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Literature summary for 3.1.3.32 extracted from

  • Freschauf, G.K.; Mani, R.S.; Mereniuk, T.R.; Fanta, M.; Virgen, C.A.; Dianov, G.L.; Grassot, J.M.; Hall, D.G.; Weinfeld, M.
    Mechanism of action of an imido-piperidine inhibitor of human polynucleotide kinase/phosphatase (2010), J. Biol. Chem., 285, 2351-2360.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 3.1.3.32

Cloned(Commentary)

Cloned (Comment) Organism
expression of wild-type and mutant enzymes in Escherichia coli strain DE3(BL21) pLysS Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
2-(1-hydroxyundecyl)-1-(4-nitrophenylamino)-6-phenyl-6,7a-dihydro-1H-pyrrolo[3,4-b]pyridine-5,7(2H,4aH)-dione i.e. A12B4C3, a potent, noncompetitive inhibitor of the phosphatase activity of human polynucleotide kinase/phosphatase in vitro. The inhibitor can form a ternary complex with PNKP and a DNA substrate, the inhibitor does not prevent DNA from binding to the phosphatase DNA binding site, but disrupts the secondary structure of PNKP, interaction between Trp402 of PNKP and the inhibitor. A12B4C3 sensitizes A549 human lung cancer cells to the topoisomerase I poison, camptothecin, but not the topoisomerase II poison, etoposide, in a manner similar to small interferingRNAagainst PNKP Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
A-549 cell
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 Homo sapiens
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MDA-MB-231 cell
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 Homo sapiens
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Synonyms

Synonyms Comment Organism
PNKP
-
 Homo sapiens
polynucleotide kinase/phosphatase
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 Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
 assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.4
-
 assay at Homo sapiens

General Information

General Information Comment Organism
physiological function the enzyme is involved in repair of DNA single and double strand breaks following exposure of cells to ionizing radiation Homo sapiens