gebhart/patrepeval huggingface dataset:
Preclinical pharmacology and pharmacokinetics of CERC‐301, a GluN2B‐selective<i>N</i>‐methyl‐D‐aspartate receptor antagonist (2015)

The preclinical pharmacodynamic and pharmacokinetic properties of 4-methylbenzyl (3S, 4R)-3-fluoro-4-[(Pyrimidin-2-ylamino) methyl] piperidine-1-carboxylate (CERC-301), an orally bioavailable selective N-methyl-D-aspartate (NMDA) receptor subunit 2B (GluN2B) antagonist, were characterized to develop a translational approach based on receptor occupancy (RO) to guide CERC-301 dose selection in clinical trials of major depressive disorder. CERC-301 demonstrated high-binding affinity (K i, 8.1 nmol L(-1)) specific to GluN2B with an IC 50 of 3.6 nmol L(-1) and no off-target activity. CERC-301 efficacy was demonstrated in the forced swim test with an efficacy dose (ED 50) of 0.3-0.7 mg kg(-1) (RO, 30-50%); increase in locomotor activity was observed at ED 50 of 2 mg kg(-1), corresponding to an RO of 75%. The predicted 50% RO concentration (Occ50) in humans was 400 nmol L(-1), similar to that predicted for rat, dog, and monkey (300, 200, and 400 nmol L(-1), respectively). Safety pharmacology and neurotoxicity studies raised no specific safety concerns. A first-in-human study in healthy males demonstrated a dose-proportional pharmacokinetic profile, with T max of ~1 h and t 1/2 of 12-17 h. Based on the preclinical and pharmacodynamic data, doses of ≥8 mg in humans are hypothesized to have an acceptable safety profile and result in clinically relevant peak plasma exposure.
Cloning and DNA sequencing of xyaA, a gene encoding an endo-beta-1,4-xylanase from an alkalophilic Bacillus strain (N137) (1995)

The gene xyaA encoding an alkaline endo-beta 1,4-xylanase from an alkalophilic Bacillus sp. strain (N137) isolated in our laboratory was cloned and expressed in Escherichia coli. The nucleotide sequence of a 1,656-bp DNA fragment containing xyaA was determined, revealing one open reading frame of 993 bp that encodes a xylanase (XyaA) of 39 kDa. This xylanase lacks a typical putative signal peptide, yet the protein is found in the Bacillus culture supernatant. In Escherichia coli, the active protein is located mainly in the periplasmic space. The xylanase activity of the cloned XyaA is an endo-acting enzyme that shows optimal activity at pH 8 and 40 degrees C. This activity is stable at a pH between 6 and 11. Incubations of XyaA at 40 degrees C for 1 h destroyed 45% of the activity.
Postmastectomy Lymphedema (2006)

LN transplantation is a safe procedure permitting good long-term results, disappearance, or a noteworthy improvement, in postmastectomy lymphedema, especially in the early stages of the disease.
Timing Fracture Repair in Patients with Severe Brain Injury (Glasgow Coma Scale Score <9) (1998)

Operation in similar patients should be done when risks are minimized by adequate resuscitation. Secondary brain injury is more common in early femur repair. Operation delay of 24 hours may be necessary to prevent hypoxia, hypotension, and low cerebral perfusion pressure.
Stimulus-secretion coupling in pancreatic β cells (1994)

Insulin secretion is triggered by a rise in the intracellular Ca2+ concentration that results from the activation of voltage-gated Ca2+ channels in the beta-cell plasma membrane. Multiple types of beta-cell Ca2+ channel have been identified in both electrophysiological and molecular biological studies, but it appears that the L-type Ca2+ channel plays a dominant role in regulating Ca2+ influx. Activity of this channel is potentiated by protein kinases A and C and is inhibited by GTP-binding proteins, which may mediate the effects of potentiators and inhibitors of insulin secretion on Ca2+ influx, respectively. The mechanisms by which elevation of intracellular Ca2+ leads to the release of insulin granules is not fully understood but appears to involve activation of Ca2+/calmodulin-dependent protein kinase. Phosphorylation by either protein kinase A or C, probably at different substrates, potentiates insulin secretion by acting at some late stage in the secretory process. There is also evidence that small GTP-binding proteins are involved in regulating exocytosis in beta cells. The identification and characterisation of the proteins involved in exocytosis in beta cells and clarification of the mechanism(s) of action of Ca2+ is clearly an important goal for the future.
Whole genome analyses of African G2, G8, G9, and G12 rotavirus strains using sequence‐independent amplification and 454® pyrosequencing (2011)

High mortality rates caused by rotaviruses are associated with several strains such as G2, G8, G9, and G12 rotaviruses. Rotaviruses with G9 and G12 genotypes emerged worldwide in the past two decades. G2 and G8 rotaviruses are however also characterized frequently across Africa. To understand the genetic constellation of African G2, G8, G9, and G12 rotavirus strains and their possible origin, sequence-independent cDNA synthesis, amplification, and 454(®) pyrosequencing of the whole genomes of five human African rotavirus strains were performed. RotaC and phylogenetic analysis were used to assign and confirm the genotypes of the strains. Strains RVA/Human-wt/MWI/1473/2001/G8P[4], RVA/Human-wt/ZAF/3203WC/2009/G2P[4], RVA/Human-wt/ZAF/3133WC/2009/G12P[4], RVA/Human-wt/ZAF/3176WC/2009/G12P[6], and RVA/Human-wt/ZAF/GR10924/1999/G9P[6] were assigned G8-P[4]-I2-R2-C2-M2-A2-N2-T2-E2-H2, G2-P[4]-I2-R2-C2-M2-A2-N2-T2-E2-H2, G12-P[4]-I1-R1-C1-M1-A1-N1-T1-E1-H1, G12-P[6]-I1-R1-C1-M1-A1-N1-T1-E1-H1, and G9-P[6]-I2-R2-C2-M2-A2-N2-T2-E2-H2 genotypes, respectively. The detection of both Wa- and DS-1-like genotypes in strain RVA/Human-wt/ZAF/3133WC/2009/G12P[4] and Wa-like, DS-1-like and P[6] genotypes in strain RVA/Human-wt/ZAF/GR10924/1999/G9P[6] implies that these two strains were generated through intergenogroup genome reassortment. The close similarity of the genome segments of strain RVA/Human-wt/MWI/1473/2001/G8P[4] to artiodactyl-like, human-bovine reassortant strains and human rotavirus strains suggests that it originated from or shares a common origin with bovine strains. It is therefore possible that this strain might have emerged through interspecies genome reassortment between human and artiodactyl rotaviruses. This study illustrates the swift characterization of all the 11 rotavirus genome segments by using a single set of universal primers for cDNA synthesis followed by 454(®) pyrosequencing and RotaC analysis.
Enantioselective Total Synthesis of (–)‐Siphonodictyal B and (+)‐8‐<i>epi</i>‐Siphonodictyal B with Phosphatidylinositol 3‐Kinase α (PI3Kα) Inhibitory Activity (2016)

The biologically interesting marine meroterpenoids (–)‐siphonodictyal B and (+)‐8‐ epi ‐siphonodictyal B were efficiently synthesized in 29–40 % overall yield in a longest linear sequence of 11 steps, starting from commercially available (+)‐sclareolide. The synthesis involved the following crucial steps: (i) stereodivergent hydrogenation of a homoallylic decalin alcohol to install the requisite C8 stereogenic centre present in the decalin fragments; (ii) coupling of the decalin fragments with an aromatic moiety to assemble the desired carbon skeletons; and (iii) deprotection from multiple O ‐protective groups on the aromatic ring to complete the project synthesis. Both (–)‐siphonodictyal B and (+)‐8‐ epi ‐siphonodictyal B showed PI3Kα inhibitory activity, with potencies comparable to that of liphagal, a naturally occurring PI3Kα inhibitor. New structure–activity relationships for this class of marine meroterpenoids were also revealed.
An architecture for query processing in persistent object stores (1992)

Query optimizers for persistent object systems should be extensible to react to user-supplied abstract types. Current architectures support only a single, non-extensible technique for controlling the optimization process. The authors propose an alternative to the current extensible architectures that will support multiple optimizer control strategies and the addition of new control strategies. The optimizer consists of a collection of optimization regions, each of which can transform queries according to a particular control strategy, set of transformations and cost model. A global optimizer control coordinates the movement of a query between these regions. This architecture provides extensibility in the optimizer's repertoire of control strategies through the addition of new regions. The authors describe their approach and demonstrate its utility by following the optimizer as it works on an example query. The optimizer will move the query between three distinct regions. The different regions illustrate different kinds of transformations and different strategies for application of those transformations.< <ETX xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">></ETX>
Design and implementation of an end-to-end architecture for 3.5 GHz shared spectrum (2015)

The paradigm of shared spectrum that allows spectrum bands that are underutilized by primary owners to be exploited opportunistically by secondary devices has been a subject of intense research in recent years. The 2008 FCC rule-making allowing unlicensed use of underutilized DTV white space represented the first step in that direction and elicited similar efforts in other countries. The 2012 PCAST report [5] in the U.S. pushed this new trend further by advocating shared use of 1000 MHz of federal government spectrum with commercial systems and set the goal to release 500 MHz of spectrum by 2022. As a first step towards this goal, the FCC targeted 3550-3700 MHz band used primarily by naval radars and fixed satellite station for release. As of writing of this paper, the FCC has announced the first set of rules for this band to enable deployment of low-powered network technologies like small cells. The proposed rules require a Spectrum Access System (SAS), akin to a TV Database (TVDB) to implement an innovative three-tiered spectrum management system - dynamic incumbents in the top tier, Priority Access License (PAL) users in the second tier and Generalized Authorized Access (GAA) users in the third tier. Realizing this vision requires a new end-to-end architecture, component protocols and novel radio systems. Our paper represents a step in this direction. Specifically, we present our candidate architecture and its end-to-end implementation that includes a scalable SAS to activate dynamic exclusion zones for incumbent protection, manage primary/secondary devices and dynamically assign spectrum. We present a new protocol Protocol for Tiered Access to Shared Spectrum (PTASS) for transactions between network entities in the architecture. We also describe in detail our prototype end-to-end 3.5 GHz LTE/Wi-Fi testbed. To the best of our knowledge, this is the first paper about the 3.5 GHz shared spectrum access system and the first end-to-end trial of a live 3.5 GHz wireless communications in practice.
Conformational behaviour of medium-sized rings. Part 12. Tri-3-methyltrianthranilide (1982)

The stepwise synthesis of the N,N′-di- and N,N′,N″-tri-substituted tri-3-methyltrianthranilides (13)–(19) are described. The amino-acid derivatives (34), (38), and (45), which are the key acyclic precursors in the synthesis of the tri-3-methyltrianthranilides, were all prepared from 2-amino-m-toluic acid (22) and 2-nitro-m-toluoyl chloride as starting materials.Tri-3-methyltrianthranilide derivatives with three equivalent N,N′,N″-substituents can exist in either propeller or helical conformations. The N,N′,N″-trimethyl derivative (14) adopts enantiomeric helical conformations in solution and the barrier to ring inversion is 26.8 kcal mol–1. The N,N′,N″-tribenzyl derivative (19) populates both propeller and helical conformations in solution: these two conformational diastereoisomers have been separated by chromatography and isolated as crystalline compounds.Tri-3-methyltrianthranilide derivatives with two or three non-equivalent N,N′,N″-substituents can, in principle, exist in either propeller or three different helical conformations. One of these three helical conformations is specifically populated in deuteriochloroform solution by compounds (13) and (15)–(17). The N,N′-dibenzyl derivative (18) populates the propeller and one helical conformation in solution: two conformational diastereoisomers have been isolated, one as an oil and the other as a crystalline compound.The N,N′-dimethyl-N″-benzyl derivative (15) undergoes spontaneous resolution when it crystallises as a 1 : 1 adduct from toluene. The N-methyl-N′-benzyl derivative (16) also forms a 1 : 1 inclusion compound on crystallisation from toluene. Although this derivative exists as only one conformational diastereoisomer of the helical type in deuteriochloroform solution, two different diastereoisomeric conformations undergo equilibration in hexadeuteriodimethyl sulphoxide with a barrier to interconversion of 16.1 kcal mol–1.
Renin–Angiotensin–Aldosterone System Inhibitors in Patients with Covid-19 (2020)

RAAS Inhibitors in Patients with Covid-19 The effects of renin–angiotensin–aldosterone system blockers on angiotensin-converting enzyme 2 levels and activity in humans are uncertain. The authors hy...
Design and Fabrication of 2D Phononic Crystals in Surface Acoustic wave Micro Devices (2006)

In this paper, we present the design and fabrication of innovative phononic crystals integrated with two sets of interdigital (IDT) electrodes for frequency band selection of surface acoustic waves (SAW). The potential applications of this device include performance improvement of SAW micro-sensors, front-end components in RF circuitries, and directional receptions of high frequency acoustic waves. Analogous to the band-gap generated by photonic crystals, the phononic crystals, two dimensional repetitive structures composed of two different elastic materials, can prohibit the propagation of elastic waves with either specific incident angles or certain bandwidth. In this paper, the prohibited bandwidth has been verified by fabricating the phononic crystals between a micromachined SAW resonator and a receiver. Both the resonator and receiver are composed of IDT electrodes deposited and patterned on a thin piezoelectric layer. To confine the prohibited bandwidth on the order of hundred MHz, the diameter of the circular pores in phononic crystals is designed to be 6 micron and the aspect ratio of each pore is 3:1. To maximize the power transduction from IDT electrodes to SAW, the spacing between two inter-digits is one-fourth the wavelength of SAW. Specifically, the spacing ranges from 3.4 microns to 9.0 microns, depending on the central frequency. Both surface and bulk micromachining are employed and integrated to fabricate the crystals as well as SAW resonator and receiver altogether. Firstly, a 1.5-micron zinc oxide, which provides well-defined central frequency, is sputtered and patterned onto silicon substrate.
DOSE-DEPENDENT EFFECTS ON THE DISPOSITION OF MONOMETHYLARSONIC ACID AND DIMETHYLARSINIC ACID IN THE MOUSE AFTER INTRAVENOUS ADMINISTRATION (1998)

The organic arsenicals monomethylarsonic acid (MMA) and dimethylarsinic acid (DMA) are the primary metabolites of inorganic arsenic, a known human carcinogen. The objective of this study was to examine if dose would affect the excretion and terminal tissue disposition of MMA and DMA in the mouse. 14C-MMA (4.84 and 484 mumol/kg) and -DMA (8.04 and 804 mumol/kg) were administered to female mice via the tail vein. The mice were placed in metabolism cages for collection of urine (1, 2, 4, 8, 12, and 24 h) and feces (24 h). The animals were then sacrificed at 24 h and tissues were removed and analyzed for radioactivity. The urine was also analyzed for parent compound and metabolites. Urinary excretion of MMA- and DMA-derived radioactivity predominated over fecal excretion. Dose did not affect the overall urinary excretion of both compounds. However, fecal excretion was significantly lower in the low-dose MMA-treated animals as opposed to in the high-dose group, whereas in the high-dose DMA-treated group excretion was lower than in the low-dose DMA group. The retention of radioactivity was low (< 2% of dose) and the distribution pattern similar for both compounds, with carcass > liver > kidney > lung. The concentration of radioactivity (% dose/g tissue) was greater in kidney than in liver, lung, and blood for both compounds. The distribution and concentration of MMA-derived radioactivity was significantly greater in the liver and lung of the high-dose group. The MMA-treated animals excreted predominantly MMA in urine and lower amounts of DMA (< 10% of the dose). The percentage excreted as DMA was significantly higher in the low-dose MMA group. In the urine of DMA-treated animals, an unstable metabolite and the parent compound were detected. Overall, it appears the dose of organic arsenical administered has a minimal effect on its excretion and terminal tissue disposition in the mouse. The rapid elimination and low retention of MMA and DMA explain in part their low acute toxicity.
<i>In-situ</i> realtime monitoring of nanoscale gold electroplating using micro-electro-mechanical systems liquid cell operating in transmission electron microscopy (2016)

The dynamics of nanoscale electroplating between gold electrodes was investigated using a microfabricated liquid cell mounted on a scanning transmission electron microscope. The electroplating was recorded in-situ for 10 min with a spatial resolution higher than 6 nm. At the beginning of the electroplating, gold spike-like structures of about 50 nm in size grew from an electrode, connected gold nanoclusters around them, and form three dimensional nanoscale structures. We visualized the elementary process of the gold electroplating, and believe that the results lead to the deeper understanding of electroplating at the nanoscale.
TRANSAMINATION REACTIONS IN PLANTS (1954)

The transamination reaction was first demonstrated by Braunstein and Kritzmann (l), and they (2) claimed that some fourteen amino acids would serve as amino donors to oc-ketoglutaric acid or oxalacetic acid.Kritzmann (3) obtained transamination with extracts of ground pea seedlings, and other workers (4, 5) observed limited transamination in plants.The first highly active plant transamination system was prepared by Albaum and Cohen (6) from oat seedlings and was shown to be active with cu-ketoglutaric acid and aspartic acid, alanine, or cysteic acid.Leonard and Burris (7) were able to demonstrate the glutamic-oxalacetic acid system in extracts from a variety of plant species and tissues and the alaninecr-ketoglutaric acid system in wheat germ.In recent years (8-11) it has become increasingly apparent that the transamination reaction in animal tissues and bacteria has a wide scope both in terms of amino group donors and amino group acceptors.Stumpf (12) employed ascending chromatography to detect the formation of glutamate,
360-Degree Video Head Movement Dataset (2017)

While Virtual Reality applications are increasingly attracting the attention of developers and business analysts, the behaviour of users watching 360-degree (i.e. omnidirectional) videos has not been thoroughly studied yet. This paper introduces a dataset of head movements of users watching 360-degree videos on a Head-Mounted Display (HMD). The dataset includes data collected from 59 users watching five 70 s-long 360-degree videos on the Razer OSVR HDK2 HMD. The selected videos span a wide range of 360-degree content for which different viewer's involvement, thus navigation patterns, could be expected. We describe the open-source software developed to produce the dataset and present the test material and viewing conditions considered during the data acquisition. Finally, we show some examples of statistics that can be extracted from the collected data, for a content-dependent analysis of users' navigation patterns. The source code of the software used to collect the data has been made publicly available, together with the entire dataset, to enable the community to extend the dataset.
Optimizing the Viewing Graph for Structure-from-Motion (2015)

The viewing graph represents a set of views that are related by pairwise relative geometries. In the context of Structure-from-Motion (SfM), the viewing graph is the input to the incremental or global estimation pipeline. Much effort has been put towards developing robust algorithms to overcome potentially inaccurate relative geometries in the viewing graph during SfM. In this paper, we take a fundamentally different approach to SfM and instead focus on improving the quality of the viewing graph before applying SfM. Our main contribution is a novel optimization that improves the quality of the relative geometries in the viewing graph by enforcing loop consistency constraints with the epipolar point transfer. We show that this optimization greatly improves the accuracy of relative poses in the viewing graph and removes the need for filtering steps or robust algorithms typically used in global SfM methods. In addition, the optimized viewing graph can be used to efficiently calibrate cameras at scale. We combine our viewing graph optimization and focal length calibration into a global SfM pipeline that is more efficient than existing approaches. To our knowledge, ours is the first global SfM pipeline capable of handling uncalibrated image sets.
Learning of Perceptual Similarity from Expert Readers for Mammogram Retrieval (2006)

Image retrieval relies critically on the similarity measure used to compare a query image to a target image in a database. In this work, we explore a similarity measure for mammogram retrieval based on supervised learning from expert readers. This approach is evaluated using data collected from an observer study with a set of clinical mammograms. Our results demonstrate that the proposed machine learning approach can be used to model the notion of similarity as judged by expert readers in their interpretation of mammogram images and that it can outperform alternative similarity measures derived from unsupervised learning.
Anti-Inflammatory Effects of Tartar Emetic and Niridazole: Suppression of Schistosome Egg Granuloma (1974)

Abstract Treatment of cerebral schistosomiasis japonica with tartar emetic produces a remarkable and rapid improvement which cannot be explained on the basis of worm destruction alone. In dracunculiasis, niridazole appears to have an anti-inflammatory effect facilitating the extraction of the adult worms. In addition to their antischistosome effects these drugs may serve to suppress the response to schistosome eggs which has been demonstrated to be a form of delayed hypersensitivity. Niridazole and tartar emetic were administered, in their recommended therapeutic doses, to mice. In unsensitized animals granulomas appeared by the 4th day and reached their peak at 16 days. Treatment with the drugs resulted in no reaction at 4 days, minimal reaction at 8 days, and marked suppression at 16 days. Mice sensitized by the prior injection of eggs developed large reactions 1 day after intravenous egg injection and massive reactions by 8 days. No reaction was seen at 24 hr in the treated animals and, at 8 days, the reactions were 50% smaller than in the controls. In egg-sensitized mice both drugs suppressed delayed footpad swelling to soluble egg antigens, another parameter of delayed hypersensitivity. The degree of inhibition of granuloma formation by niridazole and tartar emetic was similar to that of many of the major immunosuppressive drugs, neonatal thymectomy and antimacrophage serum. The rapid amelioration of cerebral schistosomiasis, the ease of guinea worm extraction, and some of the other effects of these drugs, may be explained by these observations.