gebhart/patrepeval huggingface dataset:
COX-2 inhibitors: pharmacological data and adverse effects. (2006)

The nonsteroidal anti-inflammatory drugs (NSAIDs) cover a wide range of selectivity, from the nonselective cyclooxygenase (COX) inhibitors to the preferential COX-2, and the newest coxibs, selective COX-2, with 1000-fold selectivities for COX-2. Coxibs belong to the distinct classes of sulphonamides, methylsulphones, and phenylacetic acid derivatives. The affinity of an inhibitor for COX-1 and COX-2 determinates its relative selectivity. Minor changes in the amino acid structure between the 2 enzymes results in different forms of their active sites. However, the primitive hypothesis of a dualism between an isoform totally inducible (COX-2) and the other isoform constitutive (COX-1) was not completely true. Thus, also selective COX-2 inhibitors have been shown to interact with gastrointestinal, renal, and cardiovascular systems. New insights into pharmacological data and side effect profile of coxibs have been reported in this review. They may reduce gastrointestinal-related risks, but when administered with low-dose aspirin, they could create an ulcerogenic dual-COX inhibitor. Moreover, by inhibiting COX-2, they could delay ulcer healing. Similarly to traditional NSAIDs, coxibs compromise the glomerular filtration rate in patients at increased risk, and may cause peripheral oedema and hypertension. According to the traditional ''COX-2 hypothesis'', they should not impair efficacy of coagulation. However, in combination with an oral anticoagulant they increase the International Normalized Ratio (INR) and, in some cases, cause bleeding. The altered balance between prostacyclin and thromboxane, due to selective inhibition of COX-2 without reducing COX-1, could promote a prothrombotic state and explain the observed increased cardiovascular risk. Finally, the role of COX-2 expression in the ischemic preconditioning mechanism and the recent discovery of a pro-oxidant activity of sulphones has been analysed.
ANALYSIS OF BEER CARBONYLS AT THE PART PER BILLION LEVEL BY COMBINED LIQUID CHROMATOGRAPHY AND HIGH PRESSURE LIQUID CHROMATOGRAPHY (1981)

Carbonyl compounds have been isolated from lager by low pressure distillation and recovered from the distillate as their 2,4-dinitrophenylhydrazone derivatives. The derivatives were subsequently separated into four monocarbonyl classes on a magnesia-silica gel column, and then each class resolved by HPLC. This technique has proved to be sensitive to carbonyls in lager at concentrations below 0·1 ppb and shows a high degree of resolution. So far, twelve methyl ketones, eleven saturated aldehydes and eight alkenals have been separated. The content of both fresh and aged lagers has been examined and changes in concentration discussed in relation to their reported taste thresholds.
Lung Metastasis Fails in MMTV-PyMT Oncomice Lacking S100A4 Due to a T-Cell Deficiency in Primary Tumors (2010)

Interactions between tumor and stroma cells are essential for the progression of cancer from its initial growth at a primary site to its metastasis to distant organs. The metastasis-stimulating protein S100A4 exerts its function as a stroma cell-derived factor. Genetic depletion of S100A4 significantly reduced the metastatic burden in lungs of PyMT-induced mammary tumors. In S100A4(+/+) PyMT mice, massive leukocyte infiltration at the site of the growing tumor at the stage of malignant transition was associated with increased concentration of extracellular S100A4 in the tumor microenvironment. In contrast, in S100A4(-/-) PyMT tumors, a significant suppression of T-cell infiltration was documented at the transition period. In vitro, the S100A4 protein mediated the attraction of T cells. Moreover, S100A4(+/+), but not S100A4(-/-), fibroblasts stimulated the invasion of T lymphocytes into fibroblast monolayers. In vivo, the presence of S100A4(+/+), but not S100A4(-/-), fibroblasts significantly stimulated the attraction of T lymphocytes to the site of the growing tumor. Increased levels of T cells were also observed in the premetastatic lungs of tumor-bearing mice primed to metastasize by S100A4(+/+) fibroblasts. Treatment of T cells with the S100A4 protein stimulated production of cytokines, particularly granulocyte colony-stimulating factor and eotaxin-2. The same cytokines were detected in the fluid of S100A4(+/+) PyMT tumors at the transition period. We suggest that release of S100A4 in the primary tumor stimulates infiltration of T cells and activates secretion of cytokines, thus triggering sequential events that fuel tumor cells to metastasize. Similar processes could occur in the premetastatic lungs, facilitating generation of inflammatory milieu favorable for metastasis formation.
Deep k-Nearest Neighbors: Towards Confident, Interpretable and Robust Deep Learning (2018)

Deep neural networks (DNNs) enable innovative applications of machine learning like image recognition, machine translation, or malware detection. However, deep learning is often criticized for its lack of robustness in adversarial settings (e.g., vulnerability to adversarial inputs) and general inability to rationalize its predictions. In this work, we exploit the structure of deep learning to enable new learning-based inference and decision strategies that achieve desirable properties such as robustness and interpretability. We take a first step in this direction and introduce the Deep k-Nearest Neighbors (DkNN). This hybrid classifier combines the k-nearest neighbors algorithm with representations of the data learned by each layer of the DNN: a test input is compared to its neighboring training points according to the distance that separates them in the representations. We show the labels of these neighboring points afford confidence estimates for inputs outside the model's training manifold, including on malicious inputs like adversarial examples--and therein provides protections against inputs that are outside the models understanding. This is because the nearest neighbors can be used to estimate the nonconformity of, i.e., the lack of support for, a prediction in the training data. The neighbors also constitute human-interpretable explanations of predictions. We evaluate the DkNN algorithm on several datasets, and show the confidence estimates accurately identify inputs outside the model, and that the explanations provided by nearest neighbors are intuitive and useful in understanding model failures.
Synthesis and Preliminary Pharmacology of Some 1-Methylindoles (1965)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTSynthesis and Preliminary Pharmacology of Some 1-MethylindolesRobert G. Taborsky, Peter Delvigs, Irvine H. Page, and Neville CrawfordCite this: J. Med. Chem. 1965, 8, 4, 460–466Publication Date (Print):July 1, 1965Publication History Published online1 May 2002Published inissue 1 July 1965https://pubs.acs.org/doi/10.1021/jm00328a010https://doi.org/10.1021/jm00328a010research-articleACS PublicationsRequest reuse permissionsArticle Views154Altmetric-Citations12LEARN ABOUT THESE METRICSArticle Views are the COUNTER-compliant sum of full text article downloads since November 2008 (both PDF and HTML) across all institutions and individuals. These metrics are regularly updated to reflect usage leading up to the last few days.Citations are the number of other articles citing this article, calculated by Crossref and updated daily. Find more information about Crossref citation counts.The Altmetric Attention Score is a quantitative measure of the attention that a research article has received online. Clicking on the donut icon will load a page at altmetric.com with additional details about the score and the social media presence for the given article. Find more information on the Altmetric Attention Score and how the score is calculated. Share Add toView InAdd Full Text with ReferenceAdd Description ExportRISCitationCitation and abstractCitation and referencesMore Options Share onFacebookTwitterWechatLinked InRedditEmail Other access optionsGet e-Alertsclose Get e-Alerts
Hearing aid fitting: application of telemedicine in audiology. (2003)

Telemedicine is used as a tool for therapeutic performances with the aid of telematics. The term telematics, a compound of the words telecommunication and informatics, means (in general) electronic transfer of digital data. We describe an application of telemedicine in the field of audiology: the initial fitting, setup, fine tuning, and follow-up fitting of all kinds of digital programmable and digital signal-processing devices and the fitting of hearing aids in real soundscapes. Against a backdrop of limited resources and continuous innovations, telemedicine offers the possibility of increasing the efficiency of audiological methods and decreasing expenses at the same time.
RB571, RB572, RB573, RB574, RB575, RB576, RB577 and RB578 antibodies recognize a fragment of the membrane M protein from SARS-CoV-2 by ELISA (2020)

The recombinant antibodies RB571, RB572, RB573, RB574, RB575, RB576, RB577 and RB578 detect by ELISA a synthetic peptide from the SARS-CoV-2 M protein.
Site-directed mutagenesis of recombinant human beta 2-glycoprotein I identifies a cluster of lysine residues that are critical for phospholipid binding and anti-cardiolipin antibody activity (1996)

beta2-Glycoprotein I (beta2GPI) is a phospholipid-binding serum protein with anticoagulant properties. It plays a vital role in the binding of anti-cardiolipin Abs purified from patients with autoimmune disease when assayed in a cardiolipin (CL) ELISA. Based on a three-dimensional model of beta2GPI, electrostatic calculations, and earlier peptide studies, a highly positively charged amino acid sequence, Lys282-Asn-Lys-Glu-Lys-Lys287, located in the fifth domain of beta2GPI, has been predicted to be the phospholipid binding site. We tested this hypothesis by site-directed mutagenesis of residues in the predicted phospholipid binding site and by assessing the mutants for phospholipid binding and anti-beta2GPI activity. A single amino acid change from Lys286 to Glu significantly decreased the binding of beta2GPI to CL. Double and triple mutants 2k (from Lys286, 287 to Glu286, 287), 2ka (from Lys284, 287 to Glu284, 287), and 3k (from Lys284, 286, 287 to Glu284, 286, 287) possessed no binding of Ab to beta2GPI in a CL ELISA, as well as no inhibitory activity on the binding of iodinated native beta2GPI to CL. These results indicate that the residues Lys284, Lys286, and Lys287 in the fifth domain of beta2GPI are critical for its binding to anionic phospholipids and its subsequent capture for binding of anti-beta2GPI Abs.
Minoxidil Promotes Hair Growth through Stimulation of Growth Factor Release from Adipose-Derived Stem Cells (2018)

Minoxidil directly promotes hair growth via the stimulation of dermal papilla (DP) and epithelial cells. Alternatively, there is little evidence for indirect promotion of hair growth via stimulation of adipose-derived stem cells (ASCs). We investigated whether minoxidil stimulates ASCs and if increased growth factor secretion by ASCs facilitates minoxidil-induced hair growth. Telogen-to-anagen induction was examined in mice. Cultured DP cells and vibrissae hair follicle organ cultures were used to further examine the underlying mechanisms. Subcutaneous injection of minoxidil-treated ASCs accelerated telogen-to-anagen transition in mice, and increased hair weight at day 14 post-injection. Minoxidil did not alter ASC proliferation, but increased migration and tube formation. Minoxidil also increased the secretion of growth factors from ASCs, including chemokine (C-X-C motif) ligand 1 (CXCL1), platelet-derived endothelial cell growth factor (PD-ECGF), and platelet-derived growth factor-C (PDGF-C). Minoxidil increased extracellular signal-regulated kinases 1/2 (ERK1/2) phosphorylation, and concomitant upregulation of <i>PD-ECGF</i> and <i>PDGF-C</i> mRNA levels were attenuated by an ERK inhibitor. Subcutaneous injection of CXCL1, PD-ECGF, or PDGF-C enhanced anagen induction in mice, and both CXCL1 and PDGF-C increased hair length in ex vivo organ culture. Treatment with CXCL1, PD-ECGF, or PDGF-C also increased the proliferation index in DP cells. Finally, topical application of CXCL1, PD-ECGF, or PDGF-C with 2% minoxidil enhanced anagen induction when compared to minoxidil alone. Minoxidil stimulates ASC motility and increases paracrine growth factor signaling. Minoxidil-stimulated secretion of growth factors by ASCs may enhance hair growth by promoting DP proliferation. Therefore, minoxidil can be used as an ASC preconditioning agent for hair regeneration.
Electrochemical and spectroscopic characteristics of dimethyl terephthalate (2004)

Electrochemical and spectroscopic measurements with CV, chronoamperometry and in situ spectrometry were carried out for dimethyl terephthalate, which showed vivid color change upon electrochemical stimulation, to clarify its electrochromic characteristics.
A control system for optimizing deep hole drilling conditions (2002)

An instrumentation and control system has been designed for monitoring and controlling the parameters which determine the performance of a deep hole diamond drill. Bit performance in terms of average penetration rate and life has become extremely important because time-dependent costs have become the major proportion of the total costs per meter drilled due to the deep holes encountered especially in the gold exploration drilling industry. The authors define and discuss the important parameters influencing the drill bit performance. An analysis and simulation done on an assumed model indicated that stable, well-damped, closed-loop control could be maintained over the wide range of system dynamics expected to be encountered in the system. The results obtained so far in terms of the average penetration rate are very promising compared with results obtained prior to implementing the instrumentation and control system. Preliminary results indicate average penetration rates up to 100 m for a 24-h period compared to previous rates of some 50 m for the same period.< <ETX xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">></ETX>
Graded-index AR surfaces produced by ion implantation on plastic materials (1980)

The damage tracks of high energy ions in dielectric materials can be etched until overlapping conical etch pits are obtained. If the depth of the pits is >lambda/2, an effective graded-index layer with very low reflectivity is obtained. Broadband antireflection treatment achieving reflectivities of <10(-4) has been applied to plastics like Lexan and Mylar.
Novel reagent system for converting a hydroxy-group into an iodo-group in carbohydrates with inversion of configuration (1979)

Efficient conversions of primary and secondary hydroxy-groups into iodo-groups, with inversion, in carbohydrates are described using either triphenylphosphine, iodine, and imidazole or triphenylphosphine and 2,4,5-tri-iodoimidazole in toluene at elevated temperature.
Hexalure, Pink Bollworm-<sup>1/</sup>Attractant: Masking Effect of Cis-7-Hexadecen-1-OL (1973)

Abstract Cis-7-Hexadecen-l-ol, the parent alcohol of hexalure, was found to be a powerful inhibitor of the attractant's potency. For maximum effectiveness hexalure should contain no more than 0.1% of the alcohol. A gas chromatographic procedure is described for determining the amount of the inhibitor in hexalure samples.
The optimised design and characterization of 1200 V / 2.0 m&#x2126; cm<sup>2</sup> 4H-SiC V-groove trench MOSFETs (2015)

V-groove trench MOSFETs with the 4H-SiC{0-33-8} face as the trench sidewall for the channel region have been investigated. The on-resistance and breakdown voltage strongly depend on the aperture ratio of the buried p <sup xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">+</sup> regions. The VMOSFETs with the buried p <sup xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">+</sup> regions of 71% on a 6-inch wafer exhibited a low specific on-resistance of 2.0 mΩ cm <sup xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">2</sup> with 1200 V blocking voltage. The threshold voltage is 2.3 V at 175°C, which shows the VMOSFETs have tolerability for an erroneous ignition under high temperature. The switching capability showed low switching losses over DMOSFETs on 4° off 4H-SiC(0001) face and normal operation under fast switching repetitive test (40 Vns <sup xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">-1</sup> ). The stability of the threshold voltage was demonstrated by HTGB tests.
Plasma progesterone levels following subdermal implantation of progesterone pellets in lactating women (1982)

The magnitude and duration of elevated plasma progesterone levels resulting from subdermal implantation of progesterone pellets were investigated in full nursing women. This condition was chosen because it is associated with a low rate of ovulation and minimal endogenous progesterone production. In addition, treatment with progesterone pellets was intended to be a substitute for oral or parenteral administration of synthetic progestogens to nursing mothers. A control group of full nursing women receiving no hormones provided blood samples so that basal plasma progesterone levels from the second to the sixth post-partum month could be assessed. Progesterone pellets were implanted subdermally on day 30-35 after delivery. Insertion of 2, 4 or 6 pellets each containing 100 mg of progesterone caused an initial elevation of plasma progesterone to 5.9, 9.9 and 13.5 nmol/l, respectively. This initial elevation was followed by a gradual decline, so that basal levels were attained at 70, 100 and 150 days after insertion of 2, 4 or 6 pellets. Implantation of 6 progesterone pellets led to a significant decrease in the ovulation rate of nursing women. These results indicate that subdermal implantation of 6 progesterone pellets can provide biologically effective levels of the hormone for up to 5 months.
Breaking the Barrier (2010)

In this chapter, you'll design two models. The first model you will design is a chess pawn where you will learn the techniques of modeling objects with curved surfaces for 3D printing. In the second half of the chapter, you'll switch gears and learn how to design a sundial. By designing the sundial, you will learn how to use groups, components, and shadow settings when developing and testing the model.KeywordsSection PlaneEntire ModelModeling WindowShadow SettingExtra SurfaceThese keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.
Thermal frequency drift suppression in tunable DFB lasers by plasma induced frequency shift enhancement (1994)

The authors propose enhanced-plasma-effect (EPE) lasers for coherent optical frequency division multiplexed networks. In the EPE lasers, the blue frequency shift due to the plasma effect is enhanced by incorporating a very thick p-side optical guide layer as a carrier reservoir for multiple quantum-well distributed feedback laser and it surpasses the red frequency shift due to the thermal effect. The results of demonstrating a frequency step response maintained in the blue shift region and an enhanced blue shift frequency modulation response over the whole modulation frequency range from DC are presented for the first time.< <ETX xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">></ETX>
PHARMACOKINETIC-PHARMACOGENETIC MODELLING IN THE DETECTION OF POLYMORPHISMS IN XENOBIOTIC METABOLISM<xref ref-type="fn" rid="fn1"><sup>*</sup></xref> (1990)

Study of the genetic control of xenobiotic metabolism is hindered in the areas of detecting new polymorphisms and estimating the frequency and enzyme activity of each phenotype. Using computer simulation we have looked at pharmacogenetic-pharmacokinetic models based on two alleles under Hardy-Weinberg equilibrium. The distributions of the area under the concentration-time curve (AUC) or urinary ratios were modelled and the effects of incomplete urine collections, sequential, parallel and non-linear pathways investigated. The statistical methods for the detection of bimodality in these distributions were explored. The drug/metabolite ratio, which has a good theoretical basis, was confirmed to be most sensitive and robust to changes in bioavailability, urinary excretion, hepatic blood flow and variation in non-polymorphic enzyme activity but not parallel, sequential or non-linear routes of metabolism. Graphical methods, while able to illustrate deviations from normality, were not specific in detecting bimodality and the hypothesis testing methods were found to be heavily dependent upon their assumptions.
Progress in HIV-1 Integrase Inhibitors: A Review of their Chemical Structure Diversity. (2016)

HIV-1 integrase (IN) enzyme, one of the three main enzymes of HIV-1, catalyzed the insertion of the viral DNA into the genome of host cells. Because of the lack of its homologue in human cells and its essential role in HIV-1 replication, IN inhibition represents an attractive therapeutic target for HIV-1 treatment. Since identification of IN as a promising therapeutic target, a major progress has been made, which has facilitated and led to the approval of three drugs. This review focused on the structural features of the most important IN inhibitors and categorized them structurally in 10 scaffolds. We also briefly discussed the structural and functional properties of HIV-1 IN and binding modes of IN inhibitors. The SAR analysis of the known IN inhibitors provides some useful clues to the possible future discovery of novel IN inhibitors.
C controlled trial of taurolin in established bacterial peritonitis. (1978)

Taurolin administered intraperitoneally has effected a significant reduction in morbidity in peritonitis even when all other methods of intensive care, including powerful antibiotics, have been used. Easy to use clinically, it is effective locally against all fecal pathogens and is nontoxic.
Shame and Work (2000)

Shame as an emotion has been under-explored until recently and its role in the workplace unexplored. This paper examines several major theoretical approaches to understanding shame as an emotion and how its effects are triggered in individuals Two cognitive models of shame (Lewis, 1992; Nathanson, 1992) are integrated to provide a base for understanding the shame process with application to the workplace. Based upon conjecture and personal observation, a number of potential shame triggers in the workplace are proposed, and their impact on management is explored. Finally topics for research on shame in the workplace are suggested.
Distribution and some properties of glutamine synthetase and glutamate dehydrogenase in bifidobacteria. (1987)

which are predominant in the intestinal tract of humans and some other animals, are supposed to play somerole in intestinal detoxification, prevention of senility, nutrition, resistance to infection and so on in the host.1* Wehave studied the carbohydrate metabolism of these organisms in order to obtain biochemical information on them.2~5) This paper concerns their glutamine synthetase (GS) and glutamate dehydrogenase (GDH), which play central roles in nitrogen metabolism. Bifidobacteria, kindly supplied by Dr. T. Mitsuoka of the University of Tokyo and the Institute of Physical and Chemical Research, were grown as described previously2) except that 0.02% diammoniumcitrate
Polymer in situ embedding for highly flexible, stretchable and water stable PEDOT:PSS composite conductors (2013)

Poly(3,4-ethylenedioxythiophene):poly(styrenesulfonate) and polydimethylsiloxane (PEDOT:PSS@PDMS) composite conductors have been obtained by embedding PDMS oligomers and curing agents into a 3D PEDOT:PSS aerogel. The novel 3D elastic network formed by in situ polymerization serves as a support for this brittle aerogel. The as-prepared PEDOT:PSS@PDMS conductors show highly flexible, stretchable and water stable properties.