polymerases

Tubercidin (Sparsomycin A), an adenosine analogue, is a nucleoside antibiotic. It is incorporated into DNA and inhibits polymerases, thereby inhibiting DNA replication and RNA and protein synthesis. This agent also exhibits antifungal and antiviral activities.

2'-Deoxyadenosine-5'-triphosphate (dATP) is a purine nucleotide and derivative of the nucleic acid adenosine 5'-triphosphate .1dATP is a substrate for DNA polymerase in the synthesis of DNA.2It is a noncompetitive inhibitor of ribonucleotide reductases, which provides feedback inhibition during DNA synthesis.1dATP has commonly been used in DNA synthesis, sequencing, and labeling in research applications.3,4dATP accumulates in adenosine deaminase deficiency, a disorder characterized by mutations in the gene for adenosine deaminase, the enzyme that catalyzes the deamination of adenosine and deoxyadenosine.5 1.Berg, J.M., Tymoczko, J.L., and Stryer, L.Key steps in nucleotide biosynthesis are regulated by feedback inhibitionBiochemistry(2002) 2.Berg, J.M., Tymoczko, J.L., and Stryer, L.DNA is replicated by polymerases that take instructions from templatesBiochemistry(2002) 3.Cadwell, R.C., and Joyce, G.F.Randomization of genes by PCR mutagenesisPCR Methods Appl.2(1)28-33(1992) 4.Steffens, D.L., Jang, G.Y., Sutter, S.L., et al.An infrared fluorescent dATP for labeling DNAGenome Res.5(4)393-399(1995) 5.Flinn, A.M., and Gennery, A.R.Adenosine deaminase deficiency: A reviewOrphanet J. Rare Dis.13(1)65(2018)

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.

5-(Hydroxymethyl)uracil is a product of oxidative DNA damage and is capable of enhancing or inhibiting potential epigenetic markers for transcription by bacterial RNA polymerases.

Tsugaric acid A significantly inhibits superoxide anion formation in fMLP CB-stimulated rat neutrophils and protects human keratinocytes against damage induced by ultraviolet B (UV B) light, indicating that tsugaric acid A can safeguard keratinocytes from photodamage.

(+)-Plakevulin A, extracted from the Okinawa sponge Plakortis sp, is an oxylipin that inhibits the enzymatic activities of DNA polymerases (pols) α and δ. Additionally, (+)-Plakevulin A induces cell apoptosis (apoptosis) and exhibits anticancer properties.

Aphidicolin 17-acetate is a selective inhibitor of eukaryotic DNA polymerase α (DNA polymeraseα) that does not inhibit DNA polymerases β and γ. It significantly suppresses DNA synthesis in sea urchin embryos and HeLa cells in vivo without affecting RNA and protein synthesis.