viral polymerase

Viral polymerase-IN-1 hydrochloride, a derivative of Gemcitabine, effectively inhibits influenza A and B virus infections with IC90 values between 11.4 and 15.9 μM, and shows activity against SARS-CoV-2 infection by interfering with viral RNA replication transcription within cells [1].

Galidesivir (BCX4430) is a broad-spectrum antiviral compound, an adenosine analog that inhibits viral RNA-dependent RNA polymerase (RdRp) activity.Galidesivir inhibits a wide range of RNA viral pathogens in vitro, and reduces lung infections in infected animals.

AS-136A is an orally active measles virus RNA-dependent RNA polymerase (RdRp) inhibitor with antiviral activity that inhibits measles virus and blocks viral RNA synthesis.

GS-6620 PM is a derivative of GS-6620, an orally administered anti-hepatitis C virus polymerase inhibitor and a novel potent C-nucleoside adenine analogue monophosphate prodrug.GS-6620 has limited activity against other viruses and maintains only partial activity against the closely related bovine viral diarrhea virus (EC50, 1.5 μM).

Foscarnet sodium (Phosphonoformate) is an antiviral agent used in the treatment of cytomegalovirus retinitis. Foscarnet also shows activity against human herpesviruses and HIV.

Valganciclovir hydrochloride (Valganciclovir HCl) is a hydrochloride salt form of valganciclovir, a prodrug form of ganciclovir, a nucleoside analog of 2'-deoxyguanosine, with antiviral activity. After phosphorylation, valganciclovir is incorporated into DNA, resulting in inhibition of viral DNA polymerase, and viral replication.

Penciclovir (BRL 39123) is a Herpesvirus Nucleoside Analog DNA Polymerase Inhibitor. In HSV infected cells, penciclovir is phosphorylated by viral thymidine kinase and subsequently converted by cellular kinases into the active metabolite, penciclovir triphosphate, which competitively inhibits viral HSV polymerase by blocking deoxyguanosine triphosphate substrate binding. As a result, herpes viral DNA synthesis and replication are selectively inhibited.

Tenofovir diphosphate TEA (TFV-DP TEA) is the triethylamine salt of TFV-DP, an ATP-competitive DNA polymerase inhibitor that inhibits HIV-1 reverse transcriptase. It has anti-HIV HBV potential through its incorporation into the viral DNA strand to terminate viral DNA synthesis and thus inhibit viral genome replication.

Galidesivir hydrochloride is an inhibitor of viral RNA-dependent RNA polymerase (RdRp). It inhibits SARS-CoV-2 by tightly binding to its RdRp.

Galidesivir is a viral RNA-dependent RNA polymerase (RdRP) inhibitor and broad spectrum antiviral nucleotide.In vitro, galidesivir displays antiviral activity against a range of RNA viruses, including bunyaviruses, arenaviruses, paramyxoviruses, coronaviruses, and flaviviruses (EC50values range from 3 μM to >100 μM). Galidesivir protects against Ebola and Marburg viral infection in animal models.

Dasabuvir (ABT-333) is a non-nucleoside inhibitor of the hepatitis C virus (HCV) non-structural protein 5B (NS5B), an RNA-dependent RNA polymerase. Upon administration and intracellular uptake, dasabuvir binds HCV NS5B polymerase, blocking viral RNA synthesis and replication. The HCV NS5B protein is essential for the replication of the HCV RNA genome.

PP7 is a potent inhibitor of PB1-PB2 interaction(IC50 of 8.6 μM).

Cidofovir dihydrate (HPMPC) is an anti-CMV drug, It can suppress CMV replication by selective inhibition of viral DNA polymerase and therefore prevention of viral replication and transcription. Cidofovir dihydrate is an injectable antiviral medication primarily used as a treatment for cytomegalovirus (CMV) retinitis- an infection of the retina of the eye in people with AIDS

Galidesivir triphosphate is a substrate for viral RNA-dependent RNA polymerase (RDRP), resulting in termination of viral RNA replication and thus serves as an antiviral. Galidesivir triphosphate inhibits HCV NS5B RNA polymerase activity and protects mice against Ebola. Galidesivir triphosphate (Immucillin-A triphosphate) is converted by the prodrug Galidesivir.

NHC-triphosphate is a weak alternative substrate for the viral polymerase and changes the mobility of the product in polyacrylamide electrophoresis gels.

Lobucavir inhibits the replication of the HIV virus in T cells, monocytes & macrophages in vitro by inhibiting DNA polymerase and viral DNA synthesis.

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.

ddATP (2',3'-Dideoxyadenosine 5'-triphosphate) tetrasodium is an active metabolite of 2',3'-dideoxyinosine and functions as a chain elongation inhibitor for DNA polymerase. It is utilized in DNA sequencing using the Sanger method and in research related to viral infections.

BA-AZT1 acts as an inhibitor of HBV polymerase (HBV polymerase) and sodium taurocholate cotransporting polypeptide (NTCP). It hinders the secretion of viral capsid proteins HBsAg and HBeAg, with IC50 values of 0.65 µM and 13.42 µM, respectively, and inhibits HBV DNA replication with an IC50 of 0.70 µM.

GHP-88309 is an orally active, broad-spectrum anti-paramyxovirus agent that targets viral polymerase, interrupting viral RNA synthesis. It effectively inhibits respiratory syncytial virus (RSV), measles virus (MeV), and canine distemper virus (CDV) with an EC50 of 0.06-1.2 μM. In mouse models, GHP-88309 demonstrates significant anti-infective activity.

Aranotin is a fungal toxin isolated from Arachniotus aureus with activity against RNA viruses such as poliovirus, coxsackie virus, and rhino- and parainfluenza viruses. Aranotin inhibits viral RNA synthesis by impeding the activity of RNA-dependent RNA polymerase.

Dexelvucitabine (RVT), a nucleoside reverse transcriptase inhibitor, is used potentially for the treatment of HIV infection.

Oosporein is a mycotoxin produced by Trichoderma reesei with antimicrobial, antiviral and insecticidal activities, inhibits P. infestans, inhibits herpes simplex virus type 1 DNA polymerase, and can be used in the study of viral infections.

NHC-triphosphate triammonium is an active phosphorylated intracellular metabolite of β-d-N4-Hydroxycytidine (NHC) as a triphosphate form[1]. NHC-triphosphate triammonium is a weak alternative substrate for the viral polymerase and can be incorporated into HCV replicon RNA[1][2]. In an intracellular metabolism assay, HCV replicon cells are treated with 10 μM 3H-labeled NHC, and intracellular nucleotide levels are determined after 1, 2 and 8 hours incubations. NHC is rapidly convered into the mono-, di-, and triphosphate forms, and NHC-TP reaches up to 71.12 pM after 8 hours[1].NHC-triphosphate triammonium (NHC-TP) (5-40 μM) absence leads to full-length polymerization products, it can be a weak alternative substrate. In addition, incorporation of NHC-TP instead of CTP increases the molecular weight of the polymerization product by 16 (one extra oxygen) for each event and an obvious electrophoretic shift is observed in cell-free HCV NS5B polymerization reactions[1].Huh-7 cells are incubated with (10-50 μM; 4 h) NHC or a McGuigan phosphoramidate prodrug of NHC. Intracellular levels of the parental compounds and phosphorylated metabolites are measured using LC-MS/MS. Small amounts of NHC-monophosphate (MP) and NHC-diphosphate (DP) can be observed, while NHC-triphosphate triammonium remains the most abundant metabolite[2].NHC-triphosphate triammonium (NHC-TP) metabolite may directly target the viral polymerase and behave as a nonobligate chain terminator. It plays a prominent role in inhibiting early negative-strand RNA synthesis, either through chain termination or mutagenesis, which may in turn interfere with correct replicase complex formation. [1]. Stuyver LJ,et al. Ribonucleoside analogue that blocks replication of bovine viral diarrhea and hepatitis C viruses in culture.Antimicrob Agents Chemother. 2003 Jan;47(1):244-54. [2]. Maryam Ehteshami, et al. Characterization of β-d- N4-Hydroxycytidine as a Novel Inhibitor of Chikungunya Virus.