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

Autor:	Zarn, Katherine E., Jaramillo, Sierra A., Zapata, Anthony R., Stone, Nathan E., Jones, Ashley N., Nunnally, Haley E., Settles, Erik W., Ng, Ken, Keim, Paul S., Knudsen, Steen, Nuijten, Patricia M., Tijsma, Aloys S. L., French, Christopher T.
Předmět:	POLY ADP ribose SARS-CoV-2 SARS-CoV-2 Delta variant ANTIVIRAL agents REMDESIVIR VIRAL replication POLYMERASES
Zdroj:	PLoS ONE; 9/14/2022, Vol. 17 Issue 9, p1-9, 9p
Abstrakt:	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 (EC50) 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. [ABSTRACT FROM AUTHOR]
Databáze:	Complementary Index
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