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Literature summary for 3.1.4.1 extracted from

  • Zakharenko, A.; Khomenko, T.; Zhukova, S.; Koval, O.; Zakharova, O.; Anarbaev, R.; Lebedeva, N.; Korchagina, D.; Komarova, N.; Vasiliev, V.; Reynisson, J.; Volcho, K.; Salakhutdinov, N.; Lavrik, O.
    Synthesis and biological evaluation of novel tyrosyl-DNA phosphodiesterase 1 inhibitors with a benzopentathiepine moiety (2015), Bioorg. Med. Chem., 23, 2044-2052 .
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
2,2,2-trifluoro-N-(8-(trifluoromethyl)benzo[f][1,2,3,4,5]pentathiepin-6-yl)acetamide
-
Homo sapiens
2-(dibutylamino)-N-(8-(trifluoromethyl)benzo[f]-[1,2,3,4,5]pentathiepin-6-yl)acetamide
-
Homo sapiens
2-(piperidin-1-yl)-N-(8-(trifluoromethyl)benzo[f]-[1,2,3,4,5]pentathiepin-6-yl)acetamide
-
Homo sapiens
2-(pyrrolidin-1-yl)-N-(8-(trifluoromethyl)benzo[f]-[1,2,3,4,5]pentathiepin-6-yl)acetamide
-
Homo sapiens
2-morpholino-N-(8-(trifluoromethyl)benzo[f]-[1,2,3,4,5]pentathiepin-6-yl)acetamide
-
Homo sapiens
3-(piperidin-1-yl)-N-(8-(trifluoromethyl)benzo[f]-[1,2,3,4,5]pentathiepin-6-yl)propanamide
-
Homo sapiens
3-(pyrrolidin-1-yl)-N-(8-(trifluoromethyl)benzo[f]-[1,2,3,4,5]pentathiepin-6-yl)propanamide
-
Homo sapiens
3-morpholino-N-(8-(trifluoromethyl)benzo[f]-[1,2,3,4,5]pentathiepin-6-yl)propanamide
-
Homo sapiens
aminobenzopentathiepine
-
Homo sapiens
N-phenyl-2-(piperidin-1-yl)acetamide
-
Homo sapiens
N-phenyl-2-(pyrrolidin-1-yl)acetamide
-
Homo sapiens
NSC 88915
-
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 cleaves the 3'-diester bond between tyrosine and DNA as well as removes other lesions, producing a 3'-phosphate that can be removed by polynucleotide kinase/phosphatase ?
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens Q9NKW8
-
-

Purification (Commentary)

Purification (Comment) Organism
Ni-chelating resin column chromatography and phosphocellulose P11 column chromatography, and Superdex 200 gel filtration Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
5'-(5,6-FAM-aacgtcagggtcttcc-BHQ1)-3' + H2O
-
Homo sapiens ?
-
?
additional information the enzyme cleaves the 3'-diester bond between tyrosine and DNA as well as removes other lesions, producing a 3'-phosphate that can be removed by polynucleotide kinase/phosphatase Homo sapiens ?
-
?

Synonyms

Synonyms Comment Organism
TDP1
-
Homo sapiens
tyrosyl-DNA phosphodiesterase 1
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00022
-
at pH 8.0 and 26°C Homo sapiens 2-(dibutylamino)-N-(8-(trifluoromethyl)benzo[f]-[1,2,3,4,5]pentathiepin-6-yl)acetamide
0.00128
-
at pH 8.0 and 26°C Homo sapiens 2-(piperidin-1-yl)-N-(8-(trifluoromethyl)benzo[f]-[1,2,3,4,5]pentathiepin-6-yl)acetamide
0.0013
-
at pH 8.0 and 26°C Homo sapiens 3-morpholino-N-(8-(trifluoromethyl)benzo[f]-[1,2,3,4,5]pentathiepin-6-yl)propanamide
0.00162
-
at pH 8.0 and 26°C Homo sapiens 2-morpholino-N-(8-(trifluoromethyl)benzo[f]-[1,2,3,4,5]pentathiepin-6-yl)acetamide
0.00366
-
at pH 8.0 and 26°C Homo sapiens 3-(piperidin-1-yl)-N-(8-(trifluoromethyl)benzo[f]-[1,2,3,4,5]pentathiepin-6-yl)propanamide
0.0037
-
at pH 8.0 and 26°C Homo sapiens 2-(pyrrolidin-1-yl)-N-(8-(trifluoromethyl)benzo[f]-[1,2,3,4,5]pentathiepin-6-yl)acetamide
0.00603
-
at pH 8.0 and 26°C Homo sapiens 3-(pyrrolidin-1-yl)-N-(8-(trifluoromethyl)benzo[f]-[1,2,3,4,5]pentathiepin-6-yl)propanamide
0.01
-
IC50 above 0.01 mM, at pH 8.0 and 26°C Homo sapiens aminobenzopentathiepine
0.01
-
IC50 above 0.1 mM, at pH 8.0 and 26°C Homo sapiens 2,2,2-trifluoro-N-(8-(trifluoromethyl)benzo[f][1,2,3,4,5]pentathiepin-6-yl)acetamide
0.01
-
IC50 above 0.1 mM, at pH 8.0 and 26°C Homo sapiens N-phenyl-2-(piperidin-1-yl)acetamide
0.01
-
IC50 above 0.1 mM, at pH 8.0 and 26°C Homo sapiens N-phenyl-2-(pyrrolidin-1-yl)acetamide