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Literature summary extracted from

  • Freschauf, G.K.; Karimi-Busheri, F.; Ulaczyk-Lesanko, A.; Mereniuk, T.R.; Ahrens, A.; Koshy, J.M.; Rasouli-Nia, A.; Pasarj, P.; Holmes, C.F.; Rininsland, F.; Hall, D.G.; Weinfeld, M.
    Identification of a small molecule inhibitor of the human DNA repair enzyme polynucleotide kinase/phosphatase (2009), Cancer Res., 69, 7739-7746.
    View publication on PubMed

Application

EC Number Application Comment Organism
2.7.1.78 medicine A12B4C3 enhances the radiosensitivity of human A549 lung carcinoma and MDA-MB-231 breast adenocarcinoma cells by a factor of two Homo sapiens

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.7.1.78
-
 Homo sapiens
2.7.1.78
-
 Schizosaccharomyces pombe
2.7.1.78
-
 Mus musculus
3.1.3.32
-
 Mus musculus
3.1.3.32
-
 Homo sapiens
3.1.3.32
-
 Schizosaccharomyces pombe

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.1.78 2-(1-hydroxyundecyl)-1-(4-nitrophenylamino)-6-phenyl-6,7a-dihydro-1H-pyrrolo[3,4-b]pyridine-5,7(2H,4aH)-dione A12B4C3 Homo sapiens
2.7.1.78 2-(1-hydroxyundecyl)-1-(4-nitrophenylamino)-6-phenyl-6,7a-dihydro-1H-pyrrolo[3,4-b]pyridine-5,7(2H,4aH)-dione A12B4C3 Mus musculus
2.7.1.78 2-(1-hydroxyundecyl)-1-(4-nitrophenylamino)-6-phenyl-6,7a-dihydro-1H-pyrrolo[3,4-b]pyridine-5,7(2H,4aH)-dione A12B4C3 Schizosaccharomyces pombe
2.7.1.78 2-(1-hydroxyundecyl)-1-(4-nitrophenylamino)-6-phenyl-6,7a-dihydro-1H-pyrrolo[3,4-b]pyridine-5,7(2H,4aH)-dione A12B4C3 Tequatrovirus T4
2.7.1.78 2-(hydroxy(3,4,5-trimethoxyphenyl)methyl)-1-(4-nitrophenylamino)-6-phenyl-6,7a-dihydro-1H-pyrrolo[3,4-b]pyridine-5,7(2H,4aH)-dione A6B4C3 Homo sapiens
2.7.1.78 2-(hydroxy(phenyl)methyl)-1-(4-nitrophenylamino)-6-phenyl-6,7a-dihydro-1H-pyrrolo[3,4-b]pyridine-5,7(2H,4aH)-dione A1B4C3 Homo sapiens
2.7.1.78 2-(hydroxy(thiophen-2-yl)methyl)-6-methyl-1-(phenylamino)-6,7a-dihydro-1H-pyrrolo[3,4-b]pyridine-5,7(2H,4aH)-dione A39B1C2 Homo sapiens
2.7.1.78 tert-butyl 2-(1-hydroxy-2,2-diphenylethyl)-6-methyl-5,7-dioxo-2,4a,5,6,7,7a-hexahydro-1H-pyrrolo[3,4-b]pyridine-1yl-carbamate A26B11C2 Homo sapiens
3.1.3.32 2-(1-hydroxyundecyl)-1-(4-nitrophenylamino)-6-phenyl-6,7a-dihydro-1H-pyrrolo[3,4-b]pyridine-5,7(2H,4aH)-dione A12B4C3 Homo sapiens
3.1.3.32 2-(1-hydroxyundecyl)-1-(4-nitrophenylamino)-6-phenyl-6,7a-dihydro-1H-pyrrolo[3,4-b]pyridine-5,7(2H,4aH)-dione A12B4C3 Mus musculus
3.1.3.32 2-(1-hydroxyundecyl)-1-(4-nitrophenylamino)-6-phenyl-6,7a-dihydro-1H-pyrrolo[3,4-b]pyridine-5,7(2H,4aH)-dione A12B4C3 Schizosaccharomyces pombe
3.1.3.32 2-(hydroxy(3,4,5-trimethoxyphenyl)methyl)-1-(4-nitrophenylamino)-6-phenyl-6,7a-dihydro-1H-pyrrolo[3,4-b]pyridine-5,7(2H,4aH)-dione A6B4C3 Homo sapiens
3.1.3.32 2-(hydroxy(phenyl)methyl)-1-(4-nitrophenylamino)-6-phenyl-6,7a-dihydro-1H-pyrrolo[3,4-b]pyridine-5,7(2H,4aH)-dione A1B4C3 Homo sapiens
3.1.3.32 2-(hydroxy(thiophen-2-yl)methyl)-6-methyl-1-(phenylamino)-6,7a-dihydro-1H-pyrrolo[3,4-b]pyridine-5,7(2H,4aH)-dione A39B1C2 Homo sapiens
3.1.3.32 tert-butyl 2-(1-hydroxy-2,2-diphenylethyl)-6-methyl-5,7-dioxo-2,4a,5,6,7,7a-hexahydro-1H-pyrrolo[3,4-b]pyridin-1-ylcarbamate A26B11C2 Homo sapiens

Metals/Ions

EC Number Metals/Ions Comment Organism Structure
2.7.1.78 Mg2+
-
 Homo sapiens
2.7.1.78 Mg2+
-
 Schizosaccharomyces pombe
2.7.1.78 Mg2+
-
 Tequatrovirus T4
2.7.1.78 Mg2+
-
 Mus musculus

Molecular Weight [Da]

EC Number Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
2.7.1.78 57100
-
-
 Homo sapiens
3.1.3.32 57100
-
 x * 57100 Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.7.1.78 ATP + 5'-dephospho-DNA Homo sapiens
-
 ADP + 5'-phospho-DNA
-
 r
2.7.1.78 ATP + 5'-dephospho-DNA Schizosaccharomyces pombe
-
 ADP + 5'-phospho-DNA
-
 r
2.7.1.78 ATP + 5'-dephospho-DNA Tequatrovirus T4
-
 ADP + 5'-phospho-DNA
-
 r
2.7.1.78 ATP + 5'-dephospho-DNA Mus musculus
-
 ADP + 5'-phospho-DNA
-
 r

Organism

EC Number Organism UniProt Comment Textmining
2.7.1.78 Homo sapiens
-
-
-
2.7.1.78 Mus musculus Q9JLV6
-
-
2.7.1.78 Schizosaccharomyces pombe
-
-
-
2.7.1.78 Tequatrovirus T4
-
-
-
3.1.3.32 Homo sapiens
-
-
-
3.1.3.32 Mus musculus
-
-
-
3.1.3.32 Schizosaccharomyces pombe
-
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
2.7.1.78
-
 Homo sapiens
2.7.1.78
-
 Schizosaccharomyces pombe
2.7.1.78
-
 Mus musculus
3.1.3.32
-
 Mus musculus
3.1.3.32
-
 Homo sapiens
3.1.3.32
-
 Schizosaccharomyces pombe

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.7.1.78 A-549 cell
-
 Homo sapiens
-
2.7.1.78 MDA-MB-231 cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.7.1.78 ATP + 5'-dephospho-DNA
-
 Homo sapiens ADP + 5'-phospho-DNA
-
 r
2.7.1.78 ATP + 5'-dephospho-DNA
-
 Schizosaccharomyces pombe ADP + 5'-phospho-DNA
-
 r
2.7.1.78 ATP + 5'-dephospho-DNA
-
 Tequatrovirus T4 ADP + 5'-phospho-DNA
-
 r
2.7.1.78 ATP + 5'-dephospho-DNA
-
 Mus musculus ADP + 5'-phospho-DNA
-
 r

Subunits

EC Number Subunits Comment Organism
3.1.3.32 ? x * 57100 Homo sapiens

Synonyms

EC Number Synonyms Comment Organism
2.7.1.78 hPNKP
-
 Homo sapiens
2.7.1.78 mPNKP
-
 Mus musculus
2.7.1.78 PNKP
-
 Homo sapiens
2.7.1.78 PNKP
-
 Schizosaccharomyces pombe
2.7.1.78 PNKP
-
 Tequatrovirus T4
2.7.1.78 PNKP
-
 Mus musculus
2.7.1.78 polynucleotide kinase/phosphatase
-
 Homo sapiens
2.7.1.78 polynucleotide kinase/phosphatase
-
 Schizosaccharomyces pombe
2.7.1.78 polynucleotide kinase/phosphatase
-
 Tequatrovirus T4
2.7.1.78 polynucleotide kinase/phosphatase
-
 Mus musculus
2.7.1.78 T4 PNK
-
 Tequatrovirus T4
3.1.3.32 polynucleotide kinase/phosphatase
-
 Mus musculus
3.1.3.32 polynucleotide kinase/phosphatase
-
 Homo sapiens
3.1.3.32 polynucleotide kinase/phosphatase
-
 Schizosaccharomyces pombe

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
2.7.1.78 37
-
 activity assay Homo sapiens
2.7.1.78 37
-
 activity assay Schizosaccharomyces pombe
2.7.1.78 37
-
 activity assay Tequatrovirus T4
2.7.1.78 37
-
 activity assay Mus musculus

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
2.7.1.78 7.4
-
 activity assay Homo sapiens
2.7.1.78 7.4
-
 activity assay Schizosaccharomyces pombe
2.7.1.78 7.4
-
 activity assay Tequatrovirus T4
2.7.1.78 7.4
-
 activity assay Mus musculus

Cofactor

EC Number Cofactor Comment Organism Structure
2.7.1.78 ATP
-
 Homo sapiens
2.7.1.78 ATP
-
 Schizosaccharomyces pombe
2.7.1.78 ATP
-
 Tequatrovirus T4
2.7.1.78 ATP
-
 Mus musculus

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.7.1.78 0.00006
-
-
 Homo sapiens 2-(1-hydroxyundecyl)-1-(4-nitrophenylamino)-6-phenyl-6,7a-dihydro-1H-pyrrolo[3,4-b]pyridine-5,7(2H,4aH)-dione
3.1.3.32 additional information
-
 32% inhibition at 0.05 mM Schizosaccharomyces pombe 2-(1-hydroxyundecyl)-1-(4-nitrophenylamino)-6-phenyl-6,7a-dihydro-1H-pyrrolo[3,4-b]pyridine-5,7(2H,4aH)-dione
3.1.3.32 additional information
-
 94% inhibition at 0.05 mM Mus musculus 2-(1-hydroxyundecyl)-1-(4-nitrophenylamino)-6-phenyl-6,7a-dihydro-1H-pyrrolo[3,4-b]pyridine-5,7(2H,4aH)-dione
3.1.3.32 0.00006
-
 near maximal inhibition with 0.010 mM Homo sapiens 2-(1-hydroxyundecyl)-1-(4-nitrophenylamino)-6-phenyl-6,7a-dihydro-1H-pyrrolo[3,4-b]pyridine-5,7(2H,4aH)-dione
3.1.3.32 0.0003
-
-
 Homo sapiens 2-(hydroxy(3,4,5-trimethoxyphenyl)methyl)-1-(4-nitrophenylamino)-6-phenyl-6,7a-dihydro-1H-pyrrolo[3,4-b]pyridine-5,7(2H,4aH)-dione