Updates on scientific push on Covid 19 from the Journal Science



Some great news on the scientific side. Know your enemy and you will be able to fight it! It is amazing and beautiful that this viral protease, crucial for the assembly of the virus, has been crystallized so quickly. From here, scientists will be able to design an inhibitor that should be able to stop or at least, slow down the virus and allow people to get better sooner.

Remember: we are not in 1918 anymore! The pandemic is occurring in a world that knows how to defeat it. Let’s do our part and let doctors and scientists do theirs.

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Crystal structure of SARS-CoV-2 main protease provides a basis for design of improved α-ketoamide inhibitors

Linlin Zhang1,2, Daizong Lin1,3, Xinyuanyuan Sun1,2, Ute Curth4, Christian Drosten5, Lucie Sauerhering6,7, Stephan Becker6,7, Katharina Rox8,9, Rolf Hilgenfeld1,2,*

Science 20 Mar 2020:
DOI: 10.1126/science.abb3405

Abstract: The COVID-19 pandemic caused by SARS-CoV-2 is a global health emergency. An attractive drug target among coronaviruses is the main protease (Mpro, 3CLpro), due to its essential role in processing the polyproteins that are translated from the viral RNA. We report the X-ray structures of the unliganded SARS-CoV-2 Mpro and its complex with an α-ketoamide inhibitor. This was derived from a previously designed inhibitor but with the P3-P2 amide bond incorporated into a pyridone ring to enhance the half-life of the compound in plasma. Based on the structure, we developed the lead compound into a potent inhibitor of the SARS-CoV-2 Mpro. The pharmacokinetic characterization of the optimized inhibitor reveals a pronounced lung tropism and suitability for administration by the inhalative route.

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