gebhart/patrepeval huggingface dataset:
<i>trans</i>-2-Aryl-<i>N</i>,<i>N</i>-dipropylcyclopropylamines:  Synthesis and Interactions with 5-HT<sub>1A</sub>Receptors (1996)

Twelve N,N-dipropyl-substituted derivatives of trans-2-arylcyclopropylamine have been prepared and assayed for their ability to displace [(3)H]-8-OH-DPAT from rat brain 5-HT(1A) receptors. The new derivatives include phenyl (7a), bromo- (7b) and fluorophenyl (7c-e), 2-methoxy-5-fluorophenyl (7h), and 2-hydroxy-5-fluorophenyl (7l) as well as trifluoromethylphenyl (7f) and 2,3-dichlorophenyl (7g) analogues. In the present series of compounds, electron-withdrawing substituents in the phenyl ring appear to decrease the affinity for 5-HT(1A) receptors. In contrast, electron-rich aryl groups, such as 2- or 3-thienyl (7j and 7k, respectively), provide compounds with high affinity. The additional bulk produced by the aromatic moiety in the 2-benzothienyl derivative 7i appears to be detrimental to 5-HT(1A) receptor affinity. The racemic mixtures of the interesting 7j and 7l were resolved into the enantiomers; 7j and 7l exhibited a high enantiomeric 5-HT(1A) receptor affinity ratio (75-fold and 100-fold, respectively). The enantiomers of 7j and 7l were evaluated in vivo by use of biochemical and behavioral tests in rats. Compound (1R,2R)-7j behaved as a partial agonist whereas (1R,2S)-7l appeared as an efficacious 5-HT(1A) receptor agonist, stimulating both autoreceptors and postsynaptic receptors.
Synthesis of 2-Aryl[1,2,4]triazolo[5,1-<i>b</i>]benzoxazoles by Oxidative Cyclization of<i>N</i>-(Benzoxazol-2-yl)benzamidines (1990)

The reaction of 2-aminobenzoxazoles with benzonitriles in the presence of anhydrous tin(IV) chloride gives N-(benzoxazol-2-yl)benzamidines in high yields. Cyclodehydrogenation of these compounds with lead(IV) acetate affords 2-aryl[1,2,4]triazolo[5,1-b]benzoxazoles in good yields.
Two distinct trimeric conformations of natively membrane-anchored full-length herpes simplex virus 1 glycoprotein B (2016)

Many viruses are enveloped by a lipid bilayer acquired during assembly, which is typically studded with one or two types of glycoproteins. These viral surface proteins act as the primary interface between the virus and the host. Entry of enveloped viruses relies on specialized fusogen proteins to help merge the virus membrane with the host membrane. In the multicomponent herpesvirus fusion machinery, glycoprotein B (gB) acts as this fusogen. Although the structure of the gB ectodomain postfusion conformation has been determined, any other conformations (e.g., prefusion, intermediate conformations) have so far remained elusive, thus restricting efforts to develop antiviral treatments and prophylactic vaccines. Here, we have characterized the full-length herpes simplex virus 1 gB in a native membrane by displaying it on cell-derived vesicles and using electron cryotomography. Alongside the known postfusion conformation, a novel one was identified. Its structure, in the context of the membrane, was determined by subvolume averaging and found to be trimeric like the postfusion conformation, but appeared more condensed. Hierarchical constrained density-fitting of domains unexpectedly revealed the fusion loops in this conformation to be apart and pointing away from the anchoring membrane. This vital observation is a substantial step forward in understanding the complex herpesvirus fusion mechanism, and opens up new opportunities for more targeted intervention of herpesvirus entry.
Region-specific amyloid-β accumulation in the olfactory system influences olfactory sensory neuronal dysfunction in 5xFAD mice (2021)

Our results showed that partial and asymmetrical accumulation of Aβ coincided with physiologically and structurally damaged areas in the peripheral olfactory system, which evoked hyporeactivity to some odorants. Taken together, partial olfactory dysfunction closely associated with peripheral OSN's loss could be a leading cause of AD-related hyposmia, a characteristic of early AD.
Broad-band tunable electroabsorption modulated laser for WDM application (1997)

Design and fabrication of the first 1.55-/spl mu/m wavelength tunable electroabsorption modulated laser integrated with a bent waveguide distributed-feedback (DFB) laser is reported. A low-threshold high-efficiency and stable single-longitudinal-mode operation is obtained when the electrodes of the bent DFB waveguide were uniformly pumped. In a normal configuration where the modulator part is used as an intensity modulator (i.e., AR coating on the modulator side and HR coating on the DFB side), stable single longitudinal mode output power close to 40 mW in free space is obtained with a 0-V bias to the modulator and an extinction ratio of up to 15 dB at 2.5 V. This single mode stability is due to the continuously distributed phase shift implemented in the structure thus reducing the photon pile-up inside the laser cavity as compared to an abruptly quarter-wave phase shifted DFB laser. With a nonuniform injection in the multiple electrodes, it was possible to select one particular single longitudinal mode out of the three neighboring modes inside the broad reflection band of the reflector. A wavelength tuning range of about 3.5 nm was obtained while maintaining an optical output power of more than 2 dBm from each mode. The device has a very low chirp (0.01-nm peak-to-peak) when modulated with a 2.5 Gb/s pseudorandom binary sequence (PRES) data stream and an error-free transmission over 200 km of non-DSF fiber has been demonstrated for all four wavelength channels separated by 100-GHz spacing. Also, when the modulator part of the structure is used as a phase tuning element (i.e., antireflective (AR) coating on the DFB side and HR coating on the modulator side), we have successfully demonstrated high-speed optical packet switching with a fast and wide tunable wavelength range. The optical packets can be modulated at 2.5 Gb/s and may be switched among four wavelength channels in less than one bit period.
Children's collaboration styles in a Newtonian microworld (1996)

No abstract available.
Parametrically Shielding Electromagnetic Fields by Nonlinear Metamaterials (2008)

An analytical theory is developed for parametric interactions in metamaterial multilayer structures with simultaneous nonlinear electronic and magnetic responses and with a near-zero refractive index. We demonstrate theoretically that electromagnetic fields of certain frequencies can be parametrically shielded by a nonlinear left-handed material slab, where the permittivity and permeability are both negative. The skin depth is tunable, and even in the absence of material absorption, can be much less than the wavelength of the electromagnetic field being shielded. This exotic behavior is a consequence of the intricate nonlinear response in the left-handed materials and vanishing optical refractive index at the pump frequency.
Polypropylene based thermoplastic polymers for potential recyclable HVDC cable insulation applications (2017)

Thermoplastic materials are highly desirable for power cable insulation application because of their recyclability and ease of processing. They are particularly suitable for high voltage direct current (HVDC) cable insulation because of the absence of byproducts during cable production, which may result in the reduction of undesirable space charge accumulation and the degassing cost. Polypropylene based polymers may have the potential for recyclable thermoplastic cable insulation application because of their high melting temperatures and adjustable mechanical and electrical properties. This work aimed at evaluating the potential of isotactic polypropylenes, propylene-ethylene block copolymers and random copolymers for thermoplastic cable insulation application. We investigated the melting and crystallization behavior, crystal structure, supramolecular structure, mechanical properties, space charge distribution and DC breakdown strength of six different polymers (two isotactic polypropylenes, two block copolymers and two random copolymers). A comprehensive analysis of these parameters indicates that the propylene-ethylene binary random copolymers are more potentially suitable for thermoplastic cable insulation application.
Regulation and expression of the arsenic resistance operon from Staphylococcus aureus plasmid pI258 (1992)

The arsenic resistance operon from Staphylococcus aureus plasmid pI258 was cloned and sequenced. The DNA sequence contains three genes in the order arsR, arsB, and arsC. The predicted amino acid sequences of the gene products are homologous with those of the products of the ars operons of plasmids pSX267 from Staphylococcus xylosus and R773 from Escherichia coli. The cloned staphylococcal ars operon confers resistances to arsenate, arsenite, and antimonite in S. aureus and Bacillus subtilis. The same operon was also expressed in E. coli and conferred resistance to arsenite but less resistance to arsenate and antimonite. Regulation of the pI258 ars operon was studied by using a translational arsB-blaZ fusion in S. aureus and a transcriptional arsB-luxAB fusion in E. coli. The ars operon was induced by arsenate [As(V)], arsenite [As(III)], and antimonite [Sb(III)], to which the strains were resistant, plus Bi(III) in S. aureus. Only arsenate and arsenite induced the operon in E. coli. Northern (RNA) blot DNA-RNA hybridization analysis showed inducible synthesis of a full-length ars mRNA, about 2.1 kb in size, both in S. aureus and in E. coli. S. aureus ars proteins were expressed in E. coli from the T7 phage promoter under the control of the T7 RNA polymerase. Primer extension (reverse transcriptase) analysis showed that the ars mRNA started at the same position (nucleotides 17 and 18 upstream from the arsR ATG) both in S. aureus and in E. coli. An internal deletion mutation in arsB resulted in decreased resistance to arsenate and total loss of arsenite and antimonite resistances. Partial deletion of 56 bp from the 3' end of the arsC gene resulted in loss of resistance to arsenate; the determinant retained arsenite and antimonite resistances.
MMP-9/TIMP-1imbalance induced in human dendritic cells by<i>Porphyromonas gingivalis</i> (2009)

Matrix metalloproteinase-9 (MMP-9) cleaves collagen, allowing leukocytes to traffic toward the vasculature and the lymphatics. When MMP-9 is unregulated by tissue inhibitor of metalloproteinase-1 (TIMP-1), this can lead to tissue destruction. Dendritic cells (DCs) infiltrate the oral mucosa increasingly in chronic periodontitis, characterized by infection with several pathogens including Porphyromonas gingivalis. In this study, human monocyte-derived DCs were pulsed with different doses of lipopolysaccharide of P. gingivalis 381 and of Escherichia coli type strain 25922, as well as whole live isogenic fimbriae-deficient mutant strains of P. gingivalis 381. Levels of induction of MMP-9 and TIMP-1, as well as interleukin-10 (IL-10), which reportedly inhibits MMP-9 induction, were measured by several approaches. Our results reveal that lipopolysaccharide of P. gingivalis, compared with lipopolysaccharide from E. coli type strain 25922, is a relatively potent inducer of MMP-9, but a weak inducer of TIMP-1, contributing to a high MMP-9/TIMP-1 ratio.Whole live P. gingivalis strain 381, major fimbriae mutant DPG-3 and double mutant MFB were potent inducers of MMP-9, but minor fimbriae mutant MFI was not. MMP-9 induction was inversely proportional to IL-10 induction. These results suggest that lipopolysaccharide and the minor and the major fimbriae of P. gingivalis may play distinct roles in induction by DCs of MMP-9, a potent mediator of local tissue destruction and leukocyte trafficking.
High Salt Concentrations Increase Permeability through OmpC Channels of Escherichia coli (2014)

OmpF and OmpC porin channels are responsible for the passage of small hydrophilic solutes across the outer membrane of Escherichia coli. Although these channels are two of the most extensively studied porin channels, what had yet remained elusive was the reason why OmpC shows markedly lower permeability than OmpF, despite having little difference in its channel size. The OmpC channel, however, is known to contain a larger number of ionizable residues than the OmpF channel. In this study, we examined the channel property of OmpF and OmpC using the intact cell of E. coli, and we found that the permeability of several β-lactams and lactose through OmpC became increased to the level comparable with OmpF with up to 0.3 m salt that may increase the Debye-Hückel shielding or with 2% ethanol or 0.3 m urea that may perturb the short range ordering of water molecules. Replacing 10 pore-lining residues that show different ionization behavior between OmpC and OmpF led to substantial conversion of channel property with respect to their permeability and response to external salt concentration. We thus propose that the overall configuration of ionizable residues in the channel that may orient water molecules and the electrostatic profile of the channel play a decisive role in defining the channel property of the OmpC porin rather than its channel size.
Electro-catalytic oxidative cleavage of lignin in a protic ionic liquid (2012)

Lignin is a component of lignocellulosic biomass and a promising matrix for recovering important renewable aromatic compounds. We present a new approach of electro-oxidative cleavage of lignin, dissolved in a special protic ionic liquid, using an anode with particular electro-catalytic activity. As appropriate ionic liquid triethylammonium methanesulfonate was identified, synthesised, explored for dissolution of alkali-lignin and used for electrolysis of 5 wt.% lignin solutions. As appropriate anode material, oxidation-stable ruthenium-vanadium-titanium mixed oxide electrodes were prepared and explored for their electro-catalytic activity. The electrolysis was performed at several potentials in the range from 1.0 V to 1.5 V (vs. an Ag pseudo reference electrode). A wide range of aromatic fragments was identified as cleavage products by means of GC-MS and HPLC measurements.
Heterogeneous CeO2 catalyst for the one-pot synthesis of organic carbamates from amines, CO2 and alcohols (2011)

Heterogeneous CeO2 catalyst can catalyze the one-pot synthesis of methyl benzylcarbamate from benzylamine, CO2 and methanol. The yield of methyl benzylcarbamate reached 92% at >99% benzylamine conversion and 92% benzylamine-based selectivity even in the absence of the dehydrating agents. The catalyst is reusable after the calcination at 873 K for 3 h. Various carbamates can be synthesized with good yield and high selectivity by the reaction of amines + CO2 + alcohols over CeO2. The main formation route of methyl benzylcarbamate is suggested to be the reaction of dimethyl carbonate or the precursor of dimethyl carbonate formation with benzylamine.
Regulation of adult erythropoiesis by prolyl hydroxylase domain proteins (2007)

Polycythemia is often associated with erythropoietin (EPO) overexpression and defective oxygen sensing. In normal cells, intracellular oxygen concentrations are directly sensed by prolyl hydroxylase domain (PHD)-containing proteins, which tag hypoxia-inducible factor (HIF) alpha subunits for polyubiquitination and proteasomal degradation by oxygen-dependent prolyl hydroxylation. Here we show that different PHD isoforms differentially regulate HIF-alpha stability in the adult liver and kidney and suppress Epo expression and erythropoiesis through distinct mechanisms. Although Phd1(-/-) or Phd3(-/-) mice had no apparent defects, double knockout of Phd1 and Phd3 led to moderate erythrocytosis. HIF-2alpha, which is known to activate Epo expression, accumulated in the liver. In adult mice deficient for PHD2, the prototypic Epo transcriptional activator HIF-1alpha accumulated in both the kidney and liver. Elevated HIF-1alpha levels were associated with dramatically increased concentrations of both Epo mRNA in the kidney and Epo protein in the serum, which led to severe erythrocytosis. In contrast, heterozygous mutation of Phd2 had no detectable effects on blood homeostasis. These findings suggest that PHD1/3 double deficiency leads to erythrocytosis partly by activating the hepatic HIF-2alpha/Epo pathway, whereas PHD2 deficiency leads to erythrocytosis by activating the renal Epo pathway.
Spectral Förster Resonance Energy Transfer Detection of Protein Interactions in Surface-Supported Bilayers (2006)

Förster resonance energy transfer (FRET), a fluorescence detection technique, is often used for sensing molecular interactions in solution and in membranes. Here we show that (1) FRET spectra can be recorded in single bilayers, supported on a surface, and (2) the fluorescein/rhodamine dye pair is an adequate reporter of FRET when spectral detection is used. Thus, measurements pertaining to molecular interactions in membranes can be carried out in supported bilayers. Spectral FRET has advantages over imaging FRET, which monitors only signal amplitudes at certain wavelength. There are also advantages to performing spectral FRET measurements in supported bilayers as compared to free liposomes in suspension. However, the spectral properties of dyes can be altered in an unexpected manner in an ordered bilayer structure on a surface, such that fluorescence detection in surface-supported bilayers is not always trivial.
The Thermogravimetric Noack Test: A Precise, Safe and Fast Method for Measuring Lubricant Volatility (1996)

<div class="htmlview paragraph">A new engine oil volatility method has been developed which has all the advantages of present gas chromatography (GC) methods, duplicates the results of the classic Noack methods, and is faster than both This method could end the ongoing debate between those who favor the safety and efficiency of the GC methods and those who favor the more “real” life conditions of the Noack techniques</div> <div class="htmlview paragraph">The method, called the TG Noack because it uses a Thermogravimetric Analyzer (TGA), was developed with the same ASTM round robin oils used to establish the precision of the Noack and GC methods This paper describes how test conditions were derived and how critical control parameters were identified and optimized It presents results demonstrating that the TG Noack Test is a fast (10 minutes/sample), safe (no Woods Metal, no handling of hot crucibles or oil), and repeatable (Repeatability = 3 1%) version of the classic Noack Test (1 1 correlation with R<sup>2</sup> = 0 99) Finally, the paper provides some guidelines for adapting the procedure to TGA instruments that are different from that used in the development of the method (Seiko RTG220)</div>
New clock-feedthrough compensation scheme for switched-current circuits (1998)

An improved clock-feedthrough compensation scheme for switched current system is proposed. Both the signal dependent and the constant clock-feedthrough terms are canceled by using both nMOS and pMOS current samplers and by adopting a source replication technique. The proposed current memory cell was fabricated with 0.6 /spl mu/m CMOS process. Both experimental and theoretical results on clock-feedthrough error reveal substantial reduction over the existing compensation schemes.
Nutritional Enhancement of Biocontrol of Blue Mold on Apples (1992)

Thirty-six carbohydrates and twenty-three nitrogenous compounds were evaluated for their effect on germination, and germ tube and radial growth of the pathogen Penicillium expansum, and for stimulation of growth of an antagonist Pseudomonas syringae (strain L-59-66). Compounds that strongly stimulated growth of the antagonist but had little or no stimulatory effect on germination and growth of the pathogen were evaluated for their effect on enhancing biocontrol of blue mold on ripe Golden Delicious apple. Seven amino acids and two carbohydrates met the required criteria (...)
Keyword Query Reformulation on Structured Data (2012)

Textual web pages dominate web search engines nowadays. However, there is also a striking increase of structured data on the web. Efficient keyword query processing on structured data has attracted enough attention, but effective query understanding has yet to be investigated. In this paper, we focus on the problem of keyword query reformulation in the structured data scenario. These reformulated queries provide alternative descriptions of original input. They could better capture users' information need and guide users to explore related items in the target structured data. We propose an automatic keyword query reformulation approach by exploiting structural semantics in the underlying structured data sources. The reformulation solution is decomposed into two stages, i.e., offline term relation extraction and online query generation. We first utilize a heterogenous graph to model the words and items in structured data, and design an enhanced Random Walk approach to extract relevant terms from the graph context. In the online query reformulation stage, we introduce an efficient probabilistic generation module to suggest substitutable reformulated queries. Extensive experiments are conducted on a real-life data set, and our approach yields promising results.
Synthesis and murine antineoplastic activity of bis[carbamoyloxymethyl] derivatives of pyrrolo[2,1-a]isoquinoline (1984)

The synthesis of 4,5-dihydropyrrolo[2,1-a]isoquinolines is reported. A key intermediate in the synthesis of 8-methoxy-4,5-dihydropyrrolo[2,1-a]isoquinolines, 6-hydroxy-1,2,3,4-tetrahydroisoquinoline-1-carboxylic acid (6), was prepared by using a regiospecific phenolic cyclization reaction. The P388 lymphocytic activity is reported for 1,2-bis(hydroxymethyl)-5,6-dihydro-8-methoxy-3-methylpyrrolo [2,1-a]isoquinoline bis(isopropylcarbamate) (11a), 1,2-bis(hydroxymethyl)-5,6-dihydro-8-methoxy-3-methylpyrrolo[2,1-a ]isoquinoline bis(cyclohexylcarbamate) (11b), 1,2-bis(hydroxymethyl)-5,6-dihydro-3-methylpyrrolo[2,1-a]isoqui nol ine bis(methylcarbamate) (13a), 1,2-bis(hydroxymethyl)-5,6-dihydro-3-methylpyrrolo [2,1-a]isoquinoline bis(ethylcarbamate) (13b), and 1,2-bis(hydroxymethyl)-5,6-dihydroxy-3-methylpyrrolo[2,1-a]isoq uin oline bis(cyclohexylcarbamate) (13c); all of the compounds were active. Compound 11a was tested in an expanded tumor panel and was shown to be active against B16 melanocarcinoma, CD8F1 mammary, L1210 lymphoid leukemia, colon 38, and MX-1 human tumor breast xenograft systems.
Enhanced voice over IP support in GPRS and EGPRS (2002)

In this paper we discuss the applicability of GPRS and EGPRS for the transmission of voice packets in an end-to-end packet switched scenario. We assume typical voice over IP (VoIP) applications spanning between a fixed and a mobile terminal. As the transmission delay of the voice packets has most impact on the perceived quality of service (QoS), it has been the focus of our investigations. The studies have been aided by an end-to-end simulation environment modeling the protocol stack applied in (E)GPRS. The first assessments performed are dedicated to obtaining the performance figures of standard (E)GPRS systems carrying VoIP data. In a second step, the mechanisms and procedures having most relevance to the transmission delay in (E)GPRS are identified and improvements are proposed. These improvements start from smaller modifications of the standard system and end at modifications of the multiplexing schemes applied on the radio interface. The typical transmission delay of (E)GPRS is thus stepwise improved at the expense of increased modifications of the system.