viral polymerase

Dexelvucitabine (RVT) 是一种胞苷类似物，一种口服有活性的核苷逆转录酶抑制剂。它是一种 2'-脱氧胞苷抗逆转录病毒剂。它是一种有效的抗 HIV-1病毒剂，这些病毒聚合酶中含有胸苷类似物和 或 M184V 突变。

Viral polymerase-IN-1 hydrochloride 是一种 Gemcitabine 衍生物，有效抑制甲型和乙型流感病毒 (influenza) 感染，IC90值为 11.4-15.9 μM。Viral polymerase-IN-1 hydrochloride 对 SARS-CoV-2感染具有活性。Viral polymerase-IN-1 hydrochloride 通过影响细胞中的病毒 RNA 复制 转录来抑制流感病毒感染。

PP7 是一种PB1-PB2互作抑制剂，IC50为 8.6 μM。PB1-PB2 抑制病毒聚合酶的活性，IC50为9.5 μM。它对甲型流感病毒 A 包括 (H1N1)pdm09 (EC50=1.4 μM)，A(H7N9)，A(H9N2) 亚型具有抗病毒活性。

Galidesivir (BCX4430) 是一种广谱抗病毒化合物，是一种腺苷类似物，能抑制病毒 RNA 依赖的 RNA 聚合酶 (RdRp) 活性。Galidesivir 在体外对多种 RNA 病毒病原体有抑制作用，可减少受感染动物的肺部感染。

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

AS-136A 是一种具有口服活性的麻疹病毒 RNA 依赖性 RNA 聚合酶 （RdRp） 抑制剂，具有抗病毒活性，抑制麻疹病毒，阻断病毒 RNA 的合成。

GS-6620 PM 是GS-6620的衍生物。GS-6620是一种口服的抗丙型肝炎病毒聚合酶抑制剂，是一种新型强效的C-核苷腺嘌呤类似物单磷酸酯原药。GS-6620对其他病毒的活性有限，对密切相关的牛病毒性腹泻病毒仅保持部分活性（EC50，1.5μM）。

Foscarnet sodium (Phosphonoformate) 是一种病毒 DNA 聚合酶活性抑制剂，可逆地抑制病毒复制。它是一种用于治疗巨细胞病毒性视网膜炎的抗病毒剂。

Valganciclovir hydrochloride (Valganciclovir HCl) 是 ganciclovir 的原药，具有抗巨细胞病毒活性，可抑制病毒 DNA 聚合酶和病毒复制。

Penciclovir (BRL 39123) 是一种疱疹病毒核苷类似物 DNA 聚合酶抑制剂。它作用于HSV1 和 2，IC50分别为 0.04-1.8 μg mL 和 0.06-4.4 μg mL。

Tenofovir diphosphate TEA （TFV-DP TEA）是TFV-DP的三乙胺盐，是一种ATP竞争性的DNA聚合酶 (DNA polymerases) 抑制剂，能够抑制HIV-1逆转录酶（HIV-1 reverse transcriptase）。它通过掺入病毒DNA链中，终止病毒DNA的合成，从而抑制病毒基因组的复制，具有抗HIV HBV的潜力。

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) 是丙型肝炎病毒非结构蛋白 5B 的非核苷抑制剂，是一种 RNA 依赖性 RNA 聚合酶，具有抗 HCV 的潜在活性。

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) 为针对流感病毒的抑制剂。该化合物通过阻断 PA 与 PB1 亚基间的异二聚化，有效抑制病毒 RNA 依赖性 RNA 聚合酶 (RdRP) 的活性，具有显著的抑制效果 (IC50=0.13 μM)。

ddATP (2',3'-Dideoxyadenosine 5'-triphosphate) tetrasodium 是一种 2',3'-二脱氧肌苷的活性代谢物，能够抑制 DNA polymerase 的链延长。ddATP tetrasodium 可用于 Sanger 法 DNA 测序和病毒感染研究。

BA-AZT1 是一种 HBV 聚合酶 (HBV polymerase) 和 牛磺胆酸钠共转运多肽 (NTCP) 的抑制剂。它能够抑制病毒衣壳蛋白 HBsAg 和 HBeAg 的分泌，其 IC50 分别为 0.65 µM 和 13.42 µM，同时抑制 HBV DNA 复制，IC50 为 0.70 µM。

GHP-88309 是一种口服有效的广谱抗副黏病毒 (paramyxoviruses) 剂，作用于病毒聚合酶 (viral polymerase)，干扰病毒 RNA 合成，并能够抑制呼吸道合胞病毒 (RSV)、麻疹病毒 (MeV) 和犬瘟热病毒 (CDV)，其EC50范围为0.06-1.2 μM。在小鼠模型中，GHP-88309 显示出抗感染活性。

Aranotin 是一种从金黄色蜘蛛中分离的真菌毒素，具有对抗脊髓灰质炎病毒、柯萨奇病毒、犀牛和副流感病毒等 RNA 病毒的活性。Aranotin 通过阻碍 RNA 依赖性RNA 聚合酶的活性来抑制病毒RNA 的合成。

Oosporein 是一种由三侧盲杆菌产生的霉菌毒素，具有抗菌、抗病毒和杀虫活性，抑制 P. infestans，抑制单纯疱疹病毒 1 型 DNA 聚合酶，可用于研究病毒感染。

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.

Ribavirin-13C5is intended for use as an internal standard for the quantification of ribavirin by GC- or LC-MS. Ribavirin is an antiviral guanosine nucleoside analog.1,2Upon entry into cells, ribavirin is metabolized to an active triphosphate form that induces viral RNA chain termination and inhibits viral polymerases. It reduces replication in a panel of seven RNA and four DNA viruses in Vero cells (EC50s = 2-95 μg/ml).3Ribavirin also reduces replication of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) in Vero cells (EC50= 109.5 μM).4Aerosol administration of ribavirin (30 mg/kg) reduces mortality in a mouse model of influenza A infection.5Formulations containing ribavirin have been used in the treatment of respiratory syncytial virus (RSV), hepatitis C virus (HCV), and viral hemorrhagic fevers. 1.Gilbert, B.E., and Knight, V.Biochemistry and clinical applications of ribavirinAntimicrob. Agents Chemother.30(2)201-205(1986) 2.Gordon, C.J., Tchesnokov, E.P., Woolner, E., et al.Remdesivir is a direct-acting antiviral that inhibits RNA-dependent RNA polymerase from severe acute respiratory syndrome coronavirus 2 with high potencyJ. Biol. Chem.295(20)6785-6797(2020) 3.Kirsi, J.J., North, J.A., McKernan, P.A., et al.Broad-spectrum antiviral activity of 2-β-D-ribofuranosylselenazole-4-carboxamide, a new antiviral agentAntimicrob. Agents Chemother.24(3)353-361(1983) 4.Wang, M., Cao, R., Zhang, L., et al.Remdesivir and chloroquine effectively inhibit the recently emerged novel coronavirus (2019-nCoV) in vitroCell Res.30(3)269-271(2020) 5.Wilson, S.Z., Knight, V., Wyde, P.R., et al.Amantadine and ribavirin aerosol treatment of influenza A and B infection in miceAntimicrob. Agents Chemother.17(4)642-648(1980)