatment of viral infections. Similarly, the main protease of SARS-CoV-2 is thought to be essential for viral replication and, therefore, is regarded as promising target for antiviral therapy of Covid-19.
4 extremely effective peptide substrates have been developed for monitoring the intensity of coronavirus proteases via FRET. The Covidyte™ ED450, Covidyte™ EN450, Covidyte™ TF670, and Covidyte™ IF670 peptide substrates provide strong, extended fluorescent signal for searching inhibitors of coronavirus proteases with high sensitivity.
Proteases play essential roles in protein activation, cell regulation and signaling, as well as in the generation of amino acids for protein synthesis or utilization in other metabolic pathways. FRET protease substrates are widely used for detecting protease activities, in particular, for virus protease that often require a long peptide sequence for optimal binding such as coronavirus, HIV and HCV proteases.
The internally quenched FRET peptide substrate is digested by a protease to generate the highly fluorescent peptide fragment. The fluorescence increase is proportional to the protease activity.
Tide Quencher™ dyes have been proven to be the extremely effective quenchers for developing FRET protease substrates for high throughput screening applications together with our bright Tide Fluor™ and iFluor™ dyes.
Covidicyte™ fluorescent donors Tide Fluor™ 5WS and Edans spectrum curves, visualized using AAT Bioquest Advanced Spectrum Viewer
Peptide substrate containing a 14 amino acid sequence that can be cleaved by coronavirus proteases
The dark-FRET peptide contains Tide Quencher™ 5 (TQ5) as a quencher and iFluor™ 670 as a fluorescent donor on the N-and C-terminals respectively
When the peptide is hydrolyzed by coronavirus proteases, the iFluor™ 670 fragment generates significantly enhanced fluorescence since its fluorescence is no longer quenched by TQ5
Covidyte™ TF670
Peptide substrate containing a 14 amino acid sequence that can be cleaved by coronavirus proteases
The dark-FRET peptide contains Tide Quencher™ 5 (TQ5) as a quencher and Tide Fluor™ 5 (TF5) as a fluorescent donor on the N-and C-terminals respectively
When the peptide is hydrolyzed by coronavirus proteases, the TF5 fragment generates significantly enhanced fluorescence since its fluorescence is no longer quenched by TQ5
Peptide substrate containing an 11 amino acid sequence that can be cleaved by coronavirus proteases
Peptide substrate containing a 14 amino acid sequence that can be cleaved by coronavirus proteases
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