gebhart/patrepeval huggingface dataset:
Crystallographic and molecular modeling studies on 3-ethyl-3-(4-pyridyl)piperidine-2,6-dione and its butyl analog, inhibitors of mammalian aromatase. Comparison with natural substrates: prediction of enantioselectivity for N-alkyl derivatives (1990)

Inhibitors of the cytochrome P450 enzyme aromatase, which is involved in the biosynthesis of estrogens from androgens, are of proven utility in the treatment of hormone-dependent breast cancer. The determination of the crystal structure of one such inhibitor, 3-ethyl-3-(4-pyridyl)piperidine-2,6-dione (2) and its 3-butyl analogue (3) is described. In the absence of three-dimensional structural information for the enzyme, conformational analysis and comparison with natural substrates has been performed in order to define possible "active" conformations. The enhanced inhibitory activity of 3 may be linked to hydrophobic interactions between the side chain and that portion of the enzyme that normally interacts with the B and C rings of a steroid substrate. Information gained from this study and previous studies by other workers has been combined in order to produce a hypothesis to explain the pattern of activity of N(1)-alkyl derivatives of 2. The successful application of this hypothesis to the prediction of the relative aromatase inhibitory activities of the two enantiomers of the N-octyl derivative (4) is described.
Customized RSSI Method for Passive UHF RFID Localization System (2011)

International audience
Regulation of Leukocyte-Endothelium Interaction by Fibrinogen (1999)

Introduction The binding of neutrophils and mononuclear cells to vascular endothelium is an essential prerequisite in maintaining effective immune-inflammatory responses. This process has been unraveled as a regulated “adhesion cascade” that involves the expression of multiple adhesion receptors of the integrin, selectin, and immunoglobulin gene superfamilies on both cell types. These adhesive interactions are modulated by disparate environmental signals, ranging from inflammatory and chemotactic cytokines to changes in shear force at the vessel wall. Although of paramount importance in the preservation of immune-inflammatory surveillance, dysregulation of leukocyte-endothelium interaction also constitutes one of the earliest molecular events in the pathogenesis of such vascular diseases as atherosclerosis. This dysregulation leads to the aberrant accumulation of mononuclear cells in the damaged intima. Recently, the interaction of fibrinogen with vascular cells has emerged as an alternate mechanism for recruiting leukocytes at the site of vascular injury. Although the role of fibrinogen as a risk factor for atherosclerosis has long been recognized, this pathway has been associated with complex mechanisms of intercellular adhesion, signal transduction, second-messenger generation, and modulation of gene expression in vascular cells. These studies have revealed a multifaceted and far-reaching molecular link between inflammation and hemostasis–a link that is of potential therapeutic relevance for the pathogenesis of vascular diseases.
Effects of full-time and part-time occlusion on visual acuity recovery in amblyopic children (2012)

Objective To discuss the effects of full-time and part-time occlusion(4 hours every day) on visual acuity recovery in amblyopic children.Methods Two hundreds children with anisometropic or strabismic amblyopia from 3 years old to 11 years old were chosen,the difference of best corrected visual acuity between two eyes was no less than two lines.All the cases were divided into preschool group(3-5 years old,n=66),junior group(6-8 years old,n=93) and senior group(9-11 years old,n=41).Optical correction alone was used at first three months.All the patients in each group were divided into part-time occlusion group and full-time occlusion group randomly after optical correction for three months.The visual acuity was measured at 3 months,6 months and 9 months during occlusion period.Results Amblyopia was improved significantly with optical correction alone in all groups at initial three months(average increasing 2.3 lines in preschool group,t=10.898,P0.001;average increasing 1.6 lines in junior group,t=11.563,P0.001;average increasing 1.6 lines in senior group,t= 9.823,P0.001).Improvements in visual acuity of the amblyopic eyes were continued during occlusion period.No significant difference was found between full-time and part-time occlusion group at 3 months(preschool group:t=-0.136,P=0.892;junior group:t=0.755,P=0.452;senior group:t=-0.039,P=0.969),6 months(preschool group:t=0.737,P=0.465;junior group:t=-0.838,P=0.405;senior group:t=-0.326,P=0.747) and 9 months(preschool group:t=-1.618,P=0.116;junior group:t=-1.816,P=0.075;senior group:t=1.313,P=0.207),respectively.Conclusion Based on optical correction,prescribing 4 hours of daily occlusion can improve visual acuity as effective as full-time occlusion,the effect has no difference.
Evaluation of Oxide–Oxide Composites in a Novel Combustor Wall Application (2005)

Oxide–oxide composites were evaluated in a novel combustor design requiring higher wall temperatures than the conventional combustors. The evaluation was based on a combination of numerical modeling and experimental rig testing. The modeling included computational fluid dynamics (CFD) calculations whose results were used in a thermo‐mechanical analysis using finite element modeling (FEM). The composites tested experimentally were obtained from a commercial vendor; they were reinforced using Nextel ™ 720 fibers. The rig tests showed that aluminosilicate matrix composites with higher room temperature strengths suffered cracking while the weaker alumina matrix composites performed satisfactorily. The results were consistent with numerical models that predicted residual stresses from creep during service. The models showed that in‐plane gradients and their effects were more severe than those of through‐thickness gradients and suggest that tailoring fiber architecture is important in transitioning these composites to applications.
Survey of delivery room resuscitation practices at tertiary perinatal centers in Japan (2014)

The equipment and techniques used in Japanese perinatal center delivery room resuscitation practices are highly varied. Further research is required to determine which devices and techniques are appropriate for this important and common intervention.
Alternative treatments for type 2 diabetes and associated metabolic diseases: medical therapy or endoscopic duodenal mucosal remodelling? (2021)

SCOPUS: re.j
2D11 Technique for Discrimination between Seven Motions Using Real-Time EMG Signals(The 12th International Conference on Motion and Vibration Control) (2014)

Many forearm amputees use various prosthetic hands depending on their purposes. Myoelectric prosthetic hands, which use electromyogram (EMG) signals in persisting muscles as operation signals, are attracting attention because they look similar to cosmetic prosthetic hands and can be operated by a sense of nature. The objective of this study is to develop a method of discriminating real-time motion from EMG signals. We previously proposed a real-time motion discrimination method using the hyper-sphere models. This method could discriminate between five motions (hand opening, hand closing, hand chucking, wrist extension, and wrist flexion) at a rate of above 90 percent. The discrimination processing time made was less than 300 ms by using the hyper-sphere models. Moreover, this method prevents elbow motions from interfering with hand motion discrimination. However, forearm amputees cannot go about their daily life comfortably by using only five motions. Furthermore, we think that wrist pronation and wrist supination are important in daily life. Here, we propose a real-time motion discrimination method using the hyper-sphere models for seven motions: hand opening, hand closing, hand chucking, wrist extension, wrist flexion, wrist pronation, and wrist supination. Furthermore, we also created new hyper-sphere models to maintain real-time motion discrimination. We experimentally verified that the discrimination accuracies of this method were 90 percent and the discrimination processing time was less than 300 ms. Moreover, elbow motions did not interfere with the hand motion discrimination.
Supplementary Figure 6 from NVP-AUY922: A Novel Heat Shock Protein 90 Inhibitor Active against Xenograft Tumor Growth, Angiogenesis, and Metastasis (2023)

Supplementary Figure 6 from NVP-AUY922: A Novel Heat Shock Protein 90 Inhibitor Active against Xenograft Tumor Growth, Angiogenesis, and Metastasis
Ethanol‐Induced Leukocyte Adherence and Albumin Leakage in Rat Mesenteric Venules: Role of CD18/Intercellular Adhesion Molecule‐1 (1996)

The adherence and emigration of leukocytes have been implicated as a rate-limiting step in the microvascular disturbance in a variety of pathogenic events. The objective of the present study was to investigate leukocyte-endothelial cell adhesion and endothelial barrier function in rat mesenteric microvessels exposed to ethanol, which is known to cause inflammation and injury in various organs. Mesentery of male Wistar rats was used for intravital microscopic observations. Leukocyte adherence and albumin leakage were monitored in single postcapillary venules using the intravital fluorescence microscope. Superfusion of 50 mM ethanol elicited the leukocyte adherence and albumin leakage within 60 min. Pretreatment with a monoclonal antibody directed against either CD18 or intercellular adhesion molecule-1 (ICAM-1) significantly prevented the ethanol-induced increase in leukocyte adherence and decrease in barrier function of endothelium. These results suggest that ethanol-induced leukocyte adherence is mediated by CD18 on leukocytes and ICAM-1 on endothelial cells. The present study further supports that CD18/ ICAM-1-dependent leukocyte-endothelial adhesive interactions lead to macromolecular leakage in the postcapillary venules exposed to ethanol.
O-Band 50Gb/s Ring Modulator in a 300mm Si Photonic Platform (2018)

A carrier-depletion ring modulator is demonstrated to operate at 50Gb/s in the O-band of optical communications. The high-bandwidth device was designed using an analytical model, considering also non-linear effects. A 1.9dB extinction ratio is achieved with a 3Vpp driving voltage.
Ongoing grammatical changes and global Englishes (2013)

This paper looks into how current grammatical changes in English are reflected and adopted in use in the present-day global Englishes, i.e. in lingua franca and in other L2-varieties of today. The study of ongoing changes in English has emerged as a lively field recently, and the studies of lexico-grammatical variability have identified a range of patterns of contemporary change (Leech et al. 2009; Mair & Leech 2006). Much of this research has focused on the inner core varieties of English, and only recently have we seen investigations targeting changes in the new Englishes (see Filppula 2012; Laitinen 2011). The main argument is that more emphasis should be placed on exploring the diachronic embedding of variability in today's global Englishes. This paper presents evidence on two current and ongoing changes: (a) variability in the modals of will/shall (Leech 2003) and (b) changes in the adverbial connectives of every/each/any time (Brinton 2007). I will draw evidence from two databases that represent English uses in Sweden and in Finland. These databases are currently in compilation, with the aim that they would provide good practices for developing a new generation of global English text corpora.
Depth-Profiling and Diffusion Measurements in Ice Films Using Infrared Laser Resonant Desorption (2000)

A new infrared laser resonant desorption (LRD) technique has been developed that permits depth-profiling and diffusion measurements in ice. This LRD technique utilizes an Er:YAG rotary Q-switched laser with an output wavelength of lambda = 2.94 microm and a pulse duration of approximately 100 ns. The Er:YAG laser light resonantly excites O-H stretching vibrations in the H2O molecules that form the ice. This laser resonant heating induces H2O desorption at the ice surface. Control experiments were conducted on pure and isotopically mixed laminated ice films to determine the optimum experimental parameters for the LRD depth-profiling and diffusion measurements. Depending on laser energy, the measured desorption depth was either less than, comparable to, or larger than the optical penetration depth of approximately 0.8 microm at lambda = 2.94 microm. LRD studies were used to analyze H2 18O/H2 16O stacked multilayers and laminate sandwich structures. These measurements revealed that the LRD technique can depth-profile into ice films with submicrometer spatial resolution and high sensitivity. Two types of experiments employing LRD depth-profiling were demonstrated to monitor diffusion in ice. HCl hydrate diffusion in ice was measured versus time after depositing ice/HCl/ice sandwich structures. Na diffusion into ice was studied after adsorbing Na using a continuous Na source for a given exposure time at the diffusion temperature.
Acceleration and Parallelization of ZENO/Walk-on-Spheres (2016)

This paper describes our on-going work to accelerate ZENO, a software tool based on Monte Carlo methods (MCMs), used for computing material properties at nanoscale. ZENO employs three main algorithms: (1) Walk on Spheres (WoS), (2) interior sampling, and (3) surface sampling. We have accelerated the first two algorithms. For the sake of brevity, the paper will discuss our work on the first one only as it is the most commonly used and the acceleration techniques were similar in both cases. WoS is a Brownian motion MCM for solving a class of partial differential equations (PDEs). It provides a stochastic solution to a PDE by estimating the probability that a random walk, which started at infinity, will hit the surface of the material under consideration. WoS is highly effective when the problem's geometry is additive, as this greatly reduces the number of walk steps needed to achieve accurate results. The walks start on the surface of an enclosing sphere and can make much larger jumps than in a direct simulation of Brownian motion. Our current implementation represents the molecular structure of nanomaterials as a union of possibly overlapping spheres. The core processing bottleneck in WoS is a Computational Geometry one, as the algorithm repeatedly determines the distance from query point to the material surface in each step of the random walk. In this paper, we present results from benchmarking spatial data structures, including several open-source implementations of <i>k</i>-D trees, for accelerating WoS algorithmically. The paper also presents results from our multicore and cluster parallel implementation to show that it exhibits linear strong scaling with the number of cores and compute nodes; this implementation delivers up to 4 orders of magnitude speedup compared to the original FORTRAN code when run on 8 nodes (each with dual 6-core Intel Xeon CPUs) with 24 threads per node.
Long-term activity in and among persons with transfemoral amputation (2013)

Although physical limitations associated with transfemoral amputation (TFA) have been studied in laboratory settings, little is known about habitual activity within free-living environments. A retrospective analysis of 12 mo of step activity data was performed to quantify activity levels, variations, and patterns in 17 adults with unilateral TFA. Yearly, seasonal, and monthly average daily step counts and coefficients of variation (CoVs) were examined to characterize mobility. Analysis by Medicare Functional Classification Level (MFCL) was performed to explore relationships between clinical classification and performance. Subjects averaged 1,540 prosthetic steps/day, and activity generally increased with MFCL. Activity between MFCL-2 and -3 subjects was not significantly different, suggesting that ability to engage in habitual physical activity may be similar for these groups. Relative variation (CoV) was 0.65 across subjects but was lower for those with higher activity levels. No significant differences in CoV by group were detected. Marked seasonal and monthly patterns in activity were identified. Warmer seasons and months generally promoted higher activity, but peak temperatures and humidity depressed activity. Results suggest that persons with TFA are greatly limited in regards to activity. Further, large variations within and between subjects may challenge the interpretation of step activity gathered over short periods of time.
[P4–099]: CHANGES IN TAU PROTEIN LANDSCAPE DURING ALZHEIMER's DISEASE PROGRESSION (2017)

Post-translational modifications of Tau protein are of central importance in Alzheimer's disease (AD) pathogenesis. In addition to the well-established role of hyperphosphorylation in AD, emerging evidence indicates the involvement of proteolytic cleavages in Tau pathology development. In this study we explored the disease-related changes in the composition of Tau protein species, both full length and fragments, in cortical tissue from AD subjects. Cryosections of fresh-frozen fusiform gyrus cortex from AD subjects and cognitively normal, age matched control subjects were characterized using immunoprecipitation, ELISA, immunoblotting and transcriptomic analyses. Additionally, fresh-frozen frontal cortical tissues from control subjects were used to identify proteolytic cleavage sites using proteomic methods. Full-length Tau isoforms showed changes in protein expression pattern with high correlation to disease severity. Specifically, the longest Tau isoform, Tau441 (2N4R), is selectively enriched in AD patients versus controls, with the highest enrichment in Braak stages V and VI. No difference in Tau spliced forms were observed at the RNA level, indicating the enrichment of specific isoforms occurs post-transcriptionally. One possible mechanism is differential fragmentation of Tau isoforms via proteolytic cleavage. We observed that the Tau fragmentation pattern is common and stereotypical across all patient samples, regardless of disease status, with fragments representing ∼25% of total Tau signal. The extent of Tau fragmentation, however, is inversely correlated with the extent of tauopathy and Tau441 levels. Further analyses of the fragments suggest at least one common cleavage site for all isoforms, generating a N terminal-mid domain fragment and a C-terminal fragment. Our data suggest a proteolytic mechanism that shifts the Tau protein landscape toward the enrichment of longer isoforms during Alzheimer's disease progression. The fragments we identified are likely precursors of CSF Tau fragments, and therefore have implications for interpretation of current mid-domain Tau biomarkers for AD diagnosis and progression. Further understanding of the mechanisms of Tau fragmentation would provide insight into the biological significance of CSF Tau measurements beyond the most commonly used mid-domain assays.
PCTAIRE1 Phosphorylates p27 and Regulates Mitosis in Cancer Cells (2014)

PCTAIRE1 is distant relative of the cyclin-dependent kinase family that has been implicated in spermatogenesis and neuronal development, but it has not been studied in cancer. Here, we report that PCTAIRE1 is expressed in prostate, breast, and cervical cancer cells, where its RNAi-mediated silencing causes growth inhibition with aberrant mitosis due to defects in centrosome dynamics. PCTAIRE1 was not similarly involved in proliferation of nontransformed cells, including diploid human IMR-90 fibroblasts. Through yeast two-hybrid screening, we identified tumor suppressor p27 as a PCTAIRE1 interactor. In vitro kinase assays showed PCTAIRE1 phosphorylates p27 at Ser10. PCTAIRE1 silencing modulated Ser10 phosphorylation on p27 and led to its accumulation in cancer cells but not in nontransformed cells. In a mouse xenograft model of PPC1 prostate cancer, conditional silencing of PCTAIRE1 restored p27 protein expression and suppressed tumor growth. Mechanistic studies in HeLa cells showed that PCTAIRE1 phosphorylates p27 during the S and M phases of the cell cycle. Notably, p27 silencing was sufficient to rescue cells from mitotic arrest caused by PCTAIRE1 silencing. Clinically, PCTAIRE1 was highly expressed in primary breast and prostate tumors compared with adjacent normal epithelial tissues. Together our findings reveal an unexpected role for PCTAIRE1 in regulating p27 stability, mitosis, and tumor growth, suggesting PCTAIRE1 as a candidate cancer therapeutic target.
Bruton's tyrosine kinase is required for signaling the CD79b-mediated pro-B to pre-B cell transition (2001)

Formation of the pre-BCR complex is a critical check point during B cell development and induces the transition of pro-B to pre-B cells. CD79b (Igbeta) is a signaling component in the pre-BCR complex, since differentiation to the pre-B phenotype is induced by cross-linking the CD79b expressed on developmentally arrested pro-B cells from recombination-activating gene (RAG)-2-deficient mice. Bruton's tyrosine kinase (BTK) plays important roles in B cell development. However, its molecular mechanisms in early B cell development are not fully understood. To examine whether BTK functions in CD79b-mediated signaling for the pro-B/pre-B transition, we utilized RAG2/BTK double-knockout (DKO) mice. Pro-B cells from RAG2/BTK-DKO mice did not differentiate into pre-B cells following CD79b cross-linking, although tyrosine phosphorylation of cellular proteins including Erk1/2 and phospholipase C-gamma2 was induced in the same manner as RAG2-KO mice. BTK is phosphorylated after cross-linking of CD79b on RAG2-deficient pro-B cells. These findings suggest that BTK-dependent pathways downstream of CD79b are critical for the pro-B/pre-B transition and BTK-independent signaling pathways are also activated via the pre-BCR complex.
A simple relaying strategy for diamond networks (2014)

We consider a Gaussian diamond network where a source communicates with the destination through n noninterfering half-duplex relays. Using simple approximations to the capacity of the network, we show that simple relaying strategies involving two relays and two scheduling states can achieve at least half the capacity of the whole network, independent of channel SNRs. The proof uses linear programming duality and implies an algorithm to find such a pair of relays in O(n log n) time.
The Adjustment / Satisfaction Test (A/ST) for the Subjective Evaluation of Dialogue Enhancement (2017)

Media consumption is heading towards high degrees of content personalization. It is thus crucial to assess the perceptual performance of personalized media delivery. This work proposes the Adjustment/Satisfaction Test (A/ST), a perceptual test where subjects interact with a user-adjustable system and their adjustment preferences and the resulting satisfaction levels are studied. We employ the A/ST to evaluate an object-based audio system that enables the personalization of the balance between dialogue and background, i.e., a Dialogue Enhancement system. Both the case in which the original audio objects are readily available and the case in which they are estimated by blind source separation are compared. Personalization is extensively used, resulting in clearly increased satisfaction, even in the case with blind source separation.