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Literature summary for 1.14.14.154 extracted from
- Comparison of lanosterol-14 alpha-demethylase (CYP51) of human and Candida albicans for inhibition by different antifungal azoles (2006), Toxicology, 228, 24-32.
Cloned(Commentary)
| Cloned (Comment) | Organism |
|---|---|
| expression in Spodoptera frugiperda Sf9 cell membranes under control of the p10 promoter using the baculovirus transfection system | Candida albicans |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| bifonazole | IC50: 300 nM | Candida albicans |  |
| bifonazole | IC50: 0.0008 mM | Homo sapiens | |
| bitertanol | IC50: 59 nM | Candida albicans | |
| bitertanol | IC50: 0.0013 mM | Homo sapiens | |
| clotrimazole | IC50: 91 nM | Candida albicans | |
| clotrimazole | IC50: 0.0009 mM | Homo sapiens | |
| cyproconazole | IC50: 100 nM | Candida albicans | |
| cyproconazole | IC50: 0.0228 mM | Homo sapiens | |
| epoxiconazole | IC50: 220 nM | Candida albicans | |
| epoxiconazole | IC50: 0.0020 mM | Homo sapiens | |
| fadrozole | IC50: 0.0322 mM, above | Candida albicans | |
| fadrozole | IC50: 0.10 mM, above | Homo sapiens | |
| fluconazole | IC50: 51 nM, above | Candida albicans | |
| fluconazole | IC50: 0.030 mM, above | Homo sapiens | |
| flusilazole | IC50: 85 nM | Candida albicans | |
| flusilazole | IC50: 0.0034 mM | Homo sapiens | |
| hexaconazole | IC50: 66 nM | Candida albicans | |
| hexaconazole | IC50: 0.0156 mM | Homo sapiens | |
| imazalil | IC50: 82 nM | Candida albicans | |
| imazalil | IC50: 0.0361 mM | Homo sapiens | |
| itraconazole | IC50: 39 nM | Candida albicans | |
| itraconazole | IC50: 0.030 mM | Homo sapiens | |
| ketoconazole | IC50: 64 nM | Candida albicans | |
| ketoconazole | IC50: 0.0004 mM | Homo sapiens | |
| letrozole | IC50: 0.0133 mM, above | Candida albicans | |
| letrozole | IC50: 0.10 mM, above | Homo sapiens | |
| miconazole | IC50: 72 nM | Candida albicans | |
| miconazole | IC50: 0.00006 mM | Homo sapiens | |
| additional information | inhibitory potency of fungicides, antifungal drugs, and cytostatic drugs, overview | Candida albicans | |
| additional information | inhibitory potency of fungicides, antifungal drugs, and cytostatic drugs, overview | Homo sapiens | |
| myclobutanil | IC50: 140 nM | Candida albicans | |
| myclobutanil | IC50: 0.0290 mM | Homo sapiens | |
| penconazole | IC50: 76 nM | Candida albicans | |
| penconazole | IC50: 0.0193 mM | Homo sapiens | |
| Prochloraz | IC50: 98 nM | Candida albicans | |
| Prochloraz | IC50: 0.0050 mM | Homo sapiens | |
| Propiconazole | IC50: 150 nM | Candida albicans | |
| Propiconazole | IC50: 0.0083 mM | Homo sapiens | |
| tebuconazole | IC50: 350 nM | Candida albicans | |
| tebuconazole | IC50: 0.0036 mM | Homo sapiens | |
| triadimefon | IC50: 130 nM | Candida albicans | |
| triadimefon | IC50: 0.010 mM | Homo sapiens | |
| triadimenol | IC50: 330 nM | Candida albicans | |
| triadimenol | IC50: 0.0372 mM | Homo sapiens | |
KM Value [mM]
| KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.0017 | - |
lanosterol | pH 7.4, 37°C | Homo sapiens | |
| 0.0074 | - |
lanosterol | pH 7.4, 37°C | Candida albicans | |
Metals/Ions
| Metals/Ions | Comment | Organism | Structure |
|---|---|---|---|
| Mg2+ | - |
Homo sapiens | |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| lanosterol + [reduced NADPH-hemoprotein reductase] + O2 | Homo sapiens | - |
? | production of follicular fluid-meiosis activating steroid by lanosterol demethylation | ? | |
| lanosterol + [reduced NADPH-hemoprotein reductase] + O2 | Candida albicans | - |
? | production of follicular fluid-meiosis activating steroid by lanosterol demethylation | ? | |
| additional information | Homo sapiens | enzyme inhibition may result in endocrine disruption since follicular fluid-meiosis activating steroid, the direct product of lanosterol demethylation, is involved in the control of meiosis | ? | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Candida albicans | - |
- |
- |
| Homo sapiens | - |
- |
- |
Specific Activity [micromol/min/mg]
| Specific Activity Minimum [µmol/min/mg] | Specific Activity Maximum [µmol/min/mg] | Comment | Organism |
|---|---|---|---|
| additional information | - |
- |
Homo sapiens |
| additional information | - |
- |
Candida albicans |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| lanosterol + [reduced NADPH-hemoprotein reductase] + O2 | - |
Homo sapiens | ? | production of follicular fluid-meiosis activating steroid by lanosterol demethylation | ? | |
| lanosterol + [reduced NADPH-hemoprotein reductase] + O2 | - |
Candida albicans | ? | production of follicular fluid-meiosis activating steroid by lanosterol demethylation | ? | |
| additional information | enzyme inhibition may result in endocrine disruption since follicular fluid-meiosis activating steroid, the direct product of lanosterol demethylation, is involved in the control of meiosis | Homo sapiens | ? | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| CYP51 | - |
Homo sapiens |
| CYP51 | - |
Candida albicans |
| lanosterol-14alpha-demethylase | - |
Homo sapiens |
| lanosterol-14alpha-demethylase | - |
Candida albicans |
Temperature Optimum [°C]
| Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
|---|---|---|---|
| 37 | - |
assay at | Homo sapiens |
| 37 | - |
assay at | Candida albicans |
pH Optimum
| pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
|---|---|---|---|
| 7.4 | - |
assay at | Homo sapiens |
| 7.4 | - |
assay at | Candida albicans |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.0000091 | - |
IC50: 91 nM | Candida albicans | clotrimazole | |
| 0.000039 | - |
IC50: 39 nM | Candida albicans | itraconazole | |
| 0.000051 | - |
IC50: 51 nM, above | Candida albicans | fluconazole | |
| 0.000059 | - |
IC50: 59 nM | Candida albicans | bitertanol | |
| 0.00006 | - |
IC50: 0.00006 mM | Homo sapiens | miconazole | |
| 0.000064 | - |
IC50: 64 nM | Candida albicans | ketoconazole | |
| 0.000066 | - |
IC50: 66 nM | Candida albicans | hexaconazole | |
| 0.000072 | - |
IC50: 72 nM | Candida albicans | miconazole | |
| 0.000076 | - |
IC50: 76 nM | Candida albicans | penconazole | |
| 0.000082 | - |
IC50: 82 nM | Candida albicans | imazalil | |
| 0.000085 | - |
IC50: 85 nM | Candida albicans | flusilazole | |
| 0.000098 | - |
IC50: 98 nM | Candida albicans | Prochloraz | |
| 0.0001 | - |
IC50: 100 nM | Candida albicans | cyproconazole | |
| 0.00013 | - |
IC50: 130 nM | Candida albicans | triadimefon | |
| 0.00014 | - |
IC50: 140 nM | Candida albicans | myclobutanil | |
| 0.00015 | - |
IC50: 150 nM | Candida albicans | Propiconazole | |
| 0.00022 | - |
IC50: 220 nM | Candida albicans | epoxiconazole | |
| 0.0003 | - |
IC50: 300 nM | Candida albicans | bifonazole | |
| 0.00033 | - |
IC50: 330 nM | Candida albicans | triadimenol | |
| 0.00035 | - |
IC50: 350 nM | Candida albicans | tebuconazole | |
| 0.0004 | - |
IC50: 0.0004 mM | Homo sapiens | ketoconazole | |
| 0.0008 | - |
IC50: 0.0008 mM | Homo sapiens | bifonazole | |
| 0.0009 | - |
IC50: 0.0009 mM | Homo sapiens | clotrimazole | |
| 0.0013 | - |
IC50: 0.0013 mM | Homo sapiens | bitertanol | |
| 0.002 | - |
IC50: 0.0020 mM | Homo sapiens | epoxiconazole | |
| 0.0034 | - |
IC50: 0.0034 mM | Homo sapiens | flusilazole | |
| 0.0036 | - |
IC50: 0.0036 mM | Homo sapiens | tebuconazole | |
| 0.005 | - |
IC50: 0.0050 mM | Homo sapiens | Prochloraz | |
| 0.0083 | - |
IC50: 0.0083 mM | Homo sapiens | Propiconazole | |
| 0.01 | - |
IC50: 0.010 mM | Homo sapiens | triadimefon | |
| 0.0133 | - |
IC50: 0.0133 mM, above | Candida albicans | letrozole | |
| 0.0156 | - |
IC50: 0.0156 mM | Homo sapiens | hexaconazole | |
| 0.0193 | - |
IC50: 0.0193 mM | Homo sapiens | penconazole | |
| 0.0228 | - |
IC50: 0.0228 mM | Homo sapiens | cyproconazole | |
| 0.029 | - |
IC50: 0.0290 mM | Homo sapiens | myclobutanil | |
| 0.03 | - |
IC50: 0.030 mM | Homo sapiens | itraconazole | |
| 0.03 | - |
IC50: 0.030 mM, above | Homo sapiens | fluconazole | |
| 0.0322 | - |
IC50: 0.0322 mM, above | Candida albicans | fadrozole | |
| 0.0361 | - |
IC50: 0.0361 mM | Homo sapiens | imazalil | |
| 0.0372 | - |
IC50: 0.0372 mM | Homo sapiens | triadimenol | |
| 0.1 | - |
IC50: 0.10 mM, above | Homo sapiens | fadrozole | |
| 0.1 | - |
IC50: 0.10 mM, above | Homo sapiens | letrozole | |
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