gebhart/patrepeval huggingface dataset:
N-ethoxycarbonyl-2-ethoxy-1,2-dihydroquinoline, amiloride analogues, and renal Na+/H+ antiporter (1987)

N-ethoxycarbonyl-2-ethoxy-1,2-dihydroquinoline (EEDQ) is a carboxyl-activating agent and has been shown to inhibit the renal Na+/H+ antiporter. The purposes of the present studies were to characterize the kinetics of inhibition of the Na+/H+ antiporter by EEDQ and to determine whether amiloride analogues affect the ability of EEDQ to inhibit the rate of Na+/H+ exchange. Brush-border membrane vesicles (BBMV) were prepared from rabbit kidneys; Na+/H+ exchange rate was assessed by the fluorescence quenching of acridine orange. EEDQ produced a concentration-dependent inhibition of Na+/H+ exchange; the effect was to decrease the maximum activity (Vmax) from 5.51 to 2.03 fluorescence units X mg protein-1 X S-1) and Km (from 14.1 to 8.7 mM) compared with control BBMV. Pretreatment of BBMV with amiloride before the addition of EEDQ maintained both Vmax and Km at values that were not significantly different from those for control BBMV. Compared with a series of analogues, amiloride was only the third most potent inhibitor of the rabbit renal Na+/H+ antiporter; amiloride, however, provided the greatest protection against inhibition of the antiporter by the subsequent addition of EEDQ. These findings suggest that the 2-carbonylguanidininum moiety and 6-chloro atom are important for binding of amiloride to sites at or near the antiporter; the group at position 5 is important in determining the ability of amiloride to protect against inhibition of the Na+/H+ antiporter by EEDQ. Finally, the ability of amiloride to protect against inactivation of the renal Na+/H+ antiporter by EEDQ is reversible.
The Chemistry of Nicotinamide Adenine Dinucleotide (NAD) Analogues Containing C-Nucleosides Related to Nicotinamide Riboside [1] (2002)

Oncolytic C-nucleosides, tiazofurin (2-beta-D-ribofuranosylthiazole-4-carboxamide) and benzamide riboside (3-beta-D-ribofuranosylbenzamide) are converted in cell into active metabolites thiazole-4-carboxamide- and benzamide adenine dinucleotide, TAD and BAD, respectively. TAD and BAD as NAD analogues were found to bind at the nicotinamide adenine dinucleotide (cofactor NAD) site of inosine monophosphate dehydrogenase (IMPDH), an important target in cancer treatment. The synthesis and evaluation of anticancer activity of a number of C-nucleosides related to tiazofurin and nicotinamide riboside then followed and are reviewed herein. Interestingly, pyridine C-nucleosides (such as C-nicotinamide riboside) are not metabolized into the corresponding NAD analogues in cell. Their conversion by chemical methods is described. As dinucleotides these compounds show inhibition of IMPDH in low micromolar level. Also, the synthesis of BAD in metabolically stable bis(phosphonate) form is discussed indicating the usefulness of such preformed inhibitors in drug development. Among tiazofurin analogues, Franchetti and Grifantini found, that the replacement of the sulfur by oxygen (as in oxazafurin) but not the removal of nitrogen (tiophenfurin) of the thiazole ring resulted in inactive compounds. The anti cancer activity of their synthetic dinucleotide analogues indicate that inactive compounds are not only poorly metabolized in cell but also are weak inhibitors of IMPDH as dinucleotides.
The Feasibility of Ethanol Production from Cheese Whey and Fruit Pomace in New York State (1981)

Crop Production/Industries, Production Economics, Resource/Energy Economics and Policy
E‐2‐Aroylmethylene‐3,4‐dihydro‐2H‐1,3‐benzoxazin‐4‐ones — A New Class of Heterocyclic Enamino Ketones (2004)

Abstract For Abstract see ChemInform Abstract in Full Text.
All-Optical Flip-Flop with Optical Clock Signal Using Mach-Zehnder Interferometer Bistable Laser Diode (2010)

We perform and demonstrate synchronous all-optical flip-flop operations with optical clock injection using Mach-Zehnder interferometer bistable laser diode. Saturable absorbers play the key role which allow broadband wavelength tuning of the clock wavelength.
Inhibitory effects of an anti-rheumatic agent T-614 on immunoglobulin production by cultured B cells and rheumatoid synovial tissues engrafted into SCID mice (2003)

We showed that T-614 inhibited Ig production by the cultured B cells and also decreased the high level of human IgG observed in SCID-HuRAg mice. These results may support its effect on plasma Ig in RA patients and provide insights into the mechanisms of its anti-rheumatic effect.
In Vivo Functional Analysis of the Human NF2 Tumor Suppressor Gene in Drosophila (2014)

The proper control of tissue growth is essential during normal development and an important problem in human disease. Merlin, the product of the Neurofibromatosis 2 tumor suppressor gene, has been extensively studied to understand its functions in growth control. Here we describe experiments in which we used Drosophila as an in vivo system to test the functions of the normal human NF2 gene products and patient-derived mutant alleles. Although the predominant NF2 gene isoform, isoform 1, could functionally replace the Drosophila Merlin gene, a second isoform with a distinct C-terminal tail could not. Immunofluorescence studies show that the two isoforms have distinct subcellular localizations when expressed in the polarized imaginal epithelium, and function in genetic rescue assays correlates with apical localization of the NF2 protein. Interestingly, we found that a patient-derived missense allele, NF2L64P, appears to be temperature sensitive. These studies highlight the utility of Drosophila for in vivo functional analysis of highly conserved human disease genes.
Porphyromonas gingivalis fimbria-stimulated bone resorption is inhibited through binding of the fimbriae to fibronectin (1997)

Our most recent study demonstrated that fibronectin is one of the Porphyromonas gingivalis fimbria-binding proteins. In this present study, we demonstrate with mouse embryonic calvarial cells that P. gingivalis fimbria-stimulated bone resorption is inhibited by human fibronectin. The fibronectin inhibition was dose and culture time dependent and was completely neutralized by antifibronectin antibody. The inhibitory action of fibronectin depended on fimbrial interaction with the heparin-binding and cell-attachment domains in the fibronectin structure.
New approaches in synthesis and characterization of dendritic macromolecules based on bis-mpa (2003)

First to fourth generation dendritic substituents based on 2,2-bis(hydroxymethyl)propionic acid and (1R,2S,5R)-menthoxyacetic acid were attached to 2-(hydroxymethyl)pyridinooxazoline and his[4-(hydroxymethyl)oxazoline] compounds. The new ligands obtained were assessed in palladium-catalyzed allylic alkylations. The first type of ligands exhibited enantioselectivity similar to that of a benzoyl ester derivative, whereas the latter type of ligands afforded products with higher selectivity than the analogous benzoyl ester. The activity of the dendritic catalysts decreased with increasing generation.
Arabidopsis Flower and Embryo Developmental Genes are Repressed in Seedlings by Different Combinations of Polycomb Group Proteins in Association with Distinct Sets of Cis-regulatory Elements (2016)

Polycomb repressive complexes (PRCs) play crucial roles in transcriptional repression and developmental regulation in both plants and animals. In plants, depletion of different members of PRCs causes both overlapping and unique phenotypic defects. However, the underlying molecular mechanism determining the target specificity and functional diversity is not sufficiently characterized. Here, we quantitatively compared changes of tri-methylation at H3K27 in Arabidopsis mutants deprived of various key PRC components. We show that CURLY LEAF (CLF), a major catalytic subunit of PRC2, coordinates with different members of PRC1 in suppression of distinct plant developmental programs. We found that expression of flower development genes is repressed in seedlings preferentially via non-redundant role of CLF, which specifically associated with LIKE HETEROCHROMATIN PROTEIN1 (LHP1). In contrast, expression of embryo development genes is repressed by PRC1-catalytic core subunits AtBMI1 and AtRING1 in common with PRC2-catalytic enzymes CLF or SWINGER (SWN). This context-dependent role of CLF corresponds well with the change in H3K27me3 profiles, and is remarkably associated with differential co-occupancy of binding motifs of transcription factors (TFs), including MADS box and ABA-related factors. We propose that different combinations of PRC members distinctively regulate different developmental programs, and their target specificity is modulated by specific TFs.
Arachidonic Acid Inhibits a Purified and Reconstituted Glutamate Transporter Directly from the Water Phase and Not via the Phospholipid Membrane (1995)

Glutamate is believed to be the major excitatory transmitter in the mammalian central nervous system. Keeping the extracellular concentration of glutamate low, the glutamate transporters are required for normal brain function. Arachidonic acid (AA) inhibits glutamate uptake in relatively intact preparations (cells, tissue slices, and synaptosomes (Rhoads, D.E., Ockner, R. K., Peterson, N. A., and Raghupathy, E. (1983) Biochemistry 22, 1965-1970 and Volterra, A., Trotti, D., Cassutti, P., Tromba, C., Salvaggio, A., Melcangi, R. C., and Racagni, G. (1992b) J. Neurochem. 59, 600-606). The present study demonstrates that the effect of AA occurs also in a reconstituted system, consisting of a purified glutamate transporter protein incorporated into artificial cell membranes (liposomes). The characteristics of the AA effect in this system and in intact cells are similar with regard to specificity, sensitivity, time course, changes in Vmax, and affinity. AA-ethyl ester is inactive, suggesting that the free carboxylic group is required for inhibitory activity. When incubated with proteoliposomes, AA (300 microM, 15 min) mostly partitions to the lipid phase (lipid/water about 95:5). However, uptake inhibition is abolished by rapid dilution (6.5-fold) of the incubation medium (water phase), a procedure that does not modify the amount of AA associated with lipids. On the contrary, inhibition remains sustained if the same dilution volume contains as little as 5 microM AA, a concentration inactive before saturation of liposome lipids with 300 microM AA. The same degree of inhibition (60%) is obtained by 5 microM AA following preincubation with the inactive AA-ethyl ester (300 microM) instead of AA. The lipids apparently inactivate AA by extracting it from the water phase. The results suggest that AA acts on the transporter from the water phase rather than via the membrane. This could be true for other proteins as well since gamma-aminobutyric acid uptake is similarly affected by AA.
Aminoglycoside Cross-Resistance in Mycobacterium tuberculosis Due to Mutations in the 5′ Untranslated Region of <i>whiB7</i> (2013)

Since the discovery of streptomycin's bactericidal activity against Mycobacterium tuberculosis, aminoglycosides have been utilized to treat tuberculosis (TB). Today, the aminoglycosides kanamycin and amikacin are used to treat multidrug-resistant (MDR) TB, and resistance to any of the second-line injectable antibiotics, including kanamycin, amikacin, or capreomycin, is a defining characteristic of extensively drug-resistant (XDR) TB. Resistance to kanamycin and streptomycin is thought to be due to the acquisition of unlinked chromosomal mutations. However, we identified eight independent mutations in the 5' untranslated region of the transcriptional activator whiB7 that confer low-level resistance to both aminoglycosides. The mutations lead to 23- to 145-fold increases in whiB7 transcripts and subsequent increased expression of both eis (Rv2416c) and tap (Rv1258c). Increased expression of eis confers kanamycin resistance in these mutants, while increased expression of tap, which encodes an efflux pump, is a previously uncharacterized mechanism of low-level streptomycin resistance. Additionally, high-level resistance to streptomycin arose at a much higher frequency in whiB7 mutants than in a wild-type (WT) strain. Although whiB7 is typically associated with intrinsic antibiotic resistance in M. tuberculosis, these data suggest that mutations in an uncharacterized regulatory region of whiB7 contribute to cross-resistance against clinically used second-line antibiotics. As drug resistance continues to develop and spread, understanding the mechanisms and molecular basis of antibiotic resistance is critical for the development of rapid molecular tests to diagnose drug-resistant TB strains and ultimately for designing regimens to treat drug-resistant cases of TB.
Dual-Rail with Alternating-Spacer Security Latch Design (2005)

We present a new design for a dual-rail &amp; dual-spacer latch which exhibits totally symmetrical switching behaviour, which guarantees data independent power consumption and is therefore suitable for use in secure systems. We compare the simulation results with the latest security latches. 1
Nitroalkanes in C--C Bond Forming Reactions: a Crystal Structure of a Complex of a Guanidine Catalyst and a Nitroalkane Substrate. (1993)

1,5,7-Triazabicyclo[4.4.0]dec-5-ene, a good catalyst for nitroalkanes in C-C bond forming reactions, forms a 1:1 complex with phenylnitromethane as a substrate. The mode of complexation between the catalyst and the substrate is shown by a crystal structure 3
Purification of phospholamban and characterization of its antibodies. (1986)

Phospholamban was extracted from pig heart microsomal membranes with a methanol-chloroform (2:1) mixture. The proteolipid was further purified to electrophoretic homogeneity by chromatography in organic solvents and in SDS-containing medium. Purification was about 50-fold with respect to specific 32P-phospholamban radioactivity. Antisera were produced in rabbits against phospholamban. Electroblot analysis demonstrates specific binding of the antisera to purified phospholamban and to phospholamban in preparations of cardiac sarcoplasmic reticulum and sarcolemma.
Realistic Creativity Training for Innovation Practitioners: The Know–Recognize–React Model (2017)

IntroductionIt is widely accepted in academic circles that creative thinking is an important element in innovation (e.g., Amabile, 1996; Christiaans, 1992; Dorst & Cross, 2001). Creativity is moreover believed to be the necessary pre-condition for innovation; one may argue that without the presence of a creative act, idea, or output, no innovation will happen. Indeed, Amabile
Glow-plug Ignition of Ethanol Fuels under Diesel Engine Relevant Thermodynamic Conditions (2011)

<div class="section abstract"><div class="htmlview paragraph">The requirement of reducing worldwide CO₂ emissions and engine pollutants are demanding an increased use of bio-fuels. Ethanol with its established production technology can contribute to this goal. However, due to its resistive auto-ignition behavior the use of ethanol-based fuels is limited to the spark-ignited gasoline combustion process. For application to the compression-ignited diesel combustion process advanced ignition systems are required. In general, ethanol offers a significant potential to improve the soot emission behavior of the diesel engine due to its oxygen content and its enhanced evaporation behavior.</div><div class="htmlview paragraph">In this contribution the ignition behavior of ethanol and mixtures with high ethanol content is investigated in combination with advanced ignition systems with ceramic glow-plugs under diesel engine relevant thermodynamic conditions in a high pressure and temperature vessel. The investigation focuses on optimizing the injection conditions, especially injection pressure and rate. Optical measurements are performed by high speed imaging of the fuel injection and ignition, and evaluated in terms of ignition and flame propagation. The high speed imaging technology furthermore enables to gain information on the statistical behavior of the ignition process and thus provides a direct assessment of the repeatability of the ignition and combustion process.</div><div class="htmlview paragraph">The results of the ignition investigation aim at improving the understanding of the glow-plug-induced ignition process in order to provide a reliable ignition strategy for the diesel engine operation with fuel with high ethanol content. The results show that the favorable spray targeting relative to the glow-plug depends on the glow-plug design. Furthermore a moderate injection pressure improves the ignition reliability of the ethanol fuels. The latter leads to the hypothesis that reduced injection-induced shear rates improve the ignition behavior by diminishing shear-induced quenching in the ignition zone in the direct vicinity of the hot glow-plug surface.</div></div>
An Optical Bench for Electron Optical Studies (1948)

An evacuated chamber containing a heavy lathe bed for supporting and aligning optical parts, and means for moving the essential internal components from the exterior, is described. The construction is explained in detail. Stabilized high voltage to thirty kilovolts and stabilized low voltage supplies for energizing electromagnetic lens coils are provided. The equipment may be used to illustrate the operation of such electronic equipment as cathode-ray tubes, electron microscope and diffraction apparatus, or to study the properties of phosphors and optical components such as lenses, guns, and deflection electrodes.
Effects of MAO inhibitors upon MPTP mice chronically treated with suprathreshold doses of l -dopa (2000)

Groups of mice were administered either saline or 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) (2 X 40 mg / kg, s.c., separated by a 24-hour interval) 4-6 weeks prior to behavioural testing. At testing, all the MPTP-injected mice were repeatedly administered L-dopa (20 mg / kg, s.c., five times each week, Monday-Friday), by applying a procedure that induced a severe reduction of motor activity parameters from Day 1 to Day 25. Control (uninjected mice) received only saline and were retained only for neurochemical analysis. In each of three experiments, following the reduction of the activity-stimulating effects of L-dopa by repeated administration, a restorative effect of different monoamine oxidase (MAO) inhibitors was tested by co-administration of the test compounds (irreversible MAO-B inhibitor, reversible MAO-A inhibitors, or irreversible MAO-A / mixed MAO inhibitors) with L-dopa (20 mg / kg). In each case the MAO inhibitor was injected 60 min prior to L-dopa. L-Deprenyl (3 or 10 mg / kg, s.c.), in combination with L-dopa, reinstated locomotion and total activity, but not rearing, dose-dependently, in L-dopa-tolerant mice. The reversible MAO-A inhibitors, amiflamine and alpha-ethyltryptamine, in combination with L-dopa, reinstated locomotion and total activity, leaving rearing unaffected; Ro 41-1049 (3 mg / kg, s.c.) restored all three parameters of activity; locomotor activity was restored by all three doses (1, 3, and 10 mg / kg, s.c.). On the other hand, neither the irreversible MAO-A inhibitor, clorgyline, nor the mixed MAO inhibitor, phenelzine, produced any directly effective restorative increments. Neurochemical analysis confirmed the severe striatal dopamine depletion of MPTP-treated mice. These results demonstrate a synergistic and restorative action of combining certain MAO inhibitors, namely the reversible MAO-A inhibitors, with the suprathreshold dose of L-dopa in MPTP-treated, L-dopa-tolerant mice.
GAME THEORETIC TARGET ASSIGNMENT STRATEGIES IN COMPETITIVE MULTI-TEAM SYSTEMS (2005)

The task of optimally assigning military ordinance to enemy targets, often termed the Weapon Target Assignment (WTA) problem, has become a major focus of modern military thought. Current formulations of this problem consider the enemy targets as either passive or entirely defensive. As a result, the assignment problem is solved purely as a one sided team optimization problem. In practice, however, especially in environments characterized by the presence of an intelligent adversary, this one sided optimization approach has very limited use. The presence of an adversary often necessitates incorporating its intended actions in the process of solving the weapons assignment problem. In this dissertation, we formulate the weapon target assignment problem in the presence of an intelligent adversary within the framework of game theory. We consider two teams of opposing units simultaneously targeting each other and examine several possible game theoretic solutions of this problem. An issue that arises when searching for any solution is the dimensionality of the search space which quickly becomes overwhelming even for simple problems with a small number of units on each side. To solve this scalability issue, we present a novel algorithm called Unit Level Team Resource Allocation (ULTRA), which is capable of generating approximate solutions by searching within appropriate subspaces of the search space. We evaluate the performance of this algorithm on several realistic simulation scenarios. We also show that this algorithm can be effectively implemented in real-time as an automatic target assigning controller in a dynamic multi-stage problem involving two teams with large number of units in conflict.
The Effects of Surface Mapping Corrections with Synthetic-Aperture Focusing Techniques on Ultrasonic Imaging (1983)

Image processing to improve the resolution of ultrasonic imaging systems requires an accurate knowledge of the geometry and properties of the media through which the ultrasound travels. This is particularly true when a method such as the synthetic-aperture focusing technique (SAFT) is used. For SAFT to function properly, it is necessary to know accurately the path traveled by the ultrasound from transducer to target and back again. A form of SAFT imaging is described in which the imaging routine also constructs a map of the target surface. This map is then used to calculate accurately the propagation history of the ultrasound for the SAFT processing. The resolution and positional accuracy of unprocessed images, unmapped SAFT images, and surface mapped SAFT images are compared. All but the surface mapping images show significant errors in positional accuracy for relatively small surface deviations. The surface mapping correction, however, brings the imaging accuracy back to within the limits of the mechanical experimental error. A more severely distorted surface destroys the phase relationships required for processing unless the surface variations are accounted for. In addition, results achieved with a flat ultrasonic transducer suggest significant simplifications that may ease field implementation of SAFT systems.
Non‐Invasive and Minimally Invasive Diagnosis of Varices (2010)

This chapter contains sections titled: Introduction Possible alternatives to esophagogastroduodenoscopy (EGD) Conclusions References