Any feedback?
Literature summary extracted from
- An overview of azoles targeting sterol 14?-demethylase for antileishmanial therapy (2017), Eur. J. Med. Chem., 135, 241-259 .
Application
| EC Number | Application | Comment | Organism |
|---|---|---|---|
| 1.14.14.154 | medicine | the chemotherapy of leishmaniasis is a serious problem in the field of neglected tropical diseases. Since the biosynthesis of specific sterols is vital for effective survival, normal proliferation and infectivity of Leishmania parasites, the sterol 14alpha-demethylase inhibitors obtained from azole antifungal drug discovery programs can be used in antileishmanial therapy | Leishmania mexicana |
| 1.14.14.154 | medicine | the chemotherapy of leishmaniasis is a serious problem in the field of neglected tropical diseases. Since the biosynthesis of specific sterols is vital for effective survival, normal proliferation and infectivity of Leishmania parasites, the sterol 14alpha-demethylase inhibitors obtained from azole antifungal drug discovery programs can be used in antileishmanial therapy | Leishmania major |
| 1.14.14.154 | medicine | the chemotherapy of leishmaniasis is a serious problem in the field of neglected tropical diseases. Since the biosynthesis of specific sterols is vital for effective survival, normal proliferation and infectivity of Leishmania parasites, the sterol 14alpha-demethylase inhibitors obtained from azole antifungal drug discovery programs can be used in antileishmanial therapy | Leishmania infantum |
| 1.14.14.154 | pharmacology | the chemotherapy of leishmaniasis is a serious problem in the field of neglected tropical diseases. Since the biosynthesis of specific sterols is vital for effective survival, normal proliferation and infectivity of Leishmania parasites, the sterol 14alpha-demethylase inhibitors obtained from azole antifungal drug discovery programs can be used in antileishmanial therapy | Leishmania mexicana |
| 1.14.14.154 | pharmacology | the chemotherapy of leishmaniasis is a serious problem in the field of neglected tropical diseases. Since the biosynthesis of specific sterols is vital for effective survival, normal proliferation and infectivity of Leishmania parasites, the sterol 14alpha-demethylase inhibitors obtained from azole antifungal drug discovery programs can be used in antileishmanial therapy | Leishmania major |
| 1.14.14.154 | pharmacology | the chemotherapy of leishmaniasis is a serious problem in the field of neglected tropical diseases. Since the biosynthesis of specific sterols is vital for effective survival, normal proliferation and infectivity of Leishmania parasites, the sterol 14alpha-demethylase inhibitors obtained from azole antifungal drug discovery programs can be used in antileishmanial therapy | Leishmania infantum |
Inhibitors
| EC Number | Inhibitors | Comment | Organism | Structure |
|---|---|---|---|---|
| 1.14.14.154 | 2,2-dimethyl-1,3-dichloropropane | i.e.D0870 | Leishmania infantum |  |
| 1.14.14.154 | 2,2-dimethyl-1,3-dichloropropane | i.e.D0870 | Leishmania major | |
| 1.14.14.154 | 2,2-dimethyl-1,3-dichloropropane | i.e.D0870 | Leishmania mexicana | |
| 1.14.14.154 | 3-(alpha-imidazolylbenzyl)indole | - |
Leishmania infantum | |
| 1.14.14.154 | 3-(alpha-imidazolylbenzyl)indole | - |
Leishmania major | |
| 1.14.14.154 | 3-(alpha-imidazolylbenzyl)indole | - |
Leishmania mexicana | |
| 1.14.14.154 | 3-(alpha-triazolylbenzyl)indole | - |
Leishmania infantum | |
| 1.14.14.154 | 3-(alpha-triazolylbenzyl)indole | - |
Leishmania major | |
| 1.14.14.154 | 3-(alpha-triazolylbenzyl)indole | - |
Leishmania mexicana | |
| 1.14.14.154 | bifonazole | - |
Leishmania infantum | |
| 1.14.14.154 | bifonazole | - |
Leishmania major | |
| 1.14.14.154 | bifonazole | - |
Leishmania mexicana | |
| 1.14.14.154 | clotrimazole | - |
Leishmania infantum | |
| 1.14.14.154 | clotrimazole | - |
Leishmania major | |
| 1.14.14.154 | clotrimazole | - |
Leishmania mexicana | |
| 1.14.14.154 | econazole | - |
Leishmania infantum | |
| 1.14.14.154 | econazole | - |
Leishmania major | |
| 1.14.14.154 | econazole | - |
Leishmania mexicana | |
| 1.14.14.154 | fluconazole | - |
Leishmania infantum | |
| 1.14.14.154 | fluconazole | - |
Leishmania major | |
| 1.14.14.154 | fluconazole | - |
Leishmania mexicana | |
| 1.14.14.154 | itraconazole | - |
Leishmania infantum | |
| 1.14.14.154 | itraconazole | - |
Leishmania major | |
| 1.14.14.154 | itraconazole | - |
Leishmania mexicana | |
| 1.14.14.154 | ketoconazole | - |
Leishmania infantum | |
| 1.14.14.154 | ketoconazole | - |
Leishmania major | |
| 1.14.14.154 | ketoconazole | - |
Leishmania mexicana | |
| 1.14.14.154 | meglumine antimoniate | - |
Leishmania infantum | |
| 1.14.14.154 | meglumine antimoniate | - |
Leishmania major | |
| 1.14.14.154 | meglumine antimoniate | - |
Leishmania mexicana | |
| 1.14.14.154 | miconazole | - |
Leishmania infantum | |
| 1.14.14.154 | miconazole | - |
Leishmania major | |
| 1.14.14.154 | miconazole | - |
Leishmania mexicana | |
| 1.14.14.154 | posaconazole | - |
Leishmania infantum | |
| 1.14.14.154 | posaconazole | - |
Leishmania major | |
| 1.14.14.154 | posaconazole | - |
Leishmania mexicana | |
| 1.14.14.154 | voriconazole | - |
Leishmania infantum | |
| 1.14.14.154 | voriconazole | - |
Leishmania major | |
| 1.14.14.154 | voriconazole | - |
Leishmania mexicana | |
Organism
| EC Number | Organism | UniProt | Comment | Textmining |
|---|---|---|---|---|
| 1.14.14.154 | Leishmania infantum | A2TEF2 | - |
- |
| 1.14.14.154 | Leishmania major | - |
- |
- |
| 1.14.14.154 | Leishmania mexicana | - |
- |
- |
Source Tissue
| EC Number | Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|---|
| 1.14.14.154 | amastigote | - |
Leishmania mexicana | - |
| 1.14.14.154 | amastigote | - |
Leishmania major | - |
| 1.14.14.154 | amastigote | - |
Leishmania infantum | - |
| 1.14.14.154 | promastigote | - |
Leishmania mexicana | - |
| 1.14.14.154 | promastigote | - |
Leishmania major | - |
| 1.14.14.154 | promastigote | - |
Leishmania infantum | - |
Substrates and Products (Substrate)
| EC Number | Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|---|
| 1.14.14.154 | 14alpha-methylzymosterol + [reduced NADPH-hemoprotein reductase] + O2 | - |
Leishmania mexicana | ? | - |
? | |
| 1.14.14.154 | 14alpha-methylzymosterol + [reduced NADPH-hemoprotein reductase] + O2 | - |
Leishmania infantum | ? | - |
? | |
| 1.14.14.154 | lanosterol + [reduced NADPH-hemoprotein reductase] + O2 | - |
Leishmania mexicana | ? | - |
? | |
| 1.14.14.154 | lanosterol + [reduced NADPH-hemoprotein reductase] + O2 | - |
Leishmania infantum | ? | - |
? | |
| 1.14.14.154 | obtusifoliol + [reduced NADPH-hemoprotein reductase] + O2 | - |
Leishmania mexicana | ? | - |
? | |
| 1.14.14.154 | obtusifoliol + [reduced NADPH-hemoprotein reductase] + O2 | - |
Leishmania infantum | ? | - |
? | |
IC50 Value
| EC Number | IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|---|
| 1.14.14.154 | 0.00281 | - |
pH and temperature not specified in the publication | Leishmania infantum | clotrimazole | |
| 1.14.14.154 | 0.0044 | - |
pH and temperature not specified in the publication, axenic amastigotes | Leishmania mexicana | 3-(alpha-imidazolylbenzyl)indole | |
| 1.14.14.154 | 0.00536 | - |
pH and temperature not specified in the publication | Leishmania infantum | econazole | |
| 1.14.14.154 | 0.00897 | - |
pH and temperature not specified in the publication | Leishmania infantum | bifonazole | |
General Information
| EC Number | General Information | Comment | Organism |
|---|---|---|---|
| 1.14.14.154 | malfunction | inactivation of the enzyme in promastigotes results in disruption of the membrane stability, increase of membrane fluidity, failure to maintain lipid rafts, and hypersensitivity to heat stress along with altered morphology and cytokinesis defect. The effect deletion on lipid composition and sterol biosynthesis is a complete loss of ergostane-based sterols (5-dehydroepisterol, ergosterol, and episterol) and accumulation of toxic 14-methylated sterols | Leishmania mexicana |
| 1.14.14.154 | malfunction | inactivation of the enzyme in promastigotes results in disruption of the membrane stability, increase of membrane fluidity, failure to maintain lipid rafts, and hypersensitivity to heat stress along with altered morphology and cytokinesis defect. The effect deletion on lipid composition and sterol biosynthesis is a complete loss of ergostane-based sterols (5-dehydroepisterol, ergosterol, and episterol) and accumulation of toxic 14-methylated sterols | Leishmania major |
| 1.14.14.154 | malfunction | inactivation of the enzyme in promastigotes results in disruption of the membrane stability, increase of membrane fluidity, failure to maintain lipid rafts, and hypersensitivity to heat stress along with altered morphology and cytokinesis defect. The effect deletion on lipid composition and sterol biosynthesis is a complete loss of ergostane-based sterols (5-dehydroepisterol, ergosterol, and episterol) and accumulation of toxic 14-methylated sterols | Leishmania infantum |
| 1.14.14.154 | physiological function | the enzyme is required for effective survival, normal proliferation and infectivity of Leishmania major parasites in the mammalian host. The enzyme is not required for promastigote survival or proliferation, but it is involved in the control of cell shape, differentiation, and division | Leishmania mexicana |
| 1.14.14.154 | physiological function | the enzyme is required for effective survival, normal proliferation and infectivity of Leishmania major parasites in the mammalian host. The enzyme is not required for promastigote survival or proliferation, but it is involved in the control of cell shape, differentiation, and division | Leishmania major |
| 1.14.14.154 | physiological function | the enzyme is required for effective survival, normal proliferation and infectivity of Leishmania major parasites in the mammalian host. The enzyme is not required for promastigote survival or proliferation, but it is involved in the control of cell shape, differentiation, and division | Leishmania infantum |
Use of this online version of BRENDA is free under the CC BY 4.0 license. See terms of use for full details.
Release 2023.1 (January 2023)
Legal
Curated at
Member of
