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OwnerAravindhan GANESAN, Todd HOLYOAK +2inventors
InventorsAravindhan GANESAN, Todd HOLYOAK, Subha KALYAANAMOORTHY, Norman TRAN
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A method of identifying compounds that reduce main protease (Mpro) activity of a coronavirus is described, which comprises identifying compounds that bind to and stabilize a modified Mpro in an oxidized conformation with a disulfide bond formed between Cys145 (C145) and Cys117 (C117) of Mpro, reducing the catalytic activity of the modified Mpro. The modified Mpro may comprise substitution of a residue at one or both sites of His163 (H163), and/or Phe140 (F140). A modified Mpro enzyme structure (and its in vitro synthesized form) is described, together with a system for screening or designing compounds useful in treatment or prophylaxis of coronavirus infection such as infection from SARS-CoV-2.
A method of identifying compounds that reduce main protease (Mpro) activity of a coronavirus, comprising identifying compounds that bind to and stabilize a modified Mpro in an oxidized conformation with a disulfide bond formed between Cys145 (C145) and Cys117 (C117) of Mpro.
A modified coronavirus main protease (Mpro) enzyme for use as a conformationally oxidized target to screen for binding of candidate inhibitor compounds or to design candidate inhibitor compounds for treatment or prophylaxis of infection in a subject, wherein said modified Mpro enzyme comprises a conformational state in which a disulfide bond is formed between Cys145 and Cys117 of Mpro, said modified Mpro enzyme comprising a modification selected from t His163 (H163), Phe140(F140), or both.
A system for identifying a candidate inhibitor compound of a modified coronavirus Mpro, wherein said modified Mpro is in an oxidized conformation with a disulfide bond formed between Cys145 (C145) and Cys117 (C117), reducing the catalytic activity of the modified Mpro, said system comprising:
Dependencies are inferred from the claim text.