gebhart/patrepeval huggingface dataset:
Synthesis, in Vitro Pharmacology, and Molecular Modeling of Very Potent Tacrine−Huperzine A Hybrids as Acetylcholinesterase Inhibitors of Potential Interest for the Treatment of Alzheimer's Disease (1999)

Eleven new 12-amino-6,7,10,11-tetrahydro-7, 11-methanocycloocta[b]quinoline derivatives [tacrine (THA)-huperzine A hybrids, rac-21-31] have been synthesized as racemic mixtures and tested as acetylcholinesterase (AChE) inhibitors. For derivatives unsubstituted at the benzene ring, the highest activity was obtained for the 9-ethyl derivative rac-20, previously prepared by our group. More bulky substituents at position 9 led to less active compounds, although some of them [9-isopropyl (rac-22), 9-allyl (rac-23), and 9-phenyl (rac-26)] show activities similar to that of THA. Substitution at position 1 or 3 with methyl or fluorine atoms always led to more active compounds. Among them, the highest activity was observed for the 3-fluoro-9-methyl derivative rac-28 [about 15-fold more active than THA and about 9-fold more active than (-)-huperzine A]. The activity of some THA-huperzine A hybrids (rac-19, rac-20, rac-28, and rac-30), which were separated into their enantiomers by chiral medium-pressure liquid chromatography (chiral MPLC), using microcrystalline cellulose triacetate as the chiral stationary phase, showed the eutomer to be always the levorotatory enantiomer, their activity being roughly double that of the corresponding racemic mixture, the distomer being much less active. Also, the activity of some of these compounds inhibiting butyrylcholinesterase (BChE) was tested. Most of them [rac-27-31, (-)-28, and (-)-30], which are more active than (-)-huperzine A as AChE inhibitors, turned out to be quite selective for AChE, although not so selective as (-)-huperzine A. Most of the tested compounds 19-31 proved to be much more active than THA in reversing the neuromuscular blockade induced by d-tubocurarine. Molecular modeling of the interaction of these compounds with AChE from Torpedo californica showed them to interact as truly THA-huperzine A hybrids: the 4-aminoquinoline subunit of (-)-19 occupies the same position of the corresponding subunit in THA, while its bicyclo[3.3.1]nonadiene substructure roughly occupies the same position of the corresponding substructure in (-)-huperzine A, in agreement with the absolute configurations of (-)-19 and (-)-huperzine A.
Striatal phosphoproteins in Parkinson disease and progressive supranuclear palsy. (1989)

This study was undertaken to evaluate the levels of cAMP-regulated phosphoproteins in the striatum of patients with neurodegenerative diseases of the dopaminergic system. Postmortem samples of caudate nucleus and putamen from 24 control subjects, 23 patients with Parkinson disease, and 13 patients with progressive supranuclear palsy were studied with immunoblotting techniques. The levels of tyrosine hydroxylase were reduced in patients with Parkinson disease (levels were 24% and 10% of controls in caudate nucleus and putamen, respectively) and with progressive supranuclear palsy (levels were 11% and 6% of controls in caudate nucleus and putamen, respectively). Five phosphoproteins, which are present in striatal neurons and are likely to play a role in the postsynaptic actions of dopamine, were measured. These included ARPP-16, ARPP-19, ARPP-21 (cAMP-regulated phosphoproteins of Mr 16,000, 19,000, and 21,000, respectively), DARPP-32 (dopamine- and cAMP-regulated phosphoprotein of Mr 32,000), and phosphatase inhibitor I. The levels of these phosphoproteins were inversely correlated with postmortem delay. In brains of patients with Parkinson disease or progressive supranuclear palsy with postmortem delays comparable to those of controls, the levels of these proteins as well as those of synaptic (synapsin I and synaptophysin) and glial (glial fibrillary acidic protein and myelin basic protein) markers were not significantly modified. We conclude that the levels of several phosphoproteins involved in signal transduction in striatal neurons are not altered in Parkinson disease and progressive supranuclear palsy. This observation supports the view that the striatal output neurons are intact in both diseases.
Neonatal Immunization: Response to <i>Haemophilus influenzae</i> Type b-Tetanus Toxoid Conjugate Vaccine (1995)

Neonatal immunization with PRP-T was safe and well tolerated in Finnish infants, and it would be worthwhile to further study its effects in higher risk populations.
Learning novel objects using out-of-vocabulary word segmentation and object extraction for home assistant robots (2010)

This paper presents a method for learning novel objects from audio-visual input. Objects are learned using out-of-vocabulary word segmentation and object extraction. The latter half of this paper is devoted to evaluations. We propose the use of a task adopted from the RoboCup@Home league as a standard evaluation for real world applications. We have implemented proposed method on a real humanoid robot and evaluated it through a task called “Supermarket”. The results reveal that our integrated system works well in the real application. In fact, our robot outperformed the maximum score obtained in RoboCup@Home 2009 competitions.
[Experimental study of the effect of glucosamine hydrochloride on metabolic and repair processes in connective tissue structures]. (2003)

The effects of glucosamine hydrochloride on the metabolic and repair processes were studied on a model of post-traumatic osteoarthrosis in the articular cartilage and on a model of post-traumatic keratitis in the cornea. The administration of glucosamine hydrochloride stimulated repair and favored inhibition of dystrophic post-traumatic processes in the connective-tissue structures. It is suggested that a probable mechanism of the drug action consists in stimulation of the synthesis of glucosaminoglycanes and collagen.
Voice Separation with an Unknown Number of Multiple Speakers (2020)

We present a new method for separating a mixed audio sequence, in which multiple voices speak simultaneously. The new method employs gated neural networks that are trained to separate the voices at multiple processing steps, while maintaining the speaker in each output channel fixed. A different model is trained for every number of possible speakers, and the model with the largest number of speakers is employed to select the actual number of speakers in a given sample. Our method greatly outperforms the current state of the art, which, as we show, is not competitive for more than two speakers.
Diamond Microelectrodes and CMOS Microelectronics for Wireless Transmission of Fast-Scan Cyclic Voltammetry (2007)

This paper reports on technology development at the sensor and circuit levels for wireless transmission of fast-scan cyclic voltammetry (FSCV) in neurochemical detection. Heavily conductive, boron-doped diamond is selectively deposited onto the polished tip of a tungsten microelectrode to fabricate versatile, implantable, micro-needle microprobes capable of neurochemical sensing in the brain. In addition, an integrated circuit is fabricated in a 0.5-microm CMOS technology for processing and wireless transmission of the electrochemical signals corresponding to extracellular concentration changes of various neurotransmitters. The chip consists of a current-based, second-order, front-end SigmaDelta ADC and an on-chip, RF-FSK transmitter at the back-end. The ADC core and the transmitter consume 22microA and 400microA, respectively, from a 2.6-V power supply. Major electroactive neurotransmitters such as serotonin and dopamine in micromolar concentration have been wirelessly recorded at 433MHz using 300-V/s FSCV in flow injection analysis experiments.
Regulation of vascular smooth muscle growth by cyclic nucleotides and cGMP-dependent protein kinase (2005)

The aim of this work was to elucidate the effect of cyclic nucleotide signaling on the growth of vascular smooth muscle cells (VSMCs). In particular, the role of cGKI in VSMC growth was analysed in primary and subcultured VSMCs derived from wild-type and cGKI-deficient mice. In primary VSMCs, activation of cGMP/cGKI signaling led to a strong increase in growth. In contrast, in repeatedly passaged VSMCs derived from mouse, rat and human, cGMP/cGKI had either no effect on growth or had a weak growth suppressing effect. Thus, cGKI signaling differs in primary vs. subcultured VSMCs. The further analysis of proliferation, apoptosis, cytoskeletal dynamics, and various signaling pathways indicated that an increase in integrin-mediated cell adhesion is the major mechanism for cGKI-mediated growth in primary VSMCs. Thereby, cGMP/cGKI signaling in primary VSMCs might inhibit anoikis, the programmed cell death induced by the loss of cell/matrix interactions.
Optimization and experimental validation of electrostatic adhesive geometry (2013)

This paper introduces a method to optimize the electrode geometry of electrostatic adhesives for robotic gripping, attachment, and manipulation applications. Electrostatic adhesion is achieved by applying a high voltage potential, on the order of kV, to a set of electrodes, which generates an electric field. The electric field polarizes the substrate material and creates an adhesion force. Previous attempts at creating electro-static adhesives have shown them to be effective, but researchers have made no effort to optimize the electrode configuration and geometry. We have shown that by optimizing the geometry of the electrode configuration, the electric field strength, and therefore the adhesion force, is enhanced. To accomplish this, Comsol Multiphysics was utilized to evaluate the average electric field generated by a given electrode geometry. Several electrode patterns were evaluated, including parallel conductors, concentric circles, Hilbert curves (a fractal geometry) and spirals. The arrangement of the electrodes in concentric circles with varying electrode widths proved to be the most effective. The most effective sizing was to use the smallest gap spacing allowable coupled with a variable electrode width. These results were experimentally validated on several different surfaces including drywall, wood, tile, glass, and steel. A new manufacturing process allowing for the fabrication of thin, conformal electro-static adhesive pads was utilized. By combining the optimized electrode geometry with the new fabrication process we are able to demonstrate a marked improvement of up to 500% in shear pressure when compared to previously published values.
<scp>d</scp> -Xylose as a Repressor or Inducer of Xylanase Expression in <i>Hypocrea jecorina</i> ( <i>Trichoderma reesei</i> ) (2010)

For Hypocrea jecorina (anamorph Trichoderma reesei), a filamentous fungus used for hydrolase production in different industries, it has been a long-term practice to use d-xylose as an inducing substance. We demonstrate in this study that the degree of xylanase-encoding gene induction strictly depends on the concentration of d-xylose, which was found to be optimal from 0.5 to 1 mM for 3 h of cultivation. At higher concentrations of d-xylose, a reduced level of xylanase gene expression was observed. In the present study, we also provide evidence that the d-xylose concentration-dependent induction is antagonized by carbon catabolite repressor 1. This repressor mediates its influence on d-xylose indirectly, by reducing the expression of xylanase regulator 1, the main activator of most hydrolase-encoding genes. Additionally, a direct influence of the repressor on xylanase 1 expression in the presence of d-xylose was found. Furthermore, we show that d-xylose reductase 1 is needed to metabolize d-xylose to achieve full induction of xylanase expression. Finally, a strain which expresses xylanase regulator 1 at a constant level was used to partially overcome the negative influence exerted by carbon catabolite repressor 1 on d-xylose.
Hypolipidemic effect of methanolic extract of Dolichos biflorus Linn. in high fat diet fed rats. (2005)

High fat diet fed rats showed significant increased levels of plasma and tissue total cholesterol, triglycerides, free fatty acids, phospholipids, plasma LDL cholesterol and decreased level of plasma HDL cholesterol. Methanolic extract of D. biflorus administration to high fat diet fed rats showed near to normal levels of the above lipids in plasma and tissues. Higher dose of the extract (400 mg/kg body weight) showed comparable results with standard drug atorvastatin. It is concluded that the methanolic extract of D. biflorus possesses hypolipidemic activity in high fat diet fed rats.
Bioactive Anthraquinone Derivatives from the Mangrove-Derived Fungus <i>Stemphylium</i> sp. 33231 (2014)

Four new anthraquinone derivatives (1-4) and four new alterporriol-type anthranoid dimers (14-17), along with 17 analogues, were isolated from the solid rice fermentation of the fungus Stemphylium sp. 33231 obtained from the mangrove Bruguiera sexangula var. rhynchopetala collected from the South China Sea. Their structures were elucidated using comprehensive spectroscopic methods. The absolute configurations of 1, 3, and 4 were determined by single-crystal X-ray diffraction of their derivatives (1a, 3b, and 4a). The absolute configurations of the chiral 17-19 were determined by comparing their CD spectra with 21. The inhibitory activities of most of the compounds against seven terrestrial pathogenic bacteria and two cancer cell lines were evaluated.
High-Power-Density Three-phase Interleaved Boost Converter with a Novel Coupled Inductor (2015)

Lightweight and compact high-power-density boost converters are required for many applications. This paper presents a three-phase interleaved boost converter with a novel coupled inductor that can achieve high-power-density. The novel coupled inductor is especially suitable for the three-phase interleaved boost converter, from the core structure standpoint. The electrical and magnetic characteristics of the three-phase interleaved boost converter are analyzed in detail to illustrate the effectiveness of the novel coupled inductor. Furthermore, maximum output power calculation methods for the novel coupled inductor and a non-coupled inductor are proposed to demonstrate the performance of high-power-density converters. On the basis of the calculation method, the maximum output power of the proposed coupled inductor is about 2.6 times greater than that of the non-coupled inductor under continuous current mode (CCM) conditions. The compact volume, low-weight characteristics, and the performance of the three-phase interleaved boost converter with the novel coupled inductor are discussed from both the theoretical and experimental standpoints.
ER stress affects processing of MHC class I-associated peptides (2009)

Our results demonstrate that ER stress impairs MHC I-peptide presentation, and that it differentially regulates expression of ER- vs. cytosol-derived peptides. Furthermore, this work illustrates how ER stress, a typical feature of infected and malignant cells, can impinge on cues for adaptive immune recognition.
Skin disease‐related T cells bind to endothelial selectins: expression of cutaneous lymphocyte antigen (CLA) predicts E‐selectin but not P‐selectin binding (1994)

Cutaneous lymphocyte antigen (CLA), defined by the HECA-452 antibody, is a cell surface glycoprotein found on a subset of T cells in peripheral blood that binds specifically to E-selectin. This marker is present on the majority of T cells at sites of cutaneous inflammation and immune responses. Based upon such evidence, an association between T cell CLA expression and skin homing has been proposed. To understand better this relationship, we asked whether putative disease-related, antigen-specific T cells expressed CLA. In this study, we employed T helper type 2 (TH2) T cell clones specific for house dust mite (Dermatophagoides pteronyssinus) antigens. These cells were derived from challenged skin of an individual known to react positively to epicutaneous challenge with this agent. In this study, we show that these cloned T cells showed very high homogeneous expression of CLA (nearly 500-fold higher than T cell clones derived from peripheral blood) and bound specifically to recombinant E-selectin. The CLA molecule on these cells was identified not only by HECA-452, but also by CSLEX-1, indicating that it contained sialyl-Le(x) (S-Le(x)) determinants. T cells cloned under similar conditions from peripheral blood were CLA negative or low and bound poorly to E-selectin. Surprisingly, both skin and blood clones bound comparably to P-selectin. This binding was independent of S-Le(x) or CLA expression. We conclude that in sensitized individuals, antigen-specific T cells expressing high levels of CLA localize in skin promptly after epicutaneous challenge. This localization is likely to involve the interaction of S-Le(x) determinants on the CLA molecule with E-selectin on the dermal microvasculature. We further conclude that T cells can interest with P-selectin on endothelium and that S-Le(x) does not appear to be necessary for this interaction.
A Threshold based Context Change Detection in Pervasive Environments: Application to a Smart Campus (2014)

Context awareness is an essential feature of pervasive applications and runtime detection of context changes is necessary for enabling context awareness. Context aware applications are applications that are able to adapt their behavior (self adaptivity property) according to the available resources, environmental conditions, user needs, etc. The self adaptivity property is enforced by four phases. Monitoring/Collecting context parameters, analyzing the collected context parameters to detect changes, planning appropriate adaptation actions and finally executing the planned actions to respond to the changes. In this paper, we focus and discuss the second phase (Analysis phase). Contrary to the most research activities in which the analysis phase is performed by comparing context parameters against fixed thresholds, we propose an analysis approach that uses a threshold comparison technique. Fixed as well as adaptive thresholds are applied to detect changes and trigger notifications that are used to deal with the changes.
Studies on the conformational changes in the bacterial cell wall biosynthetic enzyme UDP‐<i>N</i>‐acetylglucosamine <i>enol</i>pyruvyltransferase (MurA) (1998)

The enzyme UDP-N-acetylglucosamine (UDP-GlcNAc) enolpyruvyltransferase (MurA), the target of the antibiotic fosfomycin, was investigated by small-angle X-ray scattering (SAXS) and fluorescence spectroscopy to detect conformational changes that had been proposed on the basis of the crystal structure of unliganded and liganded MurA. The SAXS data indicate that binding of UDP-GlcNAc to free enzyme results in substantial conformational changes, which can be interpreted as the transition from an open to a closed form. Fosfomycin did not affect the structure of free enzyme or sugar-nucleotide-bound MurA. Phosphoenolpyruvate (pyruvate-P) appeared to induce a structural change upon addition to free enzyme, which differed from that observed upon binding of UDP-GlcNAc. Fluorescence experiments were performed using the hydrophobic fluorescence probe 8-anilino-1-naphthalene sulfonate (ANS). The fluorescence quenching of MurA/ANS solutions upon addition of UDP-GlcNAc or pyruvate-P was concentration dependent in a saturating manner, yielding apparent dissociation constants of K(d(UDP-GlCNAc)) = 59 microM and K(d(pyruvate-P)) = 240 microM. The results suggest that binding of substrates does not exclusively follow an ordered mechanism with UDP-GlcNAc binding first, although binding of UDP-GlcNAc to free enzyme is preferred and possibly influenced by pyruvate-P. The reaction thus appears to follow an induced-fit mechanism, in which the binding site for fosfomycin, and presumably also for pyruvate-P, is created by the interaction of free enzyme with the sugar nucleotide. The methods described here provide a tool for the characterization of site-directed mutants of MurA and the interaction of this enzyme with potential inhibitors.
Epidemiological correlates of high density lipoprotein subfractions, apolipoproteins A-I, A-II, and D, and lecithin cholesterol acyltransferase. Effects of smoking, alcohol, and adiposity. (1985)

Recent data suggest that the protection against ischemic heart disease afforded by high density lipoprotein (HDL) cholesterol (C) may be concentrated in the HDL2 subfraction. To examine the behavioral correlates of the HDL subfractions, we recalled 33 men and 17 women of a random sample from the Pacific Northwest Bell Telephone Company Health Survey. Adiposity and very low density lipoprotein (VLDL) triglyceride were negatively correlated with HDL2C. Smoking was not correlated with HDL2C, but was negatively correlated with HDL3C (men, rs = -0.635, p = 0.001; women, rs = -0.534, p = 0.014); this relationship was independent of alcohol consumption, adiposity, and VLDL triglyceride. Alcohol consumption was also more strongly related to HDL3C (men, rs = 0.248, p = 0.082; women, rs = 0.586, p = 0.007). Lecithin cholesterol acyltransferase (LCAT) mass was negatively related with HDL2C, but was positively correlated with HDL3C and apolipoprotein A-II. Smoking was negatively correlated with LCAT mass. Since it is believed that HDL3C is not associated with the risk of ischemic heart disease and since both smoking and alcohol consumption may mainly affect HDL3C, the current study suggests that the increase in risk of ischemic heart disease with smoking and the possible decrease with alcohol consumption may be mediated through mechanisms other than their effects on HDLC.
Blood cotinine levels as indicators of smoking treatment outcome (1984)

Pretreatment blood cotinine levels, expired carbon monoxide levels, and self-reported cigarette consumption were evaluated as predictors of smoking treatment outcome in 114 patients. Of these indices of nicotine intake, blood cotinine level was the most useful predictor. High blood cotinine level was the best predictor of dropping out before completion of treatment and of smoking at the end of treatment and at follow-ups. The usefulness of cotinine as a marker of tobacco dependence is discussed.
Browser Record and Replay as a Building Block for End-User Web Automation Tools (2015)

To build a programming by demonstration (PBD) web scraping tool for end users, one needs two central components: a list finder, and a record and replay tool. A list finder extracts logical tables from a webpage. A record and replay (R+R) system records a user's interactions with a webpage, and replays them programmatically. The research community has invested substantial work in list finding --- variously called wrapper induction, structured data extraction, and template detection. In contrast, researchers largely considered the browser R+R problem solved until recently, when webpage complexity and interactivity began to rise. We argue that the increase in interactivity necessitates the use of new, more robust R+R approaches, which will facilitate the PBD web tools of the future. Because robust R+R is difficult to build and understand, we argue that tool developers need an R+R layer that they can treat as a black box. We have designed an easy-to-use API that allows programmers to use and even customize R+R, without having to understand R+R internals. We have instantiated our API in Ringer, our robust R+R tool. We use the API to implement WebCombine, a PBD scraping tool. A WebCombine user demonstrates how to collect the first row of a relational dataset, and the tool collects all remaining rows. WebCombine uses the Ringer API to handle navigation between pages, enabling users to scrape from modern, interaction-heavy pages. We demonstrate WebCombine by collecting a 3,787,146 row dataset from Google Scholar that allows us to explore the relationship between researchers' years of experience and their papers' citation counts.