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Literature summary for 2.7.7.31 extracted from

  • Locatelli, G.A.; Di Santo, R.; Crespan, E.; Costi, R.; Roux, A.; Hubscher, U.; Shevelev, I.; Blanca, G.; Villani, G.; Spadari, S.; Maga, G.
    Diketo hexenoic acid derivatives are novel selective non-nucleoside inhibitors of mammalian terminal deoxynucleotidyl transferases, with potent cytotoxic effect against leukemic cells (2005), Mol. Pharmacol., 68, 538-550.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
6-(1-phenyl-1H-indol-3-yl)-2,4-dioxy-5-hexenoic acid IC50: 0.0472 mM Bos taurus
6-(1-phenylmethyl-1H-indol-3-yl)-2,4-dioxy-5-hexenoic acid IC50: 0.0079 mM Bos taurus
6-(4-benzoyl-1-phenylmethyl-1H-pyrrol-2-yl)-2,4-dioxo-5-hexenoic acid IC50: 0.0162 mM Bos taurus

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
deoxynucleoside triphosphate + DNA Bos taurus the enzyme has a key role in V(D)J recombination during lymphocyte and repertoire development diphosphate + DNAn+1
-
?

Organism

Organism UniProt Comment Textmining
Bos taurus
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
leukemia cell more than 90% of leukemic cells in acute lymphocytic leukemia and approximately 30% of leukemic cells in the chronic myelogenous leukemia crisis show elevated TDP activity Bos taurus
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thymus
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Bos taurus
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Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
deoxynucleoside triphosphate + DNA the enzyme has a key role in V(D)J recombination during lymphocyte and repertoire development Bos taurus diphosphate + DNAn+1
-
?

Synonyms

Synonyms Comment Organism
TdT
-
Bos taurus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0079
-
IC50: 0.0079 mM Bos taurus 6-(1-phenylmethyl-1H-indol-3-yl)-2,4-dioxy-5-hexenoic acid
0.0162
-
IC50: 0.0162 mM Bos taurus 6-(4-benzoyl-1-phenylmethyl-1H-pyrrol-2-yl)-2,4-dioxo-5-hexenoic acid
0.0472
-
IC50: 0.0472 mM Bos taurus 6-(1-phenyl-1H-indol-3-yl)-2,4-dioxy-5-hexenoic acid