keyword
MENU ▼
Read by QxMD icon Read
search

Lanosterol

keyword
https://www.readbyqxmd.com/read/29162893/intrinsic-short-tailed-azole-resistance-in-mucormycetes-is-due-to-an-evolutionary-conserved-aminoacid-substitution-of-the-lanosterol-14%C3%AE-demethylase
#1
Rita Caramalho, Joel D A Tyndall, Brian C Monk, Thomas Larentis, Cornelia Lass-Flörl, Michaela Lackner
Mucormycoses are emerging and potentially lethal infections. An increase of breakthrough infections has been found in cohorts receiving short-tailed azoles prophylaxis (e.g. voriconazole (VCZ)). Although VCZ is ineffective in vitro and in vivo, long-tailed triazoles such as posaconazole remain active against mucormycetes. Our goal was to validate the molecular mechanism of resistance to short-tailed triazoles in Mucorales. The paralogous cytochrome P450 genes (CYP51 F1 and CYP51 F5) of Rhizopus arrhizus, Rhizopus microsporus, and Mucor circinelloides were amplified and sequenced...
November 21, 2017: Scientific Reports
https://www.readbyqxmd.com/read/29158527/azole-sensitivity-in-leptosphaeria-pathogens-of-oilseed-rape-the-role-of-lanosterol-14%C3%AE-demethylase
#2
Thomas R Sewell, Nichola J Hawkins, Henrik U Stotz, YongJu Huang, Steven L Kelly, Diane E Kelly, Bart Fraaije, Bruce D L Fitt
Lanosterol 14-α demethylase is a key enzyme intermediating the biosynthesis of ergosterol in fungi, and the target of azole fungicides. Studies have suggested that Leptosphaeria maculans and L. biglobosa, the causal agents of phoma stem canker on oilseed rape, differ in their sensitivity to some azoles, which could be driving pathogen frequency change in crops. Here we used CYP51 protein modelling and heterologous expression to determine whether there are interspecific differences at the target-site level...
November 20, 2017: Scientific Reports
https://www.readbyqxmd.com/read/29156575/synthesis-of-oxadiazole-thiadiazole-hybrids-and-their-anticandidal-activity
#3
Serkan Levent, Betül Kaya Çavuşoğlu, Begüm Nurpelin Sağlık, Derya Osmaniye, Ulviye Acar Çevik, Özlem Atlı, Yusuf Özkay, Zafer Asım Kaplancıklı
In the field of infection management, it is a major challenge to discover a potent and safe antifungal agent due to the emergence of resistant strains. Hence, the goal of this paper is to design and synthesize novel oxadiazole-thiadiazole hybrid compounds (6a-6s) and evaluate their antifungal activity. The structures of synthesized compounds were elucidated by various methods including FT-IR, ¹H-NMR, (13)C-NMR and HR-MS spectral data. Compounds were tested against four Candida species by broth microdilution assay...
November 18, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29142437/docking-based-screening-of-ficus-religiosa-phytochemicals-as-inhibitors-of-human-histamine-h2-receptor
#4
Amit Chaudhary, Birendra Singh Yadav, Swati Singh, Pramod Kumar Maurya, Alok Mishra, Shweta Srivastva, Pritish Kumar Varadwaj, Nand Kumar Singh, Ashutosh Mani
Background: Ficus religiosa L. is generally known as Peepal and belongs to family Moraceae. The tree is a source of many compounds having high medicinal value. In gastrointestinal tract, histamine H2 receptors have key role in histamine-stimulated gastric acid secretion. Their over stimulation causes its excessive production which is responsible for gastric ulcer. Objective: This study aims to screen the range of phytochemicals present in F. religiosa for binding with human histamine H2 and identify therapeutics for a gastric ulcer from the plant...
October 2017: Pharmacognosy Magazine
https://www.readbyqxmd.com/read/29115523/characterization-of-cholesterol-metabolism-in-sertoli-cells-and-spermatogenesis-review
#5
Jin-Feng Shi, Yu-Kun Li, Kun Ren, Yuan-Jie Xie, Wei-Dong Yin, Zhong-Cheng Mo
The Sertoli cell, which is the supporting cell of spermatogenesis, has an important role in the endocrine and paracrine control of spermatogenesis. Functionally, it provides the cells of the seminiferous epithelium with nutrition, conveys mature spermatids to the lumen of seminiferous tubules, secretes androgen‑binding protein and interacts with endocrine Leydig cells. In addition, the levels of cholesterol, as well as its intermediates, vary greatly between nongonadal tissues and the male reproductive system...
November 7, 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/29112162/syntheses-of-novel-4-substituted-n-5-amino-1h-1-2-4-triazol-3-yl-pyridine-3-sulfonamide-derivatives-with-potential-antifungal-activity
#6
Krzysztof Szafrański, Jarosław Sławiński, Anna Kędzia, Ewa Kwapisz
Candidiasis represent a serious threat for patients with altered immune responses. Therefore, we have undertaken the synthesis of compounds comprising a pyridine-3-sulfonamide scaffold and known antifungally active 1,2,4-triazole substituents. Thus a series of novel 4-substituted N-(5-amino-1H-1,2,4-triazol-3-yl)pyridine-3-sulfonamides have been synthesized by multistep reactions starting from 4-chloropyridine-3-sulfonamide via N'-cyano-N-[(4-substitutedpyridin-3-yl)sulfonyl]carbamimidothioates which were further converted with hydrazine hydrate to the corresponding 1,2,4-triazole derivatives 26-36...
November 7, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29108727/reproducibility-of-serum-oxysterols-and-lanosterol-among-postmenopausal-women-results-from-epic-heidelberg
#7
Da-Lin Lu, Disorn Sookthai, Charlotte Le Cornet, Verena A Katzke, Theron S Johnson, Rudolf Kaaks, Renée T Fortner
BACKGROUND: Circulating oxysterols have been proposed as biological markers of disease risk. However, within-person reproducibility of circulating oxysterols over time is not well established. METHODS: We evaluated the one-year reproducibility of 11 oxysterols and lanosterol among 30 postmenopausal women with repeat blood samples in the European Prospective Investigation into Cancer and Nutrition (EPIC) - Heidelberg, Germany cohort. Liquid chromatography-mass spectrometry (LC/MS) was performed to quantify serum concentrations of 22R-hydroxycholesterol, 2β-hydroxycholesterol, 24S-hydroxycholesterol, 27-hydroxycholesterol, 22S-hydroxycholeterol, 24,2β-epoxycholesterol, 5α,6β-dihydroxycholestanol, 7α-hydroxycholesterol, 5β,6β-epoxycholesterol, 5α,6α-epoxycholesterol, 24-dihydrolanosterol, and lanosterol...
November 3, 2017: Clinical Biochemistry
https://www.readbyqxmd.com/read/29096293/effects-of-the-bioconcentration-and-parental-transfer-of-environmentally-relevant-concentrations-of-difenoconazole-on-endocrine-disruption-in-zebrafish-danio-rerio
#8
Miaomiao Teng, Suzhen Qi, Wentao Zhu, Yao Wang, Dezhen Wang, Kai Dong, Chengju Wang
Difenoconazole, a typical triazole fungicide, inhibits lanosterol-14R-demethylase (CYP51) to prevent fungal sterol synthesis and its residues are frequently detected in the environment due to its wide application. Previous studies have demonstrated that difenoconazole altered the triglyceride levels, and gene expression relevant to cholesterol biosynthesis in zebrafish. However, endocrine-disruption in the hypothalamus-pituitary-gonadal-liver (HPGL) axis, the effects of transferring to offspring, and the underlying mechanisms of difenoconazole in aquatic organisms are still unknown...
October 26, 2017: Environmental Pollution
https://www.readbyqxmd.com/read/29038279/a-ctg-clade-candida-yeast-genetically-engineered-for-the-genotype-phenotype-characterization-of-azole-antifungal-resistance-in-human-pathogenic-yeasts
#9
Isabelle Accoceberry, Amandine Rougeron, Nicolas Biteau, Pauline Chevrel, Valérie Fitton-Ouhabi, Thierry Noël
A strain of the opportunistic pathogenic yeast Candida lusitaniae was genetically modified for its use as a cellular model for assessing by allele replacement the impact of lanosterol C14α-demethylase ERG11 mutations on azole resistance. Candida lusitaniae was chosen because it is susceptible to azole antifungals, it belongs to the CTG clade of yeast which includes most of the Candida species pathogenic for humans, and it is haploid and easily amenable to genetic transformation and molecular modeling. In this work, allelic replacement is targeted at the ERG11 locus by the reconstitution of a functional auxotrophic marker in the 3' intergenic region of ERG11 Homologous and heterologous ERG11 alleles are expressed from the resident ERG11 promoter of C...
October 16, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/29036583/characterization-of-moss-ent-kaurene-oxidase-cyp701b1-using-a-highly-purified-preparation
#10
Chisato Noguchi, Sho Miyazaki, Hiroshi Kawaide, Osamu Gotoh, Yuzo Yoshida, Yuri Aoyama
CYP701B1 of the moss, Physcomitrella patents, might be a unique cytochrome P450 having the ent-kaurene oxidase (KO) activity occurring in nonvascular plant. Phylogenetic analysis suggested that the gene encoding CYP701B1 was diverged from a common ancestral gene encoding KO of vascular plants. CYP701B1 expressed in Phichia yeast microsomes was purified and characterized. The purified CYP701B1 catalyzed the oxidation of ent-kaurene to ent-kaurenoic acid through three successive monooxygenations, and the rate-limiting step of this oxidation might be the initial step that forms ent-kaurenol...
September 27, 2017: Journal of Biochemistry
https://www.readbyqxmd.com/read/29016354/congenital-cataract-with-lss-gene-mutations-a-new-case-report
#11
Xiaodan Chen, Li Liu
BACKGROUND: Congenital cataract is one of the major causes of blindness and amblyopia in children. About one-third of the cases are inherited. CASE PRESENTATION: We applied whole exome sequencing for a pediatric patient with congenital cataract, small penis, baldness and absence of eyebrows and detected a compound heterozygous mutation in the lanosterol synthase (LSS) gene. These two mutations were inherited from the patient's parents. Both mutations altered the amino acid coding, at highly conserved amino acid residues...
October 26, 2017: Journal of Pediatric Endocrinology & Metabolism: JPEM
https://www.readbyqxmd.com/read/28992260/simulations-of-cyp51a-from-aspergillus-fumigatus-in-a-model-bilayer-provide-insights-into-triazole-drug-resistance
#12
Anthony Nash, Johanna Rhodes
Azole antifungal drugs target CYP51A in Aspergillus fumigatus by binding with the active site of the protein, blocking ergosterol biosynthesis. Resistance to azole antifungal drugs is now common, with a leucine to histidine amino acid substitution at position 98 the most frequent, predominantly conferring resistance to itraconazole, although cross-resistance has been reported in conjunction with other mutations. In this study, we create a homology model of CYP51A using a recently published crystal structure of the paralog protein CYP51B...
September 9, 2017: Medical Mycology: Official Publication of the International Society for Human and Animal Mycology
https://www.readbyqxmd.com/read/28989971/target-abundance-based-fitness-screening-tafis-facilitates-rapid-identification-of-target-specific-and-physiologically-active-chemical-probes
#13
Arielle Butts, Christian DeJarnette, Tracy L Peters, Josie E Parker, Morgan E Kerns, Karen E Eberle, Steve L Kelly, Glen E Palmer
Traditional approaches to drug discovery are frustratingly inefficient and have several key limitations that severely constrain our capacity to rapidly identify and develop novel experimental therapeutics. To address this, we have devised a second-generation target-based whole-cell screening assay based on the principles of competitive fitness, which can rapidly identify target-specific and physiologically active compounds. Briefly, strains expressing high, intermediate, and low levels of a preselected target protein are constructed, tagged with spectrally distinct fluorescent proteins (FPs), and pooled...
September 2017: MSphere
https://www.readbyqxmd.com/read/28989252/operculina-turpethum-linn-silva-manso-as-a-medicinal-plant-species-a-review-on-bioactive-components-and-pharmacological-properties
#14
REVIEW
Shweta Gupta, Akash Ved
Operculina turpethum (Linn.) (OT) Silva Manso belongs to the family Convolvulaceae. This review incorporates literature for the phytochemical and pharmacological profile of OT herb. Exhaustive literature survey was done using all the details on phytochemistry and pharmacology of OT available. This herb was found to be a potent source of bioactive compounds such as α- and β-turpethein, turpethinic acids (A, B, C, D, and E), coumarins, cycloartenol, lanosta-5-ene, 24-methylene-δ-5-lanosterol, α- and β-rhamnose, β-sitosterol, lupeol, scopoletin, betulin, acrylamide, stigma-5,22dien-3-O-β-D-glucopyranoside, β-sitosterol-β-D-glucoside (H-1), 22,23-dihydro-α-spinosterol-β-D-glucoside (H-2), and salicylic acid (CH-2), which are useful in fevers, edema, ascites, anorexia, constipation, hepatosplenomegaly, hemorrhoids, cervical lymphadenitis, fistulas, constipation, chronic gout, fever, bronchitis, ulcers, hemorrhoids, tumors, obesity, jaundice, herpes, induce lacrimation, and other skin disorders...
July 2017: Pharmacognosy Reviews
https://www.readbyqxmd.com/read/28972118/vulnerability-of-dhcr7-mutation-carriers-to-aripiprazole-and-trazodone-exposure
#15
Zeljka Korade, Thiago C Genaro-Mattos, Keri A Tallman, Wei Liu, Krassimira A Garbett, Katalin Koczok, Istvan Balogh, Karoly Mirnics, Ned A Porter
Smith-Lemli-Opitz syndrome is a recessive disorder caused by mutations in 7-dehydrocholesterol reductase (DHCR)7 with a heterozygous (HET) carrier frequency of 1-3%. A defective DHCR7 causes accumulation of 7-dehydrocholesterol (DHC), which is a highly oxidizable and toxic compound. Recent studies suggest that several antipsychotics, including the highly prescribed pharmaceuticals, aripiprazole (ARI) and trazodone (TRZ), increase 7-DHC levels in vitro and in humans. Our investigation was designed to compare the effects of ARI and TRZ on cholesterol (Chol) synthesis in fibroblasts from DHCR7(+/-) human carriers and controls (CTRs)...
November 2017: Journal of Lipid Research
https://www.readbyqxmd.com/read/28938463/role-of-cyp51-in-the-regulation-of-t3-and-fsh-induced-steroidogenesis-in-female-mice
#16
Juan Liu, Ye Tian, Yu Ding, Dai Heng, Kaili Xu, Wenbo Liu, Cheng Zhang
Cytochrome P450 lanosterol 14α-demethylase (CYP51) is a key enzyme in sterol and steroid biosynthesis that is involved in folliculogenesis and oocyte maturation, which is regulated by follicle-stimulating hormone (FSH), as a key reproductive hormone during follicular development. Thyroid hormone (TH) is also important for normal reproductive function. Although 3,5,3'-triiodothyronine (T3) enhances FSH-induced preantral follicle growth, whether and how TH combines with FSH to regulate CYP51 expression during the preantral to early antral transition stage is unclear...
November 1, 2017: Endocrinology
https://www.readbyqxmd.com/read/28935182/eudesmane-sesquiterpenes-from-chinese-liverwort-are-substrates-of-cdrs-and-display-antifungal-activity-by-targeting-erg6-and-erg11-of-candida-albicans
#17
Siwen Li, Hongzhuo Shi, Wenqiang Chang, Yi Li, Ming Zhang, Yanan Qiao, Hongxiang Lou
We isolated twelve sesquiterpenes from Chinese liverwort Tritomaria quinquedentata (Huds.) Buch., including four new compounds. Among them, five eudesmane sesquiterpenes were ineffective against Candida albicans wild strain SC5314 but active towards efflux pumps-deficient strain DSY654 using Alamar blue assay. Further test of the most active agent of ent-isoalantolactone (8, ent-iLL) showed that it also inhibited the yeast-to-hyphal switch of DSY654 cells. The intracellular content measurement using high performance liquid chromatography (HPLC) revealed that ent-iLL was intracellularly accumulated in C...
September 9, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28927230/multi-azole-resistant-strains-of-cryptococcus-neoformans-var-grubii-isolated-from-a-flz-resistant-strain-by-culturing-in-medium-containing-voriconazole
#18
Rui Kano, Miki Okubo, Atsuhiko Hasegawa, Hiroshi Kamata
A Cryptococcus neoformans var. grubii strain, NUBS14020, was the first fluconazole (FLZ)-resistant strain isolated from a feline cryptococcosis. Subsequent work demonstrated that multi-azole-resistant strains are readily isolated from FLZ-resistant strains by culturing in medium containing voriconazole (VRZ). The resulting clones were assessed for mutation and expression of known target genes, including the loci encoding lanosterol 14-α demethylase (ERG11), an ATP-binding cassette (ABC) transporter (AFR1), or a multidrug efflux pump (MEP); mutation and/or overexpression of these genes is known to be associated with azole resistance...
November 1, 2017: Medical Mycology: Official Publication of the International Society for Human and Animal Mycology
https://www.readbyqxmd.com/read/28926063/methylglyoxal-attenuates-insulin-signaling-and-downregulates-the-enzymes-involved-in-cholesterol-biosynthesis
#19
Arati B Deshmukh, Shakuntala Bai, Aarthy T, Rubina S Kazi, Reema Banarjee, Rajeshwari Rathore, Vijayakumar Mv, Thulasiram Hv, Manoj Kumar Bhat, Kulkarni Mj
Methylglyoxal (MG) is a highly reactive dicarbonyl known to be elevated under the hyperglycemic conditions of diabetes and is implicated in the development of diabetic complications. Therefore, the current study investigates the role of MG in exacerbating insulin resistance at the insulin signaling level, as well as its effect on the global proteomic level. By using insulin sensitive rat muscle cells (L6) and Chinese hamster ovary (CHO) cells stably expressing the insulin receptor (IR) and a glucose transporter fused with green fluorescent protein (GLUT4-GFP), we have observed that MG impairs insulin signaling, inhibits GLUT4 translocation and reduces glucose uptake...
October 24, 2017: Molecular BioSystems
https://www.readbyqxmd.com/read/28888677/quantitation-of-lanosterol-in-the-vitreous-humor-of-rabbits-after-ocular-administration-of-lanosterol-thermogel-formulation-by-ultra-high-performance-liquid-chromatography-tandem-mass-spectrometry-with-the-electrospray-ionization-mode
#20
Lei Lv, Dan Li, Hui Wang, Chengjian Li, Xian Qian, Heng-Tao Dong, Jianguo Sun, Liang Zhao
Cataracts are the most common cause of blindness worldwide affecting tens of millions of people. Here, we report a simple, rapid, sensitive and specific method by ultra performance liquid chromatography-tandem mass spectrometry with the electrospray ionization mode (UPLC-ESI-MS/MS) for quantitation of lanosterol, a possible effective drug for cataracts, in the vitreous humor of rabbits after ocular administration. The injected lanosterol was prepared by dispersing lanosterol molecules into the poly-(dl-lactic acid-co-glycolic acid)-poly(ethylene glycol)-poly-(dl-lactic acid-co-glycolic acid) (PLGA-PEG-PLGA) thermogel solution...
October 13, 2017: Journal of Chromatography. A
keyword
keyword
105397
1
2
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"