gebhart/patrepeval huggingface dataset:
Identification and Characterization of Novel Tissue-Nonspecific Alkaline Phosphatase Inhibitors with Diverse Modes of Action (2009)

Tissue-nonspecific alkaline phosphatase (TNAP) is a ubiquitous enzyme expressed at high levels in bone, liver, and kidney. It appears involved in dephosphorylation of numerous phosphate monoesters, but only 2 of them, pyrophosphate and pyridoxal phosphate, have yet been unequivocally documented. Discovery and characterization of other substrates could be considerably facilitated if specific and potent modulators of TNAP activity with various modes of action were available. Here, the authors describe in detail a high-throughput screening campaign to identify inhibitors of TNAP, performed within the Molecular Library Screening Center Network (MLSCN). A novel homogeneous luminescent TNAP assay was developed and optimized with respect to the enzyme and substrate concentrations, enabling identification of a large number of compounds overlooked by a conventional colorimetric assay. Several new chemical series were identified from screening the Molecular Libraries Small Molecule Repository (MLSMR) collection and demonstrated to have diverse selectivity and mode of inhibition profiles. The nanomolar potency of some of these scaffolds surpasses currently known inhibitors. This article provides an example of a success where the Roadmap Initiative collaborative model, sponsored by the National Institutes of Health, brought together a deep knowledge of target biology from a principal investigator's laboratory, a well-designed compound collection from the MLSMR, and an industrial-level screening facility and staff at the MLSCN center to identify pharmacologically active compounds, with outstanding selectivity data from a panel of more than 200 publicly accessible assays, through a high-throughput screen.
Synthesis of novel energetic compounds. 8. Electrosynthesis of azidodinitromethyl compounds (1990)

Abstract Azidodinitromethyl compounds represent a new highly energetic class of propellant ingredients. Preparation of these materials was accomplished by means of electroxidative coupling of azide ions to dinitromethyl carbanions. Thus, anodic coupling of sodium azide with ethyl 4,4‐dinitrobutyrate produced ethyl 4‐azido‐4,4‐dinitrobutyrate. Similarly, 4‐azido‐4,4‐dinitrobutyl acetate was prepared from 4,4‐dinitrobutyl acetate and converted by way of the corresponding alcohol to the nitrate ester, 4‐azido‐4,4‐dinitrobutyl nitrate.
Simplified module assembly using back-contact crystalline-silicon solar cells (2002)

The authors are developing new module concepts that encapsulate and electrically connect all the crystalline-silicon (c-Si) photovoltaic (PV) cells in a module in a single step. The new assembly process: (1) uses back-contact c-Si cells; (2) uses a module backplane that has both the electrical circuit, encapsulant and backsheet in a single piece; and (3) uses a single-step process for assembly of these components into a module. This new process reduces module assembly cost by using planar processes that are easy to automate, by reducing the number of steps, and by eliminating low-throughput (e.g., individual cell tabbing, cell stringing, etc.) steps. They refer to this process as "monolithic module assembly" since it translates many of the advantages of monolithic module construction of thin-film PV modules to wafered c-Si PV modules. Preliminary development of the new module assembly process, and some estimations of the cost potential of the new process, are presented.
Osmotin Gene Expression Is Posttranscriptionally Regulated (1992)

Accumulation of both osmotin mRNA and osmotin protein in tissues of tobacco (Nicotiana tabacum L. var Wisconsin 38) is subject to complex developmental control. Osmotin was found to be most abundant in tobacco roots and in tissues of the outer stem comprised primarily of epidermis, and it was less abundant in the corolla. It was a minor protein in other tissues and was undetectable in some tissues, including those of developing and mature seeds. The mRNA abundances did not always reflect the amount of protein accumulation because in some tissues high levels of mRNA but not protein were measured and vice versa. Accumulation of osmotin mRNA but not protein occurred in some plant tissues due to treatment with abscisic acid, wounding, and tobacco mosaic virus infection. Ethylene induced the accumulation of osmotin mRNA and, to a small extent, protein in seedlings, but was ineffective with cultured cells. Exposure of cultured cells and plants to NaCl caused high levels of both mRNA and the protein to accumulate. Thus, the accumulation of osmotin mRNA is controlled developmentally and by at least five hormonal or environmental signals. However, posttranscriptional processes can limit osmotin accumulation.
Partitioning and reordering techniques for static test sequence compaction of sequential circuits (2002)

We propose a new static test set compaction method based on a careful examination of attributes of fault coverage curves. Our method is based on two key ideas: (1) fault-list and test-set partitioning, and (2) vector re-ordering. Typically, the first few vectors of a test set detect a large number of faults. The remaining vectors usually constitute a large fraction of the test set, but these vectors ore included to detect relatively few hard faults. We show that significant compaction can be achieved by partitioning faults into hard and easy faults. This significantly reduces the computational cost for static test set compaction without affecting quality of compaction. The second technique re-orders vectors in a test yet by moving sequences that detect hard faults to the beginning of the test set. Fault simulation of the newly concatenated re-ordered test set results in the omission of several vectors so that the compact test set is smaller than the original test set. Experiments on several ISCAS 89 sequential benchmark circuits and large production circuits show that our compaction procedure yields significant test set reductions in low execution times.
A tandem time‐of‐flight mass spectrometer (1992)

Abstract A tandem time‐of‐flight mass spectrometer Incorporating a fast atom bombardment source has been designed and constructed for the purpose of studying collision‐induced decomposition spectra. A deflection of the secondary ion beam is used to form the ion packets for time‐of‐flight analysis. A floating collision cell that represents a potential barrier to ions transversing the time‐of‐fiight tube enables ionic and neutral fragments from collision‐induced decomposition reactions to be separated in time from the parent ion. The instrument operating in the tandem mode is capable of performing charge exchange and collision‐induced decomposition studies of both positive and negative incident ions.
A solution to the charging problems in capacitive micromachined ultrasonic transducers (2005)

We report on a capacitive micromachined ultrasonic transducer (CMUT) featuring isolation posts (PostCMUT) as a solution to the charging problems caused by device fabrication and operation. This design improves the device reliability. The PostCMUTs were fabricated using a newly developed process based on the wafer-bonding technique. Paired tests showed the superior reliability characteristics of the PostCMUT design compared to those of conventional CMUT designs. No deleterious effect of the new design was seen in preliminary ultrasonic tests or in process yield. PostCMUTs, a design that serves as a solution to the aforementioned reliability problem, constitutes a major contribution to CMUT commercialization.
A novel Flt3‐deficient HIS mouse model with selective enhancement of human DC development (2016)

Humanized mice harboring human immune systems (HIS) represent a platform to study immune responses against pathogens and to screen vaccine candidates and novel immunotherapeutics. Innate and adaptive immune responses are suboptimal in HIS mice, possibly due to poor reconstitution of human antigen-presenting cells, including dendritic cells (DCs). DC homeostasis is regulated by cytokine availability, and Flt3-ligand (Flt3L) is one factor that conditions this process. Mouse myelopoiesis is essentially normal in most current HIS models. As such, developing mouse myeloid cells may limit human DC reconstitution by reducing available Flt3L and by cellular competition for specific "niches." To address these issues, we created a novel HIS model that compromises host myeloid cell development via deficiency in the receptor tyrosine kinase Flk2/Flt3. In Balb/c Rag2(-/-) Il2rg(-/-) Flt3(-/-) (BRGF) recipients, human conventional DCs and plasmacytoid DCs develop from hCD34(+) precursors and can be specifically boosted with exogenous Flt3L. Human DCs that develop in this context normally respond to TLR stimulation, and improved human DC homeostasis is associated with increased numbers of human NK and T cells. This new HIS-DC model should provide a means to dissect human DC differentiation and represents a novel platform to screen immune adjuvants and DC targeting therapies.
X-ray detection using the quantum-well exciton nonlinearity (1990)

Two related schemes for detecting X-rays based on (1) the scattering and (2) the reflection of a pulsed optical probe beam by carriers produced by the absorption of a single energetic X-ray photon are described. The detection method is based on the strong carrier density dependence of the (complex) index of refraction of the exciton absorption lines in a GaAs/AlGaAs multiple-quantum-well structure. These schemes can be used to construct a class of very sensitive gated X-ray detectors with micron spatial resolution and temporal resolution in the 10-30-ps regime.
Association of the Presence of Anti–Carbamylated Protein Antibodies in Early Arthritis With a Poorer Clinical and Radiologic Outcome (2017)

Our findings indicate that anti-CarP antibodies are present in one-third of patients with early arthritis and in one-fourth of the RF-negative and ACPA-negative patients. They are particularly associated with a more severe radiographic outcome. Anti-CarP antibody positivity may help to accurately identify those at risk of erosive evolution in an early arthritis population.
Fractional Talbot four-level phase-only holograms using ferroelectric liquid-crystal spatial light modulators (1994)

We propose a new technique for generating a four-level reconfigurable phase-only hologram, using two binary phase {0,pi} ferroelectric liquid-crystal spatial light modulators. The principle is based on the self-imaging properties of periodic structures operating in a Fresnel field double-diffraction system. Fractional Talbot planes are shown to be of particular interest. The problem of hologram bandwidth reduction that results from the holographic pattern replication is addressed. A trade-off between diffraction efficiency and hologram coding capacity is considered.
Fabrication of Na<sub>2</sub>FeP<sub>2</sub>O<sub>7</sub> glass-ceramics for sodium ion battery (2012)

New cathode candidate Na2FeP2O7 for rechargeable sodium ion second battery was successfully prepared by glass-ceramics method. The precursor glass, which is same composition in Na2FeP2O7, was prepared by melt-quenching method. Na2FeP2O7 was obtained by heat treatment of precursor glass powder with 10% glucose addition as reduction agent of Fe3+ at 620°C for 3 h in electric furnace. Na2FeP2O7 has triclinic P1-structure with a = 0.64061 nm, b = 0.938893 nm, c = 1.09716 nm, α = 64.5381°, β = 86.0580°, γ = 73.0619°. By means of electrochemical charge–discharge testing, Na2FeP2O7 exhibits 2.9 V, 88 mAh/g, in which is 90% for the theoretical capacity during 2.0–3.8 V cut-off voltages. Na2FeP2O7 ceramics has the potential for the safety cathode candidate for the sodium ion battery with a low materials cost.
Abstract 3806: Phosphaplatins are potent inducers of pigment epithelial- derived factor (PEDF) (2016)

Abstract Pigment Epithelial Derived Factor (PEDF) is a secreted glycoprotein that exhibits several biological activities, most notably as a potent anti-angiogenic agent as well as a neurotrophic factor. As such, this molecule has potential application as therapeutics for cancer and a variety of neurological diseases. However, prior art methods directed towards enhancing and stabilizing PEDF expression in vivo have met with little success. Therefore, methods that could lead to the stable expression of PEDF in vivo are still needed. We have recently shown that PEDF protein is overexpressed in tumor cells treated with platinum based drugs; phosphaplatins that are platinum-(II) and platinum-(IV) complexes coordinated to a pyrophosphate moiety. The objective of this study is to extend our previous findings by measuring PEDF expression in both malignant cells and normal neuronal tissues after treating them with these compounds. We also investigated the impact of PEDF upregulation on important biological processes such as apoptosis, proliferation and invasion of tumor cells. Our data showed that there was a significant upregulation (over 4-fold) of PEDF in brain of mice treated with phosphoplatins when compared to the control animals. The compounds were found to stimulate PEDF expression in cultured neuronal cells when assessed in vitro (P&lt;0.05 vs. untreated control groups). In tumor cells, phosphoplatins upregulated PEDF expression in a dose-dependent manner in various tumor cell lines. In one particular mouse breast tumor cell line (4T1), the data showed that phosphaplatin doses in the range of 25 to 100 μM stimulated the expression of PEDF at 12 and 24 hrs, which declined thereafter. Remarkably, a subsequent treatment of the tumor cells with phosphaplatins at 24 hrs prevented the decline of PEDF expression, suggesting a direct correlation between phosphaplatins and PEDF overexpression. The upregulation of PEDF in the tumor cells was paralleled by increased apoptosis and decreased cell proliferation and invasion. In summary, phosphaplatins mediated overexpression of PEDF in vivo suggests a potential neuroprotective effect of these compounds. While in tumors, phosphaplatins may exhibit antitumor activity via multiple effects, including anti-angiogenesis, enhanced apoptosis, and decreased proliferation and invasion, predominately through stimulating overexpression of PEDF. Citation Format: Louiza Belkacemi, Armando Rivera, Lu Yang, Rathindra N. Bose, Shaun X. Zhang. Phosphaplatins are potent inducers of pigment epithelial- derived factor (PEDF). [abstract]. In: Proceedings of the 107th Annual Meeting of the American Association for Cancer Research; 2016 Apr 16-20; New Orleans, LA. Philadelphia (PA): AACR; Cancer Res 2016;76(14 Suppl):Abstract nr 3806.
ICI 56,780 Optimization: Structure–Activity Relationship Studies of 7-(2-Phenoxyethoxy)-4(1<i>H</i>)-quinolones with Antimalarial Activity (2016)

Though malaria mortality rates are down 48% globally since 2000, reported occurrences of resistance against current therapeutics threaten to reverse that progress. Recently, antimalarials that were once considered unsuitable therapeutic agents have been revisited to improve physicochemical properties and efficacy required for selection as a drug candidate. One such compound is 4(1H)-quinolone ICI 56,780, which is known to be a causal prophylactic that also displays blood schizonticidal activity against P. berghei. Rapid induction of parasite resistance, however, stalled its further development. We have completed a full structure-activity relationship study on 4(1H)-quinolones, focusing on the reduction of cross-resistance with atovaquone for activity against the clinical isolates W2 and TM90-C2B, as well as the improvement of microsomal stability. These studies revealed several frontrunner compounds with superb in vivo antimalarial activity. The best compounds were found to be curative with all mice surviving a Plasmodium berghei infection after 30 days.
Partial-profilogram reconstruction method to measure the geometric parameters of wheels in dynamic condition (2016)

The present work poses a method for the measurement of geometric parameters of rail wheels in a dynamic condition, by reconstructing the profilogram from a portion of the wheel surface wear with artificial vision. The suggested procedure can work with a two-dimensional laser displacement transducer or by processing a sole image from a single camera with a structured light source. These two procedures require fewer devices and simpler implementation processes and allow the use of mathematical algorithms that demand less information processing, thus generating more accurate results. Railway operators may implement this method to perform predictive maintenance to their rolling stock at a fraction of the regular cost; thus achieving better precision, availability, maintenance performance and improving safety. Results were compared to those given by commercial equipment, showing similar precision but a better cost-benefit relation.
1,2,3‐thiadiazoles. I. Synthesis of sodium (or potassium) 1,2,3‐thiadiazole‐4‐thiolates <i>via</i> thiocarbazonate esters and <i>N</i>‐acylthiohydrazonate esters (1988)

Abstract A general synthesis of 1,2,3‐thiadiazole‐4‐thiolates 1 and their derivatives 2–3 by an extension of the Hurd‐Mori 1,2,3‐thiadiazole synthesis is described. Treatment of methyl (or ethyl) [1‐(alkylthio)alkylidene]hydrazinocarboxylates 11 (thiocarbazonate esters) or other N ‐acylthiohydrazonate esters [Y = ureido ( 12 ) or arenesulfonyl ( 13 )] with thionyl chloride affords 2–3 efficiently. Intermediates 11–13 are readily obtained from the N 2 ‐thioacylcarbazates 8 , N 3 ‐thioacylsemicarbazides 9 , or N 2 ‐thioacyl‐ N 1 ‐( p ‐toluenesulfonyl)hydrazides 10 , respectively, by S ‐alkylation. Physicochemical properties of the 1,2,3‐thiadiazoles 1–3 and N ‐acylthiohydrazonate esters 11–13 are also described.
Pickup carriage transporting mechanism for a disk record player and method for manufacturing the same (1985)

Views Icon Views Article contents Figures & tables Video Audio Supplementary Data Peer Review Share Icon Share Twitter Facebook Reddit LinkedIn Tools Icon Tools Reprints and Permissions Cite Icon Cite Search Site Citation Tatsuya Miki, Takashi Saito, Tooru Kishi; Pickup carriage transporting mechanism for a disk record player and method for manufacturing the same. J. Acoust. Soc. Am. 1 July 1985; 78 (1): 287. https://doi.org/10.1121/1.392478 Download citation file: Ris (Zotero) Reference Manager EasyBib Bookends Mendeley Papers EndNote RefWorks BibTex toolbar search Search Dropdown Menu toolbar search search input Search input auto suggest filter your search All ContentAcoustical Society of AmericaThe Journal of the Acoustical Society of America Search Advanced Search |Citation Search
Runtime Detection of a Bandwidth Denial Attack from a Rogue Network-on-Chip (2015)

In this paper, we propose a covert threat model for MPSoCs designed using 3rd party Network-on-Chips (NoC). We illustrate that a malicious NoC can disrupt the availability of on-chip resources, thereby causing large performance bottlenecks for the software running on the MPSoC platform. We then propose a runtime latency auditor that enables an MPSoC integrator to monitor the trustworthiness of the deployed NoC throughout the chip lifetime. For the proposed technique, our comprehensive cross-layer analysis indicates modest overheads of 12.73% in area, 9.844% in power and 5.4% in terms of network latency.
Efficient compression and handling of current source model library waveforms (2009)

This paper describes a waveform compression technique suitable for the efficient utilization, storage and interchange of the emerging current source model (CSM) based cell libraries. The technique is based on pre-processing of a collection of voltage/current waveforms for the cells in the library and then, constructing an orthogonal time-voltage/time-current waveform basis using singular-value decomposition. Compression is achieved by representing all waveforms as linear combination coefficients of adaptive subset of the basis waveforms. Experimental results indicate that adaptive waveform representation results in higher compression ratios than the waveform representation as a function of fixed set of basis functions. Interpolation and further compression are obtained by representing the coefficients as simple functions of various parameters, e.g., input slew, load capacitance, supply voltage, and temperature. The methods introduced in this paper are tested and validated on several industrial strength libraries, with spectacular compression results.
Strain-mediated all-magnetoelectric memory cell (2018)

Downscaling of magnetoelectric random access memory device (MELRAM) is considered by studying an example of the hybrid structure based on ferroelectric-magnetostrictive metal. Elastic mechanism of magnetoelectric interaction is analyzed by numerical modeling taking into account inhomogeneous distribution of anisotropic strain, ferroelectric polarization and electric field. The proposed shape of the cell allows to decrease the inhomogeneity of the strain in the magnetic subsystem and to achieve remarkable dynamic characteristics for a nanometric device sized 50×50×400 nm3: we adopted an input voltage of V0 = 90 mV and obtained a switching time tS = 1.1 ns, an output readout voltage VME = 4.7 mV, and an ultra-low energy consumption 13 aJ/bit.
Accurate, Noninvasive Detection of <i>Helicobacter pylori</i> DNA from Stool Samples: Potential Usefulness for Monitoring Treatment (2002)

A novel DNA assay demonstrating sensitive and accurate detection of Helicobacter pylori from stool samples is reported. Moreover, in three individuals tested for therapeutic response, the assay showed the disappearance of H. pylori DNA during treatment. Thus, this noninvasive molecular biology-based assay has the potential to be a powerful diagnostic tool given its ability to specifically identify H. pylori DNA.
Development of a Recombinant Nucleoprotein-Based Enzyme-Linked Immunosorbent Assay for Quantification of Antibodies against Porcine Reproductive and Respiratory Syndrome Virus (2000)

A rapid, inexpensive enzyme-linked immunosorbent assay (ELISA) to quantitate antibodies to porcine respiratory and reproductive syndrome virus (PRRSV) in serum was developed using a recombinant PRRSV nucleoprotein (rN). The sensitivity (85.3%) and specificity (81.7%) of the Kansas State University ELISA were good, correlating well (82.4%) with the IDEXX HerdChek ELISA.
N<sup>α</sup>‐acetyltransferase deficiency alters protein synthesis in <i>Saccharomyces cerevisiae</i> (1989)

Acetylation is the most frequently occurring chemical modification of the alpha-NH2 group of eukaryotic proteins and is catalyzed by a N alpha-acetyltransferase. Two-dimensional gel electrophoresis was used to compare the soluble proteins synthesized in wild type and a mutant (aaa1) yeast cells lacking N alpha-acetyltransferase. Among 855 soluble proteins identified in wild type and mutant, approximately 20% of the proteins in the mutant either disappeared or were shifted to higher pI without a change of molecular mass, and 27 proteins were observed only in the mutant. In addition, the synthesis of another 12% of the proteins in the mutant was either diminished or enhanced, suggesting that the acetylation of certain regulatory proteins may affect their expression. This is the first demonstration of the broad-based functional role of N alpha-acetylation in eukaryotic protein synthesis.