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https://www.readbyqxmd.com/read/27907120/structural-and-functional-elucidation-of-yeast-lanosterol-14%C3%AE-demethylase-in-complex-with-agrochemical-antifungals
#1
Joel D A Tyndall, Manya Sabherwal, Alia A Sagatova, Mikhail V Keniya, Jacopo Negroni, Rajni K Wilson, Matthew A Woods, Klaus Tietjen, Brian C Monk
Azole antifungals, known as demethylase inhibitors (DMIs), target sterol 14α-demethylase (CYP51) in the ergosterol biosynthetic pathway of fungal pathogens of both plants and humans. DMIs remain the treatment of choice in crop protection against a wide range of fungal phytopathogens that have the potential to reduce crop yields and threaten food security. We used a yeast membrane protein expression system to overexpress recombinant hexahistidine-tagged S. cerevisiae lanosterol 14α-demethylase and the Y140F or Y140H mutants of this enzyme as surrogates in order characterize interactions with DMIs...
2016: PloS One
https://www.readbyqxmd.com/read/27905068/inhibition-of-mevalonate-pathway-and-synthesis-of-the-storage-lipids-in-human-liver-derived-and-non-liver-cell-lines-by-lippia-alba-essential-oils
#2
Sandra Montero-Villegas, Mónica Polo, Marianela Galle, Boris Rodenak-Kladniew, María Castro, Ana Ves-Losada, Rosana Crespo, Margarita García de Bravo
The essential oils (EOs) of Lippia alba, an herb extensively used as a folk medicine in Latin America, are today promoted as an effective means of eliminating problems caused by hyperlipemia. We hypothesized that L.alba EOs inhibited cholesterol and triacylglycerols synthesis and decreased the intracellular depots of those lipids (lipid droplets), mechanisms involving the induction of a hypolipidemic response. Our aim was, therefore, to evaluate the hypolipogenic capability of the EOs of four L. alba chemotypes on liver-derived (HepG2) and non-liver (A549) human cell lines and to identify the potential biochemical targets of those chemotypes, particularly within the mevalonate pathway (MP)...
November 30, 2016: Lipids
https://www.readbyqxmd.com/read/27894599/overexpression-of-the-homologous-lanosterol-synthase-gene-in-ganoderic-acid-biosynthesis-in-ganoderma-lingzhi
#3
De-Huai Zhang, Na Li, Xuya Yu, Peng Zhao, Tao Li, Jun-Wei Xu
Ganoderic acids (GAs) in Ganoderma lingzhi exhibit anticancer and antimetastatic activities. GA yields can be potentially improved by manipulating G. lingzhi through genetic engineering. In this study, a putative lanosterol synthase (LS) gene was cloned and overexpressed in G. lingzhi. Results showed that its overexpression (OE) increased the ganoderic acid (GA) content and the accumulation of lanosterol and ergosterol in a submerged G. lingzhi culture. The maximum contents of GA-O, GA-Mk, GA-T, GA-S, GA-Mf, and GA-Me in transgenic strains were 46...
November 25, 2016: Phytochemistry
https://www.readbyqxmd.com/read/27881978/the-oxidosqualene-cyclase-from-the-oomycete-saprolegnia-parasitica-synthesizes-lanosterol-as-a-single-product
#4
Paul Dahlin, Vaibhav Srivastava, Vincent Bulone, Lauren S McKee
The first committed step of sterol biosynthesis is the cyclisation of 2,3-oxidosqualene to form either lanosterol (LA) or cycloartenol (CA). This is catalyzed by an oxidosqualene cyclase (OSC). LA and CA are subsequently converted into various sterols by a series of enzyme reactions. The specificity of the OSC therefore determines the final composition of the end sterols of an organism. Despite the functional importance of OSCs, the determinants of their specificity are not well understood. In sterol-synthesizing oomycetes, recent bioinformatics, and metabolite analysis suggest that LA is produced...
2016: Frontiers in Microbiology
https://www.readbyqxmd.com/read/27879678/new-thiazolyl-triazole-schiff-bases-synthesis-and-evaluation-of-the-anti-candida-potential
#5
Anca Stana, Alexandra Enache, Dan Cristian Vodnar, Cristina Nastasă, Daniela Benedec, Ioana Ionuț, Cezar Login, Gabriel Marc, Ovidiu Oniga, Brîndușa Tiperciuc
In the context of the dangerous phenomenon of fungal resistance to the available therapies, we present here the chemical synthesis of a new series of thiazolyl-triazole Schiff bases B1-B15, which were in vitro assessed for their anti-Candida potential. Compound B10 was found to be more potent against Candida spp. when compared with the reference drugs Fluconazole and Ketoconazole. A docking study of the newly synthesized Schiff bases was performed, and results showed good binding affinity in the active site of co-crystallized Itraconazole-lanosterol 14α-demethylase isolated from Saccharomyces cerevisiae...
November 22, 2016: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/27832119/cloning-and-functional-characterization-of-cycloartenol-synthase-from-the-red-seaweed-laurencia-dendroidea
#6
Gabriela Calegario, Jacob Pollier, Philipp Arendt, Louisi Souza de Oliveira, Cristiane Thompson, Angélica Ribeiro Soares, Renato Crespo Pereira, Alain Goossens, Fabiano L Thompson
The red seaweed Laurencia dendroidea belongs to the Rhodophyta, a phylum of eukaryotic algae that is widely distributed across the oceans and that constitute an important source of bioactive specialized metabolites. Laurencia species have been studied since 1950 and were found to contain a plethora of specialized metabolites, mainly halogenated sesquiterpenes, diterpenes and triterpenes that possess a broad spectrum of pharmacological and ecological activities. The first committed step in the biosynthesis of triterpenes is the cyclization of 2,3-oxidosqualene, an enzymatic reaction carried out by oxidosqualene cyclases (OSCs), giving rise to a broad range of different compounds, such as the sterol precursors cycloartenol and lanosterol, or triterpene precursors such as cucurbitadienol and β-amyrin...
2016: PloS One
https://www.readbyqxmd.com/read/27771819/ethylene-promotes-mycelial-growth-and-ganoderic-acid-biosynthesis-in-ganoderma-lucidum
#7
Guang Zhang, Ang Ren, Fengli Wu, Hanshou Yu, Liang Shi, Mingwen Zhao
OBJECTIVE: To investigate the effects of ethylene, in the form of ethephon (2-chloroethylphosphonic acid), on mycelial growth and ganoderic acid (GA) accumulation in the higher basidiomycete Ganoderma lucidum. RESULTS: Treatment with both 10 and 15 mM ethephon enhanced the growth of G. lucidum on solid CYM plates and in CYM liquid medium. After optimization using response surface methodology, GA reached 33 mg/g dry cell weight (DW), an increase of 90 %, compared with the control...
October 22, 2016: Biotechnology Letters
https://www.readbyqxmd.com/read/27769814/bile-acid-synthesis-precursors-in-subjects-with-genetic-hypercholesterolemia-negative-for-ldlr-apob-pcsk9-apoe-mutations-association-with-lipids-and-carotid-atherosclerosis
#8
L Baila-Rueda, A Cenarro, I Lamiquiz-Moneo, R Mateo-Gallego, A M Bea-Sanz, S Perez-Calahorra, V Marco-Benedi, F Civeira
Some oxysterols are precursors of bile acid synthesis and play an important role in cholesterol homeostasis. However, if they are involved in the pathogeny of genetic hypercholesterolemia has not been previously explored. We have studied non-cholesterol sterol markers of cholesterol synthesis (lanosterol and desmosterol) and oxysterols (7α-hydroxy-4-cholesten-3-one, 24S-hydroxycholesterol and 27-hydroxycholesterol) in 200 affected subjects with primary hypercholesterolemia of genetic origin, negative for mutations in LDLR, APOB, PCSK9 and APOE genes (non-FH GH) and 100 normolipemic controls...
October 18, 2016: Journal of Steroid Biochemistry and Molecular Biology
https://www.readbyqxmd.com/read/27760853/the-ph-responsive-transcription-factor-pacc-regulates-mycelial-growth-fruiting-body-development-and-ganoderic-acid-biosynthesis-in-ganoderma-lucidum
#9
Feng-Li Wu, Guang Zhang, Ang Ren, Zhi-Hao Dang, Liang Shi, Ai-Liang Jiang, Ming-Wen Zhao
Ganoderma lucidum is a medicinal macrofungus that is widely used in traditional Chinese medicine. Nonetheless, the scarcity of basic biological studies of this organism has hindered the further development of its commercial value. The pH-responsive transcription factor PacC/Rim101 governs the adaptation to environmental pH, the development and the secondary metabolism of many fungi. In this study, a homologue of PacC/Rim101 that encodes GlPacC was identified in the higher basidiomycete G. lucidum GlPacC is composed of 807 amino acids and contains three typical C2H2 zinc-finger domains, two potential PEST domains, a putative PKA phosphorylation site, and a putative nuclear localization signal (NLS)...
October 19, 2016: Mycologia
https://www.readbyqxmd.com/read/27754464/coumarin-antifungal-lead-compounds-from-millettia-thonningii-and-their-predicted-mechanism-of-action
#10
Daniel M Ayine-Tora, Robert Kingsford-Adaboh, William A Asomaning, Jerry J E K Harrison, Felix C Mills-Robertson, Yahaya Bukari, Patrick O Sakyi, Sylvester Kaminta, Jóhannes Reynisson
Fungal pathogens continue to pose challenges to humans and plants despite efforts to control them. Two coumarins, robustic acid and thonningine-C isolated from Millettia thonningii, show promising activity against the fungus Candida albicans with minimum fungicidal concentration of 1.0 and 0.5 mg/mL, respectively. Molecular modelling against the putative bio-molecular target, lanosterol 14α-demethylase (CYP51), revealed a plausible binding mode for the active compounds, in which the hydroxyl group binds with a methionine backbone carboxylic group blocking access to the iron catalytic site...
October 15, 2016: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/27737019/an-rnai-based-control-of-fusarium-graminearum-infections-through-spraying-of-long-dsrnas-involves-a-plant-passage-and-is-controlled-by-the-fungal-silencing-machinery
#11
Aline Koch, Dagmar Biedenkopf, Alexandra Furch, Lennart Weber, Oliver Rossbach, Eltayb Abdellatef, Lukas Linicus, Jan Johannsmeier, Lukas Jelonek, Alexander Goesmann, Vinitha Cardoza, John McMillan, Tobias Mentzel, Karl-Heinz Kogel
Meeting the increasing food and energy demands of a growing population will require the development of ground-breaking strategies that promote sustainable plant production. Host-induced gene silencing has shown great potential for controlling pest and diseases in crop plants. However, while delivery of inhibitory noncoding double-stranded (ds)RNA by transgenic expression is a promising concept, it requires the generation of transgenic crop plants which may cause substantial delay for application strategies depending on the transformability and genetic stability of the crop plant species...
October 2016: PLoS Pathogens
https://www.readbyqxmd.com/read/27638257/characteristics-of-dairy-cows-with-a-greater-or-lower-risk-of-subacute-ruminal-acidosis-volatile-fatty-acid-absorption-rumen-digestion-and-expression-of-genes-in-rumen-epithelial-cells
#12
X Gao, M Oba
The objective of this study was to examine whether lactating dairy cows with a greater or lower risk of subacute ruminal acidosis (SARA) have differences in volatile fatty acid (VFA) absorption rate, expression of genes involved in VFA metabolism and intracellular pH regulation in rumen epithelial cells, and in situ carbohydrate digestibility in the rumen. We fed 14 ruminally cannulated mid-lactating dairy cows (119 ± 47.2 d in milk; body weight 640 ± 47.9 kg) a high-grain diet consisting of 30% forage ad libitum, with an 18-d diet adaptation and a 7-d sample and data collection period...
September 13, 2016: Journal of Dairy Science
https://www.readbyqxmd.com/read/27600041/antileishmanial-activity-of-ezetimibe-inhibition-of-sterol-biosynthesis-in-vitro-synergy-with-azoles-and-efficacious-in-experimental-cutaneous-leishmaniasis
#13
Valter Viana Andrade-Neto, Edézio Ferreira Cunha-Júnior, Marilene Marcuzzo do Canto-Cavalheiro, Geórgia Correa Atella, Talita de Almeida Fernandes, Paulo Roberto Ribeiro Costa, Eduardo Caio Torres-Santos
Leishmaniasis affects mainly low-income populations in tropical regions. Radical innovation in drug discovery is time- and money-consuming, causing severe restrictions to launch new chemical entities to treat neglected diseases. Drug repositioning is an attractive strategy to attend a specific demand more easily. In this project, we have evaluated the antileishmanial activity of 30 drugs currently in clinical usage for different morbidities. Ezetimibe, clinically used to reduce intestinal cholesterol absorption in dyslipidemic patients, killed promastigotes of L...
September 6, 2016: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/27558681/evaluation-of-the-novel-antichagasic-activity-of-1-2-3-triazolo-1-5-a-pyridine-derivatives
#14
Michel Lapier, María C Zuñiga-López, Benjamín Aguilera-Venegas, Rosa Adam, Belén Abarca, Rafael Ballesteros, Rodrigo López-Muñoz, Juan Diego Maya, Claudio Olea-Azar
Trypanosoma cruzi is the causative agent of Chagas disease. This parasite is vulnerable to the effects of ROS as its main defense mechanism against exogenous agents trypanothione is also another weakness of the parasite that has been investigated related to the inhibition of enzymes belonging P450 system, mainly CYP51. In our group we have synthesized a series of triazoles known as [1,2,3]triazolo[1,5-a]pyridyl ketones, and pyridyl ketones. These families have shown interesting structural features due to the presence of electron withdrawing moieties attached to the main heterocycle (triazoles and/or pyridines) and are proposed as potential target in the parasite, by the presence of the carbonyl group being able to reduce and form a free radical that could interact with molecular oxygen generating ROS in the parasite...
August 24, 2016: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/27514516/transcriptional-profiling-analysis-of-penicillium-digitatum-the-causal-agent-of-citrus-green-mold-unravels-an-inhibited-ergosterol-biosynthesis-pathway-in-response-to-citral
#15
Qiuli OuYang, Nengguo Tao, Guoxing Jing
BACKGROUND: Green mold caused by Penicillium digitatum is the most damaging postharvest diseases of citrus fruit. Previously, we have observed that citral dose-dependently inhibited the mycelial growth of P. digitatum, with the minimum inhibitory concentration (MIC) of 1.78 mg/mL, but the underlying molecular mechanism is barely understood. RESULTS: In this study, the transcriptional profiling of the control and 1/2MIC-citral treated P. digitatum mycelia after 30 min of exposure were analyzed by RNA-Seq...
2016: BMC Genomics
https://www.readbyqxmd.com/read/27461192/metabolite-profiles-of-synovial-fluid-change-with-the-radiographic-severity-of-knee-osteoarthritis
#16
Sooah Kim, Jiwon Hwang, Jungyeon Kim, Joong Kyong Ahn, Hoon-Suk Cha, Kyoung Heon Kim
OBJECTIVES: To investigate potential pathogenic pathways in the synovial fluid of osteoarthritis (OA) patients at different disease stages [early vs. late, determined based on the Kellgren-Lawrence (KL) grading scale], through metabolite profiles that were performed by using gas-chromatography/time-of-flight mass spectrometry (GC/TOF MS). METHODS: Synovial fluid samples were obtained from 15 patients with knee OA, divided into early- (KL grade: 1 and 2) and late-stage OA (KL grade: 3 and 4)...
July 22, 2016: Joint, Bone, Spine: Revue du Rhumatisme
https://www.readbyqxmd.com/read/27449014/structure-based-design-of-cyp51-inhibitors
#17
Jun Yong Choi, William R Roush
Structure based design has been widely used in many drug development programs. In parallel with the evolution of high performance computing systems and versatile molecular modeling programs, structure based drug design has become indispensible in many research areas. CYP51 is a proven therapeutic target for anti-fungal drugs. While anti-fungal drugs targeting CYP51 have a long history and a large pool of anti-fungal CYP51 inhibitor therapeutics are now available, structure based design of therapeutic agents targeting CYP51 has only recently been attempted, Here, we present structural features of CYP51 and its complexes formed with lanosterol, azole drugs, and specifically designed inhibitors...
July 19, 2016: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/27448654/structure-based-design-of-cyp51-inhibitors
#18
Jun Yong Choi, William R Roush
Structure based design has been widely used in many drug development programs. In parallel with the evolution of high performance computing systems and versatile molecular modeling programs, structure based drug design has become indispensible in many research areas. CYP51 is a proven therapeutic target for anti-fungal drugs. While anti-fungal drugs targeting CYP51 have a long history and a large pool of anti-fungal CYP51 inhibitor therapeutics are now available, structure based design of therapeutic agents targeting CYP51 has only recently been attempted, Here, we present structural features of CYP51 and its complexes formed with lanosterol, azole drugs, and specifically designed inhibitors...
July 19, 2016: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/27431907/influenza-viral-membrane-fusion-is-sensitive-to-sterol-concentration-but-surprisingly-robust-to-sterol-chemical-identity
#19
Katarzyna E Zawada, Dominik Wrona, Robert J Rawle, Peter M Kasson
Influenza virions are enriched in cholesterol relative to the plasma membrane from which they bud. Previous work has shown that fusion between influenza virus and synthetic liposomes is sensitive to the amount of cholesterol in either the virus or the target membrane. Here, we test the chemical properties of cholesterol required to promote influenza fusion by replacing cholesterol with other sterols and assaying viral fusion kinetics. We find that influenza fusion with liposomes is surprisingly robust to sterol chemical identity, showing no significant dependence on sterol identity in target membranes for any of the sterols tested...
2016: Scientific Reports
https://www.readbyqxmd.com/read/27421732/4-methylzymosterone-and-other-intermediates-of-sterol-biosynthesis-from-yeast-mutants-engineered-in-the-erg27-gene-encoding-3-ketosteroid-reductase
#20
Terenzio Ferrante, Alessandro Barge, Silvia Taramino, Simonetta Oliaro-Bosso, Gianni Balliano
Studies in the post-squalene section of sterol biosynthesis may be hampered by the poor availability of authentic standards. The present study used different yeast strains engineered in 3-ketosteroid reductase (Erg27p) to obtain radioactive and non-radioactive intermediates of sterol biosynthesis hardly or not available commercially. Non-radioactive 3-keto 4-monomethyl sterones were purified from non-saponifiable lipids extracted from cells bearing point-mutated 3-ketosteroid reductase. Two strategies were adopted to prepare the radioactive compounds: (1) incubation of cell homogenates of an ERG27-deletant strain with radioactive lanosterol, (2) incubation of growing cells of a strain expressing point-mutated 3-ketosteroid reductase with radioactive acetate...
September 2016: Lipids
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