polymerase

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.

Ganciclovir (2'-Nor-2'-deoxyguanosine) is an ACYCLOVIR analog that is a potent inhibitor of the Herpesvirus family including cytomegalovirus. Ganciclovir is used to treat complications from AIDS-associated cytomegalovirus infections.

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.

Poly(A) polymerase enzymatically adds a polyadenosine tail of 20-200 adenine bases to the 3' end of RNA, a process that involves integrating ATP as AMP. This modification enhances RNA stability and augments mRNA translation efficiency in eukaryotic cells, evidencing the enzyme's high tailing efficiency [1] [2].

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].

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].

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].

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

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

HCVNS5B polymerase-IN-2 (Compound 298) is an inhibitor of the Ns5b polymerase. It holds potential for research into the treatment of hepatitis C virus (HCV) 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.

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

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].

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

Taq DNA polymerase, a thermostable enzyme, is utilized in polymerase chain reactions (PCR) to amplify DNA sequences [1].

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].

Resveratrol (SRT 501) is a polyphenolic natural product, a plant antitoxin with antioxidant and chemopreventive activities. Resveratrol has a wide range of targets including COX, SIRT, LOC, etc. Resveratrol induces autophagy and apoptosis.

Niraparib (MK-4827) is a PARP inhibitor that selectively targets PARP1 and PARP2 (IC50=3.8 2.1 nM), exhibiting antitumor activity, inhibiting DNA damage repair, and inducing apoptosis.

ERDRP-0519 is an orally bioavailable small-molecule inhibitor of the Measles virus (MeV) polymerase. It effectively prevents measles disease in squirrel monkeys (Saimiri sciureus) and exhibits potent inhibition of morbilliviruses in the nanomolar range.

Olaparib (KU0059436) is a small molecule inhibitor of PARP1 PARP2 (IC50=5 1 nM), with weak inhibitory activity against PARP tankyrase-1 (IC50=1.5 μM), and is selective and orally active. Olaparib exhibits autophagy and mitochondrial autophagy activation activity.

AOH1996 is an orally active ligand for the replicasome component PCNA (proliferating cell nuclear antigen), targeting the transcription-replication conflict (TRC). It interferes with the interaction of PCNA with its binding proteins, leading to DNA replication stress and apoptosis. AOH1996 causes proteasome-dependent rpb1 degradation and lethal DNA damage by stabilizing the interaction between PCNA and RNA polymerase II, and acts synergistically with DNA damaging agents to inhibit tumor cell growth.

ART558 is a potent, selective, low molecular weight, allosteric DNA polymerase activity of Polθ inhibitor (IC50=7.9 nM). ART558 can be used for the research of cancer.

1. Dehydrocorydaline (13-Methylpalmatine) exerts anti-metastatic potential via suppression of MMPs and Bcl-2 signaling in NSC-LC cells. 2. Dehydrocorydaline stimulates p38 MAPK activation, which can enhance heterodimerization of MyoD and E proteins, thus resulting in MyoD activation and myoblast differentiation. 3. Dehydrocorydaline shows antiplatelet effects, it inhibits thrombin-induced platelet aggregation in a low dose ( IC50= 34.914 ug mL). 4. Dehydrocorydaline has anti-inflammatory and antinociceptive effects. 5. Dehydrocorydaline inhibits MCF-7 cell proliferation by inducing apoptosis mediated by regulating Bax Bcl-2, activating caspases as well as cleaving PARP.

Talazoparib (LT-673) is a new-type PARP inhibitor (IC50: 0.58 nM), It similarly binds to PARP1 2 (Kis: 1.2 0.85 nM).