Month: May 2021

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Systems Pharmacology Dissection of Cholesterol Regulation Reveals Determinants of Large Pharmacodynamic Variability between Cell Lines

In individuals, heterogeneous drug-response phenotypes result from a complex interplay of dose, drug specificity, genetic background, and environmental factors, thus challenging our understanding of the underlying processes and optimal use of drugs in the clinical setting. Here, we use mass-spectrometry-based quantification of molecular response phenotypes and logic modeling to explain drug-response differences in a panel of cell lines. We apply this approach to cellular cholesterol regulation, a biological process with high clinical relevance. From the quantified molecular phenotypes elicited by various targeted pharmacologic or genetic treatments, we generated cell-line-specific models that quantified the processes beneath the idiotypic intracellular drug responses. The models revealed that, in addition to drug uptake and metabolism, further cellular processes displayed significant pharmacodynamic response variability between the cell lines, resulting in cell-line-specific drug-response phenotypes. This study demonstrates the importance of integrating different types of quantitative systems-level molecular measurements with modeling to understand the effect of pharmacological perturbations on complex biological processes. Blattmann et al. combine proteomic and metabolomic profiling with mechanistic modeling to characterize the complex processes underlying the heterogeneous drug response in cellular cholesterol regulation across a panel of different human cell lines.

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Reference：
Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

Synthetic Route of 14215-68-0, An article , which mentions 14215-68-0, molecular formula is C8H15NO6. The compound – N-((2S,3R,4R,5R,6R)-2,4,5-Trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-3-yl)acetamide played an important role in people’s production and life.

Synthesis of N4-(2-acetamido-2-deoxy-beta-D-glucopyranosyl)-L-asparagine analogues: Succinamide, L-2-hydroxysuccinamide, and L-2-hydroxysuccinamic acid hydrazide analogues

The syntheses of three analogues of N4-(2-acetamido-2-deoxy-beta-D-glucopyranosyl)-L-asparagine are described. N-(2-Acetamido-2-deoxy-beta-D-glucopyranosyl)succinamide was synthesized by the reaction of pentafluorophenyl succinamate with 2-acetamido-2-deoxy-beta-D-glucopyranosylamine. 2-Acetamido-3,4,6-tri-O-acetyl-2-deoxy-beta-D-glucopyranosylamine was synthesized, and the complete assignment of the 1H NMR spectrum is given. Reaction of the protected beta-D-glycosylamine with L-malic acid chloralid in the presence of a coupling agent (EEDQ) gave N4-(2-acetamido-3,4,6-tri-O-acetyl-2-deoxy-beta-D-glucopyranosyl)-L-malamic acid chloralid that was deprotected two ways: (1) using ammonia, which gave N4-(2-acetamido-2-deoxy-beta-D-glucopyranosyl)-L-2-hydroxysuccinamide, and (2) using hydrazine, which gave N4-(2-acetamido-2-deoxy-beta-D-glucopyranosyl)-L-2-hydroxysuccinamic acid hydrazide. (C) 2000 Elsevier Science Ltd.

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Reference：
Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

Electric Literature of 125995-03-1, Catalysts are substances that increase the reaction rate of a chemical reaction without being consumed in the process. 125995-03-1, Name is Atorvastatin lactone, molecular formula is C33H33FN2O4. In a Patent，once mentioned of 125995-03-1

Process for the preparation of amorphous atorvastatin calcium

A process for the preparation of amorphous atorvastatin calcium and hydrates thereof, which comprises: (a) hydrolysis of the precursor lactone using sodium hydroxide to form atorvastatin sodium salt solution; (b) addition of the atorvastatin sodium salt solution to a calcium chloride or calcium acetate solution in the absence or presence of seeds of amorphous atorvastatin calcium; and (c) isolation of the resultant amorphous atorvastatin calcium salt by filtration and drying.

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Reference：
Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

Chemistry is an experimental science, and the best way to enjoy it and learn about it is performing experiments.Introducing a new discovery about 10343-06-3, Name is 2,3,4,6-Tetra-o-acetyl-D-glucopyranose, Recommanded Product: 2,3,4,6-Tetra-o-acetyl-D-glucopyranose.

Process for the preparation of protected mono-sugar and oligo-sugar halides

The reaction of protected monosaccharides or oligosaccharides or protected monosaccharide and oligosaccharide derivatives containing an anomeric hydroxyl group with secondary alpha-haloenamines affords high yields of protected glycosyl halides, which are valuable intermediates for the introduction of sugar groups in the synthesis of oligosaccharides, glycolipids or glycopeptides.

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Reference：
Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

Children learn through play, and they learn more than adults might expect. Science experiments are a great way to spark their curiosity, get their minds active, and encourage them to do something that doesn’t involve a screen. 14215-68-0, C8H15NO6. A document type is Article, introducing its new discovery., Recommanded Product: 14215-68-0

The calculation of electronic parameters of an Ag/chitin/n-Si Schottky barrier diode

We have formed polymeric organic compound chitin film on n-Si substrate by adding a solution of polymeric compound chitin in N,N-dimethylacetamide and lithium chloride on top of an n-Si substrate and then evaporating solvent. It has been seen that the chitin/n-Si contact has demonstrated clearly rectifying behavior and the reverse curves exhibit a weak bias voltage dependence by the current-voltage (I-V) curves studied at room temperature. The barrier height and ideality factor values of 0.959 eV and 1.553, respectively, for this structure have been obtained from the forward bias I-V characteristics. Furthermore, the energy distribution of the interface state density located in the semiconductor band gap at the chitin/n-Si substrate in the energy range from (Ec – 0.897) to (Ec – 0.574) eV have been determined from the I-V characteristics. The interface state density, Nss, ranges from 5.965 × 1012 cm-2 eV-1 in (Ec – 0.897) eV to 1.706 × 1013 cm-2 eV-1 in (Ec – 0.574) eV and has an exponential rise with bias this energy range.

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Reference：
Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

Synthetic Route of 28244-94-2, Catalysts are substances that increase the reaction rate of a chemical reaction without being consumed in the process. 28244-94-2, Name is 4-Methylphenyl 2,3,4,6-tetra-O-acetyl-1-thio-β-D-glucopyranoside, molecular formula is C21H26O9S. In a Article，once mentioned of 28244-94-2

Synthesis of glycosyl fluorides from thio-, seleno-, and telluroglycosides and glycosyl sulfoxides using aminodifluorosulfinium tetrafluoroborates

Glycosyl fluorides can be synthesized from thio-, seleno-, and telluroglycosides and glycosyl sulfoxides using the aminodifluorosulfinium tetrafluoroborate reagents Xtalfluor-E and -M, with or without added N-bromosuccinimide. Mechanistic studies provide evidence that fluoride is delivered from the tetrafluoroborate counterion.

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Reference：
Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

Application of 14215-68-0. Let’s face it, organic chemistry can seem difficult to learn. Especially from a beginner’s point of view. Like 14215-68-0, Name is N-((2S,3R,4R,5R,6R)-2,4,5-Trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-3-yl)acetamide. In a document type is Article, introducing its new discovery.

Removal of various pollutants from water and wastewater by modified chitosan adsorbents

Chitosan-based adsorbents have attracted increasing attention in water and wastewater treatment in recent years due to its abundance and low price, as well as rich amino and hydroxyl groups. However, there are some drawbacks hindering its practical use, such as low mechanical strength, low solubility in acidic mediums, low adsorption capacity, and lack of selectivity. Therefore, a variety of modification methods, including physical and chemical modifications, have been investigated to improve the physicochemical properties of chitosan. This review provides a summary of (a) the intrinsic nature of chitosan associated with its structure and physicochemical properties; (b) the preparation strategies for modified chitosan together with its characterization; (c) the application of chitosan-based adsorbents for the removal of both organic pollutants (e.g., dyes, PPCPs, PFOS, and humus) and inorganic pollutants (e.g., heavy metal ions, nitrate, phosphate, borate, and fluoride). Recent advances in the fabrication and application of chitosan-based adsorbents involving the intrinsic nature of pollutants are highlighted in this review, as well as the effects of process variables (e.g., pH, contact time, ionic strength, competitive ions, temperature), modeling (kinetics and isotherm), adsorption mechanisms, and regeneration.

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Reference：
Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.3301-94-8, Name is 6-Butyltetrahydro-2H-pyran-2-one, molecular formula is C9H16O2. In a Review，once mentioned of 3301-94-8, Product Details of 3301-94-8

Fungal volatiles-a survey from edible mushrooms to moulds

Covering: up to January 2017 This review gives a comprehensive overview of the production of fungal volatiles, including the history of the discovery of the first compounds and their distribution in the various investigated strains, species and genera, as unravelled by modern analytical methods. Biosynthetic aspects and the accumulated knowledge about the bioactivity and biological functions of fungal volatiles are also covered. A total number of 325 compounds is presented in this review, with 247 cited references.

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Reference：
Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

Electric Literature of 14215-68-0, Children learn through play, and they learn more than adults might expect. Science experiments are a great way to spark their curiosity, get their minds active, and encourage them to do something that doesn’t involve a screen. 14215-68-0, C8H15NO6. A document type is Article, introducing its new discovery.

Design of glycosyltransferase inhibitors targeting human O-GlcNAc transferase (OGT)

Inhibition of glycosyltransferases requires the design of neutral inhibitors to allow cell permeation in contrast to their natural dianionic substrates. O-GlcNAc transferase (OGT) is a key enzyme involved in dynamic glycosylation of cytosolic and nuclear proteins in competition with phosphorylation. Designing OGT inhibitors is of prime interest for the better understanding of its biological implications. Introduction of a pyridine moiety as a pyrophosphate surrogate was evaluated, which provided moderate in vitro inhibition of OGT. Docking studies highlighted some key features for the binding of the designed inhibitors to the catalytic site of OGT where the carbohydrate moiety did not occupy its natural position but rather turned away and pointed to the solvent outside the catalytic pocket. Further investigation with cellular assays did not provide inhibition of OGT. This lack of OGT inhibition was rationalized with a permeation assay which revealed the sequestration of the inhibitors at the membrane. This journal is the Partner Organisations 2014.

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Reference：
Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

Synthetic Route of 2081-44-9. Chemistry is an experimental science, and the best way to enjoy it and learn about it is performing experiments.Introducing a new discovery about 2081-44-9, Name is Tetrahydro-2H-pyran-4-ol

Discovery and SAR study of piperidine-based derivatives as novel influenza virus inhibitors

A series of piperidine-based derivatives were identified as novel and potent inhibitors of the influenza virus through structural modification of a compound that was selected from a high-throughput screen. Various analogues were synthesized and confirmed as inhibitors. The structure-activity relationship (SAR) studies suggested that the ether linkage between the quinoline and piperidine is critical for the inhibitory activity. The optimized compound tert-butyl 4-(quinolin-4-yloxy)piperidine-1-carboxylate 11e had an excellent inhibitory activity against influenza virus infection from a variety of influenza virus strains, with EC50values as low as 0.05 muM. The selectivity index value (SI = MLD50/EC50) of 11e is over 160 000 based on cytotoxicity, measured by MTT assays of three cell lines. We carried out a time-of-addition experiment to delineate the mechanism of inhibition. The result indicates that 11e interferes with the early to middle stage of influenza virus replication.

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Reference：
Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics