gebhart/patrepeval huggingface dataset:
N,S-bis-fluorenylmethoxycarbonylglutathione: a new, very potent inhibitor of mammalian glyoxalase II. (1995)

A very potent competitive inhibitor of mammalian glyoxalase II activity, N,S-bis-fluorenylmethoxycarbonylglutathione (DiFMOC-G) has been synthesized and characterized. The Ki value for inhibition of glyoxalase II purified from calf liver is 0.08 microM. The Ki values for glyoxalase I inhibitions range from 285 to 500 fold higher than the values obtained for glyoxalase II inhibitions, depending on the source of the enzyme. Among other enzymes involved in glutathione metabolism, such as glutathione S-transferase, glutathione reductase, and glutathione peroxidase, only glutathione S-transferase is inhibited to a small extent by DiFMOC-G. Diesters of DiFMOC-G were prepared in order to improve transport of DiFMOC-G into mammalian tumor cells (rat adrenal pheochromocytoma, PC-12) in culture. Among the diesters synthesized, diisopropyl DiFMOC-G was found to be the most inhibitory to cell viability, with a [I]0.5 value of 3 microM.
Romania: the cost of scarce social policies – economic failure (2011)

This article questions the supposed efficiency and equity trade-off, presenting the Romanian case as an illustration of its failure. Scarce social policies have not made the Romanian economy more efficient; on the contrary, they have contributed to reducing productivity and speeding up recession, endangering the future long-term development of the country. Romanian social indicators are worrying: poverty is high; inequalities are growing; people's trust in institutions, in each other and in the future has reached its lowest level ever; and migration has been the solution chosen by many to overcome the difficulties of transition. Meanwhile, the domestic labour market faces penury of skilled labour in many sectors, in spite of really high unemployment, while the education system is suffering a deterioration in terms of quality and credibility. Far from being a solution, the recent measures taken by the government to reduce the deficit and balance the public budget will negatively affect the economy and retard the possibility of a more equitable society.
ChemInform Abstract: Antiviral Activity of Adamantyl‐Containing Heterocycles. (2002)

Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.
Consistency and set intersection (2002)

The study of local and global consistencies is an important topic in Constraint Networks (CN). For example, there are
Multiple inhibitory effects of garlic extracts on cholesterol biosynthesis in hepatocytes (1993)

Exposure of primary rat hepatocytes and human HepG2 cells to water-soluble garlic extracts resulted in the concentration-dependent inhibition of cholesterol biosynthesis at several different enzymatic steps. At low concentrations, sterol biosynthesis from [14C]acetate was decreased in rat hepatocytes by 23% with an IC50 (half-maximal inhibition) value of 90 micrograms/mL and in HepG2 cells by 28% with an IC50 value of 35 micrograms/mL. This inhibition was exerted at the level of hydroxymethylglutaryl-CoA reductase (HMG-CoA reductase) as indicated by direct enzymatic measurements and the absence of inhibition if [14C]mevalonate was used as a precursor. At high concentrations (above 0.5 mg/mL), inhibition of cholesterol biosynthesis was not only seen at an early step where it increased considerably with dose, but also at later steps resulting in the accumulation of the precursors lanosterol and 7-dehydrocholesterol. No desmosterol was formed which, however, was a major precursor accumulating in the presence of triparanol. Thus, the accumulation of sterol precursors seems to be of less therapeutic significance during consumption of garlic, because it requires concentrations one or two orders of magnitude above those affecting HMG-CoA reductase. Alliin, the main sulfur-containing compound of garlic, was without effect itself. If converted to allicin, it resulted in similar changes of the sterol pattern. This suggested that the latter compound might contribute to the inhibition at the late steps. In contrast, nicotinic acid and particularly adenosine caused moderate inhibition of HMG-CoA reductase activity and of cholesterol biosynthesis suggesting that these compounds participate, at least in part, in the early inhibition of sterol synthesis by garlic extracts.
Whispering Gallery Resonance from Self-Assembled Microspheres of Highly Fluorescent Isolated Conjugated Polymers (2015)

Self-assembly of highly fluorescent isolated conjugated polymers (ICPs), comprising alternating phenylene moieties with an insulating cyclic side chain and different arylene moieties, was comprehensively studied. Two out of nine ICPs were identified to form well-defined spheres of 1–6 μm diameter. The degree of twisting of the main chains was found to be an important structural factor enabling formation of spheres, for which dihedral angles >50° between the neighboring arylene moieties were required. A single microsphere with high sphericity exhibited whispering gallery mode (WGM) photoemission upon excitation with a focused laser. In this emission, sharp and periodic emission lines were superimposed on a broad photoemission spectrum. The WGM spectral profiles were very sensitive to the integrity of the spherical geometries and surface smoothness, which depends on the self-assembling condition as well as the structure of the polymer backbone. Microspherical optical resonators consisting of such highly fluorescent conjugated polymers are novel. They also present advantages in that (i) there is no need for a light waveguide and fluorescent-dye doping, (ii) its high refractive index is beneficial for light confinement, and (iii) the fabrication process is simple, not requiring sophisticated, costly microfabrication technology.
New oleanene-type triterpene saponins from Pueraria peduncularis (2002)

Two new oleanane-type triterpene saponins named pedunsaponins B (2) and C (3) were isolated from the roots of Pueraria peduncularis. Their structures were determined to be 3-O-(6-O-methyl)-beta-glucuronopyranosyl-3beta,15alpha-dihydroxyolean-12-en-16-one (2), and 3-O-beta-glucopyranosyl-(1 --> 3)-beta-glucuronopyranosyl-3beta,15alpha-dihydroxyoleana-12-en-16-one (3), on the basis of spectroscopic evidence.
Assay of Crystalline Insulin and of Serum Insulin-like Activity of Different Species on Adipose Tissue of the Rat, Mouse and Guinea Pig (1965)

MOST data concerning the measurement of serum insulin in human subjects and obtained by in vitro bioassays have employed the rat as experimental animal, using either the diaphragm or the epididymal adipose-tissue technics. Since these data have given rise to numerous speculations about the state of insulin in blood, and have furthermore contributed to current hypotheses concerning the pathogenesis of early human diabetes,1 2 3 4 it appeared pertinent to test their validity by varying the species employed in the bioassay procedure. Moreover, it appeared of interest to study the effects of various available highly purified insulins (human, pork, beef, rat and tuna . . .
Oxidative Cleavage of Olefins by In Situ-Generated Catalytic 3,4,5,6-Tetramethyl-2-iodoxybenzoic Acid/Oxone (2014)

Oxidative cleavage of a variety of olefins to the corresponding ketones/carboxylic acids is shown to occur in a facile manner with 3,4,5,6-tetramethyl-2-iodobenzoic acid (TetMe-IA)/oxone. The simple methodology involves mere stirring of the olefin and catalytic amount (10 mol %) of TetMe-IA and oxone in acetonitrile-water mixture (1:1, v/v) at rt. The reaction mechanism involves initial dihydroxylation of the olefin with oxone, oxidative cleavage by the in situ-generated 3,4,5,6-tetramethyl-2-iodoxybenzoic acid (TetMe-IBX), and oxidation of the aldehyde functionality to the corresponding acid with oxone. Differences in the reactivities of electron-rich and electron-poor double bonds have been exploited to demonstrate chemoselective oxidative cleavage in substrates containing two double bonds.
Chromatin Immunoprecipitation for Determining the Association of Proteins with Specific Genomic Sequences In Vivo (2004)

Chromatin immunoprecipitation (ChIP) is a powerful and widely applied technique for detecting the association of individual proteins with specific genomic regions in vivo. Live cells are treated with formaldehyde to generate protein-protein and protein- DNA cross-links between molecules in close proximity on the chromatin template in vivo. DNA sequences that cross-link with a given protein are selectively enriched and reversal of the formaldehyde cross-link permits recovery and quantitative analysis of the immunoprecipitated DNA. As formaldehyde inactivates cellular enzymes essentially immediately upon addition to cells, ChIP provides snapshots of protein-protein and protein- DNA interactions at a particular time point, and hence is useful for kinetic analysis of events occurring on chromosomal sequences in vivo. In addition, ChIP can be combined with microarray technology to identify the location of specific proteins on a genome-wide basis. This unit describes the ChIP protocol for Saccharomyces cerevisiae; however, it is also applicable to other organisms.
A dynamic trust-based context-aware secure authentication framework for pervasive computing environments (2010)

La prise en considération des exigences en matière de sécurité, de vie privée et de confiance au sein des environnements pervasifs (ubiquitaires) est indispensable à la fourniture des services personnalisés aux utilisateurs. L objectif de cette thèse est de disposer d une architecture souple et évolutive intégrant l authentification des utilisateurs, la préservation de leur vie privée et la gestion de la confiance en vue d optimiser la stratégie de contrôles d accès aux services personnalisés. La première contribution porte sur la proposition d un protocole d authentification mutuelle construit à partir de schémas cryptographiques robustes d établissement de clés basés sur les courbes elliptiques (MaptoPoint/Curve algorithm, Weil Pairing) et d un modèle dynamique basé sur les attributs issus des données contextuelles. La seconde contribution porte sur la conception d une nouvelle architecture bâti sur un modèle basé sur les attributs et organisée autour de 3 couches : la couche de contrôle de le vie privée qui assure la protection de la vie privée des utilisateurs en contrôlant leurs données personnelles, la couche d accès associant les processus d authentification et de contrôles d accès en intégrant des mécanismes dédiés à la gestion des paramètres de confiance et la couche de service pour la gestion des accès aux services selon le profil de l utilisateur et de son environnement. La troisième contribution porte sur le développement et la mise en œuvre d un prototype au sein de la plateforme dédiée à la fourniture de services du laboratoire Handicom de Telecom SudParis.
Thin film CIGS photovoltaic modules: monolithic integration and advanced packaging for high performance, high reliability and low cost (2011)

In recent years, thin-film photovoltaic companies started realizing their low manufacturing cost potential, and have been grabbing an increasingly larger market share. Copper Indium Gallium Selenide (CIGS) is the most promising thin-film PV material, having demonstrated the highest energy conversion efficiency in both cells and modules. However, most CIGS manufacturers still face the challenge of delivering a reliable and rapid manufacturing process that can scale effectively and deliver on the promise of this material system. HelioVolt has developed a reactive transfer process for CIGS absorber formation that has the benefits of good compositional control, and a fast high-quality CIGS reaction. The reactive transfer process is a two stage CIGS fabrication method. Precursor films are deposited onto substrates and reusable cover plates in the first stage, while in the second stage the CIGS layer is formed by rapid heating with Se confinement. HelioVolt also developed best-in-class packaging technologies that provide unparalleled environmental stability. High quality CIGS films with large grains were fabricated on the production line, and high-performance highreliability monolithic modules with a form factor of 120 cm &times; 60 cm are being produced at high yield and low cost. With conversion efficiency levels around 14% for cells and 12% for modules, HelioVolt is commercializing the process on its first production line with 20 MW capacity, and is planning its next GW-scale factory.
Reduced loss and improved mode discrimination in resonant optical waveguide arrays (2012)

Coherent laser arrays designed using resonant optical waveguides (ROWs) have proven to offer one of the most promising methods of monolithic beam combining in diode lasers. However, the high lateral transmission that provides strong optical coupling also leads to increased loss – a detriment to laser efficiency and performance. Presented is a derivation of additional design rules to eliminate lateral radiation loss from ROW arrays while still maintaining all the strong coupling properties. Additionally, it is speculated that improved mode discrimination and enhanced field uniformity should result from the proposed design modifications.
Moxifloxacin Replacement in Contemporary Tuberculosis Drug Regimens Is Ineffective against Persistent Mycobacterium tuberculosis in the Cornell Mouse Model (2018)

Tuberculosis (TB), which is caused by <i>Mycobacterium tuberculosis</i>, remains a leading killer worldwide, and disease control is hampered by the ineffective control of persistent infections. Substitution of moxifloxacin for isoniazid or ethambutol in standard anti-TB regimens reduces the treatment duration and relapse rates in animal studies, and 4-month regimens were not noninferior in clinical trials. Resuscitation-promoting factor (RPF)-dependent bacilli have recently been implicated in <i>M. tuberculosis</i> persistence. We aimed to investigate the therapeutic effects of the substitution of moxifloxacin for a drug used in the standard drug regimen in eradicating CFU count-positive and RPF-dependent persistent <i>M. tuberculosis</i> using the Cornell murine model. <i>M. tuberculosis</i>-infected mice were treated with regimens in which either isoniazid or ethambutol was replaced by moxifloxacin in the standard regimen. The efficacy of the regimens for bacterial CFU count elimination and removal of persistent tubercle bacilli, evaluated using culture filtrate (CF) derived from <i>M. tuberculosis</i> strain H37Rv, was compared to that of the standard regimen. We also measured disease relapse rates. The regimen in which moxifloxacin replaced isoniazid achieved total organ CFU count clearance at 11 weeks posttreatment, which was faster than that by the standard regimen (14 weeks), and showed a 34% lower relapse rate. The regimen in which moxifloxacin replaced ethambutol was similar to standard regimens in these regards. Importantly, neither the regimen in which moxifloxacin replaced isoniazid or ethambutol nor the standard regimen could remove CF-dependent persistent bacilli. The finding of CF-dependent persistent <i>M. tuberculosis</i> in TB treatment requires confirmation in human studies and has implications for future drug design, testing, and clinical applications.
ChemInform Abstract: TRANSFER OF A DIMEDONYL FRAGMENT IN THE REACTION OF MESOIONIC 1,3,4‐TRIAZOLE‐5‐THIONES WITH PHENYLDIMEDONYLIODONE (1981)

Abstract Die mesoionischen Triazolthione (I) reagieren mit dem mesoionischen Phenyl‐dimedonyl‐iodon (II) zu den Thioethern (III).
In-vitro-Evaluation des therapeutischen Potenzials von Masitinib für kanine Prostatakarzinome (2020)

Einleitung Beim Hund haben Prostatakarzinome eine sehr schlechte Prognose und die therapeutischen Möglichkeiten sind limitiert. Als neue Tumortherapeutika werden einige Tyrosinkinaseinhibitoren (TKI) für bestimmte Tumoren erfolgreich eingesetzt und weitere befinden sich in klinischen Prüfungen beim Menschen. So befindet sich u. a. der für den Hund zur Behandlung des Mastzelltumors zugelassene TKI Masitinib in einer klinischen Phase-III-Studie beim Menschen zur Behandlung des metastasierten, kastrationsresistenten Prostatakarzinoms.
Hypoxia-inducible factors, hypoxia, and tumor angiogenesis (2006)

It will be important to further characterize the specific roles of hypoxia-inducible factor-1alpha and hypoxia-inducible factor-2alpha during tumorigenesis to design therapies targeting the relevant isoform for specific diseases. It is also necessary to investigate the effect of reducing hypoxia-inducible factor levels on other angiogenic factors.
A New Diskless Checkpointing Approach for Multiple Processor Failures (2010)

Diskless checkpointing is an important technique for performing fault tolerance in distributed or parallel computing systems. This study proposes a new approach to enhance neighbor-based diskless checkpointing to tolerate multiple failures using simple checkpointing and failure recovery operations, without relying on dedicated checkpoint processors. In this scheme, each processor saves its checkpoints in a set of peer processors, called checkpoint storage nodes. In return, each processor uses simple XOR operations to store a collection of checkpoints for the processors for which it is a checkpoint storage node. This study defines the concept of safe recovery criterion, which specifies the requirement for ensuring that any failed processor can be recovered in a single step using the checkpoint data stored at one of the surviving processors, as long as no more than a given number of failures occur. This study further identifies the necessary and sufficient conditions for satisfying the safe recovery criterion and presents a method for designing checkpoint storage node sets that meet these requirements. The proposed scheme allows failure recovery to be performed in a distributed manner using XOR operations.
Neutrophils and mast cells. I. Human neutrophil-derived histamine-releasing activity. (1987)

Histamine release occurs during the late phase allergic reaction concomitantly with neutrophil (PMN) infiltration. To determine whether PMN might release a factor capable of causing histamine release, supernatants generated by incubating human PMN in the presence or absence of specific activators were added to rat basophilic leukemia cells (RBL) and histamine release was measured. PMN supernatants from 17 of 21 donors induced noncytotoxic histamine release. Neutrophil-derived histamine-releasing activity, termed HRA-N, was dose-dependent and supernatants from greater than or equal to 10(7) PMN/ml caused 6 to 27% net histamine release from RBL. PMN supernatants induced histamine release as effectively as did intact PMN cocultured with RBL. The capacity of various donors to generate HRA-N was not related to atopic status or gender but was inversely related to the proportion of eosinophils (EOS) contaminating the PMN isolate (the larger the proportion of EOS, the lower the histamine release). Addition of EOS to PMN during the generation of HRA-N completely inhibited histamine-releasing activity. HRA-N was not released from mononuclear cells or platelets contaminating the PMN preparation. HRA-N release was not increased by the presence of either serum-treated zymosan or phorbol myristate acetate, agents that caused dose-related release of PMN granule enzymes. Indeed, HRA-N was released from unstimulated PMN in the complete absence of granule enzyme release. HRA-N release was detectable by 15 min and the majority of release occurred between 45 and 60 min of incubation. Thus, the data indicate that HRA-N is released spontaneously from human PMN and that HRA-N release is independent of primary or secondary PMN granule release. It is attractive to suggest that release of HRA-N by PMN might act to recruit mast cells or basophils into participating in acute inflammatory reactions.
The Role of the IGF System in Cancer: From Basic to Clinical Studies and Clinical Applications (2002)

Insulin-like growth factors (IGFs) are important mediators of growth, development, and survival, are synthesized by almost any tissue in the body, and their action is modulated by a complex network of molecules, including binding proteins, proteases and receptors, which all comprise the IGF system. Evidence from in vitro and animal studies suggests that overexpression of IGFs by cancer cells and/or the nearby stroma as well as the type IGF-I receptor by the cancer cells may play a significant role in establishing a transformed phenotype in an increasing number of malignancies. More specifically, IGFs may promote cell cycle progression and inhibition of apoptosis either by directly associating with other growth factors or indirectly by interacting with other molecular systems which have an established role in carcinogenesis and cancer promotion, such as the steroid hormones and integrins. In addition, a growing number of epidemiologic studies suggest that increased serum levels of IGFs and/or altered levels of their binding proteins are associated with increased risk for developing several malignancies. These data indicate that IGF dysregulation should now be considered as an important independent factor for cancer risk, and a potential target for novel antineoplastic therapies and/or preventative strategies in high-risk groups.
Anti-(U1)snRNP Autoantibodies Inhibit Homologous Pairing Activity of the Human Recombination Complex (1997)

The co-purification of the U1snRNP particle with a high-molecular-weight human homologous pairing activity has been observed consistently. Using human autoimmune sera directed against various snRNPs, it has been found that autoantibody binding to antigenic determinants specifically associated with the U1snRNP particle inhibits the formation of paired DNA molecules by the human homologous pairing activity. Immunoprecipitation of U1snRNP with anti-(U1)RNP autoantibodies significantly reduced the homologous pairing activity in these fractions. NaDodSO4-PAGE analysis of immunoprecipitated samples has revealed their content to be mostly composed of anti-(U1)RNP precipitable material. Taken together, these results suggest that some biochemical reactions in the process of homologous pairing promoted by high-molecular-weight complex are dependent upon U1snRNP components. It is postulated that the U1snRNP may be associated with the recombination complex in human cells.
The geodesic dome phased array antenna for satellite control and communication - subarray design, development and demonstration (2004)

In this paper we present the design, development and demonstration of an L/S band subarray - a basic building block of a geodesic dome phased array antenna. As previously reported, the geodesic dome array is a highly effective, multi-function, low cost spherical phased array antenna that provides hemispherical coverage. The antenna consists of a number of near-equilateral triangular, planar subarrays arranged in an icosahedral geodesic dome configuration. This novel architecture design preserves all the advantages of a spherical phased array antenna while its fabrication is based on well-developed, easily manufacturable, and affordable planar array technology. The antenna is used for simultaneous, full-duplex communication and control of multiple satellites, and for air/space surveillance over the entire sky.