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Literature summary for 4.2.99.18 extracted from

  • Yang, S.; Meyskens, F.L.
    Apurinic/apyrimidinic endonuclease /redox effector factor-1 (APE/Ref-1) a unique target for the prevention and treatment of human melanoma (2008), Antioxid. Redox Signal., 11, 639-650.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 4.2.99.18

Application

Application Comment Organism
medicine strong candidate as a potential drug-treatable target for the prevention and treatment of human melanoma Homo sapiens

Protein Variants

Protein Variants Comment Organism
E96A APE-1 mutant displays a significantly reduced DNA-repair activity when compared with the wild-type protein Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
7-nitro-1H-indole 2-carboxylic acid CRT0044876, binds to the active site of APE/Ref-1 and effectively inhibits its AP endonuclease, 3'-phosphodiesterase and 3'-phosphatase activities at low micromolar concentrations Homo sapiens
Fe2+ inhibitory effects on APE/Ref-1 activity Homo sapiens
Pb2+ inhibitory effects on APE/Ref-1 activity Homo sapiens
PNRI-299 inhibition on AP-1 transcription Homo sapiens
reactive oxygen species reactive oxygen species not only can inhibit APE/Ref-1 activities by direct oxidation of amino acid residues, but also affects the expression level and subcellular localization of APE/Ref-1 Homo sapiens
resveratrol dock into one of the two drug-treatable pockets located in the redox domain Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
nucleus
-
 Homo sapiens 5634
-

Metals/Ions

Metals/Ions Comment Organism Structure
Co2+ CoCl2 (500 microM) is essential for AP endonuclease assay. Effects of Co on APE/Ref-1 are concentration dependent Homo sapiens
Fe pro-inflammatory activity of iron in the lung injury, at least in part, because of its induction of APE/Ref-1 Homo sapiens
Sm2+ the divalent metal ion soaked with the protein crystals is found specifically to associate with the glutamate residue Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
additional information Homo sapiens APE/Ref-1 is a critical component of the hypoxia-inducible transcriptional complex that interacts with hypoxia-inducible factor-1 and p300 ?
-
 ?
additional information Homo sapiens APE/Ref-1 is a key regulator, it markedly induces and efficiently protects melanocytes from oxidative damage by inducing the antiapoptotic machinery and stimulating cell survival ?
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
melanoma cell line wm3211, wm1205, c83-2c, c81-46A, A375, c81-61 Homo sapiens
-

Specific Activity [micromol/min/mg]

Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
additional information
-
 APE/Ref-1 accounts for 95% of the total apurinic/apyrimidinic endonuclease activity and is essential for the protection of cells against the toxic effects of several classes of DNA-damaging agents Homo sapiens
additional information
-
 APE/Ref-1 is involved in the regulation of metastatic potential in melanoma cells Homo sapiens
additional information
-
 APE/Ref-1 is very sensitive to redox-status alterations. ROS regulates its activity and expression on both transcriptional and posttranscriptional levels Homo sapiens
additional information
-
 Increased expression of APE/Ref-1 protein in nucleus of different human melanoma cell lines Homo sapiens
additional information
-
 involvement of APE/Ref-1 in the process of inflammation Homo sapiens
additional information
-
 oxidized APE/Ref-1 lacks endonuclease activity Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
additional information APE/Ref-1 is a critical component of the hypoxia-inducible transcriptional complex that interacts with hypoxia-inducible factor-1 and p300 Homo sapiens ?
-
 ?
additional information APE/Ref-1 is a key regulator, it markedly induces and efficiently protects melanocytes from oxidative damage by inducing the antiapoptotic machinery and stimulating cell survival Homo sapiens ?
-
 ?

Subunits

Subunits Comment Organism
dimer dimer removal is not affected by Pb2+, Cr6+, Fe3+ or Sn3+ Homo sapiens

Synonyms

Synonyms Comment Organism
APE/Ref-1
-
 Homo sapiens
apurinic/apyrimidinic endonuclease/redox effector factor-1
-
 Homo sapiens