I-OVYDSO STI-1558

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I-OVYDSO STI-1558

Ukujolisa kwintsholongwane engundoqo yeprotease (Mpro): ukuphazamisa ukuphindaphinda kwentsholongwane

Jeong, GU, et al. (2020). "Amaqhinga okuNyanga ngokuchasene ne-COVID-19 kunye noBume be-SARS-CoV-2: Uphononongo." Imida kwiMicrobiology 11(1723).

I-STI-1558 iyilwe ngezi propati zilandelayo:

  • I-STI-1558 yimveliso, kwaye ifom esebenzayo i-AC1115 ibophelela kwi-Cys-145 ye-catalytic domain ye-M.pro , egcinwe nge-100% kuzo zonke iintlobo ze-SARS-CoV-2 kwaye iphumeze umsebenzi obanzi wokuchasa i-SARS-CoV-2, kubandakanywa ngokuchaseneyo nohlobo lwe-SARS-CoV-2 lwantlandlolo kunye nokwahluka okuphambili kwenkxalabo (VOCs) , njengeDelta kunye ne-Omicron.
  • I-STI-1558 yi kunye neCathepsin L inhibitor, enokuthintela ukungena okusebenzayo kwentsholongwane kwiiseli ezibambayo ngaphandle kokukhawulezisa utshintsho lwentsholongwane.
  • I-bioavailability yomlomo ukuya kuthi ga kwi-76% ngokufunxa ngokukhawuleza kunye nokuvezwa kwechiza okongeziweyo kwiplasma evumela unyango kwangoko lwe-COVID ekhaya ngolawulo lomlomo.
  • Ukunqanda ukusetyenziswa kwe-CYP34A inhibitor enamandla (umzekelo, i-ritonavir) njenge-booster ukunyusa ukubonakaliswa kweplasma ukuvumela unyango oluzimeleyo kunye nomngcipheko ophantsi wokudibana kweziyobisi.
  • A imveliso yeziyobisi ngokwenziwa ngendlela eyomeleleyo, uzinzo kunye nokuveliswa kweziyobisi ngomlinganiselo omkhulu ngeendleko ezilawulwayo ivumela ukufikelela kwihlabathi jikelele kunye nokusetyenziswa.