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Literature summary for 2.7.7.7 extracted from
- Small molecule inhibitors of human DNA polymerase lambda (2011), ACS Chem. Biol., 6, 314-319.
Application
| Application | Comment | Organism |
|---|---|---|
| drug development | DNA polymerases are promising drug targets for the treatment of cancer | Homo sapiens |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| (2E)-2-(3-nitro-4-[[6-(trifluoromethyl)pyridin-3-yl]sulfanyl]benzylidene)-5-thioxo-1,3-thiazolidin-4-one | - |
Homo sapiens |  |
| (2E)-2-(4-chloro-3-ethylbenzylidene)-5-thioxo-1,3-thiazolidin-4-one | - |
Homo sapiens | |
| (2E)-2-(pentafluorobenzylidene)-5-thioxodihydrothiophen-3(2H)-one | - |
Homo sapiens | |
| (2E)-2-[4-(2-hydroxyethyl)-3-nitrobenzylidene]-5-thioxo-1,3-thiazolidin-4-one | - |
Homo sapiens | |
| (5Z)-5-(4-chloro-3-nitrobenzylidene)-2-thioxo-1,3-thiazolidin-4-one | - |
Homo sapiens | |
| (5Z)-5-[3-bromo-4-[(4-fluorobenzyl)oxy]benzylidene]-1,3-thiazolidine-2,4-dione | - |
Homo sapiens | |
| (5Z)-5-[3-bromo-4-[(4-fluorophenyl)sulfanyl]benzylidene]-2-thioxo-1,3-thiazolidin-4-one | - |
Homo sapiens | |
| (5Z)-5-[3-nitro-4-(pyridin-3-ylsulfanyl)benzylidene]-2-thioxo-1,3-thiazolidin-4-one | - |
Homo sapiens | |
| (5Z)-5-[4-(4-methylphenoxy)-3-nitrobenzylidene]-2-thioxo-1,3-thiazolidin-4-one | - |
Homo sapiens | |
| (5Z)-5-[4-(cyclohexylsulfanyl)-3-nitrobenzylidene]-2-thioxo-1,3-thiazolidin-4-one | - |
Homo sapiens | |
| (5Z)-5-[4-[(4-bromophenyl)sulfanyl]-3-nitrobenzylidene]-2-thioxo-1,3-thiazolidin-4-one | - |
Homo sapiens | |
| (5Z)-5-[4-[(4-chlorophenyl)sulfanyl]-3-nitrobenzylidene]-2-thioxo-1,3-thiazolidin-4-one | - |
Homo sapiens | |
| (5Z)-5-[4-[(4-fluorobenzyl)oxy]-3-nitrobenzylidene]-2-thioxo-1,3-thiazolidin-4-one | - |
Homo sapiens | |
| (5Z)-5-[4-[(4-fluorobenzyl)oxy]benzylidene]-2-thioxo-1,3-thiazolidin-4-one | - |
Homo sapiens | |
| (5Z)-5-[4-[(4-methylphenyl)sulfanyl]-3-nitrobenzylidene]-3-(prop-2-en-1-yl)-2-thioxo-1,3-thiazolidin-4-one | - |
Homo sapiens | |
| 2-methoxy-4-[(Z)-(4-oxo-2-thioxo-1,3-thiazolidin-5-ylidene)methyl]phenyl 2,4-dichlorobenzoate | - |
Homo sapiens | |
| 2-methoxy-4-[(Z)-(4-oxo-2-thioxo-1,3-thiazolidin-5-ylidene)methyl]phenyl 3-bromobenzoate | - |
Homo sapiens | |
| 4-chlorophenyl 2,4-dinitrophenyl sulfide | - |
Homo sapiens | |
| 4-[(4-methylphenyl)sulfanyl]-3-nitrobenzaldehyde | - |
Homo sapiens | |
| 4-[(Z)-(2,4-dioxo-1,3-thiazolidin-5-ylidene)methyl]-2-methoxyphenyl 3-bromobenzoate | - |
Homo sapiens | |
| 4-[(Z)-(4-oxo-2-thioxo-1,3-thiazolidin-5-ylidene)methyl]phenyl 2-chlorobenzoate | - |
Homo sapiens | |
| 5-(5-nitro-2-[[6-(trifluoromethyl)pyridin-3-yl]sulfanyl]benzylidene)-2-thioxo-1,3-thiazolidin-4-one | - |
Homo sapiens | |
| 5-[2-(cyclohexylsulfanyl)-5-nitrobenzylidene]-2-thioxo-1,3-thiazolidin-4-one | - |
Homo sapiens | |
| 5-[2-[(4-chlorophenyl)sulfanyl]-5-nitrobenzylidene]-2-thioxo-1,3-thiazolidin-4-one | - |
Homo sapiens | |
| 5-[2-[(4-methylphenyl)sulfanyl]-5-nitrobenzylidene]-2-thioxo-1,3-thiazolidin-4-one | - |
Homo sapiens | |
| epigallocatechin gallate | - |
Homo sapiens | |
| rhodanines | most potent inhibitors for DNA Pol lambda, they are up to 10times less active against the highly similar DNA polymerase beta, structure-activity relationships, overview. 5-Arylidene-2,4-thiazolidinediones are class I rhodanines, rhodanine class II has members of carbohydrazides, and class III contains a common 2,4-pentadione substructure element | Homo sapiens | |
| [3-[(Z)-(4-oxo-2-thioxo-1,3-thiazolidin-5-ylidene)methyl]phenoxy]acetic acid | - |
Homo sapiens | |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| deoxynucleoside triphosphate + DNAn | Homo sapiens | - |
diphosphate + DNAn+1 | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
- |
- |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| deoxynucleoside triphosphate + DNAn | - |
Homo sapiens | diphosphate + DNAn+1 | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| DNA Pol lambda | - |
Homo sapiens |
| DNA polymerase lambda | - |
Homo sapiens |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.0038 | - |
pH and temperature not specified in the publication | Homo sapiens | epigallocatechin gallate | |
| 0.0059 | - |
pH and temperature not specified in the publication, inhibition of DNA Pol lambda | Homo sapiens | (5Z)-5-[4-[(4-fluorobenzyl)oxy]benzylidene]-2-thioxo-1,3-thiazolidin-4-one | |
| 0.0081 | - |
pH and temperature not specified in the publication, inhibition of DNA Pol lambda | Homo sapiens | 5-[2-[(4-chlorophenyl)sulfanyl]-5-nitrobenzylidene]-2-thioxo-1,3-thiazolidin-4-one | |
| 0.0083 | - |
pH and temperature not specified in the publication, inhibition of DNA Pol lambda | Homo sapiens | (5Z)-5-[3-bromo-4-[(4-fluorophenyl)sulfanyl]benzylidene]-2-thioxo-1,3-thiazolidin-4-one | |
| 0.0093 | - |
pH and temperature not specified in the publication, inhibition of DNA Pol lambda | Homo sapiens | (5Z)-5-[4-(4-methylphenoxy)-3-nitrobenzylidene]-2-thioxo-1,3-thiazolidin-4-one | |
| 0.01 | - |
pH and temperature not specified in the publication, inhibition of DNA Pol lambda | Homo sapiens | 5-[2-[(4-methylphenyl)sulfanyl]-5-nitrobenzylidene]-2-thioxo-1,3-thiazolidin-4-one | |
| 0.011 | - |
pH and temperature not specified in the publication, inhibition of DNA Pol lambda | Homo sapiens | (2E)-2-(3-nitro-4-[[6-(trifluoromethyl)pyridin-3-yl]sulfanyl]benzylidene)-5-thioxo-1,3-thiazolidin-4-one | |
| 0.0124 | - |
pH and temperature not specified in the publication, inhibition of DNA Pol lambda | Homo sapiens | 4-[(Z)-(4-oxo-2-thioxo-1,3-thiazolidin-5-ylidene)methyl]phenyl 2-chlorobenzoate | |
| 0.0429 | - |
pH and temperature not specified in the publication, inhibition of DNA Pol beta | Homo sapiens | 5-[2-[(4-chlorophenyl)sulfanyl]-5-nitrobenzylidene]-2-thioxo-1,3-thiazolidin-4-one | |
| 0.0455 | - |
pH and temperature not specified in the publication, inhibition of DNA Pol beta | Homo sapiens | 5-[2-[(4-methylphenyl)sulfanyl]-5-nitrobenzylidene]-2-thioxo-1,3-thiazolidin-4-one | |
| 0.0644 | - |
pH and temperature not specified in the publication, inhibition of DNA Pol beta | Homo sapiens | (5Z)-5-[4-[(4-fluorobenzyl)oxy]benzylidene]-2-thioxo-1,3-thiazolidin-4-one | |
| 0.08 | - |
pH and temperature not specified in the publication, inhibition of DNA Pol beta | Homo sapiens | (5Z)-5-[3-bromo-4-[(4-fluorophenyl)sulfanyl]benzylidene]-2-thioxo-1,3-thiazolidin-4-one | |
| 0.0888 | - |
pH and temperature not specified in the publication, inhibition of DNA Pol beta | Homo sapiens | 4-[(Z)-(4-oxo-2-thioxo-1,3-thiazolidin-5-ylidene)methyl]phenyl 2-chlorobenzoate | |
| 0.1 | - |
above, pH and temperature not specified in the publication, inhibition of DNA Pol beta | Homo sapiens | (2E)-2-(3-nitro-4-[[6-(trifluoromethyl)pyridin-3-yl]sulfanyl]benzylidene)-5-thioxo-1,3-thiazolidin-4-one | |
| 0.1 | - |
above, pH and temperature not specified in the publication, inhibition of DNA Pol beta | Homo sapiens | (5Z)-5-[4-(4-methylphenoxy)-3-nitrobenzylidene]-2-thioxo-1,3-thiazolidin-4-one | |
General Information
| General Information | Comment | Organism |
|---|---|---|
| evolution | human DNA polymerase lambda is a member of the DNA polymerase X family | Homo sapiens |
| metabolism | high levels of DNA polymerases of the X family might cause genomic instability | Homo sapiens |
| physiological function | DNA Pol lambda has a backup role for DNA Pol beta in base-excision repair | Homo sapiens |
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