Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary extracted from

  • Strittmatter, T.; Bareth, B.; Immel, T.A.; Huhn, T.; Mayer, T.U.; Marx, A.
    Small molecule inhibitors of human DNA polymerase lambda (2011), ACS Chem. Biol., 6, 314-319.
    View publication on PubMed

Application

EC Number Application Comment Organism
2.7.7.7 drug development DNA polymerases are promising drug targets for the treatment of cancer Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.7.7 (2E)-2-(3-nitro-4-[[6-(trifluoromethyl)pyridin-3-yl]sulfanyl]benzylidene)-5-thioxo-1,3-thiazolidin-4-one
-
 Homo sapiens
2.7.7.7 (2E)-2-(4-chloro-3-ethylbenzylidene)-5-thioxo-1,3-thiazolidin-4-one
-
 Homo sapiens
2.7.7.7 (2E)-2-(pentafluorobenzylidene)-5-thioxodihydrothiophen-3(2H)-one
-
 Homo sapiens
2.7.7.7 (2E)-2-[4-(2-hydroxyethyl)-3-nitrobenzylidene]-5-thioxo-1,3-thiazolidin-4-one
-
 Homo sapiens
2.7.7.7 (5Z)-5-(4-chloro-3-nitrobenzylidene)-2-thioxo-1,3-thiazolidin-4-one
-
 Homo sapiens
2.7.7.7 (5Z)-5-[3-bromo-4-[(4-fluorobenzyl)oxy]benzylidene]-1,3-thiazolidine-2,4-dione
-
 Homo sapiens
2.7.7.7 (5Z)-5-[3-bromo-4-[(4-fluorophenyl)sulfanyl]benzylidene]-2-thioxo-1,3-thiazolidin-4-one
-
 Homo sapiens
2.7.7.7 (5Z)-5-[3-nitro-4-(pyridin-3-ylsulfanyl)benzylidene]-2-thioxo-1,3-thiazolidin-4-one
-
 Homo sapiens
2.7.7.7 (5Z)-5-[4-(4-methylphenoxy)-3-nitrobenzylidene]-2-thioxo-1,3-thiazolidin-4-one
-
 Homo sapiens
2.7.7.7 (5Z)-5-[4-(cyclohexylsulfanyl)-3-nitrobenzylidene]-2-thioxo-1,3-thiazolidin-4-one
-
 Homo sapiens
2.7.7.7 (5Z)-5-[4-[(4-bromophenyl)sulfanyl]-3-nitrobenzylidene]-2-thioxo-1,3-thiazolidin-4-one
-
 Homo sapiens
2.7.7.7 (5Z)-5-[4-[(4-chlorophenyl)sulfanyl]-3-nitrobenzylidene]-2-thioxo-1,3-thiazolidin-4-one
-
 Homo sapiens
2.7.7.7 (5Z)-5-[4-[(4-fluorobenzyl)oxy]-3-nitrobenzylidene]-2-thioxo-1,3-thiazolidin-4-one
-
 Homo sapiens
2.7.7.7 (5Z)-5-[4-[(4-fluorobenzyl)oxy]benzylidene]-2-thioxo-1,3-thiazolidin-4-one
-
 Homo sapiens
2.7.7.7 (5Z)-5-[4-[(4-methylphenyl)sulfanyl]-3-nitrobenzylidene]-3-(prop-2-en-1-yl)-2-thioxo-1,3-thiazolidin-4-one
-
 Homo sapiens
2.7.7.7 2-methoxy-4-[(Z)-(4-oxo-2-thioxo-1,3-thiazolidin-5-ylidene)methyl]phenyl 2,4-dichlorobenzoate
-
 Homo sapiens
2.7.7.7 2-methoxy-4-[(Z)-(4-oxo-2-thioxo-1,3-thiazolidin-5-ylidene)methyl]phenyl 3-bromobenzoate
-
 Homo sapiens
2.7.7.7 4-chlorophenyl 2,4-dinitrophenyl sulfide
-
 Homo sapiens
2.7.7.7 4-[(4-methylphenyl)sulfanyl]-3-nitrobenzaldehyde
-
 Homo sapiens
2.7.7.7 4-[(Z)-(2,4-dioxo-1,3-thiazolidin-5-ylidene)methyl]-2-methoxyphenyl 3-bromobenzoate
-
 Homo sapiens
2.7.7.7 4-[(Z)-(4-oxo-2-thioxo-1,3-thiazolidin-5-ylidene)methyl]phenyl 2-chlorobenzoate
-
 Homo sapiens
2.7.7.7 5-(5-nitro-2-[[6-(trifluoromethyl)pyridin-3-yl]sulfanyl]benzylidene)-2-thioxo-1,3-thiazolidin-4-one
-
 Homo sapiens
2.7.7.7 5-[2-(cyclohexylsulfanyl)-5-nitrobenzylidene]-2-thioxo-1,3-thiazolidin-4-one
-
 Homo sapiens
2.7.7.7 5-[2-[(4-chlorophenyl)sulfanyl]-5-nitrobenzylidene]-2-thioxo-1,3-thiazolidin-4-one
-
 Homo sapiens
2.7.7.7 5-[2-[(4-methylphenyl)sulfanyl]-5-nitrobenzylidene]-2-thioxo-1,3-thiazolidin-4-one
-
 Homo sapiens
2.7.7.7 epigallocatechin gallate
-
 Homo sapiens
2.7.7.7 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
2.7.7.7 [3-[(Z)-(4-oxo-2-thioxo-1,3-thiazolidin-5-ylidene)methyl]phenoxy]acetic acid
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.7.7.7 deoxynucleoside triphosphate + DNAn Homo sapiens
-
 diphosphate + DNAn+1
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.7.7.7 Homo sapiens
-
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.7.7.7 deoxynucleoside triphosphate + DNAn
-
 Homo sapiens diphosphate + DNAn+1
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.7.7.7 DNA Pol lambda
-
 Homo sapiens
2.7.7.7 DNA polymerase lambda
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.7.7.7 0.0038
-
 pH and temperature not specified in the publication Homo sapiens epigallocatechin gallate
2.7.7.7 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
2.7.7.7 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
2.7.7.7 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
2.7.7.7 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
2.7.7.7 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
2.7.7.7 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
2.7.7.7 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
2.7.7.7 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
2.7.7.7 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
2.7.7.7 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
2.7.7.7 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
2.7.7.7 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
2.7.7.7 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
2.7.7.7 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

EC Number General Information Comment Organism
2.7.7.7 evolution human DNA polymerase lambda is a member of the DNA polymerase X family Homo sapiens
2.7.7.7 metabolism high levels of DNA polymerases of the X family might cause genomic instability Homo sapiens
2.7.7.7 physiological function DNA Pol lambda has a backup role for DNA Pol beta in base-excision repair Homo sapiens