Search results for "hole"
showing 10 items of 2900 documents
Optimization of Polymer Blue-Light-Emitting Devices by Introducing a Hole-Injection Layer Doped with the Molecular Nanomagnet [Mn12O12(H2O)4(C6F5COO)…
2006
Biological effects of short-chain fatty acids in nonruminant mammals.
1993
propionate, volatile fatty acids (VFAs), cholesterol, cell prolifera tion, human gastric lipase
Effects of Pentachlorophenol and Biotic Interactions on Soil Fauna and Decomposition in Humus Soil
1995
In a laboratory experiment, effects of chemical stress (pentachlorophenol, PCP, at concentrations of 0, 50, and 500 mg/kg) and biotic interactions (nematodes in the presence or absence of collembolas and enchytraeids) on the community structure of soil animals and decomposition processes were studied. PCP was strongly adsorbed to humus that contained 65% organic matter. Numbers of fungal-feeding nematodes decreased significantly at the highest PCP concentration, while no effects were found in bacterial feeders. There were differences in the numbers of nematodes between different animal combinations, but at the highest PCP concentration, collembolas and enchytraeids had no effect on them. Nu…
Straightforward synthesis of bioconjugatable azo dyes. Part 1: Black Hole Quencher-1 (BHQ-1) scaffold
2014
Abstract Azo dyes are currently used to quench the fluorescence of energy donors in bioassays through Forster resonance energy transfer (FRET) phenomenon. Common examples of such dark quenchers are DABCYL and the three members of Black Hole Quencher® (BHQ) family. Yet, only carboxylic acid and phosphoramidite derivatives of such azo dyes are presently commercially available. This Letter presents a straightforward synthesis method to novel bioconjugatable quenchers derived from BHQ-1 scaffold and equipped with a reactive group being either azido, terminal alkyne, or maleimide. The potential utility of the ‘clickable’ azido and thiol-reactive derivatives was notably demonstrated through the p…
Multiscale Simulations of SARS-CoV-2 3CL Protease Inhibition with Aldehyde Derivatives. Role of Protein and Inhibitor Conformational Dynamics in the …
2020
<p>We here investigate the mechanism of SARS-CoV-2 3CL protease inhibition by one of the most promising families of inhibitors, those containing an aldehyde group as warhead. These compounds are covalent inhibitors that inactivate the protease forming a stable hemithioacetal complex. Inhibitor 11a is a potent inhibitor that has been already tested in vitro and in animals. Using a combination of classical and QM/MM simulations we determined the binding mode of the inhibitor into the active site and the preferred rotameric state of the catalytic histidine. In the noncovalent complex the aldehyde group is accommodated into the oxyanion hole formed by the NH main chain groups of residues …
Selenoproteins, cholesterol-lowering drugs, and the consequences: revisiting of the mevalonate pathway.
2004
3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitors (statins) and peroxisome proliferator-activated receptor alpha activators (fibrates) are the backbone of pharmacologic hypercholesterolemia and dyslipidemia treatment. Many of their clinical effects, however, are still enigmatic. This article describes how a side road of the mevalonate pathway, characterized in recent years, can rationalize a major fraction of these unexplained observations. This side road is the enzymatic isopentenylation of selenocysteine-tRNA([Ser]Sec) (Sec-tRNA), the singular tRNA to decode the unusual amino acid selenocysteine. The functionally indispensable isopentenylation of Sec-tRNA requires a unique interm…
Identification of the membrane penetrating domain of Vibrio cholerae cytolysin as a β-barrel structure
2005
Summary Vibrio cholerae cytolysin (VCC) is an oligomerizing pore-forming toxin that is related to cytolysins of many other Gram-negative organisms. VCC contains six cysteine residues, of which two were found to be present in free sulphydryl form. The positions of two intramolecular disulphide bonds were mapped, and one was shown to be essential for correct folding of protoxin. Mutations were created in which the two free cysteines were deleted, so that single cysteine substitution mutants could be generated for site-specific labelling. Employment of polarity-sensitive fluorophores identified amino acid side-chains that formed part of the pore-forming domain of VCC. The sequence commenced at…
Regulation of Farnesyl Diphosphate Synthase Gene Expression by Fatty Acids
2003
Cholesterol biosynthesis depends on the activity of regulatory enzymes, including the peroxisomal Farnesyl Diphosphate Synthase (FPPS ). Cholesterol regulates its own synthesis rate. Hence, as a response to cholesterol depletion, a feed back mechanism is activated, whereby sterol regulatory binding proteins (SREBPla, 1c and 2 ) are subjected to sequential proteolytic activation, which permits their interaction with specific DNA response elements from responsive genes. In turn, the transcriptional activity of cholesterol biosynthesis genes is induced. Conversely, cholesterol accumulation decreases SREBP maturation and transcription of controlled genes. In addition, polyunsaturated fatty acid…
Spirostane and cholestane glycosides from the bulbs of Allium nigrum L
2011
Abstract A phytochemical investigation of the fresh bulbs of Allium nigrum L. led to the isolation of new spirostane-type glycosides as two inseparable isomer mixtures, nigrosides A1/A2 (1a/1b) and nigrosides B1/B2 (2a/2b), two new cholestane-type glycosides, nigrosides C and D (3 and 4), together with the known compounds, 25(R,S)-5α-spirostan-2α,3β,6β-trio1-3-O-β- d -glucopyranosyl-(1 → 2)-O-[β- d -xylopyranosyl-(1 → 3)]-O-β- d -glucopyranosyl-(1 → 4)-β- d -galactopyranoside (5a/5b) and 25(R,S)-5α-spirostan-2α,3β,6β-trio1 3-O-β- d -glucopyranosyl-(1 → 2)-O-[4-O-(3S)-3-hydroxy-3-methylglutaryl-β- d -xylopyranosyl-(1 → 3)]-O-β- d -glucopyranosyl-(1 → 4)-β- d -galactopyranoside (6a/6b), isola…
Biologically and Pharmacologically Active Saponins from Plants: Recent Advances
2000
Saponins as triterpene or steroid glycosides were well known in ancient times for their detergent, haemolytic and fish toxic activities, properties which are correlated with the amphiphilic character of the molecules and their ability to complex cholesterol.