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Literature summary for 1.14.14.154 extracted from

  • Stana, A.; Vodnar, D.C.; Tamaian, R.; Pirn?u, A.; Vlase, L.; Ionu?, I.; Oniga, O.; Tiperciuc, B.
    Design, synthesis and antifungal activity evaluation of new thiazolin-4-ones as potential lanosterol 14alpha-demethylase inhibitors (2017), Int. J. Mol. Sci., 18, E177 .
    View publication on PubMedView publication on EuropePMC
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Application

Application Comment Organism
medicine the enzyme constitutes an important biological target for the most popular class of antifungals Candida albicans SC5314
pharmacology the enzyme constitutes an important biological target for the most popular class of antifungals Candida albicans SC5314

Inhibitors

Inhibitors Comment Organism Structure
2-(methylamino)thiazol-4(5H)-one
-
 Candida albicans SC5314
2-(naphthalen-1-ylamino)thiazol-4(5H)-one
-
 Candida albicans SC5314
5-(2,4-dichlorobenzylidene)-2-(naphthalen-1-ylamino)thiazol-4(5H)-one
-
 Candida albicans SC5314
5-(4-nitrobenzylidene)-2-(phenylamino)thiazol-4(5H)-one
-
 Candida albicans SC5314
fluconazole
-
 Candida albicans SC5314
additional information the enzyme constitutes an important biological target for the most popular class of antifungals. Inhibition of lanosterol 14alpha-demethylase leads to accumulation of 14-a-methylsterols on the fungal surface and alteration of the permeability and rigidity of the plasma membrane, which results in arrest of fungal growth. Because this enzyme is found in all eukaryotes (including humans) and because the azoles interact also with other cytochrome P450 dependent enzymes (CYP3A4), a selective inhibition towards the fungal CYP51A1 is essential for an increased therapeutic index Candida albicans SC5314

Organism

Organism UniProt Comment Textmining
Candida albicans SC5314 P10613
-
-

Synonyms

Synonyms Comment Organism
CYP51A1
-
 Candida albicans SC5314
lanosterol 14alpha-demethylase
-
 Candida albicans SC5314

General Information

General Information Comment Organism
metabolism key enzyme in the synthesis of ergosterol, an essential component of the fungal cell membrane Candida albicans SC5314
physiological function key enzyme in the synthesis of ergosterol, an essential component of the fungal cell membrane Candida albicans SC5314