gebhart/patrepeval huggingface dataset:
Metabolism-Directed Optimisation of Antithrombotics: The Prodrug Principle (2005)

Thromboembolic disorders are the major cause of mortality and morbidity in Western societies. Coagulation enzymes, such as thrombin, factor Xa and a tissue factor/factor VIIa complex, together with platelet GPIIb/IIIa receptors, are the focal point of attention in pharmaceutical research aimed at finding new antithrombotic agents. However, finding orally active drugs for these particular molecular targets has proved to be anything but straightforward. Thrombin, factor Xa, tissue factor/factor VIIa and platelet GPIIb/IIIa receptors display a preference for molecules containing highly basic arginine and/or acidic aspartate moieties, which are, however, associated with poor bioavailability after oral application. Different approaches have been taken to achieve favourable absorption, metabolism, distribution and clearance, without compromising the antithrombotic activity of the compounds. This review highlights the use of the prodrug principle in optimising antithrombotic agents.
An Anti–VEGF-B Antibody Fragment Induces Regression of Pre-Existing Blood Vessels in the Rat Cornea (2017)

The anti-VEGF-B scFv significantly regressed established but not developing corneal blood vessels in rats.
A bi-harmonic five-phase SPM machine with low ripple torque for marine propulsion (2017)

This paper addresses the design of a bi-harmonic five-phase Surface-mounted Permanent Magnet (SPM) machine for marine propulsion. The bi-harmonic characteristic results from the particular 20 slots-8 poles configuration that makes possible high value of third harmonic current injection. Thus the machine performance can be improved in terms of average torque, speed range, losses control and torque quality, this last feature being the scope of the paper. As low ripple torques are wanted at low speed, the magnet layer is defined to reduce the cogging torque and to make third harmonic current injection increasing average torque and reducing pulsating torque in the same time. According to a selection procedure based on the numerical simulations of a high number of machines, it appears that designing the rotor with two identical radially magnetized magnet that cover two-third the pole arc allows to reach this goal. Referring to an equivalent three-phase machine, the torque ripple level of the bi-harmonic five-phase machine is more than three times lower, thus being obtained with a simple control strategy that aims at achieving constant currents in the rotating frames. The time simulations of the drive confirm the significant reduction of the speed oscillation, especially at low speed.
Effect of palm oil on blood pressure, endothelial function and oxidative stress. (2005)

The pathogenesis of hypertension has been associated with endothelial dysfunction and oxidative stress. We have previously shown that palm oil (PO), with an unsaturated-to-saturated fatty acid ratio close to one and rich in antioxidants vitamins, reduces oxidative stress-induced hypertension in normal rats. Here, we investigated the cardiovascular effects of natural vitamin-rich PO using the Dahl Salt-sensitive hypertension model. Male rats were fed either a high salt (8%NaCl, HS) or low salt (0.3% NaCl, LS) diet with or without PO (Carotino, 5 g/kg daily) for four weeks. Mean arterial pressure (MAP), heart rate, blood flow and vascular resistance, vascular reactivity in vitro as well as remodelling of second-order mesenteric arteries were measured. Plasma levels of nitric oxide (NO), prostacyclin, thromboxane A(2) (TXA(2)) and isoprostane (ISO), were determined by enzyme immunoassay. Plasma, heart and kidney GSH and GSSG levels were analyzed by HPLC and aortic superoxide ((.)O(2)-) production by fluorescence spectrometry. High salt induced an elevation in MAP that was associated with decreased NO, prostacyclin and GSH: GSSG ratio. Plasma ISO and TXA(2), aortic and renal vascular resistance as well as aortic (.)O(2)- were increased. Palm oil reduced MAP, plasma TXA(2) and vascular resistance of the renal and aortic arteries, and increased the GSH: GSSG ratio and NO in the LS group. The HS-induced elevation in ISO and (.)O(2)- production and the reductions in kidney GSH: GSSG ratio, were attenuated by PO. The effect of PO was also associated with a reduced vessel wall-thickness: lumen diameter ratio and a greater relaxant effect of mesenteric arteries to acetylcholine, in the LS group. The mortality associated with HS was reduced by PO. Thus, palm oil attenuates the progression of salt-induced hypertension and mortality, via mechanisms involving modulation of endothelial function and reduction in oxidative stress.
The Tetraspanin CD53 Regulates Early B Cell Development By Promoting IL-7R Signaling (2019)

The tetraspanin CD53 has been implicated in B cell development and function. Tetraspanins are a family of transmembrane proteins important for organization of the plasma membrane and regulation of cellular migration, adhesion, and activation. CD53 has been shown to be a transcriptional target of EBF1, a critical transcription factor for early B cell development. Additional signaling for early B cell development occurs through the IL-7 receptor (IL-7R), where ligation promotes continued B cell differentiation and pro-survival/anti-apoptotic gene expression. Human deficiency of CD53 results in recurrent infections and reduced serum immunoglobulins. While prior studies have implicated a role for CD53 in regulating mature B cells, its role in early B cell development is not well understood. Herein, we show that CD53 expression rapidly increases throughout B cell development, beginning at the pre-pro-B cell stage. With a CRISPR-generated knockout mouse, we show that Cd53-/- mice have significantly reduced bone marrow (25% fewer, p&lt;0.005), splenic (35% fewer, p&lt;0.05), lymphatic (65% fewer, p&lt;0.0001), and peripheral (30% fewer, p&lt;0.005) B cells compared to wild-type (WT) littermate controls. Mirroring the human phenotype, Cd53-/- mice have significantly reduced serum IgG and IgM (40% reduced, p&lt;0.01). In addition, hematopoietic stem cells isolated from Cd53-/- mice give rise to 30% fewer B cells compared to controls in vitro (p=0.005). Analysis of bone marrow B cell development demonstrates that this loss of B cells originates with early B cell progenitors, which express nearly 50% less IL-7Ra than WT and reduced IL-7 signaling. Using mass cytometry, we identified differential signaling pathways downstream of IL-7R in B cell progenitors. Specifically, we observe impaired PI3K and STAT5 activation in pre-pro- and pro-B cells in the absence of CD53, with a consequent increase in apoptosis in these populations (p&lt;0.01). Decreased STAT5 phosphorylation was confirmed by western blot. Finally, co-immunoprecipitation studies demonstrate a physical interaction between CD53 and IL-7Ra, suggesting that these proteins associate at the cell surface. Together, these data suggest a novel role for CD53 during IL-7 signaling to promote early B cell development. Ongoing studies are focused on determining the CD53 residues required for interaction with IL-7R. Disclosures No relevant conflicts of interest to declare.
Direct mid-infrared femtosecond pulse shaping with a calomel acousto-optic programmable dispersive filter (2010)

Direct amplitude and phase shaping of mid-infrared femtosecond pulses is realized with a calomel-based acousto-optic programmable dispersive filter transparent between 0.4 and 20 μm. The shaped pulse electric field is fully characterized with high accuracy, using chirped-pulse upconversion and time-encoded arrangement spectral phase interferometry for direct electric field reconstruction techniques. Complex mid-infrared pulse shapes at a center wavelength of 4.9 μm are generated with a spectral resolution of 14 cm(-1), which exceeds by a factor of 5 the reported experimental resolutions of calomel-based filters.
Continuous operation control during electric power network faults in an adjustable speed generation system with a flywheel excited by a DC link converter (2002)

For an adjustable speed generation system with a flywheel, not only quick active power and voltage responses, but also continuous operation during electric power network faults are necessary to stabilize electric power networks. Quick active power response of 40 rad/s and voltage response of 40 rad/s are obtained in a 30 kVA test model. To realize these quick responses, a controller with multi-microprocessors is used, in which the minimum sampling time is 185 /spl mu/s. Moreover, cooperative power flow control between the rectifier and inverter is added to power, voltage and speed controls of the generator/motor. Chopper control for overvoltage suppression is added to the DC link voltage control. Continuous operation can be realized even during such electric power network faults as 1-line, 2-line and 3-line ground faults due to these controls.
A hardware spinal decoder (2012)

Spinal codes are a recently proposed capacity-achieving rateless code. While hardware encoding of spinal codes is straightforward, the design of an efficient, high-speed hardware decoder poses significant challenges. We present the first such decoder. By relaxing data dependencies inherent in the classic M-algorithm decoder, we obtain area and throughput competitive with 3GPP turbo codes as well as greatly reduced latency and complexity. The enabling architectural feature is a novel alpha-beta incremental approximate selection algorithm. We also present a method for obtaining hints which anticipate successful or failed decoding, permitting early termination and/or feedback-driven adaptation of the decoding parameters.
Cloning and expression of murine liver phosphatidylserine synthase (PSS)-2: differential regulation of phospholipid metabolism by PSS1 and PSS2 (1999)

Phosphatidylserine (PtdSer) is synthesized in mammalian cells by two base-exchange enzymes: PtdSer synthase (PSS)-1 primarily uses phosphatidylcholine as a substrate for exchange with serine, whereas PSS2 uses phosphatidylethanolamine (PtdEtn). We previously expressed murine PSS1 in McArdle hepatoma cells. The activity of PSS1 in vitro and the synthesis of PtdSer and PtdSer-derived PtdEtn were increased, whereas PtdEtn synthesis from the CDP-ethanolamine pathway was inhibited [Stone, Cui and Vance (1998) J. Biol. Chem. 273, 7293-7302]. We have now cloned and stably expressed a murine PSS2 cDNA in McArdle cells and M.9.1.1 cells [which are ethanolamine-requiring mutant Chinese hamster ovary (CHO) cells defective in PSS1]. Expression of the PSS2 in M.9.1.1 cells reversed the ethanolamine auxotrophy. However, the PtdEtn content was not normalized unless the culture medium was supplemented with ethanolamine. In both M.9.1.1 and hepatoma cells transfected with PSS2 cDNA the rate of synthesis of PtdSer and PtdSer-derived PtdEtn did not exceed that in parental CHO cells or control McArdle cells respectively, in contrast to cells expressing similar levels of murine PSS1. These observations suggest that PtdSer synthesis via murine PSS2, but not PSS1, is regulated by end-product inhibition. Moreover, expression of murine PSS2 in McArdle cells did not inhibit PtdEtn synthesis via the CDP-ethanolamine pathway, whereas expression of similar levels of PSS1 activity inhibited this pathway by approx. 50%. We conclude that murine PSS1 and PSS2, which are apparently derived from different genes, independently modulate phospholipid metabolism. In addition, mRNAs encoding the two synthases are differentially expressed in several murine tissues, supporting the idea that PSS1 and PSS2 might perform unique functions.
Evolution of activation dynamics during early stages of electrically-induced ventricular fibrillation (2002)

Previous studies suggest that the organization of epicardial activation patterns (EAP) during ventricular fibrillation (VF) changes over both time and space. To investigate whether organization of EAP changes during the first few seconds of electrically-induced VF, the authors recorded unipolar electrograms [V(t)] from 504 epicardial recording sites (21/spl times/24, 1 mm separation) during multiple runs of VF in three open-chest pigs. Activation intervals (temporal difference between local activation times defined by selecting dV/dt/sub max/ within 25 ms window) were determined at nine of the epicardial sites during 2 s segments of data taken 1, 5 and 10 s after VF induction. Activation intervals (mean/spl plusmn/SD) became longer and more regular as VF duration increased from 1-3 s (110/spl plusmn/17 ms) to 10-12 s (115/spl plusmn/15). The spatial distribution of SD over the mapped region tended to decrease over this same time period. These findings may have important implications related to therapeutic strategies which attempt to produce regional control of myocardial activation patterns during VF.
Central Mechanisms and Levodopa Response Fluctuations in Parkinsonʼs Disease (1988)

Experimental Therapeutics Branch, National Institute of Neurological and Communicative Disorders and Stroke, Bethesda, Maryland, U.S.A.
Side Population Cells Isolated from Mesenchymal Neoplasms Have Tumor Initiating Potential (2007)

Although many cancers are maintained by tumor-initiating cells, this has not been shown for mesenchymal tumors, in part due to the lack of unique surface markers that identify mesenchymal progenitors. An alternative technique to isolate stem-like cells is to isolate side population (SP) cells based on efflux of Hoechst 33342 dye. We examined 29 mesenchymal tumors ranging from benign to high-grade sarcomas and identified SP cells in all but six samples. There was a positive correlation between the percentage of SP cells and the grade of the tumor. SP cells preferentially formed tumors when grafted into immunodeficient mice, and only cells from tumors that developed from the SP cells had the ability to initiate tumor formation upon serial transplantation. Although SP cells are able to efflux rhodamine dye in addition to Hoechst 33342, we found that the ability to efflux rhodamine dye did not identify a population of cells enriched for tumor-initiating capacity. Here, we identify a subpopulation of cells within a broad range of benign and malignant mesenchymal tumors with tumor-initiating capacity. In addition, our data suggest that the proportion of SP cells could be used as a prognostic factor and that therapeutically targeting this subpopulation of cells could be used to improve patient outcome.
Scalable and Cost Efficient Resource Allocation Algorithms Using Deep Reinforcement Learning (2020)

The emergence of a new generation of applications led to the appearance of new challenges that represent improvements in current communication technologies. For this, a new network paradigm's including edge computing that allows the process of data at the edge of the network. And the 5G network slicing that represents a new generation of communication increases the capacity of mobile networks by supporting the slicing technology that allows virtual “cutting” of a telecommunications network in several slices that provide high performance in terms of bandwidth and latency. Slice allocation and placement is an important networking optimization task that still painstakingly tune heuristics to get a sufficient solution. These algorithms use data as input and outputs near-optimal solutions. Thus, we are motivated by replacing this tedious process with the recent deep reinforcement learning algorithms. In this paper, we propose three approaches for Virtual Network Functions (VNFs) slices placement in edge computing (Integer linear programming (ILP), reinforcement learning (RL), and deep reinforcement learning (DRL)). Then they are implemented and evaluated. Several scenarios are considered to study the behavior of the algorithms and to quantify the impact of network size. The results show the feasibility and efficiency of the proposed techniques in terms of server utilization, placement time, and energy consumption.
Kinetics of the decomposition of ethyl diazoacetate in aqueous acids at 0° (1961)

W. J. Albery and R. P. Bell, Trans. Faraday Soc., 1961, 57, 1942 DOI: 10.1039/TF9615701942
Functional regulation of xanthine oxidoreductase expression and localization in the mouse mammary gland: evidence of a role in lipid secretion (2002)

Xanthine oxidoreductase (XOR), a key enzyme of purine metabolism, has been implicated in the secretion of the milk fat droplet in lactating mammary epithelial cells, possibly through structural interactions with other milk fat globule proteins including butyrophilin (Btn) and adipophilin (ADPH). To help determine the mechanism by which XOR is regulated, we examined the expression and localization of XOR in the non-secretory states of late pregnancy and induced involution compared with the state of active secretion. XOR mRNA levels started to increase at mid-pregnancy, turned sharply upwards at the onset of lactation and decreased rapidly with forced involution, indicating transcriptional control of the enzyme level by differentiation and secretory function. During pregnancy and involution the enzyme was diffusely distributed in the cytoplasm, but moved rapidly to the apical membrane of the cells when secretion was activated, where it colocalized with both Btn and ADPH, similar to the situation in the milk fat globule itself. Size-exclusion chromatography of solubilized milk fat globule membrane proteins showed that XOR formed a sulphydryl-bond-dependent complex with Btn and ADPH in the milk fat globule membrane. XOR returned to a diffuse cytoplasmic localization shortly after induced involution, while Btn remained localized to the apical membrane, suggesting that localization of XOR is not dependent on the presence of Btn in the apical membrane. Our findings indicate that the expression and membrane association of XOR in the mammary gland are tightly regulated by secretory activity, and suggest that the apical membrane association of XOR regulates the coupling of lipid droplets to the apical plasma membrane during milk lipid secretion.
Cubic Equation of State for Pure Compound Vapor Pressures from the Triple Point to the Critical Point (1996)

A new procedure is proposed for obtaining the temperature dependence of the attractive energy parameter of equations of state (EOS's) . The procedure can be applied to two-parameter cubic and noncubic EOS's, and it is used for the Peng−Robinson (PR) EOS. The modified form of the PR-EOS, the ZVPR-EOS, can accurately reproduce the vapor pressure for a wide variety of pure compounds from the triple point to the critical point. The experimental information required for each pure compound is the acentric factor, the normal boiling point temperature, and the temperature and pressure coordinates at the critical and triple points. Tables of parameters and complete vapor-pressure relative-error information are provided for more than 100 compounds of industrial interest. Additionally, for the PR-EOS, Soave's noniterative calculation procedures have been extended to the low-temperature range.
Lösungsmöglichkeiten nach fehlgeschlagenen Osteosynthesen: Becken und Azetabulum (2004)

Fehlschläge nach Osteosynthesen des Beckenrings oder nach Azetabulumrekonstruktionen sind i. d. R. chirurgisch schwer zu behandeln und sollten von spezialisierten Zentren durchgeführt werden. Das Ziel der Primärversorgung der Becken- und Azetabulumver-letzungen sollte immer sein, derartige Komplikationen möglichst zu vermeiden. Da allein schon der Klassifikation, der primären Einschätzung der spezifischen Besonderheiten der Verletzung, der Zugangswahl und letztendlich der Auswahl und Ausführung der Osteosynthese eine entscheidende Bedeutung für den Erfolg der Behandlung zukommen und in allen Bereichen erhebliche Fehlermöglichkeiten vorkommen können, sollte im Einzelfall immer geprüft werden, inwieweit die persönliche Erfahrung und/oder infrastrukturellen Voraussetzungen gegeben sind, eine Definitivbehandlung außerhalb von Notfallversorgungen vorzunehmen. Es ist zu erwarten, dass im Zuge der Änderungen der Krankenhauslandschaft eine weitere Zentrierung von Becken- und Azetabulumverletzungen zu Traumazentren hin erfolgen wird.
Synthesis and properties of (O-acyl imidato)carbene complexes of chromium, molybdenum, and tungsten (1989)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTSynthesis and properties of (O-acyl imidato)carbene complexes of chromium, molybdenum, and tungstenLouis S. Hegedus, Lisa M. Schultze, and John MontgomeryCite this: Organometallics 1989, 8, 9, 2189–2195Publication Date (Print):September 1, 1989Publication History Published online1 May 2002Published inissue 1 September 1989https://pubs.acs.org/doi/10.1021/om00111a015https://doi.org/10.1021/om00111a015research-articleACS PublicationsRequest reuse permissionsArticle Views145Altmetric-Citations23LEARN 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
Experimental investigation of the impact of NZDF zero-dispersion wavelength on broadband transmission in Raman-enhanced systems (2004)

Two nonzero dispersion fibers with different zero-dispersion wavelengths (ZDW) were evaluated for C+L-band, Raman-enhanced systems. With an optimized ZDW, 80/spl times/42.7 Gb/s transmission over 800-km can be achieved without forward-error-correction or per-channel post dispersion optimization.
Azimuth and elevation estimation for multiple sound sources using two-dimensional frequency domain binaural model (2006)

Direction of arrival (DOA) estimation for multiple sound sources with only two sensors as the human being does is proposed. The frequency domain binaural model (FDBM) [Nakashima et al., Acoust. Sci. Technol. 24, 172–178 (2003)] was proposed as one binaural model. The method uses sound diffraction to estimate DOAs and segregate sound sources. The binaural model can estimate one-dimensional DOA, namely, azimuth. However, human beings can estimate not only azimuth of DOA but also elevation of that. In order to achieve an estimate of both azimuth and elevation simultaneously, a new DOA estimation algorithm based on interaural phase and level differences is proposed as a part of frequency domain binaural model. Results of DOA characteristics of the proposed binaural model estimation on multiple sound sources’ condition is compared with that of human auditory characteristics. As a result, it was confirmed that performance on accuracy of DOA estimation depends on power level ratio among sound sources. [Research was partially supported by the Ministry of Education, Science, Sports and Culture, Grant-in-Aid for Scientific Research (C), 2006, 18500135 and carried out by the Cooperative Research Project Program of the RIEC, Tohoku University (Grant No. H16.A02).]
EXTRACTION OF ESSENTIAL OILS IN THE SUPERHEATED STEAM FLUIDIZED BED (2011)

The fluidized bed extraction using superheated steam can be used for the production of volatile ingredients (essential oils) from plant materials. Depending on its properties the plant material must be pretreated. Some experimental investigations of this process and their results are presented. A simple model to describe and calculate the oil release from the plant material and the oil concentration in the steam is also represented.