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Literature summary for 3.1.4.1 extracted from

  • Khomenko, T.; Zakharenko, A.; Odarchenko, T.; Arabshahi, H.J.; Sannikova, V.; Zakharova, O.; Korchagina, D.; Reynisson, J.; Volcho, K.; Salakhutdinov, N.; Lavrik, O.
    New inhibitors of tyrosyl-DNA phosphodiesterase I (Tdp 1) combining 7-hydroxycoumarin and monoterpenoid moieties (2016), Bioorg. Med. Chem., 24, 5573-5581 .
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
2-(2,6-dimethylhept-5-en-1-yl)-5,7-dimethyl-1,3-diazatricyclo[3.3.1.1(3,7)]decan-6-one
-
Homo sapiens
3,20-dioxopregn-4-en-21-yl 4-bromobenzene-1-sulfonate
-
Homo sapiens
3-(((1R,5S)-6,6-dimethylbicyclo[3.1.1]hept-2-en-2-yl)methoxy)-7,8,9,10-tetrahydro-6H-benzo[c]chromen-6-one
-
Homo sapiens
3-(((1S,5R)-6,6-dimethylbicyclo[3.1.1]hept-2-en-2-yl)methoxy)-7,8,9,10-tetrahydro-6H-benzo[c]chromen-6-one
-
Homo sapiens
3-((3,4,5-trimethoxybenzyl)oxy)-7,8,9,10-tetrahydro-6H-benzo[c]chromen-6-one
-
Homo sapiens
3-((3-methoxybenzyl)oxy)-7,8,9,10-tetrahydro-6Hbenzo[c]chromen-6-one
-
Homo sapiens
3-(2-((1R,5S)-6,6-dimethylbicyclo[3.1.1]hept-2-en-2-yl)ethoxy)-7,8,9,10-tetrahydro-6H-benzo[c]chromen-6-one
-
Homo sapiens
3-(benzyloxy)-7,8,9,10-tetrahydro-6H-benzo[c]chromen-6-one
-
Homo sapiens
4,4'-(furan-2,5-diyl)di(benzene-1-carboximidamide)
-
Homo sapiens
4-methyl-7-((3,4,5-trimethoxybenzyl)oxy)-2H-chromen-2-one
-
Homo sapiens
6-(3-aminopropyl)-8-hydroxy-3-nitro-5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione
-
Homo sapiens
7-(((1R,5S)-6,6-dimethylbicyclo[3.1.1]hept-2-en-2-yl)methoxy)-2,3-dihydrocyclopenta[c]chromen-4(1H)-one
-
Homo sapiens
7-(((1R,5S)-6,6-dimethylbicyclo[3.1.1]hept-2-en-2-yl)methoxy)-4-methyl-2H-chromen-2-one
-
Homo sapiens
7-(((1S,5R)-6,6-dimethylbicyclo[3.1.1]hept-2-en-2-yl)methoxy)-2,3-dihydrocyclopenta[c]chromen-4(1H)-one
-
Homo sapiens
7-(((1S,5R)-6,6-dimethylbicyclo[3.1.1]hept-2-en-2-yl)methoxy)-4-methyl-2H-chromen-2-one
-
Homo sapiens
7-((3,4,5-trimethoxybenzyl)oxy)-2,3-dihydrocyclopenta[c]chromen-4(1H)-one
-
Homo sapiens
7-((3-methoxybenzyl) oxy)-4-methyl-2H-chromen-2-one
-
Homo sapiens
7-((3-methoxybenzyl)oxy)-2,3-dihydrocyclopenta[c]chromen-4(1H)-one
-
Homo sapiens
7-(2-((1R,5S)-6,6-dimethylbicyclo[3.1.1]hept-2-en-2-yl)ethoxy)-2,3-dihydrocyclopenta[c]chromen-4(1H)-one
-
Homo sapiens
7-(benzyloxy)-2,3-dihydrocyclopenta[c]chromen-4(1H)-one
-
Homo sapiens
7-(benzyloxy)-4-methyl-2H-chromen-2-one
-
Homo sapiens
N2,N2-dibutyl-N-[8-(trifluoromethyl)-1,2,3,4,5-benzopentathiepin-6-yl]glycinamide
-
Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
additional information Homo sapiens the enzyme hydrolyzes the phosphodiester bond between a catalytic tyrosine Tyr723 (human) of topoisomerase 1 and DNA 3'-phosphate ?
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens Q9NUW8
-
-

Source Tissue

Source Tissue Comment Organism Textmining
MCF-7 cell
-
Homo sapiens
-
RPMI-8226 cell
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
additional information the enzyme hydrolyzes the phosphodiester bond between a catalytic tyrosine Tyr723 (human) of topoisomerase 1 and DNA 3'-phosphate Homo sapiens ?
-
?

Synonyms

Synonyms Comment Organism
Tdp 1
-
Homo sapiens
tyrosyl-DNA phosphodiesterase I
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000675
-
pH and temperature not specified in the publication Homo sapiens 7-(((1S,5R)-6,6-dimethylbicyclo[3.1.1]hept-2-en-2-yl)methoxy)-2,3-dihydrocyclopenta[c]chromen-4(1H)-one
0.00109
-
pH and temperature not specified in the publication Homo sapiens 7-(2-((1R,5S)-6,6-dimethylbicyclo[3.1.1]hept-2-en-2-yl)ethoxy)-2,3-dihydrocyclopenta[c]chromen-4(1H)-one
0.0012
-
pH and temperature not specified in the publication Homo sapiens 3-(((1S,5R)-6,6-dimethylbicyclo[3.1.1]hept-2-en-2-yl)methoxy)-7,8,9,10-tetrahydro-6H-benzo[c]chromen-6-one
0.00123
-
pH and temperature not specified in the publication Homo sapiens 3-(((1R,5S)-6,6-dimethylbicyclo[3.1.1]hept-2-en-2-yl)methoxy)-7,8,9,10-tetrahydro-6H-benzo[c]chromen-6-one
0.00137
-
pH and temperature not specified in the publication Homo sapiens 7-(((1R,5S)-6,6-dimethylbicyclo[3.1.1]hept-2-en-2-yl)methoxy)-2,3-dihydrocyclopenta[c]chromen-4(1H)-one
0.00145
-
pH and temperature not specified in the publication Homo sapiens 3-(2-((1R,5S)-6,6-dimethylbicyclo[3.1.1]hept-2-en-2-yl)ethoxy)-7,8,9,10-tetrahydro-6H-benzo[c]chromen-6-one
0.00156
-
pH and temperature not specified in the publication Homo sapiens 7-(((1R,5S)-6,6-dimethylbicyclo[3.1.1]hept-2-en-2-yl)methoxy)-4-methyl-2H-chromen-2-one
0.00431
-
pH and temperature not specified in the publication Homo sapiens 7-(((1S,5R)-6,6-dimethylbicyclo[3.1.1]hept-2-en-2-yl)methoxy)-4-methyl-2H-chromen-2-one
0.00493
-
pH and temperature not specified in the publication Homo sapiens 3-((3-methoxybenzyl)oxy)-7,8,9,10-tetrahydro-6Hbenzo[c]chromen-6-one
0.00528
-
pH and temperature not specified in the publication Homo sapiens 7-(benzyloxy)-4-methyl-2H-chromen-2-one
0.00562
-
pH and temperature not specified in the publication Homo sapiens 3-(benzyloxy)-7,8,9,10-tetrahydro-6H-benzo[c]chromen-6-one
0.00917
-
pH and temperature not specified in the publication Homo sapiens 7-(benzyloxy)-2,3-dihydrocyclopenta[c]chromen-4(1H)-one
0.01
-
IC50 above 0.01 mM, pH and temperature not specified in the publication Homo sapiens 3-((3,4,5-trimethoxybenzyl)oxy)-7,8,9,10-tetrahydro-6H-benzo[c]chromen-6-one
0.01
-
IC50 above 0.01 mM, pH and temperature not specified in the publication Homo sapiens 4-methyl-7-((3,4,5-trimethoxybenzyl)oxy)-2H-chromen-2-one
0.01
-
IC50 above 0.01 mM, pH and temperature not specified in the publication Homo sapiens 7-((3,4,5-trimethoxybenzyl)oxy)-2,3-dihydrocyclopenta[c]chromen-4(1H)-one
0.01
-
IC50 above 0.01 mM, pH and temperature not specified in the publication Homo sapiens 7-((3-methoxybenzyl) oxy)-4-methyl-2H-chromen-2-one
0.01
-
IC50 above 0.01 mM, pH and temperature not specified in the publication Homo sapiens 7-((3-methoxybenzyl)oxy)-2,3-dihydrocyclopenta[c]chromen-4(1H)-one

General Information

General Information Comment Organism
physiological function the enzyme plays a key role in the removal of DNA damage resulting from Topo1 inhibition or caused by other anticancer drugs, e.g., temozolomide, bleomycin, etoposide, etc. Homo sapiens