gebhart/patrepeval huggingface dataset:
Synthesis of Benzannulated N-Heterocycles by a Palladium-Catalyzed C−C/C−N Coupling of Bromoalkylamines (2007)

A palladium-catalyzed domino intermolecular alkylation/intramolecular amination of functionalized aryl iodides represents a new strategy for the synthesis of benzannulated N-heterocycles, affording functionalized indolines and tetrahydroquinolines from simple precursors.
Endothelin antagonism for patients with chronic kidney disease: still a hope for the future (2014)

Endothelin is tightly involved in the regulation of vascular and renal function in health and in disease. In a variety of animal models of kidney disease, endothelin promotes renal injury through effects on inflammation and fibrosis. Furthermore, experimental data strongly suggest that blocking the actions of endothelin should be beneficial in patients with chronic kidney disease. However, despite encouraging pre-clinical and clinical evidence, endothelin antagonists are not yet an established treatment option in patients with chronic kidney disease. This article reviews key physiological and pathophysiological aspects of the endothelin system in the vasculature and the kidney, as well as results of pre-clinical and clinical studies on the use of endothelin antagonists in chronic kidney disease. We will also provide an outlook on the future of endothelin antagonism in this area, and issues to be resolved before endothelin antagonists are to become a reality for patients with chronic kidney disease.
DMBT1 is frequently downregulated in well-differentiated gastric carcinoma but more frequently upregulated across various gastric cancer types (2007)

Well-differentiated gastric carcinomas are considered to represent a distinct entity emerging via specific molecular changes different from those found in other gastric carcinoma types. The gene deleted in malignant brain tumours 1 (DMBT1) at 10q25.3-q26.1 codes for a protein presumably involved in cell differentiation and protection and has been proposed as a candidate tumour suppressor for brain and epithelial cancer. One study reported a loss of DMBT1 expression in 12.5% (5/40) of gastric cancer samples. Here, we examined in more detail DMBT1 protein and mRNA expression in 78 primary gastric tumour samples and corresponding normal gastric mucosa. DMBT1 was expressed in all non-tumour gastric mucosa tissues. Eleven out of 71 (15%) gastric tumours were negative for the DMBT1 protein in immunohistochemical analyses. Lack of DMBT1 expression was significantly more frequently found in well-differentiated gastric tumours (6/18 well-differentiated tumours vs. 5/53 other subtypes; P=0.025). Quantitative RT-PCR revealed a downregulation of the DMBT1 mRNA for 8/21 (38%) cases, while the remaining 13 cases (62%) displayed a substantial upregulation. Our data suggest that a loss of DMBT1 expression may preferentially take place in well-differentiated gastric carcinoma. However, an upregulation of DMBT1 expression is more frequently found across all gastric cancer types.
Investigation of homogeneous multi robots communication via Bluetooth (2012)

Task assignments to team of homogenous autonomous robots are in research trends in robotic field. Autonomous homogeneous multi-robot is known to have similar architecture in terms of structure and identical control system as well as their tasking. At present, most research of multi-robot mainly focuses on motion control layer. Nevertheless, a successful control and coordination of a group of robot rely on effective inter-robot communication. In this paper, in depth investigation of the Bluetooth between two homogenous mobile robots, namely MechA and MechI, is presented. MechA is pre-programmed with dedicated movement, and upon completion the data acquired is sent to MechI for coordination. A distance-based measurement was made for comparison, giving a reliable data for crisp observation. Coordination of multi-robots can be done by controlling the movement of each mobile robot through wireless communication between mobile robots with error distance of 0.0322 ± 0.0147 m.
Effects of vanadium and chromium on aluminum electromigration (1987)

A systematic study was made of electromigration in homogeneous Al-V and Al-Cr thin films. V and Cr concentrations were varied in the range of 0–2 wt. %, and films were prepared both with and without 1% Si. The addition of as little as 0.1% V caused significant improvements in lifetime relative to pure Al. In the most concentrated alloy studied, the activation energy of mass transport had increased from 0.54 eV for pure Al to 0.92 eV for Al-1.1% V. For the Al-Cr alloys, a maximum in lifetime was found at 0.4% Cr. Higher concentrations of Cr resulted in a gradual degradation of the enhanced lifetime. Lifetimes were reduced when 1% Si was added to either alloy system. Alloy microstructure was examined using transmission electron microscopy. Contrary to results for other Al alloys, lifetimes were reduced in films with extensive precipitation.
Apoptosis: One of the Mechanisms That Maintains Unresponsiveness of the Intestinal Mucosal Immune System (2001)

Intestinal mucosa is constantly exposed to environmental AGS: Activation of lamina propria (LP) T cells by luminal Ags may lead to the production of inflammatory cytokines and subsequent mucosal inflammation and tissue damage. However, in normal circumstances, LP T cells do not respond to antigenic stimulation. The mechanisms of this unresponsiveness in healthy subjects are not fully understood. In this study, we found by in vivo analysis that, except for T cells in lymph nodules of the mucosa, 15% of LP T cells underwent apoptosis in normal individuals. In contrast, there was a marked reduction in apoptosis of LP T cells in patients with inflammatory bowel disease (Crohn's disease and ulcerative colitis) and those with specific colitis. Our findings suggest that apoptosis might be a mechanism that turns off mucosal T cell responses to environmental Ags in healthy subjects, and resistance to apoptosis could be an important cause of mucosal immune dysregulation and tissue inflammation in colitis.
Deposition of Magnetoelectric Ferrite Thin Films Using Multiple Targets Technique (2016)

The magnetoelectric (ME) effect has been detected in cobalt-doped M-type hexaferrite bulk. We have demonstrated that the hexaferrite films of the M-type exhibiting the ME effect can be deposited from single targets as well as multiple targets as in the alternating target laser ablation deposition technique. The corresponding ME coupling is sufficiently high at room temperature to allow for potential device applications α = 5.2 × 10 <sup xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">-9</sup> m/s. The saturation magnetization value (4π M <sub xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">s</sub> ) of the film was measured to be 2000 G, consistent with a vibrating sample magnetometer and the ferromagnetic resonance measurement.
Application of Novel Extraction Technologies for Bioactives from Marine Algae (2013)

Marine algae are a rich source of bioactive compounds. This paper outlines the main bioactive compounds in marine algae and recent advances in novel technologies for extracting them. Novel extraction technologies reviewed include enzyme-assisted extraction, microwave-assisted extraction, ultrasound-assisted extraction, supercritical fluid extraction, and pressurized liquid extraction. These technologies are reviewed with respect to principles, benefits, and potential applications for marine algal bioactives. Advantages of novel technologies include higher yield, reduced treatment time, and lower cost compared to traditional solvent extraction techniques. Moreover, different combinations of novel techniques used for extraction and technologies suitable for thermolabile compounds are identified. The limitations of and challenges to employing these novel extraction technologies in industry are also highlighted.
Advanced GPS Hybrid Simulator Architecture (2001)

NAVSYS has developed an Advanced GPS Hybrid Simulator (AGHS) architecture to address next generation GPS testing issues for the civilian and military markets. The AGHS is a hybrid software, digital and radio frequency (RF) GPS simulator design. In addition to providing digital and RF signal simulation capability, the AGHS can also be used to record and play-back realworld GPS signals from field tests. This paper describes the modular AGHS architecture and its various uses. Digitally created simulation files were created with the system and played back into the NAVSYS Advanced GPS Receiver (AGR). Test results are included that compare the digitally created files to their real-world counterparts showing the precision that can be achieved with the AGHS digital simulation approach. Test data collected during jammer tests conducted at the Electronic Proving Grounds at Ft. Huachuca, Arizona is also presented. INTRODUCTION The next generation of GPS test and evaluation systems will need to incorporate the capability to test new technologies including (but not limited to) the new civilian and military signal structures, Controlled Reception Pattern Antennas (CRPA), the Wide Area Augmentation System (WAAS), the Local Area Augmentation System (LAAS), and the Joint Precision Approach Landing System (JPALS). There is a need for a flexible, re-programmable signal simulator architecture that can handle both the legacy GPS signals and also future signals that are planned to be implemented in the next generation GPS satellite constellation, including new frequencies, new code modulations and data formats. For high accuracy applications, such as precision approach and landing, the fidelity of the carrier phase generated by the simulator is key. Using the hybrid digital signal generation approach, high fidelity signal simulation and truth data generation is possible eliminating many of the signal uncertainties that can be added using conventional signal generation and modulation methods. The DoD is transitioning to much wider use of CRPAs to provide GPS anti-jam (A/J) improvements. Civilian use of high gain antenna arrays is also increasing for high accuracy applications. The phase-coherent multiple outputs of the AGHS can be used to simulate the effect of the GPS wave-front arriving at multiple antenna elements. Modern GPS User Equipment (UE) adopt a digital architecture where the RF inputs are converted to digital signals and digital signal processing is used to extract the GPS satellite data. To allow high accuracy testing, the simulator should provide digital signal outputs in addition
SENP1 Enhances Androgen Receptor-Dependent Transcription through Desumoylation of Histone Deacetylase 1 (2004)

SUMO (also called Sentrin) is a ubiquitin-like protein that plays an important role in regulating protein function and localization. It is known that several nuclear receptors are modified by SUMO; however, the effect of desumoylation in regulating nuclear receptor function has not been elucidated. Here we show that androgen receptor (AR)-mediated transcription is markedly enhanced by SENP1, a member of SUMO-specific protease family. SENP1's ability to enhance AR-dependent transcription is not mediated through desumoylation of AR, but rather through its ability to deconjugate histone deacetylase 1 (HDAC1), thereby reducing its deacetylase activity. HDAC1's repressive effect on AR-dependent transcription could be reversed by SENP1 and by deletion of its sumoylation sites. RNA interference depletion of endogenous HDAC1 also reduced SENP1's effect. Thus, SENP1 could regulate AR-dependent transcription through desumoylation of HDAC1. These studies provide insights on the potential role of desumoylation in the regulation of nuclear receptor activity.
Electrochemistry within a Limited Number of Molecules: Delineating the Fringe Between Stochastic and Statistical Behavior (2003)

Das Verhalten eines Ensembles aus wenigen Molekülen sollte ausgeprägt stochastisch sein und somit deutlich von den Geschwindigkeitsgesetzen üblicher chemischer Reaktionen abweichen. Diese Gegensätzlichkeit wurde am Beispiel der elektrochemischen Oxidation eines PAMAM-Dendrimers mit 64 redoxaktiven Ruthenium-Einheiten theoretisch untersucht (siehe Bild). Die maximale Anzahl adsorbierter Moleküle, für die noch stochastisches Verhalten beobachtet wird, kann entweder direkt oder anhand von instrumentellen Verzerrungen ermittelt werden.
Space Shuttle Simplified LO2 Check Valve Development Tests (1995)

The dual-flapper, swing check valve is used to prevent reverse flow to the Space Shuttle Main Engines. Upon inspection of the failed component, the spring tangs were found to be missing and heavy wear was observed on the i.d. of the spring coils. The fracture surfaces revealed that the metal had been steadily worn away until a simple overload caused the final fracture. A series of flow tests using water and a water/gas mixture was conducted to identify the flow phenomenon that produced the cyclic wear. A Plexiglas® outlet housing was utilized to view the flapper behavior under different flow conditions and to aid in high-speed photography. The tests revealed that flow instabilities induced two oscillatory flapper responses: 1) a rocking mode and 2) a chattering mode. Initially, attempts were made to reduce the spring-flapper oscillations. However, the final solution to the problem was a springless configuration that satisfied the valve's design requirements and eliminated the oscillations. The springless design relied on the inherent ability of the reverse flow momentum to close the flappers.
<i><scp>S</scp>taphylococcus aureus</i> skin colonization is promoted by barrier disruption and leads to local inflammation (2013)

Experimental mouse models of bacterial skin infections that have been described show that pathogenic microorganisms can readily invade the epidermis and dermis to produce localized infections. We used an epicutaneous mouse skin infection model to determine how the level of barrier disruption by tape-stripping correlates with persistence of Staphylococcus aureus skin colonization, concomitant induction of cutaneous inflammation and infection. Furthermore, we investigated how murine skin responds to S. aureus colonization in a physiologic setting by analysing proinflammatory cytokines and antimicrobial peptides in mouse skin. We show that previous cutaneous damage allows skin inflammation to develop and favours S. aureus persistence leading to cutaneous colonization, suggesting an interdependence of cutaneous bacteria and skin. Our study suggests that skin barrier defects favour S. aureus skin colonization, which is associated with profound cutaneous inflammation.
Downregulation of Cellular c-Jun N-Terminal Protein Kinase and NF-κB Activation by Berberine May Result in Inhibition of Herpes Simplex Virus Replication (2014)

Berberine is a quaternary ammonium salt from the protoberberine group of isoquinoline alkaloids. Some reports show that berberine exhibits anti-inflammatory, antitumor, and antiviral properties by modulating multiple cellular signaling pathways, including p53, nuclear factor κB (NF-κB), and mitogen-activated protein kinase. In the present study, we investigated the antiviral effect of berberine against herpes simplex virus (HSV) infection. Current antiherpes medicines such as acyclovir can lessen the recurring activation when used early at infection but are unable to prevent or cure infections where treatment has selected for resistant mutants. In searching for new antiviral agents against herpesvirus infection, we found that berberine reduced viral RNA transcription, protein synthesis, and virus titers in a dose-dependent manner. To elucidate the mechanism of its antiviral activity, the effect of berberine on the individual steps of viral replication cycle of HSV was investigated via time-of-drug addition assay. We found that berberine acted at the early stage of HSV replication cycle, between viral attachment/entry and genomic DNA replication, probably at the immediate-early gene expression stage. We further demonstrated that berberine significantly reduced HSV-induced NF-κB activation, as well as IκB-α degradation and p65 nuclear translocation. Moreover, we found that berberine also depressed HSV-induced c-Jun N-terminal kinase (JNK) phosphorylation but had little effect on p38 phosphorylation. Our results suggest that the berberine inhibition of HSV infection may be mediated through modulating cellular JNK and NF-κB pathways.
Sequential C−Si Bond Formations from Diphenylsilane: Application to Silanediol Peptide Isostere Precursors (2008)

The report of silanediol peptide isosteres as highly active inhibitors of proteolytic enzymes has triggered an increased interest for these compounds, thereby necessitating a general and direct synthetic access to this unusual class of protease inhibitors. In this paper, we report on the two-step assembly of the carbon-silicon backbone of a silane-containing dipeptide fragment. The synthetic scheme is comprised of an alkene hydrosilylation step with the simple precursor, diphenylsilane, using either a radical initiator or RhCl(PPh3)3, Wilkinson's catalyst, for the creation of a hydridosilane and the first new carbon-silicon bond. The next step is the reduction of this hydridosilane with lithium metal providing a silyl lithium reagent, which undergoes a highly diastereoselective addition to an optically active tert-butanesulfinimine, thus generating the second C-Si bond. This method allows sequential functionalization of the two hydrides in diphenylsilane by chemoselective discrimination.
Genetic Complexity, Structure, and Characterization of Highly Active Bovine Intestinal Alkaline Phosphatases (1998)

Mammalian alkaline phosphatases (APs) display 10-100-fold higher kcat values than do bacterial APs. To begin uncovering the critical residues that determine the catalytic efficiency of mammalian APs, we have compared the sequence of two bovine intestinal APs, i.e. a moderately active isozyme (bovine intestinal alkaline phosphatase, bIAP I, approximately 3,000 units/mg) previously cloned in our laboratory, and a highly active isozyme (bIAP II, approximately 8, 000 units/mg) of hitherto unknown sequence. An unprecedented level of complexity was revealed for the bovine AP family of genes during our attempts to clone the bIAP II cDNA from cow intestinal RNAs. We cloned and characterized two novel full-length IAP cDNAs (bIAP III and bIAP IV) and obtained partial sequences for three other IAP cDNAs (bIAP V, VI, and VII). Moreover, we identified and partially cloned a gene coding for a second tissue nonspecific AP (TNAP-2). However, the cDNA for bIAP II, appeared unclonable. The sequence of the entire bIAP II isozyme was determined instead by a classical protein sequencing strategy using trypsin, carboxypeptidase, and endoproteinase Lys-C, Asp-N, and Glu-C digestions, as well as cyanogen bromide cleavage and NH2-terminal sequencing. A chimeric bIAP II cDNA was then constructed by ligating wild-type and mutagenized fragments of bIAP I, III, and IV to build a cDNA encoding the identified bIAP II sequence. Expression and enzymatic characterization of the recombinant bIAP I, II, III, and IV isozymes revealed average kcat values of 1800, 5900, 4200, and 6100 s-1, respectively. Comparison of the bIAP I and bIAP II sequences identified 24 amino acid positions as likely candidates to explain differences in kcat. Site-directed mutagenesis and kinetic studies revealed that a G322D mutation in bIAP II reduced its kcat to 1300 s-1, while the converse mutation, i.e. D322G, in bIAP I increased its kcat to 5800 s-1. Other mutations in bIAP II had no effect on its kinetic properties. Our data clearly indicate that residue 322 is the major determinant of the high catalytic turnover in bovine IAPs. This residue is not directly involved in the mechanism of catalysis but is spatially sufficiently close to the active site to influence substrate positioning and hydrolysis of the phosphoenzyme complex.
Systematic Isolation of Genes Expressed at Low Levels in Inflorescence Apices of Arabidopsis thaliana (1999)

We constructed an equalized cDNA library from Arabidopsis inflorescence shoot apices including inflorescence meristem, floral meristem and flower tissue collected before stage 5 of flower development. The cDNA clones were arrayed on membranes and were differentially screened using cDNA pools from vegetative and inflorescence tissues as probes. Each clone was classified by expression specificity and expression level. By removing the clones that displayed hybridization signals, 384 out of 3264 clones in this library remained as candidates for inflorescence-specific mRNAs expressed at low levels. Sequence analysis of all selected clones indicated that 53 were identical and 120 were homologous to genes in public protein databases. The remaining 211 selected clones had no significant amino acid sequence similarities with those deduced from any reported genes, though 62 of them appeared in Arabidopsis expressed sequenced tags (ESTs). About 40% of the selected clones were novel, validating the present approach for gene discovery. Northern blot analysis of 22 randomly selected clones confirmed that most were expressed preferentially in inflorescence tissues. In addition, many clones were transcribed at relatively low levels. We demonstrate that the screening method of the present study is useful for systematic classification of cDNA species based on expression specificity.
Biologically active principles isolated from Salacia oblonga wall. (1995)

From the petroleum ether extract of the root bark of Salacia Oblonga wall, two biologically active fractions have been isolated by column and thin layer chromatography. The methanol eluted fraction of the extract absorbed on a column of silica gel at a concentration of 50 micrograms/ml showed 100 percent cytotoxicity on Ehrlich ascites tumour cells. The chloroform eluted fraction of the pet. ether extract and a fluorescent compound separated from it by TLC demonstrated about 60% and 76% hypoglycemic potency of an equal dose of tolbutamide (250 mg/kg) in albino rats. The results indicate the therapeutic importance of S. Oblonga wall.
Data Analysis with Open Source Tools (2010)

Collecting data is relatively easy, but turning raw information into something useful requires that you know how to extract precisely what you need. With this insightful book, intermediate to experienced programmers interested in data analysis will learn techniques for working with data in a business environment. You'll learn how to look at data to discover what it contains, how to capture those ideas in conceptual models, and then feed your understanding back into the organization through business plans, metrics dashboards, and other applications. Along the way, you'll experiment with conce
Guard Placement For Wireless Localization (2006)

Motivated by secure wireless networking, we consider the problem of placing fixed localizers that enable mobile communication devices to prove they belong to a secure region that is defined by the interior of a polygon. Each localizer views an infinite wedge of the plane, and a device can prove membership in the secure region if it is inside the wedges for a set of localizers whose common intersection contains no points outside the polygon. This model leads to a broad class of new art gallery type problems, for which we provide upper and lower bounds.
Copper‐Free Click Chemistry (2009)

This chapter contains sections titled: Introduction Bio-orthogonal Ligations Applications of Copper-free Click Chemistries Summary and Outlook References