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Disease on EC 1.14.14.154 - sterol 14alpha-demethylase

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DISEASE
TITLE OF PUBLICATION
LINK TO PUBMED
Amebiasis
Azole Antifungal Agents To Treat the Human Pathogens Acanthamoeba castellanii and Acanthamoeba polyphaga through Inhibition of Sterol 14?-Demethylase (CYP51).
Antley-Bixler Syndrome Phenotype
Cytochrome P450 oxidoreductase gene mutations and Antley-Bixler syndrome with abnormal genitalia and/or impaired steroidogenesis: molecular and clinical studies in 10 patients.
Cytochrome P450s in the synthesis of cholesterol and bile acids - from mouse models to human diseases.
Defects in cholesterol synthesis genes in mouse and in humans: lessons for drug development and safer treatments.
Aspergillosis
(New) Methods for Detection of Aspergillus fumigatus Resistance in Clinical Samples.
Azole resistance in Aspergillus: an emerging problem?
Azole-resistant Aspergillus fumigatus in the environment: Identifying key reservoirs and hotspots of antifungal resistance.
Clinical and experimental phenotype of azole-resistant Aspergillus fumigatus with a HapE splice site mutation: a case report.
Composite Survival Index to Compare Virulence Changes in Azole-Resistant Aspergillus fumigatus Clinical Isolates.
Deciphering Aspergillus fumigatus cyp51A-mediated triazole resistance by pyrosequencing of respiratory specimens.
Development of novel PCR assays to detect azole resistance-mediating mutations of the Aspergillus fumigatus cyp51A gene in primary clinical samples from neutropenic patients.
Direct Molecular Diagnosis of Aspergillosis and CYP51A Profiling from Respiratory Samples of French Patients.
Essential gene identification and drug target prioritization in Aspergillus fumigatus.
Identification of Fungal Species and Detection of Azole-Resistance Mutations in the Aspergillus fumigatus cyp51A Gene at a South Korean Hospital.
Impact of cyp51A mutations on the pharmacokinetic and pharmacodynamic properties of voriconazole in a murine model of disseminated aspergillosis.
In Vitro Biochemical Study of CYP51-Mediated Azole Resistance in Aspergillus fumigatus.
In Vivo Selection of a Unique Tandem Repeat Mediated Azole Resistance Mechanism (TR120) in Aspergillus fumigatus cyp51A, Denmark.
Incidence of Cyp51 A key mutations in Aspergillus fumigatus-a study on primary clinical samples of immunocompromised patients in the period of 1995-2013.
Molecular epidemiology of aspergillosis in Magellanic penguins and susceptibility patterns of clinical isolates.
PCR-based detection of Aspergillus fumigatus Cyp51A mutations on bronchoalveolar lavage: a multicentre validation of the AsperGenius assay® in 201 patients with haematological disease suspected for invasive aspergillosis.
Progressive Dispersion of Azole Resistance in Aspergillus fumigatus: Fatal Invasive Aspergillosis in a Patient with Acute Myeloid Leukemia Infected with an A. fumigatus Strain with a cyp51A TR46 Y121F M172I T289A Allele.
The novel fungal CYP51 inhibitor VT-1598 displays classic dose-dependent antifungal activity in murine models of invasive aspergillosis.
Atherosclerosis
Vascular gene expression in mice overexpressing human endothelin-1 targeted to the endothelium.
Candidemia
Fluconazole-resistant Candida parapsilosis strains with a Y132F substitution in the ERG11 gene causing invasive infections in a neonatal unit, South Africa.
The A395T Mutation in ERG11 Gene Confers Fluconazole Resistance in Candida tropicalis Causing Candidemia.
Candidiasis
Analysis of Global Antifungal Surveillance Results Reveals Predominance of Erg11 Y132F Alteration among Azole-Resistant Candida parapsilosis and Candida tropicalis and Country-Specific Isolate Dissemination.
ERG11 Gene Mutations and MDR1 Upregulation Confer Pan-Azole Resistance in Candida tropicalis Causing Disseminated Candidiasis in an Acute Lymphoblastic Leukemia Patient on Posaconazole Prophylaxis.
Nitrate Esters of Heteroaromatic Compounds as Candida albicans CYP51 Enzyme Inhibitors.
Susceptibility of clinical isolates of Candida species to fluconazole and detection of Candida albicans ERG11 mutations.
Candidiasis, Invasive
General hospital outbreak of invasive candidiasis due to azole-resistant Candida parapsilosis associated with an Erg11 Y132F mutation.
Candidiasis, Vulvovaginal
A phase 2, randomized, double-blind, placebo-controlled, dose-ranging study to evaluate the efficacy and safety of orally administered VT-1161 in the treatment of recurrent vulvovaginal candidiasis.
Correlation between azole susceptibilities, genotypes, and ERG11 mutations in Candida albicans isolates associated with vulvovaginal candidiasis in China.
Carcinogenesis
Atorvastatin inhibits pancreatic carcinogenesis and increases survival in LSL-Kras(G12D) -LSL-Trp53(R172H) -Pdx1-Cre mice.
Carcinoma
A New Survival Model Based on Cholesterol Biosynthesis-Related Genes for Prognostic Prediction in Clear Cell Renal Cell Carcinoma.
Carcinoma, Hepatocellular
Nitric oxide stimulates cellular degradation of human CYP51A1, the highly conserved lanosterol 14?-demethylase.
Novel cholesterol biosynthesis inhibitors targeting human lanosterol 14alpha-demethylase (CYP51).
The ubiquitously expressed human CYP51 encodes lanosterol 14 alpha-demethylase, a cytochrome P450 whose expression is regulated by oxysterols.
Cataract
Phenotypes of Recessive Pediatric Cataract in a Cohort of Children with Identified Homozygous Gene Mutations (An American Ophthalmological Society Thesis).
Chagas Disease
4-Aminopyridyl-based CYP51 inhibitors as anti-Trypanosoma cruzi drug leads with improved pharmacokinetic profile and in vivo potency.
4-aminopyridyl-based lead compounds targeting CYP51 prevent spontaneous parasite relapse in a chronic model and improve cardiac pathology in an acute model of Trypanosoma cruzi infection.
A new era for chagas disease drug discovery?
A Non-azole CYP51 Inhibitor Cures Chagas Disease in a Mouse Model of Acute Infection.
Antitrypanosomal Treatment with Benznidazole Is Superior to Posaconazole Regimens in Mouse Models of Chagas Disease.
Clinical Candidate VT-1161's Antiparasitic Effect In Vitro, Activity in a Murine Model of Chagas Disease, and Structural Characterization in Complex with the Target Enzyme CYP51 from Trypanosoma cruzi.
Complexes of Trypanosoma cruzi sterol 14alpha-demethylase (CYP51) with two pyridine-based drug candidates for Chagas disease: Structural basis for pathogen-selectivity.
CYP51 from Trypanosoma cruzi: a phyla-specific residue in the B' helix defines substrate preferences of sterol 14alpha-demethylase.
Design or screening of drugs for the treatment of Chagas disease: what shows the most promise?
Development of a Fluorescence-based Trypanosoma cruzi CYP51 Inhibition Assay for Effective Compound Triaging in Drug Discovery Programmes for Chagas Disease.
Different Therapeutic Outcomes of Benznidazole and VNI Treatments in Different Genders in Mouse Experimental Models of Trypanosoma cruzi Infection.
Dynamics of CYP51: implications for function and inhibitor design.
Identification of Pyrazolo[3,4-e][1,4]thiazepin based CYP51 inhibitors as potential Chagas disease therapeutic alternative: In vitro and in vivo evaluation, binding mode prediction and SAR exploration.
Nitroheterocyclic compounds are more efficacious than CYP51 inhibitors against Trypanosoma cruzi: implications for Chagas disease drug discovery and development.
Recent Developments in Sterol 14-demethylase Inhibitors for Chagas Disease.
Review on Experimental Treatment Strategies Against Trypanosoma cruzi.
Second Generation Analogues of the Cancer Drug Clinical Candidate Tipifarnib for Anti-Chagas Disease Drug Discovery.
Sequence variation in CYP51A from the Y strain of Trypanosoma cruzi alters its sensitivity to inhibition.
Stairway to Heaven or Hell? Perspectives and Limitations of Chagas Disease Chemotherapy.
Sterol 14-demethylase inhibitors for Trypanosoma cruzi infections.
Sterol 14?-Demethylase Structure-Based Design of VNI (( R)- N-(1-(2,4-Dichlorophenyl)-2-(1 H-imidazol-1-yl)ethyl)-4-(5-phenyl-1,3,4-oxadiazol-2-yl)benzamide)) Derivatives To Target Fungal Infections: Synthesis, Biological Evaluation, and Crystallographic Analysis.
Sterol 14?-Demethylase Structure-Based Optimization of Drug Candidates for Human Infections with the Protozoan Trypanosomatidae.
Structural insights into inhibition of sterol 14alpha-demethylase in the human pathogen Trypanosoma cruzi.
Structurally simple inhibitors of lanosterol 14alpha-demethylase are efficacious in a rodent model of acute Chagas disease.
Trypanosoma cruzi CYP51 Inhibitor Derived from a Mycobacterium tuberculosis Screen Hit.
VFV as a New Effective CYP51 Structure-Derived Drug Candidate for Chagas Disease and Visceral Leishmaniasis.
Coccidioidomycosis
Efficacy of the Investigational Antifungal VT-1161 in Treating Naturally Occurring Coccidioidomycosis in Dogs.
The Novel Fungal Cyp51 Inhibitor VT-1598 Is Efficacious in Experimental Models of Central Nervous System Coccidioidomycosis Caused by Coccidioides posadasii and Coccidioides immitis.
Coinfection
Detection of azole-susceptible and azole-resistant Aspergillus coinfection by cyp51A PCR amplicon melting curve analysis.
Colorectal Neoplasms
Characterisation of the oxysterol metabolising enzyme pathway in mismatch repair proficient and deficient colorectal cancer.
Communicable Diseases
A convergent, scalable and stereoselective synthesis of azole CYP51 inhibitors.
Cryptococcosis
In Silico Structural Modeling and Analysis of Interactions of Tremellomycetes Cytochrome P450 Monooxygenases CYP51s with Substrates and Azoles.
Cystic Fibrosis
High airborne level of Aspergillus fumigatus and presence of azole-resistant TR34/L98H isolates in the home of a cystic fibrosis patient harbouring chronic colonisation with azole-resistant H285Y A. fumigatus.
Cysts
The antifungal drug isavuconazole is both amebicidal and cysticidal against Acanthamoeba castellanii.
Dandruff
Functional expression and characterization of CYP51 from dandruff-causing Malassezia globosa.
Dyslipidemias
Role of dipeptidyl peptidase IV (DPP4) in the development of dyslipidemia: DPP4 contributes to the steroid metabolism pathway.
Three-dimensional quantitative structure-activity relationship analysis of human CYP51 inhibitors.
Epilepsy
Screening of novel epilepsy-related genes and isolation and identification of cDNAs.
Galactosemias
Novel phenotypes and loci identified through clinical genomics approaches to pediatric cataract.
Heart Failure
Mouse Knockout of the Cholesterogenic Cytochrome P450 Lanosterol 14{alpha}-Demethylase (Cyp51) Resembles Antley-Bixler Syndrome.
Hypercholesterolemia
Elevated cellular cholesterol in Familial Alzheimer's presenilin 1 mutation is associated with lipid raft localization of ?-amyloid precursor protein.
Lead nitrate-induced development of hypercholesterolemia in rats: sterol-independent gene regulation of hepatic enzymes responsible for cholesterol homeostasis.
Hypersensitivity
A Novel Zn2-Cys6 Transcription Factor AtrR Plays a Key Role in an Azole Resistance Mechanism of Aspergillus fumigatus by Co-regulating cyp51A and cdr1B Expressions.
Hypothyroidism
Effect of hypothyroidism on CYP51 and FSHR expression in rat ovary.
Infections
4-Aminopyridyl-based CYP51 inhibitors as anti-Trypanosoma cruzi drug leads with improved pharmacokinetic profile and in vivo potency.
4-aminopyridyl-based lead compounds targeting CYP51 prevent spontaneous parasite relapse in a chronic model and improve cardiac pathology in an acute model of Trypanosoma cruzi infection.
A Crucial Role for Ergosterol in Plasma Membrane Composition, Localisation, and Activity of Cdr1p and H+-ATPase in Candida albicans.
A Non-azole CYP51 Inhibitor Cures Chagas Disease in a Mouse Model of Acute Infection.
Antitrypanosomal Activity of Sterol 14?-Demethylase (CYP51) Inhibitors VNI and VFV in the Swiss Mouse Models of Chagas Disease Induced by the Trypanosoma cruzi Y Strain.
Assessing anti-T. cruzi candidates in vitro for sterile cidality.
Contributions of both ATP-binding cassette transporter and Cyp51A proteins are essential for azole resistance in Aspergillus fumigatus.
Crystal structures of Trypanosoma brucei sterol 14alpha-demethylase and implications for selective treatment of human infections.
CYP51 as drug targets for fungi and protozoan parasites: past, present and future.
ERG3 and ERG11 genes are critical for the pathogenesis of Candida albicans during the oral mucosal infection.
Essential gene identification and drug target prioritization in Aspergillus fumigatus.
Expression and homology modelling of sterol 14alpha-demethylase of Magnaporthe grisea and its interaction with azoles.
Fluconazole-resistant Candida parapsilosis strains with a Y132F substitution in the ERG11 gene causing invasive infections in a neonatal unit, South Africa.
High airborne level of Aspergillus fumigatus and presence of azole-resistant TR34/L98H isolates in the home of a cystic fibrosis patient harbouring chronic colonisation with azole-resistant H285Y A. fumigatus.
Identification of Pyrazolo[3,4-e][1,4]thiazepin based CYP51 inhibitors as potential Chagas disease therapeutic alternative: In vitro and in vivo evaluation, binding mode prediction and SAR exploration.
In Vitro and In Vivo Studies of the Antiparasitic Activity of Sterol 14?-Demethylase (CYP51) Inhibitor VNI against Drug-Resistant Strains of Trypanosoma cruzi.
Opposite expression of CYP51A1 and its natural antisense transcript AluCYP51A1 in adenovirus type 37 infected retinal pigmented epithelial cells.
Organocatalytic, enantioselective synthesis of VNI: a robust therapeutic development platform for Chagas, a neglected tropical disease.
Pharmacodynamics and Dose-Response Relationships of Liposomal Amphotericin B against Different Azole-Resistant Aspergillus fumigatus Isolates in a Murine Model of Disseminated Aspergillosis.
Principles of a New Protocol for Prediction of Azole Resistance in Candida albicans Infections on the Basis of ERG11 Polymorphisms.
Sequence variation in CYP51A from the Y strain of Trypanosoma cruzi alters its sensitivity to inhibition.
Sterol 14-demethylase inhibitors for Trypanosoma cruzi infections.
Structural basis for conservation in the CYP51 family.
The antifungal drug isavuconazole inhibits the replication of human cytomegalovirus (HCMV) and acts synergistically with anti-HCMV drugs.
The Candida albicans lanosterol 14-alpha-demethylase (ERG11) gene promoter is maximally induced after prolonged growth with antifungal drugs.
The Tetrazole VT-1161 Is a Potent Inhibitor of Trichophyton rubrum through Its Inhibition of T. rubrum CYP51.
Uncovering New Mutations Conferring Azole Resistance in the Aspergillus fumigatus cyp51A Gene.
Invasive Pulmonary Aspergillosis
Failure of voriconazole therapy due to acquired azole resistance in Aspergillus fumigatus in a kidney transplant recipient with chronic necrotizing aspergillosis.
Impact of in vivo Triazole and Echinocandin Combination Therapy for Invasive Pulmonary Aspergillosis: Enhanced Efficacy against Cyp51 Mutant Isolates.
Isavuconazole (BAL4815) Pharmacodynamic Target Determination in an in vivo Murine Model of Invasive Pulmonary Aspergillosis against Wild Type and Cyp51 Mutant Isolates of Aspergillus fumigatus.
Posaconazole pharmacodynamic target determination against wild-type and Cyp51 mutant isolates of Aspergillus fumigatus in an in vivo model of invasive pulmonary aspergillosis.
Leishmaniasis
Sterol 14alpha-Demethylase (CYP51) as a Therapeutic Target for Human Trypanosomiasis and Leishmaniasis.
Leishmaniasis, Visceral
Sterol 14?-Demethylase Structure-Based Optimization of Drug Candidates for Human Infections with the Protozoan Trypanosomatidae.
Targeting Ergosterol Biosynthesis in Leishmania donovani: Essentiality of Sterol 14alpha-demethylase.
VFV as a New Effective CYP51 Structure-Derived Drug Candidate for Chagas Disease and Visceral Leishmaniasis.
Leukemia
Cholesterol is essential for mitosis progression and its deficiency induces polyploid cell formation.
Sterol stringency of proliferation and cell cycle progression in human cells.
Leukemia, Myeloid, Acute
Comparison of Two Molecular Assays for Detection and Characterization of Aspergillus fumigatus Triazole Resistance and Cyp51A Mutations in Clinical Isolates and Primary Clinical Samples of Immunocompromised Patients.
Progressive Dispersion of Azole Resistance in Aspergillus fumigatus: Fatal Invasive Aspergillosis in a Patient with Acute Myeloid Leukemia Infected with an A. fumigatus Strain with a cyp51A TR46 Y121F M172I T289A Allele.
Two missense mutations, E123Q and K151E, identified in the ERG11 allele of an azole-resistant isolate of Candida kefyr recovered from a stem cell transplant patient for acute myeloid leukemia.
Lipidoses
Suppression of cytochrome P450 reductase expression in hepatoma cells replicates the hepatic lipidosis observed in hepatic POR-null mice.
Liver Diseases
Novel phenotypes and loci identified through clinical genomics approaches to pediatric cataract.
Lung Diseases
Targeted gene disruption of the 14-alpha sterol demethylase (cyp51A) in Aspergillus fumigatus and its role in azole drug susceptibility.
Mastitis
The A756T Mutation of the ERG11 Gene Associated With Resistance to Itraconazole in Candida Krusei Isolated From Mycotic Mastitis of Cows.
Meningitis, Cryptococcal
The Fungal Cyp51 Inhibitor VT-1129 Is Efficacious in an Experimental Model of Cryptococcal Meningitis.
The novel fungal CYP51 inhibitor VT-1598 is efficacious alone and in combination with liposomal amphotericin B in a murine model of cryptococcal meningitis.
Meningoencephalitis
CYP51 is an essential drug target for the treatment of primary amoebic meningoencephalitis (PAM).
Metabolic Syndrome
STUDIES ON THE EXPRESSION LEVELS OF STEROL-METABOLIZING ENZYMES IN THE OBESE MODEL SHR/NDmcr-cp RATS.
Mycoses
A Non-azole CYP51 Inhibitor Cures Chagas Disease in a Mouse Model of Acute Infection.
A yeast sterol auxotroph (erg25) is rescued by addition of azole antifungals and reduced levels of heme.
Characteristics of the heterologously expressed human lanosterol 14alpha-demethylase (other names: P45014DM, CYP51, P45051) and inhibition of the purified human and Candida albicans CYP51 with azole antifungal agents.
Crystal structure of cytochrome P450 14alpha -sterol demethylase (CYP51) from Mycobacterium tuberculosis in complex with azole inhibitors.
Discovery of 1,2,3-selenadiazole analogues as antifungal agents using a scaffold hopping approach.
Evaluation of the combination mode of azoles antifungal inhibitors with CACYP51 and the influence of Site-directed mutation.
Fluconazole binding and sterol demethylation in three CYP51 isoforms indicate differences in active site topology.
Host-induced gene silencing of cytochrome P450 lanosterol C14?-demethylase-encoding genes confers strong resistance to Fusarium species.
In Silico Structural Modeling and Analysis of Interactions of Tremellomycetes Cytochrome P450 Monooxygenases CYP51s with Substrates and Azoles.
In vitro and in vivo effects of 14alpha-demethylase (ERG11) depletion in Candida glabrata.
Lead optimization generates selenium-containing miconazole CYP51 inhibitors with improved pharmacological profile for the treatment of fungal infections.
Pyridylethanol(phenylethyl)amines are non-azole, highly selective Candida albicans sterol 14?-demethylase inhibitors.
Study on the efficiency of dsRNAs with increasing length in RNA-based silencing of the Fusarium CYP51 genes.
Three-dimensional quantitative structure-activity relationship analysis of human CYP51 inhibitors.
X-ray structure of 4,4'-dihydroxybenzophenone mimicking sterol substrate in the active site of sterol 14alpha-demethylase (CYP51).
[Small Animal Aspergillosis and Cryptococcosis in Japan].
Neoplasms
A transcriptome-based protein network that identifies new therapeutic targets in colorectal cancer.
Human Lanosterol 14-Alpha Demethylase (CYP51A1) Is a Putative Target for Natural Flavonoid Luteolin 7,3'-Disulfate.
Patterns of expression of cytochrome P450 genes in progression of hepatitis C virus-associated hepatocellular carcinoma.
Second Generation Analogues of the Cancer Drug Clinical Candidate Tipifarnib for Anti-Chagas Disease Drug Discovery.
Targeting C4-demethylating genes in the cholesterol pathway sensitizes cancer cells to EGF receptor inhibitors via increased EGF receptor degradation.
Three-dimensional quantitative structure-activity relationship analysis of human CYP51 inhibitors.
Neurofibromatoses
Why increased nuchal translucency is associated with congenital heart disease; a systematic review on genetic mechanisms.
Neurofibromatosis 1
Why increased nuchal translucency is associated with congenital heart disease; a systematic review on genetic mechanisms.
Non-alcoholic Fatty Liver Disease
Integrated analysis of hepatic mRNA and miRNA profiles identified molecular networks and potential biomarkers of NAFLD.
Obesity
STUDIES ON THE EXPRESSION LEVELS OF STEROL-METABOLIZING ENZYMES IN THE OBESE MODEL SHR/NDmcr-cp RATS.
Parasitic Diseases
4-aminopyridyl-based lead compounds targeting CYP51 prevent spontaneous parasite relapse in a chronic model and improve cardiac pathology in an acute model of Trypanosoma cruzi infection.
Plant Diseases
A world-wide analysis of reduced sensitivity to DMI fungicides in the banana pathogen Pseudocercospora fijiensis.
Precursor Cell Lymphoblastic Leukemia-Lymphoma
ERG11 Gene Mutations and MDR1 Upregulation Confer Pan-Azole Resistance in Candida tropicalis Causing Disseminated Candidiasis in an Acute Lymphoblastic Leukemia Patient on Posaconazole Prophylaxis.
Pulmonary Aspergillosis
Azole-resistant Aspergillus fumigatus isolates carrying TR34 /L98H mutations in Taiwan.
Correlation between Triazole Treatment History and Susceptibility in Clinically Isolated Aspergillus fumigatus.
Failure of voriconazole therapy due to acquired azole resistance in Aspergillus fumigatus in a kidney transplant recipient with chronic necrotizing aspergillosis.
Pulmonary Disease, Chronic Obstructive
Emergence of Aspergillus fumigatus azole resistance in azole-naïve patients with chronic obstructive pulmonary disease and their homes.
Retinal Degeneration
Opposite expression of CYP51A1 and its natural antisense transcript AluCYP51A1 in adenovirus type 37 infected retinal pigmented epithelial cells.
sterol 14alpha-demethylase deficiency
Mouse Knockout of the Cholesterogenic Cytochrome P450 Lanosterol 14{alpha}-Demethylase (Cyp51) Resembles Antley-Bixler Syndrome.
Trypanosomiasis
CYP51: A Major Drug Target in the Cytochrome P450 Superfamily.
Sterol 14alpha-Demethylase (CYP51) as a Therapeutic Target for Human Trypanosomiasis and Leishmaniasis.
Tuberculosis
1,4-Benzothiazine and 1,4-benzoxazine imidazole derivatives with antifungal activity: a docking study.
A Nano-MgO and Ionic Liquid-Catalyzed 'Green' Synthesis Protocol for the Development of Adamantyl-Imidazolo-Thiadiazoles as Anti-Tuberculosis Agents Targeting Sterol 14?-Demethylase (CYP51).
A novel sterol 14alpha-demethylase/ferredoxin fusion protein (MCCYP51FX) from Methylococcus capsulatus represents a new class of the cytochrome P450 superfamily.
An old activity in the cytochrome P450 superfamily (CYP51) and a new story of drugs and resistance.
Azole-antifungal binding to a novel cytochrome P450 from Mycobacterium tuberculosis: implications for treatment of tuberculosis.
Biophysical characterization of the sterol demethylase P450 from Mycobacterium tuberculosis, its cognate ferredoxin, and their interactions.
Bulky 1,4-benzoxazine derivatives with antifungal activity.
Characterization and catalytic properties of the sterol 14alpha-demethylase from Mycobacterium tuberculosis.
Characterization of G-Quadruplex Motifs in espB, espK, and cyp51 Genes of Mycobacterium tuberculosis as Potential Drug Targets.
Concerning P450 evolution: Structural Analyses Support Bacterial Origin of Sterol 14?-Demethylases.
Conformational dynamics in the F/G segment of CYP51 from Mycobacterium tuberculosis monitored by FRET.
Conservation and cloning of CYP51: a sterol 14 alpha-demethylase from Mycobacterium smegmatis.
Conservation in the CYP51 family. Role of the B' helix/BC loop and helices F and G in enzymatic function.
Crystal structure of cytochrome P450 14alpha -sterol demethylase (CYP51) from Mycobacterium tuberculosis in complex with azole inhibitors.
Crystal structures of Trypanosoma brucei sterol 14alpha-demethylase and implications for selective treatment of human infections.
CYP121, CYP51 and associated redox systems in Mycobacterium tuberculosis: towards deconvoluting enzymology of P450 systems in a human pathogen.
CYP51 from Trypanosoma brucei is obtusifoliol-specific.
CYP51-like gene of Mycobacterium tuberculosis actually encodes a P450 similar to eukaryotic CYP51.
cyp51A-based mechanism of azole resistance in Aspergillus fumigatus: Illustration by a new 3D Structural Model of Aspergillus fumigatus CYP51A protein.
Electrochemical reduction of sterol-14alpha-demethylase from Mycobacterium tuberculosis (CYP51b1).
Electrochemistry of cytochromes p450: analysis of current-voltage characteristics of electrodes with immobilized cytochromes p450 for the screening of substrates and inhibitors.
Fluconazole binding and sterol demethylation in three CYP51 isoforms indicate differences in active site topology.
Folding requirements are different between sterol 14alpha-demethylase (CYP51) from Mycobacterium tuberculosis and human or fungal orthologs.
Genetic basis for differential activities of fluconazole and voriconazole against Candida krusei.
Homology modeling of lanosterol 14alpha-demethylase of Candida albicans and Aspergillus fumigatus and insights into the enzyme-substrate Interactions.
Interaction of Mycobacterium tuberculosis CYP130 with heterocyclic arylamines.
Molecular Oxygen Activation and Proton Transfer Mechanisms in Lanosterol 14alpha-Demethylase Catalysis.
Molecular simulations of fluconazole-mediated inhibition of sterol biosynthesis.
MT FdR: a ferredoxin reductase from M. tuberculosis that couples to MT CYP51.
Multiple drug binding modes in Mycobacterium tuberculosis CYP51B1.
Mycobacterium tuberculosis CYP130: crystal structure, biophysical characterization, and interactions with antifungal azole drugs.
Peroxo-iron mediated deformylation in sterol 14alpha-demethylase catalysis.
Rapid P450 heme iron reduction by laser photoexcitation of Mycobacterium tuberculosis CYP121 and CYP51B1. Analysis of CO complexation reactions and reversibility of the P450/P420 equilibrium.
Small-Molecule Scaffolds for CYP51 Inhibitors Identified by High-Throughput Screening and Defined by X-Ray Crystallography.
Spin equilibrium and O?-binding kinetics of Mycobacterium tuberculosis CYP51 with mutations in the histidine-threonine dyad.
Sterol 14 alpha-demethylase, an abundant and essential mixed-function oxidase.
Structural basis of human CYP51 inhibition by antifungal azoles.
Structural diversities of active site in clinical azole-bound forms between sterol 14alpha-demethylases (CYP51s) from human and Mycobacterium tuberculosis.
Structure-based rational screening of novel hit compounds with structural diversity for cytochrome P450 sterol 14alpha-demethylase from Penicillium digitatum.
Substrate recognition sites in 14alpha-sterol demethylase from comparative analysis of amino acid sequences and X-ray structure of Mycobacterium tuberculosis CYP51.
Three-dimensional models of 14?-sterol demethylase (Cyp51A) from Aspergillus lentulus and Aspergillus fumigatus: an insight into differences in voriconazole interaction.
Three-dimensional models of wild-type and mutated forms of cytochrome P450 14alpha-sterol demethylases from Aspergillus fumigatus and Candida albicans provide insights into posaconazole binding.
Trypanosoma cruzi CYP51 Inhibitor Derived from a Mycobacterium tuberculosis Screen Hit.
X-ray structure of 4,4'-dihydroxybenzophenone mimicking sterol substrate in the active site of sterol 14alpha-demethylase (CYP51).
[Expression of the Mycobacterium tuberculosis cytochrome CYP51 gene in Escherichia coli]
[Genetic heterogeneity of cytochrome CYP51 in clinical strains of Mycobacterium tuberculosis]
[Structural-functional motifs of sterol 14-alpha demethylases (CYP51)]