Mpro

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Mpro Inhibitor STI-1558

Targeting tus kab mob lub ntsiab protease (Mpro): interrupting virus replication

Jeong, GU, et al. (2020). "Cov tswv yim kho mob tiv thaiv COVID-19 thiab tus yam ntxwv ntawm tus yam ntxwv ntawm SARS-CoV-2: Kev Ntsuam Xyuas." Frontiers hauv Microbiology 11 (1723).

STI-1558 yog tsim los nrog cov khoom hauv qab no:

  • STI-1558 yog prodrug, thiab nws daim ntawv nquag AC1115 khi rau Cys-145 ntawm catalytic domain ntawm M.pro , uas yog 100% kev txuag nyob rau hauv tag nrho cov SARS-CoV-2 variants thiab ua tiav ib tug dav-spectrum anti-SARS-CoV-2 kev ua, nrog rau cov thawj SARS-CoV-2 strain as well as predominant variants of concern (VOCs) , xws li Delta thiab Omicron.
  • STI-1558 yog Kuj tseem muaj Catepsin L inhibitor, uas tuaj yeem thaiv cov kab mob nkag tau zoo mus rau hauv lub host cell yam tsis muaj kev hloov pauv ntawm tus kab mob.
  • Qhov ncauj bioavailability txog li 76% nrog rau kev nqus sai thiab txhim kho cov tshuaj tiv thaiv kab mob hauv plasma tso cai rau kev kho mob ntxov ntawm COVID hauv tsev los ntawm kev tswj hwm qhov ncauj.
  • Tsis txhob siv cov tshuaj muaj zog CYP34A inhibitor (xws li ritonavir) ua cov tshuaj txhawb kom nce cov ntshav plasma. tso cai rau kev kho mob ib leeg nrog kev pheej hmoo tsawg rau kev sib cuam tshuam tshuaj.
  • A cov khoom siv tshuaj nrog robust formulation, stability thiab loj-scale tshuaj siv tshuaj nrog tswj tus nqi tso cai rau kev nkag mus rau thoob ntiaj teb thiab kev thov.