dna polymerase i

Azelaic acid (Anchoic acid) is a component of hair and skin conditioners and is produced by the ozonolysis of oleic acid. Azelaic acid has bacteriostatic activity against Propionibacterium acnes and Staphylococcus epidermidis by inhibiting protoprotein synthesis in microbial cells. Azelaic acid also has the ability to inhibit pigmentation due to its free radical scavenging action.

Bakuchiol possesses anti-tumor,and anti-helmenthic properties. It has cytotoxic activity, mainly due to its DNA polymerase1 inhibiting activity. Bakuchiol has anti-bacterial activity against oral pathogens, has great potential for use in food additives and mouthwash for preventing and treating dental caries.

DNA polymerase-IN-1, a DNA polymerase inhibitor, exhibited antiproliferative activity against tumor cells with a half-inhibitory concentration (IC50) of 20.7 μM. DNA polymerase-IN-1 inhibited Taq DNA polymerase with an IC50 of less than 250 μM. DNA polymerase-IN-1 was shown to inhibit Taq DNA polymerase by RT- DNA polymerase-IN-1 showed antiretroviral activity in vitro by RT-PCR assay and can be used to study oxidative damage and colorectal cancer.

Ibezapolstat (ACX-362E) is an orally active DNA polymerase IIIC inhibitor, an antibiotic with antibacterial activity that inhibits Clostridioides difficile (C. difficile) and can be used for studying Clostridioides difficile infections.

DNA polymerase-IN-6 (Compound 27) exhibits inhibitory activity against DNA polymerase, with EC50 values of 0.33 µM for HCMV, 1.9 µM for HSV-1, 0.76 µM for HSV-2, and 0.066 µM for EBV.

DNA polymerase-IN-7 is a non-competitive inhibitor of DNA polymerase beta (DNA Polymeraseβ) with an IC50 of 112 nM and a Ki of 35 nM. It effectively inhibits the lyase activity of DNA polymerase beta and interferes with the binding of the lyase domain to DNA. This compound is applicable in cancer research, including studies on cervical cancer.

DNA polymerase-IN-2 (Compd 3c), a coumarin derivative, inhibits Taq DNA polymerase with an IC50 value of 48.25 μM and shows potential for value-added disease research [1].

DNA polymerase-IN-3 (Compd 5b), a coumarin derivative, inhibits Taq DNA polymerase and shows potential applications in proliferative disease research [1].

DNA polymerase-IN-4 (Compd 5c), a coumarin derivative, demonstrates antiretroviral activity with an IC50 of 134.22 μM [1].

DNA polymerase-IN-5 (compound 42) is a broad-spectrum antiviral agent effective against herpesviruses. It exhibits inhibitory activity against CMV and VZV with IC50 values of 6.6 μM and 4.8 μM, respectively.

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.

4-Demethoxy-7,9-di-epi-daunorubicin is a derivative of Daunorubicin and an anthracycline antibiotic (antibiotics). It binds to calf thymus DNA, forming a complex with stacked DNA base pairs. This compound inhibits nucleic acid polymerases in prokaryotes, including Escherichia coli DNA polymerase I (DNA polymerase I) and RNA polymerase (RNA polymerase). 4-Demethoxy-7,9-di-epi-daunorubicin is utilized in cancer and infection research.

Kelletinin I inhibit preferentially DNA polymerase alpha.

Thiocoraline is a depsipeptide and DNAbis-intercalator originally isolated fromMicromonosporawith antibacterial and anticancer activities.1,2It is active against the Gram-positive bacteriaS. aureus,B. subtilis, andM. luteus(MICs = 0.05, 0.05, and 0.03 μg/ml, respectively) but not Gram-negativeE. coli,K. pneumoniae, orP. aeruginosa(MICs = >100 μg/ml for all).1Thiocoraline inhibits RNA and DNA polymerase and thymidylate synthase (IC50s = 6, 6, and 15 μg/ml, respectively), as well as RNA and DNA synthesisin vitro(IC50s = 0.008 and 0.4 μg/ml, respectively). It is cytotoxic to P388, A549, HT-29, and MEL-28 cancer cells (IC50s = 0.002, 0.002, 0.01, and 0.002 μg/ml, respectively). 1.Romero, F., Espilego, F., Pérez Baz, J., et al.Thiocoraline, a new depsipeptide with antitumor activity produced by a marine Micromonospora. I. Taxonomy, fermentation, isolation, and biological activitiesJ. Antibiot. (Tokyo)50(9)734-737(1997) 2.Negri, A., Marco, E., García-Hernández, V., et al.Antitumor activity, X-ray crystal structure, and DNA binding properties of thiocoraline A, a natural bisintercalating thiodepsipeptideJ. Med. Chem.50(14)3322-3333(2007)

POL1-IN-1 (Compound 3A) can effectively inhibit the transcription of RNA polymerase I in the A375 malignant melanoma cell line but has no effect on polymerase II.

Pidnarulex HCl is the salt form of CX-5461, a first-in-class non-genotoxic small molecule targeted inhibitor of RNA polymerase I (Pol I) that activates the p53 pathway without causing DNA damage. CX-5461 selectively inhibits rRNA synthesis by Pol I in the nucleolus, but does not inhibit mRNA synthesis by RNA Polymerase II (Pol II) and does not inhibit DNA replication or protein synthesis. Inhibition of Pol I results in nucleolar stress and release of ribosomal proteins (RP) from the nucleolus. The RP bind to Mdm2 and liberate p53 to orchestrate apoptosis in cancer cells. CX-5461 demonstrates a favorable preclinical profile, potently and selectively kills cancer cells, demonstrates robust in vivo efficacy in multiple models, and has demonstrated oral bioavailability in multiple species.

Antiviral agent 34 is a potent, orally active, broad-spectrum small-molecule inhibitor against influenza A/B viruses, targeting the core site of influenza virus RNA-dependent RNA polymerase (RdRp) with an EC₅₀ of 0.8 nM against H1N1. Antiviral agent 34 can be used for studying the mechanisms of influenza virus infection and for drug development.

BRC4wt, an acetylated peptide originating from the BRC4 repeat within human BRCA2 (1521-1536), acts as an inhibitor of the BRCA2 and RAD51 protein-protein interaction. When linked to the cationic cell-penetrating peptide (Arg)9, it effectively shortens DNA replication tract lengths and diminishes the frequency of homologous repair of camptothecin-induced DNA damage in vitro. Additionally, BRC4wt enhances the efficacy of the poly(ADP-ribose) polymerase (PARP) inhibitor olaparib in inducing cell death in HeLa human cervical cancer and U2OS human osteosarcoma cells, albeit it does not affect non-cancerous hTERT RPE-1, MRC-5, or MCF-10A cells.

ZYN57939 (MTR-106) is RNA polymerase I inhibitor for treating RNA polymerase I- mediated diseases. ZYN57939 showed inhibitory activity with IC50 of 0.855 μM against human HT- 29 cancer cell lines.