rna polymerase

RNA polymerase-IN-3 is an inhibitor of bacterial RNA polymerase (RNAP) with antimicrobial properties. It suppresses RNA synthesis by competitively blocking UTP from binding to RNAP, with an inhibitory concentration (IC50) of 0.28 μM. RNA polymerase-IN-3 holds potential for research into bacterial infections.

RNA polymerase II-IN-1 (compound 19iv), an amatoxin, selectively inhibits RNA polymerase II (Pol II) with an IC50 of 36.66 nM and exhibits heightened cytotoxicity towards cancer cells while reducing toxicity in normal cells compared to α-Amanitin [1].

RNA polymerase II-IN-2 (compound 20iii), a potent inhibitor of RNA polymerase II (Pol II) with a K i value of 9.5 nM, exhibits cytotoxicity against cancer cells, demonstrating toxicity levels 2 and 5 times higher than α-amanitin in CHO and HEK293 cells, respectively [1].

RNA polymerase-IN-1 (compound 4) acts as an inhibitor of DNA-dependent RNA polymerase. Additionally, it inhibits CYP isozymes [1].

RNA polymerase-IN-2 (compound 5) acts as an inhibitor of DNA-dependent RNA polymerase. Additionally, it inhibits CYP isozymes [1].

T7 RNA polymerase, expressed by Escherichia coli from the T7 bacteriophage RNA polymerase gene, is a highly specific enzyme utilized for in vitro transcription (IVT) of mRNA. This polymerase requires Mg 2+ and selects only DNA templates that contain the T7 promoter sequence, whether single-stranded or double-stranded. It employs NTPs to synthesize RNA that is complementary to the single-stranded DNA following the promoter [1] [2].

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.

Ribavirin (Tribavirin) is a synthetic nucleoside analog of ribofuranose with activity against hepatitis C virus and other RNA viruses.

Rifabutin (LM-427) inhibits bacterial DNA-dependent RNA polymerase, thereby suppressing the initiation of RNA formation and leading to inhibition of RNA synthesis and transcription. Rifabutin is a semisynthetic ansamycin antibiotic with potent antimycobacterial properties.

Rifapentine (Rifapentinum) is a long-acting, cyclopentyl-substituted derivative of rifamycin used to treat mycobacterium infections.

Juglone (Regianin) is a natural naphthoquinone found in the black walnut (J. nigra) and other plants in the Juglandaceae family. Juglone also irreversibly inhibits peptidyl-prolyl cis/trans isomerases of the parvulin family, including human Pin1, yeast Ess1/Ptf1, and E. coli parvulin (Ki = 55.9 nM). Juglone also blocks transcription by RNA polymerases I, II, and III (IC50s = 2-7 μM) and attenuates kidney fibrosis in rats treated with unilateral ureteral obstruction, both through Pin1-independent mechanisms.

Fidaxomicin (Tiacumicin B) is a semisynthetic macrolide antibiotic used to treat Clostridium difficile-associated diarrhea in adults. Fidaxomicin has minimal systemic absorption and has not been linked to serum enzyme elevations during therapy or to instances of clinically apparent, acute liver injury.

Rifalazil (KRM-1648) is a benzophenazine antibiotic with antibacterial activity. It inhibits bacterial RNA polymerase, blocking the β-subunit, and is used in Chlamydia infection research.

AVG-233 is an orally available RNA-dependent RNA polymerase (RdRp) inhibitor with antiviral activity that blocks respiratory syncytial virus and SARS-CoV-2 replication.AVG-233 is used in the study of respiratory syncytial virus infections.

Clevudine (Levovir) is a synthetic pyrimidine analogue with activity against hepatitis B virus (HBV). Intracellularly, clevudine is phosphorylated to its active metabolites, clevudine monophosphate and triphosphate. The triphosphate metabolite competes with thymidine for incorporation into viral DNA, thereby causing DNA chain termination and inhibiting the function of HBV DNA polymerase (reverse transcriptase). Clevudine has a long half-life and shows significant reduction of covalently closed circular DNA (cccDNA), therefore the patient is less likely to have a relapse after treatment is discontinued.

2'-beta-C-Methyl inosine (2'-C-Methylinosine) is an HCV RNA polymerase inhibitor with antiviral activity and is being studied for the treatment of hepatitis C virus infection.

Filibuvir (PF-00868554) is a selective and noncovalent inhibitor of HCV NS5B RNA-dependent RNA polymerase. Filibuvir inhibits genotype 1a and 1b replicons with EC50s of 59 nM.

Favipiravir is a potent and selective RNA-dependent RNA polymerase inhibitor for the treatment of influenza virus infections.

Metarrestin (ML246) is a first-in-class perinucleolar compartment inhibitor with a favorable PK profile, which effectively suppresses metastasis. Metarrestin disrupts the nucleolar structure and inhibits RNA polymerase (Pol) I transcription, at least in part by interacting with the translation elongation factor eEF1A2.

Quarfloxin (CX-3543) is a fluoroquinolone derivative with antineoplastic activity with IC50 values in the nanomolar range in neuroblastoma cells. Quarfloxin disrupts the interaction between the nucleolin protein and a G-quadruplex DNA structure in the ribosomal DNA template.

BMH-21, a small molecule DNA intercalator, binds ribosomal DNA and inhibits RNA polymerase I (Pol I) transcription and not affects phosphorylation of H2AX.

Emivirine (MKC-442) is a potent and selective nonnucleoside reverse transcriptase inhibitor for human immunodeficiency virus type 1.

Cynaroside (Luteolin 7-O-Glucoside) is a flavone, a flavonoid-like chemical compound. It has an anti-oxidant effect, inhibiting lipid and protein oxidation.

Thio-ITP, also known as 6-Thioinosine 5'-triphosphate, is a competitive inhibitor of RNA polymerase activity. It exhibits a strong apparent affinity towards the polymerases, with Ki values of 40.9 μM for RNA polymerase I and 38.0 μM for RNA polymerase II.