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Literature summary for 1.14.14.154 extracted from

  • Emami, S.; Tavangar, P.; Keighobadi, M.
    An overview of azoles targeting sterol 14?-demethylase for antileishmanial therapy (2017), Eur. J. Med. Chem., 135, 241-259 .
    View publication on PubMed

Application

Application Comment Organism
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
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
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
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
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
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

Inhibitors Comment Organism Structure
2,2-dimethyl-1,3-dichloropropane i.e.D0870 Leishmania infantum
2,2-dimethyl-1,3-dichloropropane i.e.D0870 Leishmania major
2,2-dimethyl-1,3-dichloropropane i.e.D0870 Leishmania mexicana
3-(alpha-imidazolylbenzyl)indole
-
Leishmania infantum
3-(alpha-imidazolylbenzyl)indole
-
Leishmania major
3-(alpha-imidazolylbenzyl)indole
-
Leishmania mexicana
3-(alpha-triazolylbenzyl)indole
-
Leishmania infantum
3-(alpha-triazolylbenzyl)indole
-
Leishmania major
3-(alpha-triazolylbenzyl)indole
-
Leishmania mexicana
bifonazole
-
Leishmania infantum
bifonazole
-
Leishmania major
bifonazole
-
Leishmania mexicana
clotrimazole
-
Leishmania infantum
clotrimazole
-
Leishmania major
clotrimazole
-
Leishmania mexicana
econazole
-
Leishmania infantum
econazole
-
Leishmania major
econazole
-
Leishmania mexicana
fluconazole
-
Leishmania infantum
fluconazole
-
Leishmania major
fluconazole
-
Leishmania mexicana
itraconazole
-
Leishmania infantum
itraconazole
-
Leishmania major
itraconazole
-
Leishmania mexicana
ketoconazole
-
Leishmania infantum
ketoconazole
-
Leishmania major
ketoconazole
-
Leishmania mexicana
meglumine antimoniate
-
Leishmania infantum
meglumine antimoniate
-
Leishmania major
meglumine antimoniate
-
Leishmania mexicana
miconazole
-
Leishmania infantum
miconazole
-
Leishmania major
miconazole
-
Leishmania mexicana
posaconazole
-
Leishmania infantum
posaconazole
-
Leishmania major
posaconazole
-
Leishmania mexicana
voriconazole
-
Leishmania infantum
voriconazole
-
Leishmania major
voriconazole
-
Leishmania mexicana

Organism

Organism UniProt Comment Textmining
Leishmania infantum A2TEF2
-
-
Leishmania major
-
-
-
Leishmania mexicana
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
amastigote
-
Leishmania mexicana
-
amastigote
-
Leishmania major
-
amastigote
-
Leishmania infantum
-
promastigote
-
Leishmania mexicana
-
promastigote
-
Leishmania major
-
promastigote
-
Leishmania infantum
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
14alpha-methylzymosterol + [reduced NADPH-hemoprotein reductase] + O2
-
Leishmania mexicana ?
-
?
14alpha-methylzymosterol + [reduced NADPH-hemoprotein reductase] + O2
-
Leishmania infantum ?
-
?
lanosterol + [reduced NADPH-hemoprotein reductase] + O2
-
Leishmania mexicana ?
-
?
lanosterol + [reduced NADPH-hemoprotein reductase] + O2
-
Leishmania infantum ?
-
?
obtusifoliol + [reduced NADPH-hemoprotein reductase] + O2
-
Leishmania mexicana ?
-
?
obtusifoliol + [reduced NADPH-hemoprotein reductase] + O2
-
Leishmania infantum ?
-
?

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00281
-
pH and temperature not specified in the publication Leishmania infantum clotrimazole
0.0044
-
pH and temperature not specified in the publication, axenic amastigotes Leishmania mexicana 3-(alpha-imidazolylbenzyl)indole
0.00536
-
pH and temperature not specified in the publication Leishmania infantum econazole
0.00897
-
pH and temperature not specified in the publication Leishmania infantum bifonazole

General Information

General Information Comment Organism
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
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
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
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
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
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