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Literature summary extracted from
- Sterol 14-demethylase inhibitors for Trypanosoma cruzi infections (2008), Adv. Exp. Med. Biol., 625, 61-80.
Inhibitors
| EC Number | Inhibitors | Comment | Organism | Structure |
|---|---|---|---|---|
| 1.14.14.154 | 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 |  |
| 1.14.14.154 | benznidazole | - |
Trypanosoma cruzi | |
| 1.14.14.154 | D0870 | - |
Trypanosoma cruzi | |
| 1.14.14.154 | econazole | - |
Trypanosoma cruzi | |
| 1.14.14.154 | fluconazole | - |
Trypanosoma cruzi | |
| 1.14.14.154 | itraconazole | - |
Candida albicans | |
| 1.14.14.154 | itraconazole | - |
Homo sapiens | |
| 1.14.14.154 | itraconazole | - |
Trypanosoma cruzi | |
| 1.14.14.154 | ketoconazole | - |
Candida albicans | |
| 1.14.14.154 | ketoconazole | - |
Homo sapiens | |
| 1.14.14.154 | ketoconazole | - |
Trypanosoma cruzi | |
| 1.14.14.154 | miconazole | - |
Trypanosoma cruzi | |
| 1.14.14.154 | 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 | |
| 1.14.14.154 | 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 | |
| 1.14.14.154 | posaconazole | - |
Trypanosoma cruzi | |
| 1.14.14.154 | ravuconazole | - |
Trypanosoma cruzi | |
| 1.14.14.154 | TAK-187 | - |
Trypanosoma cruzi | |
| 1.14.14.154 | voriconazole | - |
Trypanosoma cruzi | |
Metals/Ions
| EC Number | Metals/Ions | Comment | Organism | Structure |
|---|---|---|---|---|
| 1.14.14.154 | Fe2+ | heme-iron in the active site | Trypanosoma cruzi | |
Organism
| EC Number | Organism | UniProt | Comment | Textmining |
|---|---|---|---|---|
| 1.14.14.154 | Candida albicans | - |
- |
- |
| 1.14.14.154 | Homo sapiens | - |
- |
- |
| 1.14.14.154 | Mycobacterium tuberculosis | - |
- |
- |
| 1.14.14.154 | Trypanosoma brucei | - |
- |
- |
| 1.14.14.154 | Trypanosoma cruzi | Q7Z1V1 | strains Tulahuen, Peru, Y, EP, CL, SC-28, Colombiana, Bertoldo, YuYu and VL-10 | - |
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 | epimastigote | - |
Trypanosoma cruzi | - |
Substrates and Products (Substrate)
| EC Number | Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|---|
| 1.14.14.154 | lanosterol + [reduced NADPH-hemoprotein reductase] + O2 | active site contains an isoleucine, lanosterol is the preferred substrate | Trypanosoma cruzi | ? + [oxidized NADPH-hemoprotein reductase] + H2O | - |
? | |
| 1.14.14.154 | 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
| EC Number | Synonyms | Comment | Organism |
|---|---|---|---|
| 1.14.14.154 | CYP51 | - |
Homo sapiens |
| 1.14.14.154 | CYP51 | - |
Trypanosoma brucei |
| 1.14.14.154 | CYP51 | - |
Mycobacterium tuberculosis |
| 1.14.14.154 | CYP51 | - |
Candida albicans |
| 1.14.14.154 | CYP51 | - |
Trypanosoma cruzi |
IC50 Value
| EC Number | IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|---|
| 1.14.14.154 | 0.0000001 | - |
strain EP or Y, intracellular amastigote, Vero cell as host cell | Trypanosoma cruzi | ravuconazole | |
| 1.14.14.154 | 0.00000025 | - |
strain EP, intracellular amastigote, Vero cell as host cell | Trypanosoma cruzi | posaconazole | |
| 1.14.14.154 | 0.0000003 | - |
strain EP or Y, intracellular amastigote, Vero cell as host cell | Trypanosoma cruzi | TAK-187 | |
| 1.14.14.154 | 0.0000005 | - |
strain Tulahuen, intracellular amastigote | Trypanosoma cruzi | posaconazole | |
| 1.14.14.154 | 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 | |
| 1.14.14.154 | 0.000001 | - |
strain Tulahuen, intracellular amastigote | Trypanosoma cruzi | ketoconazole | |
| 1.14.14.154 | 0.000001 | - |
strain Tulahuen, intracellular amastigote | Trypanosoma cruzi | itraconazole | |
| 1.14.14.154 | 0.000001 | - |
strain Y, intracellular amastigote, macrophage as host cell | Trypanosoma cruzi | ketoconazole | |
| 1.14.14.154 | 0.000002 | - |
intracellular amastigote, macrophages as host cell | Trypanosoma cruzi | itraconazole | |
| 1.14.14.154 | 0.000002 | - |
strain Y, intracellular amastigote, Vero cell as host cell | Trypanosoma cruzi | ketoconazole | |
| 1.14.14.154 | 0.000004 | - |
strain Tulahuen, intracellular amastigote | Trypanosoma cruzi | voriconazole | |
| 1.14.14.154 | 0.00001 | - |
intracellular amastigote, Vero cell as host cell | Trypanosoma cruzi | D0870 | |
| 1.14.14.154 | 0.00001 | - |
strain Peru, intracellular amastigote, macrophage as host cell | Trypanosoma cruzi | ketoconazole | |
| 1.14.14.154 | 0.000014 | - |
strain EP, epimastigote | Trypanosoma cruzi | posaconazole | |
| 1.14.14.154 | 0.00002 | - |
strain Tulahuen, intracellular amastigote | Trypanosoma cruzi | miconazole | |
| 1.14.14.154 | 0.0001 | - |
epimastigote | Trypanosoma cruzi | D0870 | |
| 1.14.14.154 | 0.0001 | - |
strain EP or Y, epimastigote | Trypanosoma cruzi | ravuconazole | |
| 1.14.14.154 | 0.0001 | - |
strain Y, epimastigote | Trypanosoma cruzi | ketoconazole | |
| 1.14.14.154 | 0.0002 | - |
strain Peru, epimastigote | Trypanosoma cruzi | ketoconazole | |
| 1.14.14.154 | 0.0005 | - |
strain Tulahuen, murine 3T3 fibroblast as host cell | Trypanosoma cruzi | posaconazole | |
| 1.14.14.154 | 0.001 | - |
strain Tulahuen, murine 3T3 fibroblast as host cell | Trypanosoma cruzi | itraconazole | |
| 1.14.14.154 | 0.0015 | - |
strain Tulahuen, intracellular amastigote | Trypanosoma cruzi | benznidazole | |
| 1.14.14.154 | 0.008 | - |
strain Tulahuen, intracellular amastigote | Trypanosoma cruzi | fluconazole | |
| 1.14.14.154 | 0.008 | - |
strain Tulahuen, intracellular amastigote, murine 3T3 fibroblast as host cell | Trypanosoma cruzi | fluconazole | |
| 1.14.14.154 | 0.01 | - |
strain Tulahuen, murine 3T3 fibroblast as host cell | Trypanosoma cruzi | miconazole | |
| 1.14.14.154 | 0.02 | - |
strain Tulahuen, epimastigote | Trypanosoma cruzi | miconazole | |
| 1.14.14.154 | 0.02 | - |
strain Tulahuen, epimastigote | Trypanosoma cruzi | econazole | |
| 1.14.14.154 | 0.02 | - |
strain Tulahuen, murine 3T3 fibroblast as host cell | Trypanosoma cruzi | benznidazole | |
| 1.14.14.154 | 0.03 | - |
strain Tulahuen, murine 3T3 fibroblast as host cell | Trypanosoma cruzi | ketoconazole | |
| 1.14.14.154 | 0.03 | - |
strain Tulahuen, murine 3T3 fibroblast as host cell | Trypanosoma cruzi | voriconazole | |
| 1.14.14.154 | 0.1 | - |
strain Tulahuen, murine 3T3 fibroblast as host cell | Trypanosoma cruzi | fluconazole | |
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