gebhart/patrepeval huggingface dataset:
Altering substrate preference of carboxypeptidase Y by a novel strategy of mutagenesis eliminating wild type background (1993)

To change the substrate preference of carboxypeptidase Y the putative substrate binding pocket was subjected to random mutagenesis. Based upon the three-dimensional structure of a homologous enzyme from wheat, we hypothesized that Tyr147, Leu178, Glu215, Arg216, Ile340 and Cys341 are the amino acid residues of carboxypeptidase Y that constitute S1, the binding pocket for the penultimate amino acid side chain of the substrate. We developed a new and generally applicable mutagenesis strategy to facilitate efficient screening of a large number of mutants with multiple changes in carboxypeptidase Y. The key feature is the elimination of wild type background by introducing a nonsense codon at each target site for subsequent mutagenesis by degenerate oligonucleotides. The entire hypothesized S1 binding pocket and subsets of it were subjected to saturation mutagenesis by this strategy, and screening yielded a number of mutant enzymes which have up to 150 times more activity (kcat/Km) towards CBZ-Lys-Leu-OH than the wild type enzyme. All selected mutants with increased activity have mutations at position 178. Mutagenesis of positions 215 and 216 has virtually no effect on the activity, while mutating positions 340 and 341 generally reduces activity.
Organic sulfites containing a 1,2-oxazine ring. (1980)

The reaction of 5-hydroxy-2-phenyltetrahydro-2H-1, 2-oxazin-3-one derivatives (2) with thionyl chloride in the presence of pyridine afforded a mixture of stereoisomers of bis (3-oxo-2-phenyltetrahydro-2H-1, 2-oxazine-5-yl) sulfite derivatives (3) in total yields of 75-83%. On high-performance liquid chromatography, two meso-diastereoisomers (3-I and 3-II) and a racemic compound (3-III) were isolated.
The Fcγ Receptor–Mediated Respiratory Burst of Rolling Neutrophils to Cytokine-Activated, Immune Complex-Bearing Endothelial Cells Depends on L-Selectin But Not on E-Selectin (1998)

Intracellular H2O2 generation, as a measure of the respiratory burst, was determined after stimulation of neutrophils by immune complex (IC)-bearing human umbilical vein endothelial cells. Under static conditions, neutrophils basically responded to the immune deposits on resting endothelial cells. The rotating shear forces of approximately 0.7 dynes/cm2, corresponding to the physiological flow in postcapillary venules, completely abolished this basal H2O2 generation. After activation of the IC-bearing endothelial layers with interleukin-1 (IL-1) or tumor necrosis factor (TNF), or both, for 4 hours, rolling adhesion of the neutrophils was induced, accompanied by considerable H2O2 production. The neutrophil respiratory burst was prominently inhibited by anti-FcgammaRIII MoAb 3G8 (72.4%), and partially by MoAb 2E1 against FcgammaRII (38.5%). Both MoAbs together inhibited the Fc-mediated H2O2 generation by 93. 4%. The respiratory burst and rolling adhesion were markedly blocked by MoAb LAM1-3 against L-selectin (91.3%), whereas the nonfunctional anti-L-selectin MoAb LAM1-14 was ineffective. F(ab)2' fragments of MoAb 7A9 against E-selectin inhibited neutrophil rolling by 98.6%, but not the respiratory burst. Moreover, rolling adhesion of neutrophils and the related oxidative burst were CD11b/CD18- independent. In summary, L-selectin has a unique auxiliary function in triggering the FcgammaR-mediated respiratory burst of rolling neutrophils to IC-bearing endothelial cells, thereby substituting CD11b/CD18 under conditions of flow.
Applications of Noble Gas Radiation Detectors to Counter-terrorism (2002)

Radiation detectors are essential tools in the detection, analysis and disposition of potential terrorist devices containing hazardous radioactive and/or fissionable materials. For applications where stand‐off distance and source shielding are limiting factors, large detectors have advantages over small ones. The ability to distinguish between Special Nuclear Materials and false‐positive signals from natural or man‐made benign sources is also important. Ionization chambers containing compressed noble gases, notably xenon and helium‐3, can be scaled up to very large sizes, improving the solid angle for acceptance of radiation from a distant source. Gamma spectrometers using Xe have a factor of three better energy resolution than NaI scintillators, allowing better discrimination between radioisotopes. Xenon detectors can be constructed so as to have extremely low leakage currents, enabling them to operate for long periods of time on batteries or solar cells. They are not sensitive to fluctuations in ambient temperature, and are therefore suitable for deployment in outdoor locations. Position‐sensitive 3He chambers have been built as large as 3000 cm2, and with spatial resolution of less than 1 mm. Combined with coded apertures made of cadmium, they can be used to create images of thermal neutron sources. The natural background of spallation neutrons from cosmic rays generates a very low count rate, so this instrument could be quite effective at identifying a man‐made source, such as a spontaneous fission source (Pu) in contact with a moderator (high explosive).
Anti-Inflammatory Activity of Gallic Acid (1992)

Gallic acid was found to possess antiinflammatory activity towards zymosan-induced acute food pad swelling in mice. In vitro studies on the mode of action of gallic acid revealed that this compound interferes with the functioning of polymorphonuclear leukocytes (PMNs). Scavenging of superoxide anions, inhibition of myeloperoxidase release and activity as well as a possible interference with the assembly of active NADPH-oxidase may account for the inhibition of inflammatory process by gallic acid. Structure-activity relationship analysis showed that the o-dihydroxy group of gallic acid is important for the inhibitory activity in vitro.
Bacillus subtilis mutS mutL operon: identification, nucleotide sequence and mutagenesis (1996)

The Bacillus subtilis mutS and mutL genes, involved in the DNA mismatch repair system, have been cloned and characterized. From sequence analysis the two genes appear to be organized in a single operon, located immediately downstream of the cotE gene (approximately 150 degrees on the genetic map). The deduced MutS protein is 49% identical to HexA and MutL is 46% identical to HexB of Streptococcus pneumoniae. Deletion of both mutS and mutL resulted in an increase in the frequency of spontaneous mutations and abolished the marker effect observed in transformation. The expression of the mut operon was studied with the use of a mutSL-lacZ transcriptional fusion. An increase in expression was observed during late exponential growth.
Multichannel imaging using diffractive optics (1993)

A multiple imaging system can produce a two-dimensional array of images from a single input object. The basic components of our implementation are a high-performance Fourier processor and a suitably designed diffraction grating that is placed in the frequency phase. We have made use of a single diffractive element Fourier transform lens, corrected for coma, astigmatism, and field curvature. The lens is designed to have the proper amount of distortion to produce an optical transform. The optical processing system consists of two of these lenses spaced a distance equal to the sum of their focal lengths. We employ an iterative algorithm to produce the necessary phase diffraction grating that generates a multiplicity of equal energy plane waves from a single incident plane wave. The method is based on an iterative Fourier- transform scheme that makes use of known constraints to synthesize the phase structure. The constraints include the known Fourier modulus (array of point sources), the phase-only requirement in the grating plane, and fabrication requirements such as discrete phase levels. The iterative algorithm provides an efficient means to calculate grating profiles that give rise to large arrays of images. System performance over a relatively wide field-of-view is characterized by calculating the modulation transfer function at various points in the image plane.
Generation of Narrow-Bandwidth Paired Photons: Use of a Single Driving Laser (2006)

We describe a generator of narrow-band paired photons. A single retroreflected Ti:sapphire laser is used to cool, render transparent, and parametrically pump a cloud of (87)Rb atoms. We attain a paired-photon generation rate into opposing fibers of 600 counts/s with an intensity correlation function that has a width of 5 ns, and violates the Cauchy-Schwartz criteria by a factor of 2000.
&lt;tex&gt;$M$&lt;/tex&gt;-Band Biorthogonal Interpolating Wavelets via Lifting Scheme (2004)

Recently, the lifting scheme was generalized to the multidimensional and multiband cases and was used to design M-band interpolating scaling filters and their duals. Based on this idea, we develop a new lifting pattern, namely, the progressive lifting pattern. This pattern allows us to pairwise generate M-band interpolating filterbanks and wavelets by the order from lowpass to highpass filters. A complete lifting procedure is divided into M - 1 simple steps, in each step, a pair of filters (the l'th filter and its dual) are generated. In this way, an M -band biorthogonal interpolating filterbank/wavelet is determined by M(M - 1) lifting filters. The first 2(M 1) lifting filters completely characterize the two scaling filters as well as the vanishing moments of bandpass and highpass filters; the residual (M - 1) (M - 2) lifting filters are used to pairwise optimize the bandpass and highpass filters in terms of the criterion of stopband energy minimization. The obtained M-band biorthogonal interpolating filterbanks and wavelets provide excellent frequency characteristics, in particular, low stopband sidelobes. Furthermore, the pattern is also utilized to design signal-adapted interpolating filterbanks and their rational coefficient counterparts in terms of subband coding gain. The obtained filterbanks achieve large subband coding gains. The rational coefficient filterbanks preserve the biorthogonality and allow wavelet transforms from integers to integers and a unifying lossy/lossless coding framework at the cost of a slight degradation in subband coding gain.
Résultats obtenus en fonds de poche à acier par la mise en place d'une couche de sécurité incurvée en blocs préfabriqués de bétons réfractaires (1991)

Les fonds de poches à acier classiques entraînent des pertes de métal de 10 à 15 pour mille. Les fonds de poches inclinés les réduisent, mais au prix d’infiltrations de métal et de soulèvements de ces fonds.Le présent texte expose la solution retenue à Sollac Dunkerque, basée sur une couche de sécurité ayant la forme d’une calotte sphérique, le trou de coulée se situant au point bas. Les détails de mise en œuvre et les résultats obtenus sont exposés.
Policy management of strategy (hoshin kanri) (2003)

Abstract This paper reports on an Economic and Social Research Council investigation of Policy Management (Hoshin Kanri) practice in UK‐based companies. It covers: The background to the emerging literature. The research applied a tracer approach where strategic objectives were followed by researchers in real time to see how these were developed, deployed and managed. The findings are presented under categories using each of the FAIR (focus, alignment, integration, review) framework areas for good practice strategic management. The characterizing features of Policy Management are summarized. Policy Management is compared to the Balanced Scorecard. Management by Objectives. The conclusion is that Policy Management is a good approach for building strategy into daily management on an organization‐wide basis. Copyright © 2003 John Wiley & Sons, Ltd.
Foveal Shape and Structure in a Normal Population (2011)

Foveal structure strongly correlates with its neurovascular organization. The findings support a developmental model in which the size of the FAZ determines the extent of centrifugal migration of inner retinal layers, which counteracts in some way the centripetal packing of cone photoreceptors.
Metabolic and transcriptomic signatures of rice floral organs reveal sugar starvation as a factor in reproductive failure under heat and drought stress (2015)

Heat and drought stress are projected to become major challenges to sustain rice (Oryza sativa L.) yields with global climate change. Both stresses lead to yield losses when they coincide with flowering. A significant knowledge gap exists in the mechanistic understanding of the responses of rice floral organs that determine reproductive success under stress. Our work connects the metabolomic and transcriptomic changes in anthers, pistils before pollination and pollinated pistils in a heat-tolerant (N22) and a heat-sensitive (Moroberekan) cultivar. Systematic analysis of the floral organs revealed contrasts in metabolic profiles across anthers and pistils. Constitutive metabolic markers were identified that can define reproductive success in rice under stress. Six out of nine candidate metabolites identified by intersection analysis of stressed anthers were differentially accumulated in N22 compared with Moroberekan under non-stress conditions. Sugar metabolism was identified to be the crucial metabolic and transcriptional component that differentiated floral organ tolerance or susceptibility to stress. While susceptible Moroberekan specifically showed high expression of the Carbon Starved Anthers (CSA) gene under combined heat and drought, tolerant N22 responded with high expression of genes encoding a sugar transporter (MST8) and a cell wall invertase (INV4) as markers of high sink strength.
Voltage spectra of two-phase PWM techniques in inverter fed AC drives (2002)

The voltage spectra of different types of two-phase PWM techniques for three-phase voltage inverters are investigated and compared. Different PWM control methods are suggested and adequate analytical equations of the motor voltage harmonics are given. The two-phase PWMs, however, for the low fundamental voltage region and the same commutation frequency of the inverter results in considerably higher voltage harmonics and, therefore, higher motor harmonic losses and torque pulsations than the three-phase modulation. The two-phase PWMs can only produce better results than the three-phase ones in the high voltage region. The theoretical results are verified by computer calculations as well as by means of simulation and experimental investigations.
Improving Urban Road Extraction in High-Resolution Images Exploiting Directional Filtering, Perceptual Grouping, and Simple Topological Concepts (2006)

In this letter, the problem of detecting urban road networks from high-resolution optical/synthetic aperture radar (SAR) images is addressed. To this end, this letter exploits a priori knowledge about road direction distribution in urban areas. In particular, this letter presents an adaptive filtering procedure able to capture the predominant directions of these roads and enhance the extraction results. After road element extraction, to both discard redundant segments and avoid gaps, a special perceptual grouping algorithm is devised, exploiting colinearity as well as proximity concepts. Finally, the road network topology is considered, checking for road intersections and regularizing the overall patterns using these focal points. The proposed procedure was tested on a pair of very high resolution images, one from an optical sensor and one from a SAR sensor. The experiments show an increase in both the completeness and the quality indexes for the extracted road network
Number-resolved imaging of excited-state atoms using a scanning autoionization microscope (2013)

We report on a scanning microscopy technique for atom-number-resolved imaging of excited-state atoms. A tightly focused laser beam leads to local autoionization and the resulting ions are counted electronically. Scanning the beam across the cloud builds up an image of the density distribution of excited atoms, with access to the full counting statistics at each spatial sampling point and an overall detection efficiency of $21%$. We apply this technique to the measurement of a spatially inhomogeneous electric field with a spatial resolution of 50 $\ensuremath{\mu}$m and a sensitivity to electric-field gradients of 0.04 V cm${}^{\ensuremath{-}2}$.
Fluoreszenzfarbstoffe mit großen Stokes‐Shifts – lösliche Dihydropyrrolopyrroldione (1987)

Abstract Die Synthese von 3,6‐Diaryl‐2,5‐dihydropyrrolo[3,4‐ c ]pyrrol‐1,4‐dionen 1a–d und 3,6‐Diaryl‐2,5‐dihydro‐2,5‐dimethylpyrrolo[3,4‐ c ]pyrrol‐1,4‐dionen e–h wird beschrieben. Durch Einführen von tert ‐Butylgruppen in die Arylreste werden leichtlösliche Fluoreszenzfarbstoffe erhalten. Über den Mechanismus einer konformativen Umwandlung nach der Anregung werden Stokes‐Shifts bis zu 70 nm bei Fluoreszenzquantenausbeuten von bis zu 95% erzielt.
Gestational and Lactational Exposure of Rats to Xenoestrogens Results in Reduced Testicular Size and Sperm Production (1995)

This study assessed whether exposure of male rats to two estrogenic, environmental chemicals, 4-octylphenol (OP) and butyl benzyl phthalate (BBP) during gestation or during the first 21 days of postnatal life, affected testicular size or spermatogenesis in adulthood (90-95 days of age). Chemicals were administered via the drinking water or concentrations of 10-1000 micrograms/l (OP) or 1000 micrograms/l (BBP), diethylstilbestrol (DES; 100 micrograms/l) and an octylphenol polyethoxylate (OPP; 1000 micrograms/l), which is a weak estrogen or nonestrogenic in vitro, were administered as presumptive positive and negative controls, respectively. Controls received the vehicle (ethanol) in tap water. In study 1, rats were treated from days 1-22 after births in studies 2 and 3, the mothers were treated for approximately 8-9 weeks, spanning a 2-week period before mating throughout gestation and 22 days after giving birth. With the exception of DES, treatment generally had no major adverse effect or body weight: in most instances, treated animals were heavier than controls at day 22 and at days 90-95. Exposure to OP, OPP, or BBP at a concentration of 1000 micrograms/1 resulted in a small (5-13%) but significant (p < 0.01 or p < 0.0001) reduction in mean testicular size in studies 2 and 3, an effect that was still evident when testicular weight was expressed relative to body, weight or kidney weight. The effect of OPP is attributed to its metabolism in vivo to OP. DES exposure caused similar reductions in testicular size but also caused reductions in body weight, kidney weight, and litter size. Ventral prostate weight was reduced significantly in DES-treated rats and to minor extent in OP-treated rats. Comparable but more minor effects of treatment with DES or OP on testicular size were observed in study 1. None of the treatments had any adverse effect on testicular morphology or on the cross-sectional area of the lumen or seminiferous epithelium at stages VII-VIII of the spermatogenic cycle, but DES, OP, and BBP caused reductions of 10-21% (p < 0.05 to p < 0.001) in daily sperm production. Humans are exposed to phthalates, such as BBP, and to alkylphenol polyethoxylates, such as OP, but to what extent is unknown. More detailed studies are warranted to assess the possible risk to the development of the human testis from exposure to these and other environmental estrogens.
Direct inhibition of growth and antagonism of insulin action by glucocorticoids in human breast cancer cells in culture. (1979)

We have examined the interaction of dexamethasone with the ZR75-1 human breast cancer cell line to determine if glucocorticoids might directly inhibit growth of breast cancer cells. Growth of these cells in serum-free medium was stimulated significantly by physiological concentrations of insulin (0.1 to 1.0 nM). Pharmacological concentrations of dexamethasone (10 nM) reduced cell number below that found in controls and nearly abolished the effect of insulin after several days in culture. Thymidine and uridine, but not leucine, incorporation into macromolecules or acetate incorporation into fatty acids were similarly inhibited by dexamethasone in the presence of absence of insulin. Dexamethasone did not inhibit insulin effects by altering insulin receptor affinity or concentration, as determined by Scatchard analyses of insulin binding. Net thymidine uptake into the trichloroacetic acid-soluble fraction of the cell was stimulated by insulin and inhibited by dexamethasone also inhibited thymidine kinase activity multiple potential sites of glucocorticoid action that directly oppose the effects of insulin. They also suggest that glucocorticoids have a direct inhibitory effect on proliferation of human breast cancer cells, which may help explain breast tumor regression following pharmacological glucocorticoid therapy.
Directional needle for antegrade guide wire placement with vertical arterial puncture. (1988)

A directional needle with a closed pencil-point tip and a distal side hole was developed to permit antegrade guide wire placement by way of a 90 degrees puncture angle. It has been used in over 25 patients without technical difficulties or complications. It has been very effective for catheterization of the superficial femoral artery for angioplasty, diagnostic studies, and chemotherapy infusion, providing easy antegrade access in patients in whom the traditional antegrade approach may be difficult.
Characteristic Phase Transition of Aqueous Solution of Poly(<i>N</i>-isopropylacrylamide) Functionalized with Spirobenzopyran (2004)

A novel functional copolymer was synthesized by modifying poly(N-isopropylacrylamide) with spirobenzopyran. The phase transition properties of the aqueous solution of this copolymer exhibited a logic-gate response to the light irradiation and to increased temperature, which has three different modes depending on the pH of the solution. Especially, a great increase in turbidity was observed even in dilute aqueous solution containing only 0.10 wt % of the copolymer although the copolymer contained spirobenzopyrans by only 1.1 mol %. It was confirmed also that the spirobenzopyran residues were isomerized by the influence of thermally induced phase transition of the same system. The main chain of thermoresponsive polymer and photoresponsive chromophores, which are linked closely together, affected each other.
Treatment of advanced gastrointestinal tumors with genetically modified autologous mesenchymal stromal cells (TREAT-ME1): study protocol of a phase I/II clinical trial (2015)

EU Clinical Trials Register/European Union Drug Regulating Authorities Clinical Trials Database number: 2012-003741-15.
Histological cartilage changes in a rabbit model of osteoarthritis. (1987)

The anterior cruciate ligament was severed in the right knee of 36 rabbits which were then killed 12 weeks after surgery. Changes in water content and fixed charge density were correlated with the surface area of induced cartilage fibrillation. Histological changes including cartilage hypertrophy, reduced cell density, matrix alterations, cystic lesions, and enlarged perichondrocytic lacunae were found to precede cartilage fibrillation. The observed histological changes are in agreement with an enzymatic degradation of articular cartilage in osteoarthritis.