Protein Tyrosine Kinases

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  1. SARS-CoV Mpro inhibitor

    XP-59 is a potent inhibitor of the SARS-CoV Mpro, with a Ki of 0.1 μM.
  2. proteinase inhibitor

    FOY 251, an anti-proteolytic active metabolite Camostate, acts as a proteinase inhibitor. FOY 251 inhibits SARS-CoV-2 infection in cells assay.

  3. Merafloxacin, also known as CI 934, is a fluoroquinolone antibacterial, which was also identified as a -1 PRF inhibitor of SARS-CoV-2. Frameshift inhibition by merafloxacin is robust to mutations within the pseudoknot region and is similarly effective on -1 PRF of other beta coronaviruses. Importantly, frameshift inhibition by merafloxacin substantially impedes SARS-CoV-2 replication in Vero E6 cells, thereby providing the proof of principle of targeting -1 PRF as an effective antiviral strategy for SARS-CoV-2.
  4. AMY-101 TFA (Cp40 TFA), a peptidic inhibitor of the central complement component C3 (KD = 0.5 nM), inhibits naturally occurring periodontitis in non-human primates (NHPs). AMY-101 (Cp40) exhibits a favorable anti-inflammatory activity in models with COVID-19 severe pneumonia with systemic hyper inflammation.

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