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SterolsSterol 14-DemethylaseHistone DemethylasesJumonji Domain-Containing Histone DemethylasesOxidoreductases, N-DemethylatingRetinoblastoma-Binding Protein 2LanosterolMethylationHistonesOxidoreductases, O-DemethylatingPhytosterolsErgosterolCholestadienolsSterol Regulatory Element Binding Protein 1Aminopyrine N-DemethylaseHistone-Lysine N-MethyltransferaseLysineCytochrome P-450 Enzyme SystemSterol Regulatory Element Binding Protein 2CholesterolOxidoreductasesStigmasterolAzolesEpigenesis, GeneticAniline HydroxylaseDesmosterolVanillic AcidF-Box ProteinsTranylcypromineSulfonium CompoundsCholestenesKetoconazoleNitroanisole O-DemethylaseSterol Regulatory Element Binding ProteinsDehydrocholesterolsSqualeneMicrosomes, LiverPargylineChromatin Immunoprecipitation14-alpha Demethylase InhibitorsRepressor ProteinsChromatinCytochrome P-450 CYP2E1MiconazoleCholestanesDNA MethylationMolecular Sequence DataCholestanetriol 26-MonooxygenaseCo-Repressor ProteinsPromoter Regions, GeneticSasaRetinoblastoma Binding ProteinsEconazoleTranscription FactorsTranscription, GeneticHydroxymethylglutaryl CoA ReductasesLiverMutationHistone DeacetylasesHydroxycholesterolsAntifungal AgentsDimethylnitrosamineDNA-Binding ProteinsGene SilencingNuclear ProteinsCell Line, TumorPolycomb-Group ProteinsGene Expression RegulationSterol O-AcyltransferaseProtein BindingRNA InterferenceAmino Acid SequenceSubstrate SpecificityMevalonic AcidGene Knockdown TechniquesProtein Structure, TertiaryDioxygenasesFluconazoleEmbryonic Stem CellsDealkylationGas Chromatography-Mass SpectrometryCCAAT-Enhancer-Binding ProteinsChromatin Assembly and DisassemblyMental Retardation, X-LinkedMicrosomesProtein MethyltransferasesCell LineSteroid IsomerasesXanthomatosis, CerebrotendinousKetoglutaric AcidsSmith-Lemli-Opitz SyndromeDrug Resistance, FungalTriparanolMedroxyprogesteroneHEK293 CellsBiocatalysisGene Expression Regulation, DevelopmentalCyclin A1Candida albicansCells, Cultured
Cyp51Lanosterol 14-demethylaseInhibitorsInhibit the enzyme lanosterolPrecursorsDependent enzymeCompoundsSynthesis of ergosterolBiosynthesis of sterolsFungalERG11Ergosterol in fungiConversion of lanosterol to ergosterolFungiOxidoreductaseHemeCytochrome P450OverexpressionEukaryotic membranesAzoleAccumulationCandidaCatalyzesMetabolicYeastAntifungalMutationsReactionActivityContents
Cyp515
  • The demethylated products of the CYP51 reaction are vital intermediates in pathways leading to the formation of cholesterol in humans, ergosterol in fungi, and other types of sterols in plants. (wikipedia.org)
  • Human Sterol 14Alpha-Demethylase (Cyp51) as a Target for Anticancer Chemotherapy: Towards Structure-Aided Drug Design. (expasy.org)
  • The CYP51 family (sterol 14α-demethylase) certainly belongs to the second group. (vanderbilt.edu)
  • At the amino acid sequence identity across the kingdoms as low as 22-27%, all CYP51 family members catalyze one essentially the same three-step reaction of the oxidative removal of the 14α-methyl group from sterol precursors, enabling the formation of cholesterol in humans vs. ergosterol/egrosterol-like compounds in human pathogens. (vanderbilt.edu)
  • Validation of Human Sterol 14α-Demethylase (CYP51) Druggability: Structure-Guided Design, Synthesis, and Evaluation of Stoichiometric, Functionally Irreversible Inhibitors. (guidetopharmacology.org)
Lanosterol 14-demethylase3
  • Other names in common use include obtusufoliol 14-demethylase, lanosterol 14-demethylase, lanosterol 14alpha-demethylase, and sterol 14alpha-demethylase. (wikipedia.org)
  • The molecular mechanisms of azole resistance in Candida albicans include alterations in the target enzyme (lanosterol 14-demethylase) and overexpression of efflux transporters that decrease the intracellular concentration of the drug. (seq.es)
  • Overexpression of genes encoding lanosterol 14-demethylase (erg11) and efflux transporters (mdr1 and cdr) implicated in the development of resistance was monitored in matched sets of susceptible and resistant isolates. (seq.es)
Inhibitors2
Inhibit the enzyme lanosterol2
  • Imidazoles inhibit the enzyme lanosterol-14-α-demethylase, a cytochrome P-450-dependent enzyme that converts lanosterol to ergosterol. (davidgessner.com)
  • The exact mechanism of action for luliconazole's anti-fungal activity is still not known, but luliconazole is thought to inhibit the enzyme lanosterol demethylase. (drugbank.com)
Precursors2
  • accumulation of methylated sterol precursors. (health29.in)
  • This results in an accumulation of methylated sterol precursors and a depletion of ergosterol within the cell membrane thus weakening the structure and function of the fungal cell membrane. (nih.gov)
Dependent enzyme4
  • The antifungal azoles target fungal ergosterol biosynthesis by inhibiting the fungal CYP450-dependent enzyme lanosterol 14-α-demethylase, which blocks the conversion of lanosterol to ergosterol and leads to accumulation of aberrant sterol compounds and depletion of ergosterol in the fungal cell membrane. (davidgessner.com)
  • Azole antifungals work by inhibiting the cytochrome P450 dependent enzyme lanosterol 14-alpha-demethylase, which converts lanosterol to ergosterol, the main sterol in the fungal cell membrane. (davidgessner.com)
  • P-450 dependent enzyme, sterol 14α-demethylase, in fungi by binding to the heme cofactor located on the enzyme. (health29.in)
  • Ketoconazole blocks the synthesis of ergosterol, a key component of the fungal cell membrane, through the inhibition of cytochrome P-450 dependent enzyme lanosterol 14α-demethylase responsible for the conversion of lanosterol to ergosterol in the fungal cell membrane. (nih.gov)
Compounds3
  • Compounds that specifically inhibit STEROL 14-DEMETHYLASE. (davidgessner.com)
  • A new fructofuranoside glycerol, dryoptkirbioside (1), along with thirteen known compounds (2-14), was isolated from the MeOH extract of Dryopteris kirbi rhizomes by silica gel column chromatography, Sephadex LH-20 column chromatography, and semipreparative HPLC. (bvsalud.org)
  • Advances in synthetic biology and metabolic engineering have enabled de novo biosynthesis of sterols and steroids in yeast, which is a green and safe production route for these valuable steroidal compounds. (springeropen.com)
Synthesis of ergosterol3
  • By blocking fungal cytochrome P450-dependent enzymes, azoles disrupt the synthesis of ergosterol, which is the principal sterol in fungal cell membranes. (davidgessner.com)
  • Lanosterol demethylase is needed for the synthesis of ergosterol, which is a major component of the fungus cell membranes. (drugbank.com)
  • these agents inhibit the synthesis of ergosterol, a major fungal cell ̶ membrane sterol. (medscape.com)
Biosynthesis of sterols2
  • As a member of this family, lanosterol 14α-demethylase is responsible for an essential step in the biosynthesis of sterols. (davidgessner.com)
  • In this review, we summarize the metabolic engineering strategies developed and employed for improving the de novo biosynthesis of sterols and steroids in yeast based on the regulation mechanisms, and introduce the recent progresses in de novo synthesis of some typical sterols and steroids in yeast. (springeropen.com)
Fungal1
  • Because ergosterol constitutes a fundamental component of fungal membranes, many antifungal medications have been developed to inhibit 14α-demethylase activity and prevent the production of this key compound. (wikipedia.org)
ERG111
  • La sobreexpresión de los genes que codifican para la enzima lanosterol 14-a-desmetilasa (erg11) y para los transportadores de membrana (mdr1 y cdr) se monitorizó por comparación con aislamientos isogénicos sensibles. (seq.es)
Ergosterol in fungi1
Conversion of lanosterol to ergosterol1
  • Ketoconazole interacts with 14-α-sterol demethylase, a cytochrome P-450 enzyme necessary for the conversion of lanosterol to ergosterol. (com.bd)
Fungi1
  • Although the lanosterol 14α-demethylase is present in a wide variety of organisms, the enzyme is studied primarily in the context of fungi, where it plays an essential role in mediating membrane permeability. (wikipedia.org)
Oxidoreductase1
  • The systematic name of this enzyme class is sterol,NADPH:oxygen oxidoreductase (14-methyl cleaving). (wikipedia.org)
Heme1
  • The free-living nematode Caenorhabditis eleganslacks the capacity to synthesize heme but is able to take it from the cytochromes respiration sterols protist bacteria it feeds on (15). (medicinelakex1.com)
Cytochrome P4501
Overexpression1
  • Lack of an Intron in Cytochrome b and Overexpression of Sterol 14 alpha-Demethylase Indicate a Potential Risk for QoI and DMI Resistance Development in Neophysopella spp. (rothamsted.ac.uk)
Eukaryotic membranes1
  • Sterols represent the signature of eukaryotic membranes as well as serve as regulatory molecules that control growth and development processes. (vanderbilt.edu)
Azole1
  • The cyp51A gene encodes the target of azoles, lanosterol sistance in A. fumigatus is an emerging problem and may 14-demethylase, and this enzyme catalyzes a step in the develop during azole therapy. (cdc.gov)
Accumulation1
  • This metabolic inhibition also results in accumulation of 14α-methyl-3,6-diol, a toxic metabolite. (com.bd)
Candida1
  • Los mecanismos de resistencia a fluconazol en Candida albicans incluyen alteraciones en la enzima diana (lanosterol 14-a-desmetilasa) y sobreexpresión de transportadores activos de membrana que disminuyen la concentración intracelular de los azoles. (seq.es)
Catalyzes1
Metabolic1
  • In the present review, we will focus on the regulatory principles and metabolic engineering strategies for improving the de novo production of sterols and steroids in yeast, and introduce the recent progresses in de novo biosynthesis of typical sterols and steroids. (springeropen.com)
Yeast2
  • The endogenous sterol pathway in yeast is highlighted in yellow, heterogenous synthesis of animal-derived sterols in yeast is highlighted in red, heterogenous synthesis of phytosterols in yeast is highlighted in green and steroids derived from sterols are highlighted in blue. (springeropen.com)
  • Besides, non-conventional yeast like Yarrowia lipolytica and Pichia pastoris have also been engineered to produce some sterols and steroids, like pregnenolone and cholesterol (Hirz et al. (springeropen.com)
Antifungal1
Mutations1
Reaction1
Activity1
  • These sterols localize to the plasma membrane of cells, where they play an important structural role in the regulation of membrane fluidity and permeability and also influence the activity of enzymes, ion channels, and other cell components that are embedded within. (wikipedia.org)
Contents1