pa , influenza

PA (224-233), Influenza is a 10-aa peptide fragment of the polymerase 2 protein in the Influenza A virus.

Baloxavir (S-033447) is a first-in-class cap-dependent endonuclease inhibitor of the influenza virus polymerase PA subunit.

RO-7 is a next-generation polymerase (PA) endonuclease inhibitor of influenza A and B viruses.

RdRP-IN-8 (compound 45) is an antiviral agent targeting influenza viruses. It inhibits the viral RNA-dependent RNA polymerase (RdRP) activity by disrupting the heterodimerization of the PA and PB1 subunits, with an IC50 value of 0.13 μM.

ATV03 is an antiviral agent exhibiting potent activity against both type A and type B influenza viruses. It inhibits the type A (H3N2) and type B influenza viruses with EC50 values of 0.78 nM and 2.02 nM, respectively. The mechanism of action of ATV03 involves the inhibition of the polymerase acidic protein (PA) and RNA-dependent RNA polymerase (RdRp), as well as the disruption of nucleoprotein, thereby exerting its antiviral effects against influenza.

ATV2301 is an orally potent anti-influenza compound with an EC50 of 1.88 nM for H1N1 and 4.77 nM for H3N2. Its anti-influenza activity results from its impact on polymerase acidic protein (PA), nucleoprotein (NP), and RNA-dependent RNA polymerase (RdRp).

PAN endonuclease-IN-2 (compound T-31) is a PAN endonuclease inhibitor (IC50: 0.15 μM) and has antiviral properties with broad-spectrum anti-influenza activity. PAN, as the N-terminal PA subunit of the polymerase-RNA complex, possesses a cap-dependent endonuclease (CEN) active site, facilitating RNA cleavage and initiating the synthesis of new RNA molecules. PAN endonuclease-IN-2 targets both influenza HA and RdRp complexes, thereby disrupting viral entry into host cells and impeding viral replication.

PAC/NP-IN-1 (Compound 30) is a dual-target influenza inhibitor that specifically binds to nucleoprotein (NP) and the C-terminal domain of the PA protein (PAc). It inhibits the influenza A virus A/WSN/33 (H1N1) with an EC50 of 3.63 μM and an IC50 of 3.08 μM. PAC/NP-IN-1 is utilized in influenza infection research.

Anti-Influenza agent 10 (Compound 41) is an inhibitor of the RNA-dependent RNA polymerase (RdRp) of the influenza A virus. It shows potent antiviral activity against the A/PR/8/34(H1N1) strain, with an IC50 of 0.29 μM and a KD of 4.11 μM. The compound functions by disrupting the interaction between the PA and PB1 subunits, inhibiting the assembly of the viral RdRp complex, and thereby blocking transcription and replication of the viral genome. Anti-Influenza agent 10 also demonstrates significant broad-spectrum efficacy against various influenza strains, such as H3N2, H3N8, and H9N2, with IC50 values of 3.96, 1.91, and 1.45 μM, respectively. It is useful for research on influenza A virus infections.

Influenza virus-IN-6 (Compound 35) is a potent inhibitor of the N-terminal domain of the polymerase acidic protein (PA N) endonuclease subunit of the influenza virus, with an inhibitory concentration 50 (IC 50) value of 0.20 μM [1].

Baloxavir-D5 is the deuterated form of Baloxavir. Baloxavir (T14495) (Baloxavir acid), derived from the prodrug Baloxavir (T14495) marboxil, acts as a first-in-class, effective, and selective cap-dependent endonuclease (CEN) inhibitor targeting the PA subunit of influenza A and B virus polymerase. It inhibits the transcription and replication of viral RNA, demonstrating potent antiviral activity.

Baloxavir-d1 is a deuterium-labeled form of Baloxavir. Baloxavir (Baloxavir acid), derived from the precursor Baloxavirmarboxil, is a pioneering and selective inhibitor of the cap-dependent endonuclease (CEN) within the polymerase PA subunit of both influenza A and B viruses. It impedes viral RNA transcription and replication, exhibiting potent antiviral activity.