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Stenoparib, an inhibitor of cellular poly (ADP-ribose) polymerases (PARPs), blocks in vitro replication of SARS-CoV-2 variants

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  • معلومة اضافية
    • Contributors:
      Gallay, Philippe A.; Flinn Foundation; Arizona Board of Regents Technology and Research Initiative Fund; Cowden Endowment for Microbiology; Allarity Therapeutics; Viroclinics-DDL
    • بيانات النشر:
      Public Library of Science (PLoS)
    • الموضوع:
      2022
    • Collection:
      PLOS Publications (via CrossRef)
    • نبذة مختصرة :
      We recently published a preliminary assessment of the activity of a poly (ADP-ribose) polymerase (PARP) inhibitor, stenoparib, also known as 2X-121, which inhibits viral replication by affecting pathways of the host. Here we show that stenoparib effectively inhibits a SARS-CoV-2 wild type (BavPat1/2020) strain and four additional variant strains; alpha (B.1.1.7), beta (B.1.351), delta (B.1.617.2) and gamma (P.1) in vitro , with 50% effective concentration (EC 50 ) estimates of 4.1 μM, 8.5 μM, 24.1 μM, 8.2 μM and 13.6 μM, respectively. A separate experiment focusing on a combination of 10 μM stenoparib and 0.5 μM remdesivir, an antiviral drug, resulted in over 80% inhibition of the alpha variant, which is substantially greater than the effect achieved with either drug alone, suggesting at least additive effects from combining the different mechanisms of activity of stenoparib and remdesivir.
    • الرقم المعرف:
      10.1371/journal.pone.0272916
    • الدخول الالكتروني :
      http://dx.doi.org/10.1371/journal.pone.0272916
      https://dx.plos.org/10.1371/journal.pone.0272916
    • Rights:
      http://creativecommons.org/licenses/by/4.0/
    • الرقم المعرف:
      edsbas.E8500D4F