gebhart/patrepeval huggingface dataset:
Data from Anticancer steroid sulfatase inhibitors: synthesis of a potent fluorinated second-generation agent, <i>in vitro</i> and <i>in vivo</i> activities, molecular modeling, and protein crystallography (2023)

&lt;div&gt;Abstract&lt;p&gt;An improved steroid sulfatase inhibitor was prepared by replacing the &lt;i&gt;N&lt;/i&gt;-propyl group of the second-generation steroid-like inhibitor (&lt;b&gt;2&lt;/b&gt;) with a &lt;i&gt;N&lt;/i&gt;-3,3,3-trifluoropropyl group to give (&lt;b&gt;10&lt;/b&gt;). This compound is 5-fold more potent &lt;i&gt;in vitro&lt;/i&gt;, completely inhibits rat liver steroid sulfatase activity after a single oral dose of 0.5 mg/kg, and exhibits a significantly longer duration of inhibition over (&lt;b&gt;2&lt;/b&gt;). These biological properties are attributed to the increased lipophilicity and metabolic stability of (&lt;b&gt;10&lt;/b&gt;) rendered by its trifluoropropyl group and also the potential H-bonding between its fluorine atom(s) and Arg&lt;sup&gt;98&lt;/sup&gt; in the active site of human steroid sulfatase. Like other sulfamates, (&lt;b&gt;10&lt;/b&gt;) is expected to be sequestered, and transported by, erythrocytes &lt;i&gt;in vivo&lt;/i&gt; because it inhibits human carbonic anhydrase II (hCAII) potently (IC&lt;sub&gt;50&lt;/sub&gt;, 3 nmol/L). A congener (&lt;b&gt;4&lt;/b&gt;), which possesses a &lt;i&gt;N&lt;/i&gt;-(pyridin-3-ylmethyl) substituent, is even more active (IC&lt;sub&gt;50&lt;/sub&gt;, 0.1 nmol/L). To rationalize this, the hCAII-(&lt;b&gt;4&lt;/b&gt;) adduct, obtained by cocrystallization, reveals not only the sulfamate group and the backbone of (&lt;b&gt;4&lt;/b&gt;) interacting with the catalytic site and the associated hydrophobic pocket, respectively, but also the potential H-bonding between the &lt;i&gt;N&lt;/i&gt;-(pyridin-3-ylmethyl) group and Nε&lt;sub&gt;2&lt;/sub&gt; of Gln&lt;sup&gt;136&lt;/sup&gt;. Like (&lt;b&gt;2&lt;/b&gt;), both (&lt;b&gt;10&lt;/b&gt;) and its phenolic precursor (&lt;b&gt;9&lt;/b&gt;) are non-estrogenic using a uterine weight gain assay. In summary, a highly potent, long-acting, and nonestrogenic steroid sulfatase inhibitor was designed with hCAII inhibitory properties that should positively influence &lt;i&gt;in vivo&lt;/i&gt; behavior. Compound (&lt;b&gt;10&lt;/b&gt;) and other related inhibitors of this structural class further expand the armory of steroid sulfatase inhibitors against hormone-dependent breast cancer. [Mol Cancer Ther 2008;7(8):2435–44]&lt;/p&gt;&lt;/div&gt;
IL-32 is increased along with tryptase in lesional psoriatic skin and is up-regulated by substance P in human mast cells. (2011)

Auteur(s) : Duraisamy Kempuraj1, Pio Conti2, Magdalini Vasiadi1, Konstantinos-Dionysios Alysandratos1, Michael Tagen1, Dimitrios Kalogeromitros3, Taxiarchis Kourelis1, Stamatios Gregoriou3, Michael Makris3, Nikolaos G Stavrianeas4, Theoharis C Theoharides1,5,6,7 1Molecular Immunopharmacology and Drug Discovery Laboratory, Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, Boston, MA 02111, USA 2Immunology Division, Department of Oncology and Neuroscience, [...]
Electrical Characterization of a Corona Discharge for Surface Treatment (1975)

Electrical characterization is based on a display of voltage and charge which appears as a simple parallelogram. The area is a measure of energy input per cycle and is independent of voltage waveform but very dependent on the maximum voltage. A useful model for such corona discharges employs a Zener diode to simulate the corona drop. The buffer dielectric plays a major roll in controlling the corona power, and the air gap importance depends on the electrode system employed. Proper interpretation of the voltage-charge traces provides insight as to the corona performance and serves as a diagnostic procedure for obtaining optimum performance.
Cytokine Secretion by Stimulated Monocytes Depends on the Growth Phase and Heat Treatment of Bacteria (1999)

The consumption of food containing lactic acid bacteria (LAB) has been shown to exert immunomodulatory effects in humans. The specific cellular interaction of these bacteria with immuno-competent cells has not yet been fully understood. Since the TNF-alpha secretion of stimulated monocytes is an important initial response to a bacterial challenge, we investigated the potential of LAB originating from the human intestine or fermented food in comparison to the effect of invasive pathogens. The challenge of monocytes with three LAB strains, Listeria monocytogenes or enterohaemorrhagic Escherichia coli (EHEC) elicited a strain specific, dose-dependent biphasic TNF-alpha secretion. The concentration (EDmax) of bacteria or bacterial cell wall components necessary to induce maximal TNF-alpha secretion (TNFmax) by monocytes was mathematically approximated. It was shown for exponentially growing LAB strains that the maximal TNF-alpha secretion (TNFmax) was stronger (57 to 78%) upon stimulation with living bacteria than with heat killed cells. In contrast to log-phase bacteria, the maximal TNF-alpha secretion of monocytes (TNFmax) was higher (15 to 55%) after the stimulation with heat killed, stationary-phase bacteria when compared to that of live LAB. Thus, monocyte stimulation was clearly affected by the growth phase of bacteria. Purified cell walls of LAB strains revealed only a limited potential for monocyte stimulation. LPS exhibited a higher capacity to stimulate monocytes than purified gram positive cell walls or muramyldipeptide. In comparison to pathogenic bacteria, the maximal secretory TNF-alpha response (TNFmax) was up to 2 fold higher with LAB strains. In general, the amount of bacteria (EDmax) necessary to induce maximal TNF-alpha secretion (TNFmax) was approximately 1 to 3 log higher for heat killed bacteria when compared to live bacterial cells illustrating the significant lower potential of heat killed bacteria to activate monocytes.
Improving Stereo Sub-Pixel Accuracy for Long Range Stereo (2007)

Dense stereo algorithms are able to estimate disparities at all pixels including untextured regions. Typically these disparities are evaluated at integer disparity steps. A subsequent sub-pixel interpolation often fails to propagate smoothness constraints on a sub-pixel level. The determination of sub-pixel accurate disparities is an active field of research, however, most sub-pixel estimation algorithms focus on textured image areas in order to show their precision. We propose to increase the sub-pixel accuracy in low- textured regions in three possible ways: First, we present an analysis that shows the benefit of evaluating the disparity space at fractional disparities. Second, we introduce a new disparity smoothing algorithm that preserves depth discontinuities and enforces smoothness on a sub-pixel level. Third, we present a novel stereo constraint (gravitational constraint) that assumes sorted disparity values in vertical direction and guides global algorithms to reduce false matches, especially in low-textured regions. Our goal in this work is to obtain an accurate 3D reconstruction. Large- scale 3D reconstruction will benefit heavily from these sub- pixel refinements, especially with a multi-baseline extension. Results based on semi-global matching , obtained with the above mentioned algorithmic extensions are shown for the Middlebury stereo ground truth data sets. The presented improvements, called ImproveSubPix, turn out to be one of the top-performing algorithms when evaluating the set on a sub-pixel level while being computationally efficient. Additional results are presented for urban scenes. The three improvements are independent of the underlying type of stereo algorithm and can also be applied to sparse stereo algorithms.
Miniaturized On-Chip NFC Antenna versus Screen-Printed Antenna for the Flexible Disposable Sensor Strips (2020)

With the ongoing trend toward miniaturization via system-on-chip (SoC), both radio-frequency (RF) SoCs and on-chip multi-sensory systems are gaining significance. This paper compares the inductance of a miniaturized on-chip near field communication (NFC) antenna versus the conventional screen-printed on-substrate ones that have been used for the transfer of sensory data from a chip to a cell phone reader. Furthermore, the transferred power efficiency in a coupled NFC system is calculated for various chip coil geometries and the results are compared. The proposed NFC antenna was fabricated via a lithography process for an application-specific integrated circuit (ASIC) chip. The chip had a small area of 2.4 × 2.4 mm2, therefore a miniaturized NFC antenna was designed, whereas the screen-printed on-substrate antennas had an area of 35 × 51 mm2. This paper investigates the effects of different parameters such as conductor thickness and materials, double layering, and employing ferrite layers with different thicknesses on the performance of the on-chip antennas using full-wave simulations. The presence of a ferrite layer to increase the inductance of the antenna and mitigate the interactions with backplates has proven useful. The best performance was obtained via double-layering of the coils, which was similar to on-substrate antennas, while a size reduction of 99.68% was gained. Consequently, the coupling factors and maximum achievable power transmission efficiency of the on-chip antenna and on-substrate antenna were studied and compared.
Monitoring and verification of event-driven transportation systems in discrete manufacturing (2020)

Reliable, yet flexible operation of manufacturing systems is important for efficient and economically viable production. Model-based analysis and verification methods are becoming increasingly important to achieve such an operation. In this work, we outline a model-based approach to monitor and verify transportation systems commonly employed in discrete manufacturing. To provide guaranteed verification and monitoring results despite uncertainties and the event-driven nature of the considered transportation systems, we combine tailored first principle models with suitable set-based feasibility formulations. Simulation examples and results from an industrial test plant underline the performance and real-time capability of the presented approach.
The State of the Art in Multiple Object Tracking Under Occlusion in Video Sequences (2003)

In this paper, we present a review of existing techniques and systems for tracking multiple occluding objects using one or more cameras. Following a formulation of the occlusion problem, we divide these techniques into two groups: mergesplit (MS) approaches and straight-through (ST) approaches. Then, we consider tracking in ball game applications, with emphasis on soccer. Based on this assessment of the state of the art, we identify what appear to be the most promising approaches for tracking in general and for soccer in particular. 1.
International Conference on Advanced Nanoscience and Nanotechnology. (2019)

Join NanoTech-2020: Submit your research & get an award for the best research in Nenoscience and Nanotechnology. NanoTech-2020 offers rising researcher grants to remarkable scientists, outstanding alumni orearly academicians who have particular enthrallment in Nenoscience and Nanotechnology. The Award endeavours in giving an expert improvement open door for researchers academician, Scientist, healthcare professionals associating with partners from different parts of the world, and making systems and long haul relations. The Committee annually invites applications for the awards below on a broad range of research topics from various Scientist, Researchers, Healthcare Professionals currently registered for NanoTech-2020.
ChemInform Abstract: General Approach for the Synthesis of Ajmaline/Sarpagine Indole Alkaloids: Enantiospecific Total Synthesis of (+)‐Ajmaline (I), Alkaloid G (II), and Norsuaveoline (III) via the Asymmetric Pictet—Spengler Reaction. (1999)

Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.
A Study of Light-Sensitive Ideality Factor and Voltage-Dependent Carrier Collection of CdTe Solar Cells in Forward Bias (2013)

Two features that distinguish CdS/CdTe solar cells from traditional c-silicon cells have been widely confirmed by experiment: 1) The ideality factor of the diode current is sensitive to photon flux input, and 2) the photocurrent is voltage dependent. Here, numerical simulation of one-sided p-type CdTe junctions has been performed in order to interpret the experimental characteristics under forward bias. In these calculations, we assumed a distribution of trapping states within the CdTe bandgap. Detailed discussions have been divided into two parts: light-dependent forward current and voltage-dependent carrier collection. The former has demonstrated that recombination loss increases with increased optical generation. As a result, the diode current, in a certain forward bias region, depends on illumination. With this mechanism, the ideality factor of simulated J-V curves shows a variation consistent with experimental curves. Carrier collection loss under voltage bias is the combined result of carrier diffusion, drift, and recombination during transport. Simulations that are based on our assumption have demonstrated that collection loss increases at higher forward bias and depends on wavelength, carrier mobility, and carrier lifetime.
Construction of optimal indexes (1977)

An algorithm to design index structures for a data base is presented. This index, instead of partitioning a data base based on attribute-value pairs, effects a partition based on the nature of the user queries. A significant feature of the algorithm is that instead of working with the actual attribute values in a record, it operates on a hash vector signature representation of the records. It is shown that this reduces the space required to store the index. However, it also introduces errors due to false drops. It is shown how this error can be kept within a specified limit.
A Review of Multiple-Choice Item-Writing Guidelines for Classroom Assessment (2002)

Abstract A taxonomy of 31 multiple-choice item-writing guidelines was validated through a logical process that included two sources of evidence: the consensus achieved from reviewing what was found in 27 textbooks on educational testing and the results of 27 research studies and reviews published since 1990. This taxonomy is mainly intended for classroom assessment. Because textbooks have potential to educate teachers and future teachers, textbook writers are encouraged to consider these findings in future editions of their textbooks. This taxonomy may also have usefulness for developing test items for large-scale assessments. Finally, research on multiple-choice item writing is discussed both from substantive and methodological viewpoints.
Asymmetric 1,3-dipolar reactions of cyclic vinyl p-tolyl sulfimines with diazoalkanes (2005)

1,3-Dipolar reactions of vinyl p-tolyl sulfilimines 1 and 2 with diazoethane afforded mixtures of adducts with almost complete -facial-selectivity and a high exo/endoselectivity, under smooth conditions. The antiapproach with respect to the tolyl group, and the exoarrangement of the dipole are clearly favored on steric grounds. Reactions with diazomethane are slower and less stereoselective.
Framework for Flight Loads Analysis of Trajectory-Based Manoeuvres with Pilot Models (2014)

A framework is presented to allow the investigation of interactions between manual control and flight control systems for large flexible aircraft. It allows the fast simulation of particular flight test manoeuvres designed to expose unwanted interactions between the pilot and aircraft flight dynamics. It combines a trajectory generation scheme and an aeroelastic aircraft model together with pilot models to conduct flight loads analysis relevant to trajectory-based flight test manoeuvres. The ability of the framework to assess the impact of variations in pilot control characteristics on flight loads is illustrated through the simulation of two manoeuvres. The first required the pilot to align the aircraft from an offset position in minimum time and the second required avoiding an obstacle by following a four-dimensional trajectory. Pilot models representative of pilot control behavior were derived by applying a parameter identification scheme to data gathered through a series of manual control experiments. The pilot models were coupled with a nonlinear flexible aircraft model to demonstrate the effects on pilot–vehicle system frequency response due to changes in task and intersubject differences. Worst case wing loads were then obtained and compared to aircraft loads envelopes.
Intermolecular Cross-Linking of Na+−Ca2+ Exchanger Proteins: Evidence for Dimer Formation (2008)

The cardiac Na (+)-Ca (2+) exchanger (NCX1) is modeled to contain nine transmembrane segments (TMS) with a pair of oppositely oriented, conserved sequences called the alpha-repeats that are important in ion transport. Residue 122 in the alpha-1 repeat is in proximity to residue 768 in TMS 6, and the two residues can be cross-linked . During studies on the substrate specificity of this intramolecular cross-link, we found evidence that NCX1 can form dimers. At 37 degrees C in the absence of extracellular Na (+), copper phenanthroline catalyzes disulfide bond formation between cysteines at position 122 in adjacent NCX1 proteins. Dimerization was confirmed by histidine tag pull-down experiments that demonstrate the association of untagged NCX1 with histidine-tagged NCX1. Dimerization occurs along a face of the protein that includes parts of the alpha-1 and alpha-2 repeats as well as parts of TMS 1 and TMS 2. We do not see cross-linking between residues in TMS 5, TMS 6, or TMS 7. These data provide the first evidence for dimer formation by the Na (+)-Ca (2+) exchanger.
Large Expression Differences in Genes for Iron and Zinc Homeostasis, Stress Response, and Lignin Biosynthesis Distinguish Roots ofArabidopsis thalianaand the Related Metal HyperaccumulatorThlaspi caerulescens (2006)

The micronutrient zinc has an essential role in physiological and metabolic processes in plants as a cofactor or structural element in 300 catalytic and noncatalytic proteins, but it is very toxic when available in elevated amounts. Plants tightly regulate their internal zinc concentrations in a process called zinc homeostasis. The exceptional zinc hyperaccumulator species Thlaspi caerulescens can accumulate up to 3% of zinc, but also high amounts of nickel and cadmium, without any sign of toxicity. This should have drastic effects on the zinc homeostasis mechanism. We examined in detail the transcription profiles of roots of Arabidopsis thaliana and T. caerulescens plants grown under deficient, sufficient, and excess supply of zinc. A total of 608 zinc-responsive genes with at least a 3-fold difference in expression level were detected in A. thaliana and 352 in T. caerulescens in response to changes in zinc supply. Only 14% of these genes were also zinc responsive in A. thaliana. When comparing A. thaliana with T. caerulescens at each zinc exposure, more than 2,200 genes were significantly differentially expressed (>or=5-fold and false discovery rate < 0.05). While a large fraction of these genes are of yet unknown function, many genes with a different expression between A. thaliana and T. caerulescens appear to function in metal homeostasis, in abiotic stress response, and in lignin biosynthesis. The high expression of lignin biosynthesis genes corresponds to the deposition of lignin in the endodermis, of which there are two layers in T. caerulescens roots and only one in A. thaliana.
Destruction of Triplet Excitons in Anthracene by Injected Electrons (1966)

Received 6 December 1965DOI:https://doi.org/10.1103/PhysRevLett.16.401©1966 American Physical Society
Photoelectrochemical Deposition of CdZnSe Thin Films on the Se-Modified Au Electrode (2008)

Photoelectrochemical deposition of CdZnSe thin films on the Se-modified Au electrode using electrochemical quartz crystal microgravimetry (EQCM) and voltammetry is described. Corrosion of pre-deposited Se electrodes by illumination at a fixed potential resulted in <TEX>$Se^{2-}$</TEX> species, which was manifest from the EQCM frequency changes. <TEX>$Se^{2-}$</TEX> species generated from the photocorrosion reacted with <TEX>$Cd^{2+}$</TEX> and <TEX>$Zn^{2+}$</TEX> ions in the electrolyte to form CdZnSe films on the Au electrode. The effect of electrolyte composition on the composition and band gap of CdZnSe films was studied in detail. Also, photoelectrochemistry, EDX, Raman spectroscopy were used for the characterization of CdZnSe thin films.
Total Synthesis of an Experimental Antitubercular Drug CDRI-830 (2014)

Abstract The triarylmethane antituberculosis drug CDRI-830 is synthesized. The triarylmethane derivative 4 is prepared from ether 6 by a rearrangement process. The total synthesis of the drug CDRI-830 is achieved in a good overall yield of 35% from a simple thiophene derivative 8.
Reference Systems for Kinase Drug Discovery: Chemical Genetic Approaches to Cell-Based Assays (2004)

Protein kinases play key roles in a number of diseases, including cancer, inflammation, and diabetes. Disregulation of kinase-based signal transduction networks results in aberrant cell differentiation, activation, proliferation, and invasion. The growing importance of kinases as a major class of drug targets across multiple large clinical indications, together with the large number of kinases in the genome (~518), has generated a critical need for technologies that enable the identification of potent and selective kinase inhibitors with good drug-like properties. In this review, we describe methods used for developing cell-based assays for kinase inhibitors, discuss advantages and disadvantages of each approach, and describe new chemical genetic methods as reference systems for establishing cell-based assays and their use for functional selectivity profiling of kinase inhibitors.
Ten years of experience with the pneumococcal non-typeableHaemophilus influenzaeprotein D-conjugate vaccine (Synflorix) in children (2020)

<b>Introduction</b>: Pneumococcal diseases (including pneumonia, meningitis and sepsis) are among the leading vaccine-preventable causes of death in under-5-year-olds. Pneumococci are also one of the main bacterial pathogens associated with acute otitis media (AOM). Infant immunization programs with pneumococcal conjugate vaccines (PCVs) have led to stark reductions in pneumococcal disease rates.<b>Areas covered</b>: We summarized the development of the pneumococcal non-typeable <i>Haemophilus influenzae</i> protein D-conjugate vaccine (PHiD-CV) and evidence of its protective effect in children, since its licensure one decade ago. We highlighted the most recent data from post-licensure studies on invasive pneumococcal disease (IPD), pneumonia and AOM and from health economic evaluations. We present results from a model estimating PHiD-CV's impact on pneumococcal-related deaths.<b>Expert opinion</b>: Recent data from post-licensure studies confirm the previously demonstrated positive impact of PHiD-CV on IPD, pneumonia, AOM and AOM-related interventions (e.g., antibiotic use). Despite the success of infant PHiD-CV (and other PCV) programs, pneumococcal diseases still pose a substantial public health burden. Further reducing this burden will require improving access to currently available PCVs, increasing vaccination coverage and addressing the remaining burden due to non-vaccine serotypes. Future availability of lower-cost PCVs, PCVs with a broader serotype coverage and serotype-independent vaccines may contribute to this.