gebhart/patrepeval huggingface dataset:
Solid lipid nanoparticles (SLNs) to improve oral bioavailability of poorly soluble drugs (2004)

The purpose of this work was to improve the oral bioavailability of poorly soluble drugs by incorporation into solid lipid nanoparticles (SLNs). All-trans retinoic acid (ATRA) was used as a poorly soluble model drug. Different formulations of SLNs loaded with ATRA were successfully prepared by a high-pressure homogenization method and using Compritol 888 ATO as lipid matrix. The particle size and distribution, drug loading capacity, drug entrapment efficiency (EE %), zeta potential, and long-term physical stability of the SLNs were investigated in detail. Drug release from two sorts of ATRA-SLN was studied and compared with the diffusion from ATRA solution in 0.1 M HCl, distilled water and phosphate buffer (pH 7.40), using a dialysis bag method. A pharmacokinetic study was conducted in male rats after oral administration of 8 mg kg(-1) ATRA in different formulations and it was found that the relative bioavailability of ATRA in SLNs was significantly increased compared with that of an ATRA solution. The amount of surfactant also had a marked effect on the oral absorption of ATRA with SLN formulations. Although an emulsion formulation also increased ATRA absorption, it was too unstable for use in clinical situations. The absorption mechanism of the SLN formulations was discussed. These results indicate that ATRA absorption is enhanced significantly by employing SLN formulations. SLNs offer a new approach to improve the oral bioavailability of poorly soluble drugs.
Pathogenesis and treatment of Sj??gren??s syndrome (1997)

The criteria for diagnosis of primary Sjögren's syndrome continue to be controversial, leading to confusion in clinical practice and in the research literature. Among Sjögren's syndrome patients who fulfill the European criteria, only 15% of those would fulfill the San Diego criteria. This difference in disease classification leads to difficulty in evaluating clinical trials and in elucidating pathogenetic mechanisms, because different patient populations are evaluated. As a result of the ease and safety of minor salivary gland biopsy, Sjögren's syndrome serves as a prototype model to study the immunopathogenic features of a human organ-specific autoimmune disease. Critical features of pathogenesis include: 1) failure to "delete" autoimmune T cells at the level of thymic selection; 2) "homing" of autoimmune lymphocytes to salivary and lacrimal glands via high endothelial venules; 3) clonal expansion of autoimmune T cells in the glands; 4) upregulation of major histocompatibility antigens and adhesive molecules by epithelial cells in the glands; 5) secretion of proinflammatory cytokines by both lymphocytes and epithelial cells; 6) decreased neural innervation of the glands; 7) failure of residual glandular tissue express secretory functions; and 8) failure to remove autoimmune T cells by normal mechanisms of apoptosis. Each of these steps is regulated by cell-matrix interactions, cytokine and growth factor secretion, cell membrane receptor stimulation, "second" signals in the cytoplasm, and nuclear transcription factors. Recent studies on each of these steps in Sjögren's syndrome have suggested their role in pathogenesis and, consequently, their potential as sites for therapeutic intervention.
Canonical and Noncanonical Wnt Proteins Program Dendritic Cell Responses for Tolerance (2013)

Ag-presenting dendritic cells (DCs) interpret environmental signals to orchestrate local and systemic immune responses. They govern the balance between tolerance and inflammation at epithelial surfaces, where the immune system must provide robust pathogen responses while maintaining tolerance to commensal flora and food Ags. The Wnt family of secreted proteins, which control epithelial and hematopoietic development and homeostasis, is emerging as an important regulator of inflammation. In this study, we show that canonical and noncanonical Wnts directly stimulate murine DC production of anti-inflammatory cytokines. Wnt3A triggers canonical β-catenin signaling and preferentially induces DC TGF-β and VEGF production, whereas Wnt5A induces IL-10 through alternative pathways. The Wnts also alter DC responses to microbe- or pathogen-associated molecular patterns, inhibiting proinflammatory cytokine induction in response to TLR ligands and promoting DC generation of Foxp3(+) regulatory T cells. Moreover, although both Wnts suppress proinflammatory responses to bacterial endotoxin and to TLR1/2, TLR7, and TLR9 ligands, Wnt5A, but not Wnt3A, inhibits IL-6 production in response to the viral mimic, polyinosinic:polycytidylic acid. Thus, Wnt family members directly and differentially regulate DC functions, an ability that may contribute to the balance between tolerance and inflammation at epithelial sites of exposure to microbes and environmental Ags.
The dilating effect of histamine on pial arteries of cats and its mediation by H2 receptors. (1979)

We studied the effect of histamine and H1 or H2 blockers on the diameter of pial arteries (39-227 micron) using microapplication into the perivascular space. Concentration-response curves for histamine showed dilations which started at 10(-7) M and were maximal at 10(-5) and 10(-4) M. The H2 blocker, cimetidine, induced no vascular reaction over the whole concentration range tested (10(-7) to 10(-3) M). The H1 blocker, mepyramine, was not vasoactive in the concentration range from 10(-7) to 5 X 10(-5) M and evoked dilations at higher concentrations. The concentration-response curve for histamine was only slightly displaced by 10(-5) M mepyramine but was significantly shifted to the right by 10(-5) M cimetidine. The dilating effect of histamine could be reduced in a stepwise manner by increasing concentrations of cimetidine. These findings are in accordance with a selective antagonism between histamine and cimetidine at the H2 receptors of smooth muscle cells of pial arteries. The insignificant role of H1 receptors in histamine-induced dilations is supported by the finding that a combination of H1 and H2 blockers resulted in the same reduction of histamine-induced dilation as did the application of the H2 blocker.
The Primary Synchronization Signal of 5G NR (2018)

Initial access is the process that a user equipment (UE) establishes initial connection to the cellular network, and the first step is to detect the presence of primary synchronization signal (PSS) and secondary synchronization signal (SSS) to conduct cell-search and downlink synchronization. This paper focus on the PSS waveform of 5G New Radio (NR). We present two waveforms suitable for NR-PSS: m sequence and Zadoff-Chu (ZC) sequence, then discuss their properties of autocorrelation and cross-correlation when adopted for NR-PSS. In addition, we discuss their feasibility since frequency allocation for 5G NR includes millimeterwave (mmWave) bands that may bring large frequency offset. On the basis of matched-filter detection with hypothesis, we further evaluate the frequency offset estimation performance of these two sequence.
Sensor and navigation system integration for autonomous unmanned aerial vehicle applications (2003)

In this paper, the authors present the development of an autonomous mobile platform designed to test the performance of optical and electronic sensors that will be installed in an autonomous unmanned aerial vehicle. This system allows the analysis of the necessary sensors and communications between the base station and the mobile vehicle without the risks involved in a real flying helicopter. The authors describe all the sensors and navigation systems that are needed in an autonomous helicopter, the way in which they have been implemented in the platform, the acquisition through a control architecture based on a microcontroller that sends all information to a remote station on the ground and the results obtained in the performed tests.
“Cellular astronomy”—A foreseeable future in cytometry (2004)

Advances in electro-optic technology within the past 2 years, notably the development of high-intensity light-emitting diodes and highly efficient charge-coupled device cameras, have made it feasible to produce small, simple, rugged, automated fluorescence image cytometers, with selling prices well below 10,000 US dollars, that can make measurements previously the exclusive domain of flow and scanning cytometers costing many times more. It should be feasible to apply the new cytometric technology in scientific and geographic areas for which a previous generation of instruments was too complex and too expensive, e.g., to problems of diagnosis and management of infectious diseases prevalent at critical levels in resource-poor areas, such as the human immunodeficiency virus, malaria, and tuberculosis.
Atopic Eczema: Genetic Associations and Potential Links to Developmental Exposures (2017)

Atopic eczema (AE), or atopic dermatitis (AD), is a common inflammatory skin disease with a disrupted epidermal barrier and an allergic immune response. AD/AE is prominently characterized by a symptomatic itch and transient skin lesions. Infants compose a significant percentage affected. Two models have been proposed to explain AD/AE skin pathology: the gut microbiome-focused inside-outside model and the outside-inside model concentrating on the disrupted skin barrier/skin microbiome. Gene disruptions contributing to epidermal structure, as well as those in immune system genes, are implicated. Over 30 genes have been linked to AD/AE with Flg and Tmem79/Matt alterations being common. Other linked disruptions are in the interleukin-1 family of cytokines/receptors and the T<sub>H</sub>2 gene family of cytokines. Inheritable epigenetic modifications of the genes or associated proteins may also be involved. Skin barrier disruption and the allergic immune response have been the main foci in mechanistic studies of AD/AE, but the role of the environment is becoming more apparent. Thus, an examination of in utero exposures could be very helpful in understanding the heterogeneity of AD/AE. Although research is limited, there is evidence that developmental exposure to environmental tobacco smoke or phthalates may impact disease. Management for AD/AE includes topical corticosteroids and calcineurin inhibitors, which safely facilitate improvements in select individuals. Disease heterogeneity warrants continued research not only into elucidating disease mechanism(s), via identification of contributing genetic alterations, but also research to understand how/when these genetic alterations occur. This may lead to the cure that those affected by AD/AE eagerly await.
Further Studies on the Antibotulinal Effectiveness of Nisin in Acidic Media (1981)

ABSTRACT The antibotulinal effectiveness of nisin in TPYG broth was increased somewhat by lowering the pH to pH 5.5. The ability of nisin to inhibit the outgrowth of strain 56A spores was markedly increase at pH 5.5 by comparison to its effectiveness at higher pHs observed in previous studies. The increased effectiveness of nisin at pH 5.5 was less notable for the strain 69A, 113B, and 213B spores. The nisin sensitivity of the type E spores was essentially unchanged from that observed in earlier studies at higher pHs. At pH 6, nisin levels of 5000 I.U./ml were insufficient to prevent spore outgrowth by C. botulinum in cooked meat medium. Comparatively, much lower levels of nisin were effective in preventing botulinal outgrowth in TPYG broth at pH 6. The decreased effectiveness of nisin in cooked meat medium may be due to the binding of nisin to meat particles, and this binding is apparently not affected by lowering the pH to pH 6.0.
Allosteric Functional Switch of Neurokinin A-Mediated Signaling at the Neurokinin NK2 Receptor: Structural Exploration (2009)

The neurokinin NK2 receptor is known to pre-exist in equilibrium between at least three states: resting-inactive, calcium-triggering, and cAMP-producing. Its endogeneous ligand, NKA, mainly induces the calcium response. Using a FRET-based assay, we have previously discovered an allosteric modulator of the NK2 receptor that has the unique ability to discriminate among the two signaling pathways: calcium-signaling is not affected while cAMP signaling is significantly decreased. A series of compounds have been prepared and studied in order to better understand the structural determinants of this allosteric functional switch of a GPCR. Most of them display the same allosteric profile, with smooth pharmacomodulation. One compound however exhibits significantly improved modulatory properties of NKA induced signaling when compared to the original modulator.
NOx Virtual Sensor Based on Structure Identification and Global Optimization (2005)

&lt;div class="htmlview paragraph"&gt;On-line measurement of engine NOx emissions is the object of a substantial effort, as it would strongly improve the control of CI engines. Many efforts have been directed towards hardware solutions, in particular to physical sensors, which have already reached a certain degree of maturity.&lt;/div&gt; &lt;div class="htmlview paragraph"&gt;In this paper, we are concerned with an alternative approach, a virtual sensor, which is essentially a software code able to estimate the correct value of an unmeasured variable, thus including in some sense an input/output model of the process. Most virtual sensors are either derived by fitting data to a generic structure (like an artificial neural network, ANN) or by physical principles. In both cases, the quality of the sensor tends to be poor outside the measured values. In this paper, we present a new approach: the data are screened for hidden analytical structures, combining structure identification and evolutionary algorithms, and these structures are then used to develop the sensor presented. While the computational time for the sensor design can be significant (e.g. 1 or more hours), the resulting formula is very compact and proves able to predict the behaviour of the system at other operating points.&lt;/div&gt; &lt;div class="htmlview paragraph"&gt;The method has been validated with NOx data from a production engine measured with a Horiba Mexa 7000. The approach is able to yield a good prediction behaviour over a whole cycle. The results are consistent with physical knowledge.&lt;/div&gt;
Fast Maze Router (1978)

This paper describes a method of generating a path between two points of a cellular array, with some cells being specified as obstacles. The method combines two techniques: A line search is first directed toward the target. This is a fast and extremely effective method on boards with plenty of space. When the line search hits an obstacle, an expansion technique typical for the Lee-type algorithms is then used to “bubble” around the obstacle. The line search can then continue toward the target again.
Ras Transformation Results in an Elevated Level of Cyclin D1 and Acceleration of G <sub>1</sub> Progression in NIH 3T3 cells (1995)

Ectopic overexpression of v-H-Ras protein in NIH 3T3 cells resulted in cellular transformation and an acceleration of G1 progression of these cells. A shortened G1 phase was found to be associated with an increased level of cyclin D1 but not cyclin E protein. Using an antisense blocking method, reduced synthesis of cyclin D1 in v-H-Ras transformants resulted in a slower G1 progression rate of these cells. Although constitutive overexpression of cyclin D1 in NIH 3T3 cells accelerated G1 progression, cells remained untransformed. Furthermore, inhibition of cyclin D1 synthesis greatly impaired the soft-agar cloning efficiency of v-H-Ras transformants. These results suggest that increased expression of cyclin D1 is necessary but not sufficient for the transforming activity of v-H-Ras. Similar effect on cell cycle progression was also observed in Raf-transformed cells. In addition to cyclin D1, cyclin E protein was found to be elevated in Src transformants. This may account for the further shortening of the G1 phase of these cells. Activation of an additional Ras-independent pathway was suggested to be responsible for the further acceleration of the G1 phase in Src transformants.
Urban Localization with Street Views using a Convolutional Neural Network for End-to-End Camera Pose Regression (2019)

International audience
Multiple Inflow Pulsed Arterial Spin-Labeling Reveals Delays in the Arterial Arrival Time in Minor Stroke and Transient Ischemic Attack (2010)

Our purpose was to use multiple inflow pulsed ASL to investigate whether hemodynamic AAT information is sensitive to hemispheric asymmetry in acute ischemia. The cohorts included 15 patients with acute minor stroke or TIA and 15 age-matched controls. Patients were scanned by using a stroke MR imaging protocol at a median time of 74 hours. DWI lesion volumes were small and functional impairment was low; however, perfusion abnormalities were evident. Prolonged AAT values were more likely to reside in the affected hemisphere (significant when compared with controls, P < .048). An advantage of this ASL technique is the ability to use AAT information in addition to CBF to characterize ischemia.
Development and Application of a New Method To Extract Bacterial DNA from Soil Based on Separation of Bacteria from Soil with Cation-Exchange Resin (1992)

A new method for the extraction of bacterial DNA from soil has been developed. Soil samples of 50 g were dispersed, and bacteria were released by use of a cation-exchange resin; subsequently, bacteria were separated from soil particles by low-speed centrifugation and lysed with lysozyme and ionic detergent, and the DNA was then purified by CsCl-ethidium bromide equilibrium density centrifugation. The extracted DNA was of high molecular weight and sufficiently pure for restriction enzyme digestion, DNA-DNA hybridization, and amplification by the polymerase chain reaction. The advantages of the new method are that the separation of bacteria from soil is considerably faster than by repeated blending, more samples can be handled, and furthermore no aerosols are formed during separation. Also, we investigated whether the CsCl-ethidium bromide equilibrium density centrifugation could be replaced by purification using Gene-Clean. However, this method produced DNAs which were insufficiently pure for several types of analysis. The new method was used to study survival of a 2,4-dichlorophenoxyacetic acid (2,4-D)-degrading Pseudomonas cepacia DBO1 (pRO101) in unamended soil and in soil amended with 2,4-D. We found that the degrading strain, irrespective of inoculation level, was able to grow to the same high numbers in soil amended with 2,4-D, while the strain in nonamended soil were maintained at the inoculation level. Detection based on DNA extraction and subsequent dot blot DNA-DNA hybridization was in accordance with detection by plating on selective medium.
5-Methyl-2-pyrrolidone analogs of oxotremorine as selective muscarinic agonists (1988)

A series of N-(4-amino-2-butynyl)-5-methyl-2-pyrrolidones modified only in the amino group was synthesized. The compounds were agonists, partial agonists, and antagonists on the isolated guinea pig ileum. They had greater affinity and lower intrinsic efficacy at ileal muscarinic receptors than the identically modified N-(4-amino-2-butynyl)-2-pyrrolidones and N-(4-amino-2-butynyl)succinimides. Dissociation constants in the three series were correlated, suggesting that the compounds had similar mode of binding to muscarinic receptors. The 5-methyl-2-pyrrolidones were 10- to 20-fold less potent as muscarinic agonists on the guinea pig urinary bladder than on the ileum and also elicited lower relative maximal responses on the bladder. For example, the trimethylammonium (9) and azetidino (10) analogues were equipotent (EC50 = 0.2 microM) with the selective muscarinic stimulant N-(1-methyl-4-pyrrolidino-2-butynyl)-N-methylacetamide, BM 5 (2), as agonists on the ileum, but on the bladder 9 and 10 were relatively weak partial agonists, whereas 2 was an antagonist. Compound 10, like 2 and the dimethylamino analogue 8, also differentiated between centrally mediated muscarinic effects in vivo as it was potent in producing analgesia and hypothermia but did not elicit tremor. Instead, 10 antagonized oxotremorine-induced tremor. Thus, 10 resembled 2 in its actions except that the greater intrinsic efficacy of 10 shifted the balance between agonist and antagonist properties slightly toward agonism. Manipulation of intrinsic efficacy by minor changes in chemical structure is emphasized as a means of attaining selectivity.
The effect of compounding ingredients on microbial degradation of vulcanized natural rubber (1990)

Abstract A series of natural rubber vulcanizates containing varied amounts of sulfur and an accelerator (N‐cyclohexyl‐2‐benzothiazyl sulfenamide, CBS) were prepared and their resistance to attack by a strain of Nocardia , capable of utilizing natural rubber as carbon substrate, was examined. The higher the content of sulfur or CBS, the less the weight loss of the vulcanizates after microbial attack. In this system of curing without a filler, the rate of microbial degradation was suggested to depend on the cross‐link density estimated from the swelling. Addition of calcium carbonate as a filler did not affect the microbial degradation, and in some cases slightly enhanced it. Addition of carbon black, however, made the vulcanizate apparently more resistant to microbial attack. The specimens with HAF grade carbon black loading were more resistant than those with SRF grade.
Software thread integration for embedded system display applications (2006)

Embedded systems require control of many concurrent real-time activities, leading to system designs that feature a variety of hardware peripherals, with each providing a specific, dedicated service. These peripherals increase system size, cost, weight, and design time. Software thread integration (STI) provides low-cost thread concurrency on general-purpose processors by automatically interleaving multiple threads of control into one. This simplifies hardware to software migration (which eliminates dedicated hardware) and can help embedded system designers meet design constraints, such as size, weight and cost. We have developed concepts for performing STI and have implemented many in our automated postpass compiler Thrint. Here we present the transformations and examine how well the compiler integrates threads for two display applications. We examine the integration procedure, the processor load, and code memory expansion. Integration allows reclamation of CPU idle time, allowing run-time speedups of 1.6x to 3.6x.
A new PLL frequency synthesizer with high switching speed (1992)

A phase-locked loop (PLL) frequency synthesizer with high switching speed is proposed. Mobile communication networks are evolving towards microcellulars operating in narrowband TDMA and microwave bands to meet the rapidly increasing demands for both voice and data services. Therefore, synthesizers with high switching speed are required for the realization. However, it will be difficult for conventional synthesizers to provide switching times of shorter than 1 ms. The PLL synthesizer proposed is composed entirely of digital signal processors except for a voltage-controlled oscillator (VCO). The VCO control signal is derived by the subtraction of the linear reference phase and the feedback phase; therefore, it does not need the band-limited loop filter which limits the ability of the loop to switch fast. The experimental results show that it can provide switching times as short as 0.1 ms, which is 10/sup 2/ approximately 10/sup 3/ times higher than conventional PLL synthesizers, and spurs of less than -60 dB.< <ETX xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">&gt;</ETX>