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Literature summary for 4.2.99.18 extracted from
- Efficient inhibition of human AP endonuclease 1 (APE1) via substrate masking by abasic site-binding macrocyclic ligands (2015), Chem. Commun. (Camb.), 51, 15948-15951 .
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| 2,7-BisNP-NH | strong inhibition | Homo sapiens |  |
| 2,7-BisNP-O | strong inhibition | Homo sapiens | |
| ATCA | strong inhibition | Homo sapiens | |
| CRT0044876 | weak inhibition | Homo sapiens | |
| Ethidium bromide | weak inhibition | Homo sapiens | |
| additional information | bis-naphthalene macrocycles, which bind with high affinity and selectivity to abasic sites in DNA, efficiently inhibit their cleavage by APE1 (IC50 value is 55-60 nM in the kinetic assay with a model THF substrate). Substrate masking by non-covalent abasic-site ligands is an efficient strategy for inhibition of APE1. Inhibition of abasic site-specific endonuclease activity of nuclear extracts and gel-based assays for APE1 inhibition | Homo sapiens |
KM Value [mM]
| KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| additional information | - |
additional information | Michaelis-Menten kinetic study, overview | Homo sapiens |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | P27695 | - |
- |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| commercial preparation | recombinant, polyhistidine-tagged APE1 | Homo sapiens | - |
| glioblastoma cell | - |
Homo sapiens | - |
| U-87MG cell | - |
Homo sapiens | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| additional information | a fluorophore-labelled 17-mer oligonucleotide DNA substrate is used | Homo sapiens | ? | - |
? | |
Subunits
| Subunits | Comment | Organism |
|---|---|---|
| ? | x * 35000, native enzyme, SDS-PAGE | Homo sapiens |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| AP endonuclease 1 | - |
Homo sapiens |
| APE1 | - |
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 |
|---|---|---|---|
| 8 | - |
assay at | Homo sapiens |
Ki Value [mM]
| Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
|---|---|---|---|---|---|
| additional information | - |
additional information | inhibition kinetics | Homo sapiens |
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Release 2023.1 (January 2023)
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