gebhart/patrepeval huggingface dataset:
Preparation of Heteroaryl Ethers from Azine <i>N</i>-Oxides and Alcohols (2016)

The heteroaryl ether is an important structural feature in molecules of biological interest, yet it remains a challenge to synthesize. A new and practical method for the synthesis of heteroaryl ethers is reported. In the presence of PyBroP, a variety of nonaromatic alcohols readily add to azine N-oxides to afford the corresponding heteroaryl ethers. The reaction conditions are mild, economical, chemoselective, and compatible with a broad range of substrates. Thirty-eight examples are provided, as is a discussion of reaction optimization and mechanism.
Protective effect of low frequency low energy pulsing electromagnetic fields on acute experimental myocardial infarcts in rats (1999)

This series of experiments assesses the effect of exposure to low-frequency pulsing electromagnetic fields (PEMFs) in 340 rats with acute experimental myocardial infarcts. The left anterior descending artery was ligated with suture thread, and the rats underwent total body exposure to PEMFs until they were killed. Twenty-four hours after surgery, the necrotic area was evaluated by staining with triphenyltetrazolium chloride. A significant reduction of the necrotic area was observed in the animals exposed to PEMFs compared with the nonexposed controls. Exposure for up to 6 days does not appear to affect the area of necrosis, although in exposed animals an increase of vascular invasion of the necrotic area is observed: 24.3 % as against 11.3 % in controls. No effect on the necrotic area size from exposure was found when the left anterior descending artery was occluded for 60 min, followed by reperfusion. The results reported show that exposure to PEMFs is able to limit the area of necrosis after an acute ischemic injury caused by permanent ligation of the left anterior descending artery. These data are in agreement with the protective effect of PEMFs observed on acute ischemia in skin free flaps in rats and in cerebral infarcts in rabbits.
<i>N</i>‐Glycosylation of Yeast Proteins (1981)

The enzyme transferring the oligosaccharide from DolPP-(GlcNAc)2(Glc)3 to asparagine residues of glycoproteins has been solubilized from yeast membranes by extraction with detergents. Enzyme activity was tested by measuring transfer of the glycosyl moiety from DolPP-[14C]saccharides to the hexapeptide Tyr-Asn-Leu-Thr-Ser-Val. The rate of transfer was linear for 20 min, with about 40% of dolichyl-diphosphate-bound radioactivity transferred to the peptide. The solubilized enzyme has been characterized as follows: 1. The enzyme is most efficiently solubilized (60% of the membrane-associated activity) by 0.5% Nonidet P40 at a protein/detergent ratio of 2. Octylglucoside solubilizes one third of the activity, but strongly inhibits the reaction if present in the test at a concentration of 1%. 2. Divalent cations are absolutely required. 1 mM Mn2+ is optimal; Mg2+ at a concentration of 10mM yields only one third the activity observed with Mn2+. 3. The enzyme transfers besides dolichyl-diphosphate-bound (GlcNAc)2(Man)9(Glc)3 also (GlcNAc)2(Man)1 and (GlcNAc)2; the rate decreases in this order. No transfer is observed from DolPP-(GlcNAc)2(Man)9 and from DolPP-GlcNAc. 4. The Km value for DolPP-(GlcNAc)2(Man)9(Glc)3 of 0.5 microM does not differ significantly from that for DolPP-(GlcNAc)2 of 1.2 microM. A broad pH-optimum for the reaction with both substrates was found between 6.5 and 7.7. 5. However, a clear difference in Km values for the hexapeptide was observed with difference dolichol-linked sugar derivatives. With DolPP-(GlcNAc)2 a peptide concentration of 0.6 mM resulted in half-maximal transfer rate, whereas 0.05 mM peptide were sufficient with DolPP-(GlcNAc)2(Man)9(Glc)3 as donor.
Development of a high power 12GHz PPM focused traveling wave tube (1975)

An analytical and experimental program to demonstrate the technical feasibility of a high efficiency coupled cavity traveling wave tube with periodic permanent magnetic focusing operating at 12.06 GHz, with 1 to 2 kilowatts CW power is described. Such a tube would ultimately be used for broadcasting power transmission from a satellite. The electron gun was designed to be demountable with a replaceable cathode, and the tube to be operable in a bakeable vacuum chamber with its collector replaced by a collector. Therefore, the high efficiency design was concerned with the slow wave structure only, utilizing velocity resynchronization. A special adapter was designed which incorporated an electromagnet refocusing section and a collector baseplate to facilitate testing the collector. CW output power of 1000 watts yielding 21.5% electronic efficiency was demonstrated, with a minimum output power of 525 watts across the specified 160 MHz bandwidth.
An isotype-specific trans-acting factor is defective in a mutant B cell line that expresses HLA-DQ, but not -DR or -DP. (1991)

The B lymphoblastoid cell line clone 13 (a subclone of the mutant cell line P3JHR-1) has been found to express high levels of HLA-DQ; by contrast, HLA-DR and -DP antigens are not expressed and cannot be induced by interferon gamma. Northern blot analysis using gene-specific probes indicated that the lack of surface expression of the DR and DP antigens is due to a marked decrease in the levels of steady-state RNA for both the alpha and beta chains. Southern blots demonstrated that none of the transcriptionally repressed genes are grossly deleted. Preparations of interspecific transient heterokaryons between clone 13 and the class II antigen-positive murine B cell lymphoma, A20, resulted in reactivation of the DRA gene and surface expression of both the DR and DP molecules. The efficiency of the DRA promoter relative to the DQB promoter is markedly and specifically diminished in clone 13 (P3JHR-1) as compared with the parental cell line, Jijoye, as assayed both by transient expression of appropriate chloramphenicol acetyltransferase gene (CAT) constructs and by in vitro transcription analysis. These data clearly demonstrate the existence of an isotype-specific trans-acting factor, and provide direct evidence that the highly homologous class II genes have distinct regulatory mechanisms.
The Effect of Endovascular Irradiation on Platelet Recruitment at Sites of Balloon Angioplasty in Pig Coronary Arteries (2000)

Endovascular irradiation at 15Gy or 30Gy after balloon angioplasty results in incomplete endothelial recovery, impaired resolution of intramural hemorrhage, and a dose-dependent increase in platelet recruitment at 1 month.
<title>Progress in the <emph type="1">en-face</emph> optical coherence tomography applied to eye imaging</title> (2007)

A review is presented of the research on high resolution imaging of the eye based on en-face OCT. This can provide a dual display of images with different depth resolutions, where the two images are OCT and the other confocal. Two applications are presented: (i) OCT/ICG systems where the confocal channel is tuned to the fluorescence of indocyanine green and (ii) aberration corrections in both OCT and confocal channels using closed loop adaptive optics for enhanced contrast and transversal resolution.
Concepto de la vida en Góngora: una orientación del desengaño barroco (2008)

El desengaño es el tópico del Barroco, sobre todo del Barroco español. Aun sin recordar\nel título de la clásica obra de Luis Rosales1, cualquier manual de literatura española no\ndeja de citar estas palabras en las páginas dedicadas a la época2. En realidad, otros tópicos\nrelacionados con el Barroco, como el sueño, el tiempo o la fugaciadad de la vida, simbolizados\npor las ruinas y flores, se unen unánimemente al sentimiento del desengaño. Y,\ncon ello, los manuales literarios enfrentan el pesimismo y la artificialidad del Barroco al\nvitalismo y naturalismo del Renacimiento. Pero ¿es cierta esta dicotomía?
Macromolecular Translocation Inhibitor II (Zn2+-binding Protein, Parathymosin) Interacts with the Glucocorticoid Receptor and Enhances Transcription in Vivo (2005)

Macromolecular translocation inhibitor II (MTI-II), which was first identified as an in vitro inhibitor of binding between the highly purified glucocorticoid receptor (GR) and isolated nuclei, is an 11.5-kDa Zn(2+)-binding protein that is also known as ZnBP or parathymosin. MTI-II is a small nuclear acidic protein that is highly conserved in rats, cows, and humans and widely distributed in mammalian tissues, yet its physiological function is unknown. To elucidate its in vivo function in relation to GR, we transiently transfected mammalian cells with an expression plasmid encoding MTI-II. Unexpectedly, we found that the expression of MTI-II enhances the transcriptional activity of GR. The magnitude of the transcriptional enhancement induced by MTI-II is comparable with that induced by the steroid receptor coactivator SRC-1. In contrast, MTI-II had little effect on the transcriptional activity of estrogen receptor. Immunoprecipitation analysis showed that in the presence of glucocorticoid hormone, GR coprecipitates with MTI-II, and, vice versa, MTI-II coprecipitates with GR. The expression of various deletion mutants of MTI-II revealed that the central acidic domain is essential for the enhancement of GR-dependent transcription. Microscopic analysis of MTI-II fused to green fluorescent protein and GR fused to red fluorescent protein in living HeLa cells showed that MTI-II colocalizes with GR in discrete subnuclear domains in a hormone-dependent manner. Coexpression of MTI-II with the coactivator SRC-1 or p300 further enhances GR-dependent transcription. Immunoprecipitation analysis showed that in the presence of glucocorticoid hormone, p300 and CREB-binding protein are coprecipitated with MTI-II. Furthermore, the knockdown of endogenous MTI-II by RNAi reduces the transcriptional activity of GR in cells. Moreover, expression of MTI-II enhances the glucocorticoid-dependent transcription of the endogenous glucocorticoid-inducible enzyme in cells. Taken together, these results indicate that MTI-II enhances GR-dependent transcription via a direct interaction with GR in vivo. Thus, MTI-II is a new member of the GR-coactivator complex.
Properties of bisphosphonates in the 13762 rat mammary carcinoma model of tumor-induced bone resorption. (2003)

Bone metastasis from primary tumors is a clinically important complication of neoplastic progression. The role of parathyroid hormone-related protein (PTHrP) and transforming growth factor (TGF)-beta1 in this process has been clearly established. The current study describes an in vivo model of 13762 rat mammary carcinoma tumor cell-induced osteolysis in which PTHrP and TGF-beta1 expression is observed. Exposure of in vitro-cultured 13762 cells to doxorubicin, cis-platinum, carboplatin, methotrexate, 5-fluorouracil, paclitaxel, alendronate, risedronate, or pamidronate for 72 h resulted in varying effects on cell proliferation (IC(50) values of 0.005, 0.4, 1.9, >40, 17.9, 0.003, >40, >40, and 33.6 micro M, respectively). Tumor cells were implanted into the intramedullary space of the proximal tibia of rats, and the time course of tumor progression was evaluated using radiographic and microcomputed tomography scanning techniques. Trabecular bone mineral density, cortical bone mineral density, and whole bone mineral density were measured (in mg/cm(3)). In untreated animals, radiographic evidence of osteolysis was evident 7 days after implantation. Trabecular bone mineral density and whole bone mineral density were significantly decreased by 21 days after implantation (48% and 26%, respectively). Bisphosphonates showed broad protective activity against tumor-driven osteolysis, Immunohistochemical evaluation of s.c. and intratibially implanted cells demonstrated the expression of PTHrP and TGF-beta1. The results of this study demonstrate the ability of 13762 rat mammary carcinoma cells to elicit a measurable osteolysis and that bisphosphonates inhibit the tumor-induced bone resorption in this model.
A Novel Piezoelectric Strain Sensor for Simultaneous Damping and Tracking Control of a High-Speed Nanopositioner (2013)

This paper presents a novel piezoelectric strain sensor for damping and accurate tracking control of a high-speed nanopositioning stage. Piezoelectric sensors have the benefit of simple interface circuitry, low cost, high sensitivity, and high bandwidth. Although piezoelectric sensors have been successfully used as vibration sensors in smart structures, complications arise when they are used in a feedback loop for tracking. As piezoelectric strain sensors exhibit a capacitive source impedance, a high-pass filter is created, typically with a cut-off frequency of 1 to 10 Hz. This filter can cause significant errors and destabilize a tracking control system. Here, we overcome this problem by using a low-frequency bypass technique to replace the low-frequency component of the strain measurement with an estimate based on the open-loop system. Once the low-frequency filter is accounted for, any standard control system can be applied. In this paper, an analog integral resonant controller together with an integral tracking controller are implemented on a flexure-guided nanopositioner. The resulting closed-loop bandwidth is experimentally demonstrated to be 1.86 kHz. The nanopositioner is installed in an Atomic Force Microscope to obtain open- and closed-loop images at line rates of 40 and 78 Hz. Images recorded in closed loop show a significant improvement due to the elimination of nonlinearity.
Reduction of Serum Cholesterol in Postmenopausal Women With Previous Myocardial Infarction and Cholesterol Malabsorption Induced by Dietary Sitostanol Ester Margarine (1997)

Dietary use of sitostanol ester margarine normalizes LDL cholesterol in about one third of women with previous myocardial infarction, especially in those with high baseline absorption and low synthesis of cholesterol, and in combination with statins reduces the needed drug dose.
High performance reconfigurable multi-processor-based computing on FPGAs (2010)

Multi-processor architectures are a promising solution to provide the required computational performance for applications in the area of high performance computing. Multi- and many-core Systems-on-Chip offer the possibility to host an application, partitioned in a number of tasks, on the different cores on one silicon die. Unfortunately, a partitioning of the tasks near to the performance optimum is the challenge in this domain and often a show-stopper for the success story of multi- and many-core hardware. The missing feature of these architectures is runtime adaptivity of the underlying hardware, which offers to tailor the hardware to the application in order to meet the task mapping process coming from top-down development. Especially, this Meet-in-the-Middle solution offers the novel hardware and software approach of RAMPSoC, which is described in this paper.
Supporting long TCP options in Multipath TCP (2015)

The extensibility of TCP is severely limited by the Data Offset field
of the TCP header that limits the number of bytes that can be used in
each segment to transport options. This document considers Multipath
TCP as the starting point and analyses different alternatives to
improve the ability of Multipath TCP to transport TCP extensions.
Effect of chemical structures of polyimides on photosensitivity of liquid crystal alignment using a polarized UV exposure (1999)

Unidirectional liquid crystal (LC) alignment produced by polarized UV exposure was examined using polyimides (PIs) synthesized using different diamines. The dichroic ratio of the resulting LC cells suggests that the UV photosensitivity is primarily controlled by the chemical structures of the PIs used. The UV absorption and fluorescence spectra of the PI films, and molecular conformations of the diamines, indicate that the photosensitivity is controlled by the UV absorption efficiencies and molecular conformations of the PIs.
Task-Free Functional MRI in Cervical Dystonia Reveals Multi-Network Changes That Partially Normalize with Botulinum Toxin (2013)

Cervical dystonia is characterized by involuntary, abnormal movements and postures of the head and neck. Current views on its pathophysiology, such as faulty sensorimotor integration and impaired motor planning, are largely based on studies of focal hand dystonia. Using resting state fMRI, we explored whether cervical dystonia patients have altered functional brain connectivity compared to healthy controls, by investigating 10 resting state networks. Scans were repeated immediately before and some weeks after botulinum toxin injections to see whether connectivity abnormalities were restored. We here show that cervical dystonia patients have reduced connectivity in selected regions of the prefrontal cortex, premotor cortex and superior parietal lobule within a distributed network that comprises the premotor cortex, supplementary motor area, primary sensorimotor cortex, and secondary somatosensory cortex (sensorimotor network). With regard to a network originating from the occipital cortex (primary visual network), selected regions in the prefrontal and premotor cortex, superior parietal lobule, and middle temporal gyrus areas have reduced connectivity. In selected regions of the prefrontal, premotor, primary motor and early visual cortex increased connectivity was found within a network that comprises the prefrontal cortex including the anterior cingulate cortex and parietal cortex (executive control network). Botulinum toxin treatment resulted in a partial restoration of connectivity abnormalities in the sensorimotor and primary visual network. These findings demonstrate the involvement of multiple neural networks in cervical dystonia. The reduced connectivity within the sensorimotor and primary visual networks may provide the neural substrate to expect defective motor planning and disturbed spatial cognition. Increased connectivity within the executive control network suggests excessive attentional control and while this may be a primary trait, perhaps contributing to abnormal motor control, this may alternatively serve a compensatory function in order to reduce the consequences of the motor planning defect inflicted by the other network abnormalities.
Expanding horizons in complement drug discovery: challenges and emerging strategies (2017)

The complement system is best known for its role in innate immunity, providing a first line of defence against infection, maintaining tissue homeostasis by flagging apoptotic cells and debris for removal, and orchestrating crosstalk between adaptive and innate immunity. In a growing number of diseases, complement is known to drive pathogenesis or to contribute as an inflammatory amplifier of a disease trigger. Association of complement with common and devastating diseases has driven an upsurge in complement drug discovery, but despite a wealth of knowledge in the complexities of the cascade, and many decades of effort, very few drugs have progressed to late-stage clinical studies. The reasons for this are becoming clear with difficulties including high target concentration and turnover, lack of clarity around disease mechanism and unwanted side effects. Lessons learnt from drugs which are either approved, or are currently in late-stage development, or have failed and dropped off the drug development landscape, have been invaluable to drive a new generation of innovative drugs which are progressing through clinical development. In this review, the challenges associated with complement drug discovery are discussed and the current drug development landscape is reviewed. The latest approaches to improve drug characteristics are explored and those agents which employ these technologies to improve accessibility to patients are highlighted.
Pesquisando o lazer de um grupo de idosos no Brasil (2007)

Esta pesquisa exploratoria objetivou identificar e analisar o que os idosos que participam de um Projeto de Extensao Universitaria entendem por lazer, atraves de quais atividades o vivenciam e alguns fatores que interferem na fetivacao de suas experiencias. Constatou-se que o lazer assume funcoes de descanso e diversao, sendo o aspecto sociabilizacao fundamental para a escolha das atividades. As vivencias pertencem a todos os campos de interesses do lazer, ocorrem principalmente durante a semana e sao na maioria gratuitas, apesar de haver certas praticas pagas muito adotadas pelos idosos do grupo.
Pharmacokinetics of Intravesical Doxorubicin in Superficial Bladder Cancer Patients (1994)

The urine and plasma pharmacokinetics of intravesical doxorubicin were studied in 8 patients with a history of superficial bladder cancer. Patients received 6 weekly treatments of 40 mg. doxorubicin in 20 ml. physiological saline. Doxorubicin was detectable (0.2 ng./ml. or more) in plasma from 6 of 8 patients during the initial treatment. The maximal concentrations ranged from 0.5 to 4.5 ng./ml. (mean 1.4). Doxorubicin was not detected in plasma from 7 of 8 patients during treatment 2 and not detected in any patient during treatment 4. The doxorubicin concentrations in urine decreased to approximately 50% at 5 minutes after dosing due to dilution by post-catheterization residual urine, and decreased by a further 6-fold by the end of the 2-hour treatment due to urine production. The recovery of doxorubicin at the end of treatment averaged 88.3%, with an additional recovery of 3.7% during the subsequent 4 hours. Urinary pH (range 5.5 to 8.5) did not affect the stability nor the systemic absorption of doxorubicin. In conclusion, we found that for intravesical doxorubicin therapy there was insignificant systemic exposure to doxorubicin, the highest systemic absorption from the bladder occurred shortly after surgery, there was high target site (bladder tissue) specificity, insignificant metabolism and/or degradation of doxorubicin, and dilution of urinary doxorubicin concentrations and, therefore, decreased tumor exposure to the drug due to residual urine and urine production.
Extracellular release of protease III (<i>ptr</i>) by <i>Escherichia coli</i> K12 (1991)

Escherichia coli strains carrying the protease III structural gene (ptr) on a plasmid secreted the protein into the growth medium. Plasmid-encoded beta-lactamase and chloramphenicol acetyl transferase, which served as periplasmic and cytoplasmic markers during cell fractionation, were not released into the growth medium. There appeared to be some strain dependence on the proficiency of the secretion system. Protease III was not detectably processed upon export through the outer cell membrane.
<title>Tools for texture- and color-based search of images</title> (1997)

Currently there are quite a few image retrieval systems that use color and texture as features to search images. However, by using global features these methods retrieve results that often do not make much perceptual sense. It is necessary to constrain the feature extraction within homogeneous regions, so that the relevant information within these regions can be well represented. This paper describes our recent work on developing an image segmentation algorithm which is useful for processing large and diverse collections of image data. A compact color feature representation which is more appropriate for these segmented regions is also proposed. By using the color and texture features and a region-based search, we achieve a very good retrieval performance compared to the entire image based search.