Relevant bibliographies by topics / Sterol 14α-demethylase / Journal articles
To see the other types of publications on this topic, follow the link: Sterol 14α-demethylase.

Journal articles on the topic 'Sterol 14α-demethylase'

Author: Grafiati
Published: 5 June 2025
Last updated: 1 August 2025

Create a spot-on reference in APA, MLA, Chicago, Harvard, and other styles

Select a source type:

Consult the top 50 journal articles for your research on the topic 'Sterol 14α-demethylase.'

Next to every source in the list of references, there is an 'Add to bibliography' button. Press on it, and we will generate automatically the bibliographic reference to the chosen work in the citation style you need: APA, MLA, Harvard, Chicago, Vancouver, etc.

You can also download the full text of the academic publication as pdf and read online its abstract whenever available in the metadata.

Browse journal articles on a wide variety of disciplines and organise your bibliography correctly.

1

Munayyer, Hanan K., Paul A. Mann, Andrew S. Chau та ін. "Posaconazole Is a Potent Inhibitor of Sterol 14α-Demethylation in Yeasts and Molds". Antimicrobial Agents and Chemotherapy 48, № 10 (2004): 3690–96. http://dx.doi.org/10.1128/aac.48.10.3690-3696.2004.

Full text
Abstract:
ABSTRACT Posaconazole (POS; SCH 56592) is a novel triazole that is active against a wide variety of fungi, including fluconazole-resistant Candida albicans isolates and fungi that are inherently less susceptible to approved azoles, such as Candida glabrata. In this study, we compared the effects of POS, itraconazole (ITZ), fluconazole (FLZ), and voriconazole (VOR) on sterol biosynthesis in strains of C. albicans (both azole-sensitive and azole-resistant strains), C. glabrata, Aspergillus fumigatus, and Aspergillus flavus. Following exposure to azoles, nonsaponifiable sterols were extracted and
APA, Harvard, Vancouver, ISO, and other styles
2

Orozco, Alison S., Lindsey M. Higginbotham, Christopher A. Hitchcock, et al. "Mechanism of Fluconazole Resistance inCandida krusei." Antimicrobial Agents and Chemotherapy 42, no. 10 (1998): 2645–49. http://dx.doi.org/10.1128/aac.42.10.2645.

Full text
Abstract:
ABSTRACT The mechanisms of fluconazole resistance in three clinical isolates of Candida krusei were investigated. Analysis of sterols of organisms grown in the absence and presence of fluconazole demonstrated that the predominant sterol of C. krusei is ergosterol and that fluconazole inhibits 14α-demethylase in this organism. The 14α-demethylase activity in cell extracts of C. kruseiwas 16- to 46-fold more resistant to inhibition by fluconazole than was 14α-demethylase activity in cell extracts of two fluconazole-susceptible strains of Candida albicans. Comparing the carbon monoxide difference
APA, Harvard, Vancouver, ISO, and other styles
3

Lepesheva, G. I., T. Y. Hargrove, R. D. Ott, W. D. Nes, and M. R. Waterman. "Biodiversity of CYP51 in trypanosomes." Biochemical Society Transactions 34, no. 6 (2006): 1161–64. http://dx.doi.org/10.1042/bst0341161.

Full text
Abstract:
Sterol 14α-demethylases (CYP51) are metabolic cytochromes P450, found in each biological kingdom. They catalyse a single three-step reaction included in all sterol biosynthetic pathways. Plant CYP51s have strict preference towards their physiological substrate O (obtusifoliol), which is C-4-monomethylated. Natural substrates of animal/fungal CYP51 (lanosterol, 24,25-dihydrolanosterol or 24-methylenelanosterol) are C-4-dimethylated. CYP51 from the pathogenic protozoa TB (Trypanosoma brucei) is the first example of O-specific sterol 14α-demethylase in non-photosynthetic organisms. Surprisingly,
APA, Harvard, Vancouver, ISO, and other styles
4

Ibrahim, Mohammed Auwal, Murtala Bindawa Isah, Nasir Tajuddeen, Saadatu Auwal Hamza та Aminu Mohammed. "Interaction of Stigmasterol with Trypanosomal Uridylyl Transferase, Farnesyl Diphosphate Synthase and Sterol 14α-demethylase: An In Silico Prediction of Mechanism of Action". Letters in Drug Design & Discovery 16, № 7 (2019): 799–807. http://dx.doi.org/10.2174/1570180815666180711110324.

Full text
Abstract:
Background: Trypanosomiasis is one of the neglected tropical diseases and continues to cause serious morbidity, mortality and economic loss. Current anti-trypanosomal drugs are antiquated and suffer from a number of serious setbacks, thereby necessitating the search for new drugs. Stigmasterol has previously demonstrated in vitro and in vivo anti-trypanosomal activity. Methods: Herein, stigmasterol was docked into three validated anti-trypanosomal drug targets; uridylyl transferase, farnesyl diphosphate synthase and sterol 14α-demethylase, in order to elucidate the possible biochemical targets
APA, Harvard, Vancouver, ISO, and other styles
5

Hull, Claire M., Josie E. Parker, Oliver Bader, et al. "Facultative Sterol Uptake in an Ergosterol-Deficient Clinical Isolate of Candida glabrata Harboring a Missense Mutation inERG11and Exhibiting Cross-Resistance to Azoles and Amphotericin B." Antimicrobial Agents and Chemotherapy 56, no. 8 (2012): 4223–32. http://dx.doi.org/10.1128/aac.06253-11.

Full text
Abstract:
ABSTRACTWe identified a clinical isolate ofCandida glabrata(CG156) exhibiting flocculent growth and cross-resistance to fluconazole (FLC), voriconazole (VRC), and amphotericin B (AMB), with MICs of >256, >256, and 32 μg ml−1, respectively. Sterol analysis using gas chromatography-mass spectrometry (GC-MS) revealed that CG156 was a sterol 14α-demethylase (Erg11p) mutant, wherein 14α-methylated intermediates (lanosterol was >80% of the total) were the only detectable sterols.ERG11sequencing indicated that CG156 harbored a single-amino-acid substitution (G315D) which nullified the functi
APA, Harvard, Vancouver, ISO, and other styles
6

Lamb, David C., Michel Cannieux, Andrew G. S. Warrilow та ін. "Plant Sterol 14α-Demethylase Affinity for Azole Fungicides". Biochemical and Biophysical Research Communications 284, № 3 (2001): 845–49. http://dx.doi.org/10.1006/bbrc.2001.5010.

Full text
APA, Harvard, Vancouver, ISO, and other styles
7

Yu, Jin Hui, Ting Qi, Li Xiong, et al. "Fungicides Inhibition Analysis by Molecular Docking and Sensitivity Testing of Penicillium italicum." Applied Mechanics and Materials 380-384 (August 2013): 4170–74. http://dx.doi.org/10.4028/www.scientific.net/amm.380-384.4170.

Full text
Abstract:
Blue mold, caused by Penicillium. italicum, is one of the most damaging postharvest diseases of citrus fruit. P. italicum Sterol 14α-demethylase (PiCYP51), an important enzyme in membrance sterol biosynthesis, is a key target of antifungal compounds for citrus disease caused by P. italicum. The three-dimensional structure of PiCYP51 from P. italicum Chinese isolate (HS-1) was constructed through homology modeling basing on the crystal structure of human CYP51. After molecular dynamics (MD) simulation, the refined model was assessed by PROCHECK on the quality. Following evaluation on the reliab
APA, Harvard, Vancouver, ISO, and other styles
8

Franz, Renate, Steven L. Kelly, David C. Lamb, Diane E. Kelly, Markus Ruhnke, and Joachim Morschhäuser. "Multiple Molecular Mechanisms Contribute to a Stepwise Development of Fluconazole Resistance in Clinical Candida albicans Strains." Antimicrobial Agents and Chemotherapy 42, no. 12 (1998): 3065–72. http://dx.doi.org/10.1128/aac.42.12.3065.

Full text
Abstract:
ABSTRACT From each of two AIDS patients with oropharyngeal candidiasis, fiveCandida albicans isolates from recurrent episodes of infection which became gradually resistant against fluconazole during antimycotic treatment were analyzed for molecular changes responsible for drug resistance. In both patients, a single C. albicans strain was responsible for the recurrent infections, but the CARE-2 fingerprint pattern of the isolates exhibited minor genetic alterations, indicating that microevolution of the strains took place during fluconazole therapy. In the isolates from patient 1, enhanced mRNA
APA, Harvard, Vancouver, ISO, and other styles
9

Warfield, Jasmine, William N. Setzer та Ifedayo Ogungbe. "Interactions of antiparasitic sterols with sterol 14α-demethylase (CYP51) of human pathogens". SpringerPlus 3, № 1 (2014): 679. http://dx.doi.org/10.1186/2193-1801-3-679.

Full text
APA, Harvard, Vancouver, ISO, and other styles
10

Sen, Kakali, та John C. Hackett. "Peroxo−Iron Mediated Deformylation in Sterol 14α-Demethylase Catalysis". Journal of the American Chemical Society 132, № 30 (2010): 10293–305. http://dx.doi.org/10.1021/ja906192b.

Full text
APA, Harvard, Vancouver, ISO, and other styles
11

Mellado, E., G. Garcia-Effron, M. J. Buitrago, L. Alcazar-Fuoli, M. Cuenca-Estrella та J. L. Rodriguez-Tudela. "Targeted Gene Disruption of the 14-α Sterol Demethylase (cyp51A) in Aspergillus fumigatus and Its Role in Azole Drug Susceptibility". Antimicrobial Agents and Chemotherapy 49, № 6 (2005): 2536–38. http://dx.doi.org/10.1128/aac.49.6.2536-2538.2005.

Full text
Abstract:
ABSTRACT The role of Aspergillus fumigatus 14α-sterol demethylase (Cyp51A) in azole drug susceptibility was assessed. Targeted disruption of cyp51A in azole-susceptible and -resistant strains decreased MICs from 2- to 40-fold. The cyp51A mutants were morphologically indistinguishable from the wild-type strain, retaining the ability to cause pulmonary disease in neutropenic mice.
APA, Harvard, Vancouver, ISO, and other styles
12

Leaver, David. "Synthesis and Biological Activity of Sterol 14α-Demethylase and Sterol C24-Methyltransferase Inhibitors". Molecules 23, № 7 (2018): 1753. http://dx.doi.org/10.3390/molecules23071753.

Full text
Abstract:
Sterol 14α-demethylase (SDM) is essential for sterol biosynthesis and is the primary molecular target for clinical and agricultural antifungals. SDM has been demonstrated to be a valid drug target for antiprotozoal therapies, and much research has been focused on using SDM inhibitors to treat neglected tropical diseases such as human African trypanosomiasis (HAT), Chagas disease, and leishmaniasis. Sterol C24-methyltransferase (24-SMT) introduces the C24-methyl group of ergosterol and is an enzyme found in pathogenic fungi and protozoa but is absent from animals. This difference in sterol meta
APA, Harvard, Vancouver, ISO, and other styles
13

BAE, Soo-Han, та Young-Ki PAIK. "Cholesterol biosynthesis from lanosterol: development of a novel assay method and characterization of rat liver microsomal lanosterol Δ24-reductase". Biochemical Journal 326, № 2 (1997): 609–16. http://dx.doi.org/10.1042/bj3260609.

Full text
Abstract:
The membrane-bound sterol Δ24-reductase (24-reductase) catalyses anaerobic reduction of the 24(25)-enes of lanosterol and other obligatory intermediates of cholesterol biosynthesis from lanosterol. A novel assay method and properties of the 24-reductase are described. More than a 120-fold induction of the 24-reductase activity was achieved by feeding rats a diet containing 5% cholestyramine plus 0.1% lovastatin in chow and by modulating diurnal variation. With this enzyme induction condition, lanosterol was converted efficiently into dihydrolanosterol in both intact hepatic microsomes and fres
APA, Harvard, Vancouver, ISO, and other styles
14

Lepesheva, Galina I., Laura Friggeri, and Michael R. Waterman. "CYP51 as drug targets for fungi and protozoan parasites: past, present and future." Parasitology 145, no. 14 (2018): 1820–36. http://dx.doi.org/10.1017/s0031182018000562.

Full text
Abstract:
AbstractThe efficiency of treatment of human infections with the unicellular eukaryotic pathogens such as fungi and protozoa remains deeply unsatisfactory. For example, the mortality rates from nosocomial fungemia in critically ill, immunosuppressed or post-cancer patients often exceed 50%. A set of six systemic clinical azoles [sterol 14α-demethylase (CYP51) inhibitors] represents the first-line antifungal treatment. All these drugs were discovered empirically, by monitoring their effects on fungal cell growth, though it had been proven that they kill fungal cells by blocking the biosynthesis
APA, Harvard, Vancouver, ISO, and other styles
15

Hargrove, Tatiana Y., Zdzislaw Wawrzak, Jialin Liu, Michael R. Waterman, W. David Nes та Galina I. Lepesheva. "Structural complex of sterol 14α-demethylase (CYP51) with 14α-methylenecyclopropyl-Δ7-24, 25-dihydrolanosterol". Journal of Lipid Research 53, № 2 (2011): 311–20. http://dx.doi.org/10.1194/jlr.m021865.

Full text
APA, Harvard, Vancouver, ISO, and other styles
16

Shumyantseva, V. V., T. V. Bulko, G. P. Kuznetsova та ін. "Electrochemical reduction of sterol-14α-demethylase from Mycobacterium tuberculosis (CYP51b1)". Biochemistry (Moscow) 72, № 6 (2007): 658–63. http://dx.doi.org/10.1134/s0006297907060090.

Full text
APA, Harvard, Vancouver, ISO, and other styles
17

Podust, Larissa M., Liudmila V. Yermalitskaya, Galina I. Lepesheva, Vladimir N. Podust, Enrique A. Dalmasso та Michael R. Waterman. "Estriol Bound and Ligand-free Structures of Sterol 14α-Demethylase". Structure 12, № 11 (2004): 1937–45. http://dx.doi.org/10.1016/j.str.2004.08.009.

Full text
APA, Harvard, Vancouver, ISO, and other styles
18

Waterman, Michael R., та Galina I. Lepesheva. "Sterol 14α-demethylase, an abundant and essential mixed-function oxidase". Biochemical and Biophysical Research Communications 338, № 1 (2005): 418–22. http://dx.doi.org/10.1016/j.bbrc.2005.08.118.

Full text
APA, Harvard, Vancouver, ISO, and other styles
19

Ghabbour, Hazem A., Maha M. Qabeel, Wagdy M. Eldehna, Abdullah Al-Dhfyan, and Hatem A. Abdel-Aziz. "Design, Synthesis, and Molecular Docking of 1-(1-(4-Chlorophenyl)-2-(phenylsulfonyl)ethylidene)-2-phenylhydrazine as Potent Nonazole Anticandidal Agent." Journal of Chemistry 2014 (2014): 1–8. http://dx.doi.org/10.1155/2014/154357.

Full text
Abstract:
1-(1-(4-Chlorophenyl)-2-(phenylsulfonyl)ethylidene)-2-phenylhydrazine (13) was designed and synthesized as potential nonazole anticandidal agent and precisely characterized by IR,1H NMR,13C NMR, and ESI-MS. The anti-Candidaactivity of13was evaluated against fourCandidaspecies (C. albicans, C. krusei, C. parapsilosis, andC. glabrata). Compound13displayed good anticandidal activities (MIC=0.39, 0.195, 0.39, and 1.56 μmol/mL, resp.) in comparison with that of the standard drug fluconazole (MIC=0.195, inactive, 1.56, and 1.56 μmol/mL, resp.) againstC. albicans, C. krusei, C. parapsilosis, andC. gl
APA, Harvard, Vancouver, ISO, and other styles
20

Fink, Martina, Jure Ačimovič, Tadeja Režen, Nataša Tanšek та Damjana Rozman. "Cholesterogenic Lanosterol 14α-Demethylase (CYP51) Is an Immediate Early Response Gene". Endocrinology 146, № 12 (2005): 5321–31. http://dx.doi.org/10.1210/en.2005-0781.

Full text
Abstract:
Lanosterol 14α-demethylase (CYP51) responds to cholesterol feedback regulation through sterol regulatory element binding proteins (SREBPs). The proximal promoter of CYP51 contains a conserved region with clustered regulatory elements: GC box, cAMP-response elements (CRE-like), and sterol regulatory element (SRE). In lipid-rich (SREBP-poor) conditions, the CYP51 mRNA drops gradually, the promoter activity is diminished, and no DNA-protein complex is observed at the CYP51-SRE1 site. The majority of cAMP-dependent transactivation is mediated through a single CRE (CYP51-CRE2). Exposure of JEG-3 ce
APA, Harvard, Vancouver, ISO, and other styles
21

Abdul-Hammed, Misbaudeen, Ibrahim Adedotun Olaide, Hadijat Motunrayo Adegoke, et al. "Antifungal Activities of Phytochemicals from Annona muricate (Sour Sop): Molecular Docking and Chemoinformatics Approach." Majalah Obat Tradisional 27, no. 3 (2022): 218. http://dx.doi.org/10.22146/mot.77380.

Full text
Abstract:
Fungal infection has become a persistent problem in humans and is sometimes life-threatening in immune-compromised individuals. This work aims to study phytochemicals from Annona muricata (sour sop) as probable antifungal agents against Candida albicans sterol 14α-demethylase target receptor by Computer Aided-Drug Design (CADD) approach using voriconazole and fluconazole as standard drugs. A modern method of drug discovery by molecular docking and chemoinformatics was used to screen 131 isolated phytochemicals with medicinal properties from Annona muricata against Candida albicans ‘sterol 14α-
APA, Harvard, Vancouver, ISO, and other styles
22

LAMB, David C., Kay FOWLER, Tobias KIESER та ін. "Sterol 14α-demethylase activity in Streptomyces coelicolor A3(2) is associated with an unusual member of the CYP51 gene family". Biochemical Journal 364, № 2 (2002): 555–62. http://dx.doi.org/10.1042/bj20011380.

Full text
Abstract:
The annotation of the genome sequence of Streptomyces coelicolor A3(2) revealed a cytochrome P450 (CYP) resembling various sterol 14α-demethylases (CYP51). The putative CYP open reading frame (SC7E4.20) was cloned with a tetrahistidine tag appended to the C-terminus and expressed in Escherichia coli. Protein purified to electrophoretic homogeneity was observed to bind the 14-methylated sterols lanosterol and 24-methylene-24,25-dihydrolanosterol (24-MDL). Reconstitution experiments with E. coli reductase partners confirmed activity in 14α-demethylation for 24-MDL, but not lanosterol. An S. coel
APA, Harvard, Vancouver, ISO, and other styles
23

NKININ, STEPHENSON W., JAMES R. STRINGER, SCOTT P. KEELY, KENNETH D. R. SETCHELL, JOSÉ-LUIS GINER та EDNA S. KANESHIRO. "Pneumocystis carinii Sterol 14α-Demethylase Activity in Saccharomyces cerevisiae erg11 Knockout Mutant: Sterol Biochemistry". Journal of Eukaryotic Microbiology 58, № 4 (2011): 383–92. http://dx.doi.org/10.1111/j.1550-7408.2011.00556.x.

Full text
APA, Harvard, Vancouver, ISO, and other styles
24

Tatsumi, Yoshiyuki, Maria Nagashima, Toshiyuki Shibanushi, et al. "Mechanism of Action of Efinaconazole, a Novel Triazole Antifungal Agent." Antimicrobial Agents and Chemotherapy 57, no. 5 (2013): 2405–9. http://dx.doi.org/10.1128/aac.02063-12.

Full text
Abstract:
ABSTRACTThe mechanism of action of efinaconazole, a new triazole antifungal, was investigated withTrichophyton mentagrophytesandCandida albicans. Efinaconazole dose-dependently decreased ergosterol production and accumulated 4,4-dimethylsterols and 4α-methylsterols at concentrations below its MICs. Efinaconazole induced morphological and ultrastructural changes inT. mentagrophyteshyphae that became more prominent with increasing drug concentrations. In conclusion, the primary mechanism of action of efinaconazole is blockage of ergosterol biosynthesis, presumably through sterol 14α-demethylase
APA, Harvard, Vancouver, ISO, and other styles
25

Price, Claire L., Andrew G. S. Warrilow, Josie E. Parker, et al. "Novel Substrate Specificity and Temperature-Sensitive Activity of Mycosphaerella graminicola CYP51 Supported by the Native NADPH Cytochrome P450 Reductase." Applied and Environmental Microbiology 81, no. 10 (2015): 3379–86. http://dx.doi.org/10.1128/aem.03965-14.

Full text
Abstract:
ABSTRACTMycosphaerella graminicola(Zymoseptoria tritici) is an ascomycete filamentous fungus that causes Septoria leaf blotch in wheat crops. In Europe the most widely used fungicides for this major disease are demethylation inhibitors (DMIs). Their target is the essential sterol 14α-demethylase (CYP51), which requires cytochrome P450 reductase (CPR) as its redox partner for functional activity. TheM. graminicolaCPR (MgCPR) is able to catalyze the sterol 14α-demethylation of eburicol and lanosterol when partnered withCandida albicansCYP51 (CaCYP51) and that of eburicol only withM. graminicolaC
APA, Harvard, Vancouver, ISO, and other styles
26

Emami, Saeed, Pegah Tavangar та Masoud Keighobadi. "An overview of azoles targeting sterol 14α-demethylase for antileishmanial therapy". European Journal of Medicinal Chemistry 135 (липень 2017): 241–59. http://dx.doi.org/10.1016/j.ejmech.2017.04.044.

Full text
APA, Harvard, Vancouver, ISO, and other styles
27

Yoshida, Yuzo, та Yuri Aoyama. "Sterol 14α-demethylase and its inhibition: structural considerations on interaction of azole antifungal agents with lanosterol 14α-demethylase (P-45014DM) of yeast". Biochemical Society Transactions 19, № 3 (1991): 778–82. http://dx.doi.org/10.1042/bst0190778.

Full text
APA, Harvard, Vancouver, ISO, and other styles
28

Doyle, Patricia S., Chiung-Kuang Chen, Jonathan B. Johnston, et al. "A Nonazole CYP51 Inhibitor Cures Chagas’ Disease in a Mouse Model of Acute Infection." Antimicrobial Agents and Chemotherapy 54, no. 6 (2010): 2480–88. http://dx.doi.org/10.1128/aac.00281-10.

Full text
Abstract:
ABSTRACT Chagas’ disease, the leading cause of heart failure in Latin America, is caused by the kinetoplastid protozoan Trypanosoma cruzi. The sterols of T. cruzi resemble those of fungi, both in composition and in biosynthesis. Azole inhibitors of sterol 14α-demethylase (CYP51) successfully treat fungal infections in humans, and efforts to adapt the success of antifungal azoles posaconazole and ravuconazole as second-use agents for Chagas’ disease are under way. However, to address concerns about the use of azoles for Chagas’ disease, including drug resistance and cost, the rational design of
APA, Harvard, Vancouver, ISO, and other styles
29

Lamb, David C., Diane E. Kelly та Steven L. Kelly. "Molecular diversity of sterol 14α-demethylase substrates in plants, fungi and humans". FEBS Letters 425, № 2 (1998): 263–65. http://dx.doi.org/10.1016/s0014-5793(98)00247-6.

Full text
APA, Harvard, Vancouver, ISO, and other styles
30

Jackson, Colin J., David C. Lamb, Timothy H. Marczylo та ін. "Conservation and cloning of CYP51: a sterol 14α-demethylase from Mycobacterium smegmatis". Biochemical and Biophysical Research Communications 301, № 2 (2003): 558–63. http://dx.doi.org/10.1016/s0006-291x(02)03078-4.

Full text
APA, Harvard, Vancouver, ISO, and other styles
31

Lepesheva, Galina I., та Michael R. Waterman. "Sterol 14α-demethylase cytochrome P450 (CYP51), a P450 in all biological kingdoms". Biochimica et Biophysica Acta (BBA) - General Subjects 1770, № 3 (2007): 467–77. http://dx.doi.org/10.1016/j.bbagen.2006.07.018.

Full text
APA, Harvard, Vancouver, ISO, and other styles
32

Wright, Gerard D., Todd Parent та John F. Honek. "Non-sterol structural probes of the lanosterol 14α-demethylase from Saccharomyces cerevisiae". Biochimica et Biophysica Acta (BBA) - Protein Structure and Molecular Enzymology 1040, № 1 (1990): 95–101. http://dx.doi.org/10.1016/0167-4838(90)90151-5.

Full text
APA, Harvard, Vancouver, ISO, and other styles
33

Mwenechanya, Roy, Julie Kovářová, Nicholas J. Dickens та ін. "Sterol 14α-demethylase mutation leads to amphotericin B resistance in Leishmania mexicana". PLOS Neglected Tropical Diseases 11, № 6 (2017): e0005649. http://dx.doi.org/10.1371/journal.pntd.0005649.

Full text
APA, Harvard, Vancouver, ISO, and other styles
34

Sayantan, Pradhan, та Sinha Chittaranjan. "Mycobacterium tuberculosis sterol 14α-demethylase inhibitor sulfonamides : Identified by high-throughput screening". Journal of Indian Chemical Society Vol. 94, May-2017 (2017): 457–68. https://doi.org/10.5281/zenodo.5625120.

Full text
Abstract:
Department of Chemistry, Inorganic Chemistry Section, Jadavpur University, Kolkata-700 032, India <em>E-mail </em>: c_r_sinha@yahoo.com Fax : 91-33-2414658 <em>Manuscript received 13 January 2017, accepted 07 February 2017</em> Tuberculosis is a deadly infectious disease caused by Mycobacterium tuberculosis. Sterol 14<strong>&alpha;</strong>-demethylase cytochrome P450 51(CYP51) is a key target for antibiotic therapy. Azoles are used to disturb functional activity of CYP51 and thus promising antifungal agents. Sulfonamides, anti-microbial drug, also act as antifungal candidate. In this work hi
APA, Harvard, Vancouver, ISO, and other styles
35

Parker, J. E., M. Merkamm, N. J. Manning, D. Pompon, S. L. Kelly та D. E. Kelly. "Differential Azole Antifungal Efficacies Contrasted Using a Saccharomyces cerevisiae Strain Humanized for Sterol 14α-Demethylase at the Homologous Locus". Antimicrobial Agents and Chemotherapy 52, № 10 (2008): 3597–603. http://dx.doi.org/10.1128/aac.00517-08.

Full text
Abstract:
ABSTRACT Inhibition of sterol-14α-demethylase, a cytochrome P450 (CYP51, Erg11p), is the mode of action of azole antifungal drugs, and with high frequencies of fungal infections new agents are required. New drugs that target fungal CYP51 should not inhibit human CYP51, although selective inhibitors of the human target are also of interest as anticholesterol agents. A strain of Saccharomyces cerevisiae that was humanized with respect to the amino acids encoded at the CYP51 (ERG11) yeast locus (BY4741:huCYP51) was produced. The strain was validated with respect to gene expression, protein locali
APA, Harvard, Vancouver, ISO, and other styles
36

Matsumoto, Masaru, Kazuya Ishida, Akihiro Konagai, Kazunori Maebashi, and Takemitsu Asaoka. "Strong Antifungal Activity of SS750, a New Triazole Derivative, Is Based on Its Selective Binding Affinity to Cytochrome P450 of Fungi." Antimicrobial Agents and Chemotherapy 46, no. 2 (2002): 308–14. http://dx.doi.org/10.1128/aac.46.2.308-314.2002.

Full text
Abstract:
ABSTRACT SS750 [(R)-(−)-2-(2,4-difluorophenyl)-1-(ethylsulfonyl)-1,1-difluoro-3-(1H-1,2,4-triazol-1-yl)-2-propanol] is a new triazole, and its potential as an antifungal agent was evaluated by in vitro and in vivo studies. In a comparison of the MICs at which 50% of isolates are inhibited (MIC50s) for all strains of Candida species and Cryptococcus neoformans tested, SS750 was four times or more active than fluconazole and had activity comparable to that of itraconazole. The most important advantage of SS750 was that, when the MIC90s were compared, SS750 had 64 and 32 times greater antifungal
APA, Harvard, Vancouver, ISO, and other styles
37

Essid, Rym, Sarra Kefi, Bilel Damergi, et al. "Promising Antileishmanial Activity of Micromeria nervosa Essential Oil: In Vitro and In Silico Studies." Molecules 29, no. 8 (2024): 1876. http://dx.doi.org/10.3390/molecules29081876.

Full text
Abstract:
The present study aimed to evaluate the leishmanicidal potential of the essential oil (EO) of Micromeria (M.) nervosa and to investigate its molecular mechanism of action by qPCR. Furthermore, in silicointeraction study of the major M. nervosa EO compounds with the enzyme cytochrome P450 sterol 14α-demethylase (CYP51) was also performed. M. nervosa EO was analyzed by gas chromatography-mass spectrometry (GC-MS). Results showed that α-pinene (26.44%), t-cadinol (26.27%), caryophyllene Oxide (7.73 ± 1.04%), and α-Cadinene (3.79 ± 0.12%) are the major compounds of M. nervosa EO. However, limited
APA, Harvard, Vancouver, ISO, and other styles
38

Martel, Claire M., Josie E. Parker, Andrew G. S. Warrilow, Nicola J. Rolley, Steven L. Kelly та Diane E. Kelly. "Complementation of a Saccharomyces cerevisiae ERG11/CYP51 (Sterol 14α-Demethylase) Doxycycline-Regulated Mutant and Screening of the Azole Sensitivity of Aspergillus fumigatus Isoenzymes CYP51A and CYP51B". Antimicrobial Agents and Chemotherapy 54, № 11 (2010): 4920–23. http://dx.doi.org/10.1128/aac.00349-10.

Full text
Abstract:
ABSTRACT Aspergillus fumigatus sterol 14α-demethylase isoenzymes CYP51A and CYP51B were heterologously expressed in a Saccharomyces cerevisiae mutant (YUG37-erg11), wherein native ERG11/CYP51 expression is controlled using a doxycycline-regulatable promoter. When cultured in the presence of doxycycline, recombinant YUG37-pcyp51A and YUG37-pcyp51B yeasts were able to synthesize ergosterol and grow; a control strain harboring reverse-oriented cyp51A could not. YUG37-pcyp51A and YUG37-pcyp51B constructs showed identical sensitivity to itraconazole, posaconazole, clotrimazole, and voriconazole. Co
APA, Harvard, Vancouver, ISO, and other styles
39

Lepesheva, Galina I., Tatiana Y. Hargrove, Spencer Anderson та ін. "Structural Insights into Inhibition of Sterol 14α-Demethylase in the Human PathogenTrypanosoma cruzi". Journal of Biological Chemistry 285, № 33 (2010): 25582–90. http://dx.doi.org/10.1074/jbc.m110.133215.

Full text
APA, Harvard, Vancouver, ISO, and other styles
40

Lamb, David C., Diane E. Kelly, K. Venkateswarlu та ін. "Generation of a Complete, Soluble, and Catalytically Active Sterol 14α-Demethylase−Reductase Complex†". Biochemistry 38, № 27 (1999): 8733–38. http://dx.doi.org/10.1021/bi9825089.

Full text
APA, Harvard, Vancouver, ISO, and other styles
41

Lamb, D. "Expression, purification, reconstitution and inhibition of Ustilago maydis sterol 14α-demethylase (CYP51; P45014DM)". FEMS Microbiology Letters 169, № 2 (1998): 369–73. http://dx.doi.org/10.1016/s0378-1097(98)00505-9.

Full text
APA, Harvard, Vancouver, ISO, and other styles
42

Suryadevara, Praveen Kumar, Kishore Kumar Racherla, Srinivas Olepu та ін. "Dialkylimidazole inhibitors of Trypanosoma cruzi sterol 14α-demethylase as anti-Chagas disease agents". Bioorganic & Medicinal Chemistry Letters 23, № 23 (2013): 6492–99. http://dx.doi.org/10.1016/j.bmcl.2013.08.015.

Full text
APA, Harvard, Vancouver, ISO, and other styles
43

Park, Hyoung-Goo, Im-Soon Lee, Young-Jin Chun та ін. "Heterologous expression and characterization of the sterol 14α-demethylase CYP51F1 from Candida albicans". Archives of Biochemistry and Biophysics 509, № 1 (2011): 9–15. http://dx.doi.org/10.1016/j.abb.2011.02.002.

Full text
APA, Harvard, Vancouver, ISO, and other styles
44

Qian, Hengwei, Meilin Duan, Xiaomei Sun та ін. "The binding mechanism between azoles and FgCYP51B, sterol 14α-demethylase of Fusarium graminearum". Pest Management Science 74, № 1 (2017): 126–34. http://dx.doi.org/10.1002/ps.4667.

Full text
APA, Harvard, Vancouver, ISO, and other styles
45

Calonne, Maryline, Anissa Lounès-Hadj Sahraoui, Estelle Campagnac та ін. "Propiconazole inhibits the sterol 14α-demethylase in Glomus irregulare like in phytopathogenic fungi". Chemosphere 87, № 4 (2012): 376–83. http://dx.doi.org/10.1016/j.chemosphere.2011.12.027.

Full text
APA, Harvard, Vancouver, ISO, and other styles
46

Lamb, David C., Segula Maspahy, Diane E. Kelly та ін. "Purification, Reconstitution, and Inhibition of Cytochrome P-450 Sterol Δ22-Desaturase from the Pathogenic Fungus Candida glabrata". Antimicrobial Agents and Chemotherapy 43, № 7 (1999): 1725–28. http://dx.doi.org/10.1128/aac.43.7.1725.

Full text
Abstract:
ABSTRACT Sterol Δ22-desaturase has been purified from a strain of Candida glabrata with a disruption in the gene encoding sterol 14α-demethylase (cytochrome P-45051; CYP51). The purified cytochrome P-450 exhibited sterol Δ22-desaturase activity in a reconstituted system with NADPH–cytochrome P-450 reductase in dilaurylphosphatidylcholine, with the enzyme kinetic studies revealing a Km for ergosta-5,7-dienol of 12.5 μM and aV max of 0.59 nmol of this substrate metabolized/min/nmol of P-450. This enzyme is encoded by CYP61 (ERG5) in Saccharomyces cerevisiae, and homologues have been shown in the
APA, Harvard, Vancouver, ISO, and other styles
47

Eddouzi, Jamel, Josie E. Parker, Luis A. Vale-Silva, et al. "Molecular Mechanisms of Drug Resistance in Clinical Candida Species Isolated from Tunisian Hospitals." Antimicrobial Agents and Chemotherapy 57, no. 7 (2013): 3182–93. http://dx.doi.org/10.1128/aac.00555-13.

Full text
Abstract:
ABSTRACTAntifungal resistance ofCandidaspecies is a clinical problem in the management of diseases caused by these pathogens. In this study we identified from a collection of 423 clinical samples taken from Tunisian hospitals two clinicalCandidaspecies (Candida albicansJEY355 andCandida tropicalisJEY162) with decreased susceptibility to azoles and polyenes. For JEY355, the fluconazole (FLC) MIC was 8 μg/ml. Azole resistance inC. albicansJEY355 was mainly caused by overexpression of a multidrug efflux pump of the major facilitator superfamily, Mdr1. The regulator of Mdr1,MRR1, contained a yet-u
APA, Harvard, Vancouver, ISO, and other styles
48

Scott, Nicola A., Laura J. Sharpe, Isabelle M. Capell-Hattam, Samuel J. Gullo, Winnie Luu та Andrew J. Brown. "The cholesterol synthesis enzyme lanosterol 14α-demethylase is post-translationally regulated by the E3 ubiquitin ligase MARCH6". Biochemical Journal 477, № 2 (2020): 541–55. http://dx.doi.org/10.1042/bcj20190647.

Full text
Abstract:
Cholesterol synthesis is a tightly controlled pathway, with over 20 enzymes involved. Each of these enzymes can be distinctly regulated, helping to fine-tune the production of cholesterol and its functional intermediates. Several enzymes are degraded in response to increased sterol levels, whilst others remain stable. We hypothesised that an enzyme at a key branch point in the pathway, lanosterol 14α-demethylase (LDM) may be post-translationally regulated. Here, we show that the preceding enzyme, lanosterol synthase is stable, whilst LDM is rapidly degraded. Surprisingly, this degradation is n
APA, Harvard, Vancouver, ISO, and other styles
49

Kelly, S. L., D. C. Lamb, M. Cannieux, et al. "An old activity in the cytochrome P450 superfamily (CYP51) and a new story of drugs and resistance." Biochemical Society Transactions 29, no. 2 (2001): 122–28. http://dx.doi.org/10.1042/bst0290122.

Full text
Abstract:
Cytochrome P450 51 (CYP51) is sterol 14α-demethylase, known also as Ergllp in yeast. First studied in yeast, where it is one of three CYPs in the genome, it has subsequently gained attention as the only CYP found so far in different kingdoms of life. As such it is central to considerations of CYP evolution. Recent use of CYP51-inhibiting antifungal drugs, such as fluconazole, has also been associated with dramatic CYP51 evolution to numerous resistant forms in fungal pathogens. CYP51 has also been discovered in mycobacteria where antifungal azoles have effect and might be of value against tube
APA, Harvard, Vancouver, ISO, and other styles
50

Nakayama, Hironobu, Noboru Nakayama, Mikio Arisawa та Yuko Aoki. "In Vitro and In Vivo Effects of 14α-Demethylase (ERG11) Depletion in Candida glabrata". Antimicrobial Agents and Chemotherapy 45, № 11 (2001): 3037–45. http://dx.doi.org/10.1128/aac.45.11.3037-3045.2001.

Full text
Abstract:
ABSTRACT Sterol 14α-demethylase (ERG11) is the target enzyme of azole antifungals that are widely used for the treatment of fungal infections. Candida glabrata is known to be less susceptible to fluconazole than most Candida albicansstrains, and the incidence of C. glabrata infection has been increasing mostly in conjunction with the use of azole antifungals. Recently, it has been reported that C. glabrata can rescue the defect of ergosterol biosynthesis by incorporating cholesterol from serum. To explore the effect of inactivating Erg11p in C. glabrata, we generated mutant strains in which th
APA, Harvard, Vancouver, ISO, and other styles
We offer discounts on all premium plans for authors whose works are included in thematic literature selections. Contact us to get a unique promo code!

To the bibliography