gebhart/patrepeval huggingface dataset:
Synthesis, Biotransformation, and Pharmacokinetic Studies of 9-(β-d-Arabinofuranosyl)-6-azidopurine:  A Prodrug for Ara-A Designed To Utilize the Azide Reduction Pathway (1996)

As a part of our efforts to design prodrugs for antiviral nucleosides, 9-(beta-D-arabinofuranosyl)-6-azidopurine (6-AAP) was synthesized as a prodrug for ara-A that utilizes the azide reduction biotransformation pathway. 6-AAP was synthesized from ara-A via its 6-chloro analogue 4. The bioconversion of the prodrug was investigated in vitro and in vivo, and the pharmacokinetic parameters were determined. For in vitro studies, 6-AAP was incubated in mouse serum and liver and brain homogenates. The half-lives of 6-AAP in serum and liver and brain homogenates were 3.73, 4.90, and 7.29 h, respectively. 6-AAP was metabolized primarily in the liver homogenate microsomal fraction by the reduction of the azido moiety to the amine, yielding ara-A. However, 6-AAP was found to be stable to adenosine deaminase in a separate in vitro study. The in vivo metabolism and disposition of ara-A and 6-AAP were conducted in mice. When 6-AAP was administered by either oral or intravenous route,the half-life of ara-A was 7-14 times higher than for ara-A administered intravenously. Ara-A could not be found in the brain after the intravenous administration of ara-A. However, after 6-AAP administration (by either oral or intravenous route), significant levels of ara-A were found in the brain. The results of this study demonstrate that 6-AAP is converted to ara-A, potentially increasing the half-life and the brain delivery of ara-A. Further studies to utilize the azide reduction approach on other clinically useful agents containing an amino group are in progress in our laboratories.
Exchange tab stabilized readback transducers for areal densities exceeding 20 Gb/in/sup 2/ (2001)

We present results from a high-density giant magnetoresistive magnetic recording reader using exchange bias stabilization. This novel reader design approach reduces the amount of parasitic resistance, as the sense current is not delivered through high resistivity permanent magnets. Heads were demonstrated to deliver areal densities in excess of 24 Gb/inch/sup 2/. The electrical performance of these heads, in particular, amplitude sensitivity, microtrack profiles and areal density capability are presented. Reader film properties and manufacturability of this approach are discussed in detail.
Nearly ubiquitous tissue distribution of the scrapie agent precursor protein (1992)

The "modified host protein" model of scrapie proposes that the transmissible agent is composed of the degradation-resistant protein, Sp33-37, and that clinical and pathologic signs result from neurotoxic accumulations of this protein. Sp33-37 is an abnormal, amyloidogenic isoform of the normally occurring cellular protein Cp33-37. This study investigated the tissue distribution of Cp33-37 in hamster. In brain, Cp33-37 was most concentrated in the hippocampal formation. Immunohistochemical studies localized Cp33-37 to neurons and surrounding neuropil in hippocampus; septal, caudate, and thalamic nuclei; dorsal root ganglia cells; and large-diameter dorsal root axons. In non-neuronal hamster tissues, Cp33-37 was detected in circulating leukocytes, heart, skeletal muscle, lung, intestinal tract, spleen, testis, ovary, and some other organs. The presence of Cp33-37 in extracerebral tissues indicates that its function is not unique to brain. These results indicate that the molecular substrate for the production of Sp33-37, the scrapie agent, and scrapie amyloid is present in a variety of cerebral and extracerebral sites.
Polymorphism of Tissue and Serum Amyloid A (AA and SAA) Proteins in the Mouse (1978)

Amino acid sequence studies of the amino terminal 25 residues of amyloid A (AA) protein and the serum precursor (SAA) induced with casein or LPS indicate differences in the sequence at position 6 and significant heterogeneity at several other positions in SAA. These findings suggest that SAA is a polymorphic serum protein and raise the possibility that only certain forms of SAA are processed to the tissue amyloid fibril.
Pharmacological characterization of cebranopadol a novel analgesic acting as mixed nociceptin/orphanin FQ and opioid receptor agonist (2016)

The aim of the study was to investigate the in vitro and in vivo pharmacological profile of cebranopadol, a novel agonist for opioid and nociceptin/orphanin FQ (N/OFQ) receptors (NOP). In vitro cebranopadol was assayed in calcium mobilization studies in cells coexpressing NOP or opioid receptors and chimeric G-proteins and in a bioluminescence resonance energy transfer (BRET) assay for studying receptor interaction with G-protein and <i>β</i>-arrestin 2. The mouse tail withdrawal and formalin tests were used for investigating cebranopadol antinociceptive properties. In calcium mobilization studies cebranopadol showed the following rank order of potency NOP = mu > kappa ≥ delta. In BRET studies, cebranopadol promoted NOP and mu receptors interaction with G-protein with similar high potency and efficacy. However, cebranopadol did not stimulated NOP-<i>β</i>-arrestin 2 interactions and displayed reduced potency at mu/<i>β</i>-arrestin 2. In vivo, cebranopadol exhibits highly potent and extremely long-lasting antinociceptive effects. The effects of cebranopadol in the tail withdrawal assay were sensitive to both SB-612111 and naloxone. Collectively the present results confirm and extend previous finding demonstrating that cebranopadol, by acting as mixed NOP/opioid receptor agonist, elicits robust analgesic effects in different pain models.
<title>Chromatic adaptation performance of different RGB sensors</title> (2000)

Chromatic adaptation transforms are used in imaging system to map image appearance to colorimetry under different illumination sources. In this paper, the performance of different chromatic adaptation transforms (CAT) is compared with the performance of transforms based on RGB primaries that have been investigated in relation to standard color spaces for digital still camera characterization and image interchange. The chromatic adaptation transforms studied are von Kries, Bradford, Sharp, and CMCCAT2000. The RGB primaries investigated are ROMM, ITU-R BT.709, and 'prime wavelength' RGB. The chromatic adaptation model used is a von Kries model that linearly scales post-adaptation cone response with illuminant dependent coefficients. The transforms were evaluated using 16 sets of corresponding color dat. The actual and predicted tristimulus values were converted to CIELAB, and three different error prediction metrics, (Delta) E<SUB>Lab</SUB>, (Delta) E<SUB>CIE94</SUB>, and (Delta) E<SUB>CMC(1:1</SUB>) were applied to the results. One-tail Student-t tests for matched pairs were calculated to compare if the variations in errors are statistically significant. For the given corresponding color data sets, the traditional chromatic adaptation transforms, Sharp CAT and CMCCAT2000, performed best. However, some transforms based on RGB primaries also exhibit good chromatic adaptation behavior, leading to the conclusion that white-point independent RGB spaces for image encoding can be defined. This conclusion holds only if the linear von Kries model is considered adequate to predict chromatic adaptation behavior.
A spectral system with the spatial resolution for plasma motion detection in the GOL-3 multi-mirror trap (2016)

A spectral system with the spatial resolution intended for diagnosing rotation of the plasma in the GOL-3 facility is described. The system is capable of measuring the radial dependences of the Doppler shift and broadening of spectral lines emitted by the plasma from various points in it. A DFS-24 double focusing spectrometer with a reciprocal linear dispersion of 0.45 nm/mm is the basis for the spectral system. If a radiation source is axially symmetric and extended, it is possible to obtain the intensity of spectral lines on the surface of the photosensitive area of a CCD array with the spatial resolution across the plasma by forming an image of the plasma in the sagittal focal plane of the entrance collimation lens, though the spectrometer astigmatism is strong. As a result, a spatial resolution of 0.8 mm has been attained in the developed system at a 55-mm field of view.
Development of a multi-channel waveform-sampling front-end ASIC and DOI detector for APD based animal PET (2003)

A new multi-channel waveform sampling front-end (WSFE) application specific integrated circuit (ASIC) for positron emission tomography (I5ET) has been developed to digitize signals from scintillating crystals at an early stage to suppress noise while facilitating signal processing. Each channel of the chip consists of a preamplifier, a variable gain amplifier (VGA) and a fast analog to digital converter (ADC). This multi-channel chip will be used to readout each pixel of a phoswich detector based on GSO scintillators coupled individually to a multi-array avalanche photodiode (APD). Two WSFE ASIC have been developed together with some low noise preamplifiers in a separate chip.
Ethylene dications substituted with electron-donating groups (1989)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTEthylene dications substituted with electron-donating groupsTomohiko Ohwada and Koichi ShudoCite this: J. Org. Chem. 1989, 54, 22, 5227–5237Publication Date (Print):October 1, 1989Publication History Published online1 May 2002Published inissue 1 October 1989https://doi.org/10.1021/jo00283a012RIGHTS & PERMISSIONSArticle Views699Altmetric-Citations15LEARN 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 InReddit PDF (1 MB) Get e-Alerts Get e-Alerts
Proton Transport in HTFSI–TFSI–EMI Mixtures: Experiment and Theory (2008)

We report measurements of the conductivity of a series of mixtures of ionic liquids and acids. We find in particular that mixtures of 1-ethyl-3-methylimidazolium (EMI, )–bis(trifluoromethylsulfonyl)imide [TFSI, ] with the acid H–TFSI have promising conduction properties for applications to fuel cell membranes. However, these mixtures have a peculiar dependence of conductivity on acid concentration. We present a series of model calculations at coarse-grained and molecular dynamics levels which suggest that the observed nonmonotonic dependence of conductivity on acid concentration arises because of proton clustering in the mixtures and possibly because of phase separation at the higher acid concentrations.
Toll-like receptor-2 deficiency induces schizophrenia-like behaviors in mice (2015)

Dysregulation of the immune system contributes to the pathogenesis of neuropsychiatric disorders including schizophrenia. Here, we demonstrated that toll-like receptor (TLR)-2, a family of pattern-recognition receptors, is involved in the pathogenesis of schizophrenia-like symptoms. Psychotic symptoms such as hyperlocomotion, anxiolytic-like behaviors, prepulse inhibition deficits, social withdrawal, and cognitive impairments were observed in TLR-2 knock-out (KO) mice. Ventricle enlargement, a hallmark of schizophrenia, was also observed in TLR-2 KO mouse brains. Levels of p-Akt and p-GSK-3α/β were markedly higher in the brain of TLR-2 KO than wild-type (WT) mice. Antipsychotic drugs such as haloperidol or clozapine reversed behavioral and biochemical alterations in TLR-2 KO mice. Furthermore, p-Akt and p-GSK-3α/β were decreased by treatment with a TLR-2 ligand, lipoteichoic acid, in WT mice. Thus, our data suggest that the dysregulation of the innate immune system by a TLR-2 deficiency may contribute to the development and/or pathophysiology of schizophrenia-like behaviors via Akt-GSK-3α/β signaling.
Digital Diffractive Optics: Numeric Type (2009)

This chapter contains sections titled: Computer-generated Holograms Designing CGHs Multiplexing CGHs Various CGH Functionality Implementations
Etomidate Adversely Alters Determinants of Left Ventricular Afterload in Dogs with Dilated Cardiomyopathy (1998)

The results of this investigation indicate arterial pressure is maintained during etomidate anesthesia as a consequence of increases in left ventricular (LV) afterload that further diminish LV systolic and diastolic performance in the presence of impaired LV function.
Photolithographically Patterned TiO2 Films for Electrolyte-Gated Transistors (2016)

Metal oxides constitute a class of materials whose properties cover the entire range from insulators to semiconductors to metals. Most metal oxides are abundant and accessible at moderate cost. Metal oxides are widely investigated as channel materials in transistors, including electrolyte-gated transistors, where the charge carrier density can be modulated by orders of magnitude upon application of relatively low electrical bias (2 V). Electrolyte gating offers the opportunity to envisage new applications in flexible and printed electronics as well as to improve our current understanding of fundamental processes in electronic materials, e.g. insulator/metal transitions. In this work, we employ photolithographically patterned TiO2 films as channels for electrolyte-gated transistors. TiO2 stands out for its biocompatibility and wide use in sensing, electrochromics, photovoltaics and photocatalysis. We fabricated TiO2 electrolyte-gated transistors using an original unconventional parylene-based patterning technique. By using a combination of electrochemical and charge carrier transport measurements we demonstrated that patterning improves the performance of electrolyte-gated TiO2 transistors with respect to their unpatterned counterparts. Patterned electrolyte-gated (EG) TiO2 transistors show threshold voltages of about 0.9 V, ON/OFF ratios as high as 1 × 10(5), and electron mobility above 1 cm(2)/(V s).
Discovery of Novel Allosteric Inhibitors of Deoxyhypusine Synthase (2020)

Deoxyhypusine synthase (DHPS) utilizes spermidine and NAD as cofactors to incorporate a hypusine modification into the eukaryotic translation initiation factor 5A (eIF5A). Hypusine is essential for eIF5A activation, which, in turn, plays a key role in regulating protein translation of selected mRNA that are associated with the synthesis of oncoproteins, thereby enhancing tumor cell proliferation. Therefore, inhibition of DHPS is a promising therapeutic option for the treatment of cancer. To discover novel lead compounds that target DHPS, we conducted synthetic studies with a hit obtained via high-throughput screening. Optimization of the ring structures of the amide compound (<b>2</b>) led to bromobenzothiophene (<b>11g</b>) with potent inhibitory activity against DHPS. X-ray crystallographic analysis of <b>11g</b> complexed with DHPS revealed a dramatic conformational change in DHPS, which suggests the presence of a novel allosteric site. These findings provide the basis for the development of novel therapy distinct from spermidine mimetic inhibitors.
On-Chip Active Messages for Speed, Scalability, and Efficiency (2014)

This paper describes and quantifies the benefits of adding low-overhead active messages to many-core, cache-coherent chip-multiprocessors. The active messages we analyze are user defined and trigger the atomic execution of a custom software handler at the destination. Programmers can use these active messages to both move data with less overhead than cache coherency and, more importantly, explicitly send computation to data. Doing so greatly improves (11× speed, 4.8× energy) communication idioms such as shared object modification, reductions, data walks, point-to-point communication, and all-to-all communication. Active messages enhance program scalability: applications using them run 63 percent faster with 11 percent less energy on 256 cores. The relative benefits of active messages grow with larger numbers of cores.
Limited Protection Conferred by a DNA Vaccine against a Lethal Pseudorabies Virus Infection at Day 5 Postvaccination (2007)

No pseudorabies virus (PRV)-specific neutralizing or immunoglobulin G1-type antibodies were detected in sera 5 days after injection of a DNA vaccine against PRV infection in pigs. PRV-stimulated peripheral blood mononuclear cells produced gamma interferon mRNA in vitro. Two out of five pigs recovered from lethal PRV infection without attenuation of nasal viral excretion.
Evaluation of machine learning techniques for Barret’s and dysplasia discrimination of the esophagus from in vivo optical coherence tomography images (2021)

Optical Coherence Tomography (EOCT) systems can acquire high-resolution in vivo, real-time images of the human esophagus and so, they can be an important tool for the early diagnosis and prognosis of serious esophageal diseases such as Barrett&amp;rsquo;s, dysplasia and esophageal cancer. In this study, we compare various machine learning methods for tissue segmentation and classification of esophageal tissue using in vivo OCT images. An automated algorithm is proposed able to detect normal tissue from Barrett&amp;rsquo;s Esophagus (BE) and dysplasia. The classification was based on several features extracted from each A-Scan of EOCT images. The areas of the epithelium were annotated as normal, BE or dysplasia by an expert.The results of various machine learning (ML) classifiers have shown that a neural network based approach provided the best performance, separating BE from dysplasia, for individual A-Scans, with an accuracy of 89%.
Supplementary Figure Legend from 3,5-Bis(2,4-Difluorobenzylidene)-4-piperidone, a Novel Compound That Affects Pancreatic Cancer Growth and Angiogenesis (2023)

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Dictionary‐based estimation of spectra for wide‐gamut color imaging (2011)

Abstract With the widespread use of commercialized wide‐gamut displays, the demand for wide‐gamut image content is increasing. To acquire wide‐gamut image content using camera systems, color information should be accurately reconstructed from recorded image signals for a wide range of colors. However, it is difficult to obtain color information accurately, especially for saturated colors, if conventional color cameras are used. Spectrum‐based color image reproduction can solve this problem; however, bulky spectral imaging systems are required for this purpose. To acquire spectral images more conveniently, a new spectral imaging scheme has been proposed that uses two types of data: high spatial‐resolution red, green, and blue (RGB) images and low spatial‐resolution spectral data measured from the same scene. Although this method estimates spectral images with high overall accuracy, the error becomes relatively large when multiple different colors, especially those with high saturation, are arranged in a small region. The main reason for this error is that the spectral data are utilized as low‐order spectral statistics of local spectra in this method. To solve this problem, in this study, a nonlinear estimation method based on sparse and redundant dictionaries was used for spectral image estimation—where the dictionary contains a number of spectra—without loss of information from the low spatial‐resolution spectral data. The estimated spectra are represented by a mixture of a few spectra included in the dictionary. Therefore, the respective feature of every spectrum is expected to be preserved in the estimation, and the color saturation is also preserved for any region. Experiments performed using the simulated data showed that the dictionary‐based estimation can be used to obtain saturated colors accurately, even when multiple colors are arranged in a small region. © 2011 Wiley Periodicals, Inc. Col Res Appl, 2013
Microcolumns in liquid chromatography (1981)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTMicrocolumns in liquid chromatographyMilos NovotnyCite this: Anal. Chem. 1981, 53, 12, 1294A–1308APublication Date (Print):October 1, 1981Publication History Published online21 September 2008Published inissue 1 October 1981https://pubs.acs.org/doi/10.1021/ac00235a001https://doi.org/10.1021/ac00235a001research-articleACS PublicationsRequest reuse permissionsArticle Views236Altmetric-Citations88LEARN 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
Alternating electric field capacitively coupled micro-electroporation (2014)

Electroporation of biological solutions is typically performed using galvanically coupled electrodes and the administration of high-voltage, direct current (DC) pulses.
Lipid profiling of complex biological mixtures by liquid chromatography/mass spectrometry using a novel scanning quadrupole data‐independent acquisition strategy (2017)

In particular the high specificity afforded by the scanning quadrupole improves qualitative information for lipid identification.
On estimating noncausal nonminimum phase ARMA models of non-Gaussian processes (1990)

The authors address the problem of estimating the parameters of non-Gaussian ARMA (autoregressive moving-average) processes using only the cumulants of the noisy observation. The measurement noise is allowed to be colored Gaussian or independent and identically non-Gaussian distributed. The ARMA model is not restricted to be causal or minimum phase and may even contain all-pass factors. The unique parameter estimates of both the MA and AR parts are obtained by linear equations. The structure of the proposed algorithm facilitates asymptotic performance evaluation of the parameter estimators and model order selection using cumulant statistics. The method is computationally simple and can be viewed as the least-squares solution to a quadratic model fitting of a sampled cumulant sequence. Identifiability issues are addressed. Simulations are presented to illustrate the proposed algorithm.< <ETX xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">&gt;</ETX>