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Literature summary for 1.14.14.154 extracted from

  • Buckner, F.S.
    Sterol 14-demethylase inhibitors for Trypanosoma cruzi infections (2008), Adv. Exp. Med. Biol., 625, 61-80.
    View publication on PubMed
Search for more literature for 1.14.14.154

Inhibitors

Inhibitors Comment Organism Structure
7-chloro-3-[(2R,3R)-3-(2,4-difluorophenyl)-3-hydroxy-4-(1H-1,2,4-triazol-1-yl)butan-2-yl]-4a,8a-dihydroquinazolin-4(3H)-one
-
 Trypanosoma cruzi
benznidazole
-
 Trypanosoma cruzi
D0870
-
 Trypanosoma cruzi
econazole
-
 Trypanosoma cruzi
fluconazole
-
 Trypanosoma cruzi
itraconazole
-
 Candida albicans
itraconazole
-
 Homo sapiens
itraconazole
-
 Trypanosoma cruzi
ketoconazole
-
 Candida albicans
ketoconazole
-
 Homo sapiens
ketoconazole
-
 Trypanosoma cruzi
miconazole
-
 Trypanosoma cruzi
additional information yeast cells are more sensitive to azole drugs than mammalian cells, yeast cells have lower P450 enzyme content and a higher IC50 value Candida albicans
additional information azole antifungals have higher IC50 values against the human CYP51 than against that of Candida albicans by a factor of ca. 30 Homo sapiens
posaconazole
-
 Trypanosoma cruzi
ravuconazole
-
 Trypanosoma cruzi
TAK-187
-
 Trypanosoma cruzi
voriconazole
-
 Trypanosoma cruzi

Metals/Ions

Metals/Ions Comment Organism Structure
Fe2+ heme-iron in the active site Trypanosoma cruzi

Organism

Organism UniProt Comment Textmining
Candida albicans
-
-
-
Homo sapiens
-
-
-
Mycobacterium tuberculosis
-
-
-
Trypanosoma brucei
-
-
-
Trypanosoma cruzi Q7Z1V1 strains Tulahuen, Peru, Y, EP, CL, SC-28, Colombiana, Bertoldo, YuYu and VL-10
-

Purification (Commentary)

Purification (Comment) Organism
-
 Trypanosoma cruzi

Source Tissue

Source Tissue Comment Organism Textmining
amastigote
-
 Trypanosoma cruzi
-
epimastigote
-
 Trypanosoma cruzi
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
lanosterol + [reduced NADPH-hemoprotein reductase] + O2 active site contains an isoleucine, lanosterol is the preferred substrate Trypanosoma cruzi ? + [oxidized NADPH-hemoprotein reductase] + H2O
-
 ?
obtusifoliol + [reduced NADPH-hemoprotein reductase] + O2 presence of the large phenylalanine side chain in the active site seems to lead to preferred processing of obtusifoliol Trypanosoma brucei 4alpha-methyl-5alpha-ergosta-8,14,24(28)-trien-3beta-ol + formate + [oxidized NADPH-hemoprotein reductase] + H2O
-
 ?

Synonyms

Synonyms Comment Organism
CYP51
-
 Homo sapiens
CYP51
-
 Trypanosoma brucei
CYP51
-
 Mycobacterium tuberculosis
CYP51
-
 Candida albicans
CYP51
-
 Trypanosoma cruzi

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000001
-
 strain EP or Y, intracellular amastigote, Vero cell as host cell Trypanosoma cruzi ravuconazole
0.00000025
-
 strain EP, intracellular amastigote, Vero cell as host cell Trypanosoma cruzi posaconazole
0.0000003
-
 strain EP or Y, intracellular amastigote, Vero cell as host cell Trypanosoma cruzi TAK-187
0.0000005
-
 strain Tulahuen, intracellular amastigote Trypanosoma cruzi posaconazole
0.000001
-
 strain EP or Y, intracellular amastigote, Vero cell as host cell Trypanosoma cruzi 7-chloro-3-[(2R,3R)-3-(2,4-difluorophenyl)-3-hydroxy-4-(1H-1,2,4-triazol-1-yl)butan-2-yl]-4a,8a-dihydroquinazolin-4(3H)-one
0.000001
-
 strain Tulahuen, intracellular amastigote Trypanosoma cruzi ketoconazole
0.000001
-
 strain Tulahuen, intracellular amastigote Trypanosoma cruzi itraconazole
0.000001
-
 strain Y, intracellular amastigote, macrophage as host cell Trypanosoma cruzi ketoconazole
0.000002
-
 intracellular amastigote, macrophages as host cell Trypanosoma cruzi itraconazole
0.000002
-
 strain Y, intracellular amastigote, Vero cell as host cell Trypanosoma cruzi ketoconazole
0.000004
-
 strain Tulahuen, intracellular amastigote Trypanosoma cruzi voriconazole
0.00001
-
 intracellular amastigote, Vero cell as host cell Trypanosoma cruzi D0870
0.00001
-
 strain Peru, intracellular amastigote, macrophage as host cell Trypanosoma cruzi ketoconazole
0.000014
-
 strain EP, epimastigote Trypanosoma cruzi posaconazole
0.00002
-
 strain Tulahuen, intracellular amastigote Trypanosoma cruzi miconazole
0.0001
-
 epimastigote Trypanosoma cruzi D0870
0.0001
-
 strain EP or Y, epimastigote Trypanosoma cruzi ravuconazole
0.0001
-
 strain Y, epimastigote Trypanosoma cruzi ketoconazole
0.0002
-
 strain Peru, epimastigote Trypanosoma cruzi ketoconazole
0.0005
-
 strain Tulahuen, murine 3T3 fibroblast as host cell Trypanosoma cruzi posaconazole
0.001
-
 strain Tulahuen, murine 3T3 fibroblast as host cell Trypanosoma cruzi itraconazole
0.0015
-
 strain Tulahuen, intracellular amastigote Trypanosoma cruzi benznidazole
0.008
-
 strain Tulahuen, intracellular amastigote Trypanosoma cruzi fluconazole
0.008
-
 strain Tulahuen, intracellular amastigote, murine 3T3 fibroblast as host cell Trypanosoma cruzi fluconazole
0.01
-
 strain Tulahuen, murine 3T3 fibroblast as host cell Trypanosoma cruzi miconazole
0.02
-
 strain Tulahuen, epimastigote Trypanosoma cruzi miconazole
0.02
-
 strain Tulahuen, epimastigote Trypanosoma cruzi econazole
0.02
-
 strain Tulahuen, murine 3T3 fibroblast as host cell Trypanosoma cruzi benznidazole
0.03
-
 strain Tulahuen, murine 3T3 fibroblast as host cell Trypanosoma cruzi ketoconazole
0.03
-
 strain Tulahuen, murine 3T3 fibroblast as host cell Trypanosoma cruzi voriconazole
0.1
-
 strain Tulahuen, murine 3T3 fibroblast as host cell Trypanosoma cruzi fluconazole