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Literature summary extracted from

  • Konkle, M.E.; Hargrove, T.Y.; Kleshchenko, Y.Y.; von Kries, J.P.; Ridenour, W.; Uddin, M.J.; Caprioli, R.M.; Marnett, L.J.; Nes, W.D.; Villalta, F.; Waterman, M.R.; Lepesheva, G.I.
    Indomethacin amides as a novel molecular scaffold for targeting Trypanosoma cruzi sterol 14alpha-demethylase (2009), J. Med. Chem., 52, 2846-2853.
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

EC Number Cloned (Comment) Organism
1.14.14.154 subcloned into the pCW vector (Nde I/Hind III cloning sites) and expressed in Escherichia coli Trypanosoma cruzi

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.14.14.154 2-phenyl-N-pyridin-4-ylbutanamide
-
 Trypanosoma cruzi
1.14.14.154 2-[1-[(4-chlorophenyl)carbonyl]-5-methoxy-2-methyl-1H-indol-3-yl]-N-(1-pyridin-4-ylethyl)acetamide
-
 Trypanosoma cruzi
1.14.14.154 2-[1-[(4-chlorophenyl)carbonyl]-5-methoxy-2-methyl-1H-indol-3-yl]-N-(2-phenylpropyl)acetamide most potent inhibitor, antiparasitic activities at concentrations less than 0.01 mM Trypanosoma cruzi
1.14.14.154 2-[1-[(4-chlorophenyl)carbonyl]-5-methoxy-2-methyl-1H-indol-3-yl]-N-(2-pyridin-3-ylethyl)acetamide
-
 Trypanosoma cruzi
1.14.14.154 2-[1-[(4-chlorophenyl)carbonyl]-5-methoxy-2-methyl-1H-indol-3-yl]-N-(pyridin-2-ylmethyl)acetamide
-
 Trypanosoma cruzi
1.14.14.154 2-[1-[(4-chlorophenyl)carbonyl]-5-methoxy-2-methyl-1H-indol-3-yl]-N-(pyridin-4-ylmethyl)acetamide
-
 Trypanosoma cruzi
1.14.14.154 2-[1-[(4-chlorophenyl)carbonyl]-5-methoxy-2-methyl-1H-indol-3-yl]-N-pyridin-2-ylacetamide
-
 Trypanosoma cruzi
1.14.14.154 2-[1-[(4-chlorophenyl)carbonyl]-5-methoxy-2-methyl-1H-indol-3-yl]-N-pyridin-3-ylacetamide
-
 Trypanosoma cruzi
1.14.14.154 2-[1-[(4-chlorophenyl)carbonyl]-5-methoxy-2-methyl-1H-indol-3-yl]-N-pyrimidin-2-ylacetamide
-
 Trypanosoma cruzi
1.14.14.154 2-[1-[(4-chlorophenyl)carbonyl]-5-methoxy-2-methyl-1H-indol-3-yl]-N-[(6-chloropyridin-3-yl)methyl]acetamide
-
 Trypanosoma cruzi
1.14.14.154 2-[1-[(4-chlorophenyl)carbonyl]-5-methoxy-2-methyl-1H-indol-3-yl]-N-[2-(3-chlorophenyl)ethyl]acetamide most potent inhibitor, antiparasitic activities at concentrations less than 0.01 mM Trypanosoma cruzi
1.14.14.154 2-[1-[(4-chlorophenyl)carbonyl]-5-methoxy-2-methyl-1H-indol-3-yl]-N-[[6-(trifluoromethyl)pyridin-3-yl]methyl]acetamide
-
 Trypanosoma cruzi
1.14.14.154 3-(2-furyl)-5,6-dihydroimidazo[2,1-b][1,3]thiazole most potent inhibitor Trypanosoma cruzi
1.14.14.154 3-benzyl-1-pyridin-4-ylpyrrolidine-2,5-dione
-
 Trypanosoma cruzi
1.14.14.154 3-methyl-4-nitro-N-pyridin-4-ylbenzamide
-
 Trypanosoma cruzi
1.14.14.154 3-oxo-N-pyridin-4-yl-3H-benzo[f]chromene-2-carboxamide
-
 Trypanosoma cruzi
1.14.14.154 3-thien-2-yl-5,6-dihydroimidazo[2,1-b][1,3]thiazole
-
 Trypanosoma cruzi
1.14.14.154 N-pyridin-4-yl-9H-xanthene-9-carboxamide strongest binding compound Trypanosoma cruzi
1.14.14.154 Nalpha-[(4-methylcyclohexyl)carbonyl]-N-pyridin-4-yltryptophanamide strongest binding compound Trypanosoma cruzi

Metals/Ions

EC Number Metals/Ions Comment Organism Structure
1.14.14.154 Iron
-
 Trypanosoma cruzi

Organism

EC Number Organism UniProt Comment Textmining
1.14.14.154 Trypanosoma cruzi
-
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
1.14.14.154
-
 Trypanosoma cruzi

Source Tissue

EC Number Source Tissue Comment Organism Textmining
1.14.14.154 amastigote
-
 Trypanosoma cruzi
-
1.14.14.154 trypomastigote
-
 Trypanosoma cruzi
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.14.14.154 24-methylenedihydrolanosterol + [reduced NADPH-hemoprotein reductase] + O2 preferred substrate Trypanosoma cruzi ? + [oxidized NADPH-hemoprotein reductase] + H2O
-
 ?
1.14.14.154 lanosterol + [reduced NADPH-hemoprotein reductase] + O2
-
 Trypanosoma cruzi ? + [oxidized NADPH-hemoprotein reductase] + H2O
-
 ?

Synonyms

EC Number Synonyms Comment Organism
1.14.14.154 CYP51
-
 Trypanosoma cruzi

Cofactor

EC Number Cofactor Comment Organism Structure
1.14.14.154 cytochrome P450
-
 Trypanosoma cruzi