As a dedicated designer and manufacter of biotech products, NEST has assisted plenties of academics and researchers in achieving distinct accomplishment. The following is the journal article accomplished by the Research Team led by Prof. Zhang Yuyang, which is included in the academic journal Acta Pharmacologica Sinica. In this article, the structure basis of the feline drug GC376, an effective inhibition of SARS-CoV-2 is demonstrated.
The main content can be concluded as follows.
Abstract: In the case of the severe crisis brought forth by the coronavirus pandemic, it is of highly significance to seek efficient drugs to inhibit the pandemic. Through structural analysis of GC376 and effective in vitro assays, it is clearly manifested that GC376 is an effective and safe drug candidate suitable for use against COVID-19 by inhibiting SARS-CoV-2 M PRO. Since the function of Mpro is indispensable to the viral life cycle, inhibiting the activity of Mpro is of vital importance to impede the coronavirus replication. Firstly, through thermal shift assay (TSA) to assess the effect of selected nine drug on SARS-CoV-2 Mpro, it is proven that GC376, a dipeptidyl bisulfifite adduct salt and a potentially broad-spectrum antiviral drug, interacts directly with SARS-COV-2 MPro. Secondly, verifying the structure of GC376 bound SARS-COV-2 Mpro at the resolution of 2.35 ? and comparing the GC376-bound Mpro with those of the previously reported, researchers verify the potential of GC376 to act as a covalent inhibitor to prevent the binding and cleavage of substrates by SARS-CoV-2 Mpro. In addition, tests on the ability of GC376 to inhibit SARS-CoV-2 infection showed a 50% maximal effect concentration (EC50) of 0.18 μM and a 50% cytotoxic concentration (CC50) of more than 200 μM, indicating a strong safety profile. Above all, the conclusion can be drawn that GC376 may act as a broad-spectrum drug for different variants of SARS-COV-2 and worthy of further testing in clinical trials.
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