gebhart/patrepeval huggingface dataset:
Differential Regulation of 6- and 7-Transmembrane Helix Variants of μ-Opioid Receptor in Response to Morphine Stimulation (2020)

The pharmacological effect of opioids originates, at the cellular level, by their interaction with the μ-opioid receptor (mOR) resulting in the regulation of voltage-gated Ca2+ channels and inwardly rectifying K+ channels that ultimately modulate the synaptic transmission. Recently, an alternative six trans-membrane helix isoform of mOR, (6TM-mOR) has been identified, but its function and signaling are still largely unknown. Here, we present the structural and functional mechanisms of 6TM-mOR signaling activity upon binding to morphine. Our data suggest that despite the similarity of binding modes of the alternative 6TM-mOR and the dominant seven trans-membrane helix variant (7TM-mOR), the interaction with morphine generates different dynamic responses in the two receptors, thus, promoting the activation of different mOR-specific signaling pathways. We characterize a series of 6TM-mOR-specific cellular responses, and observed that they are significantly different from those for 7TM-mOR. Morphine stimulation of 6TM-mOR does not promote a cellular cAMP response, while it increases the intracellular Ca2+ concentration and reduces the cellular K+ conductance. Our findings indicate that 6TM-mOR has a unique contribution to the cellular opioid responses. Therefore, it should be considered as a relevant target for the development of novel pharmacological tools and medical protocols involving the use of opioids.
ChemInform Abstract: MODIFIKATIONEN VON ANTIBIOTIKA 10. MITT. NEUE BETA‐LACTAM‐ANTIBIOTIKA, DERIVATE DER 3‐HYDROXY‐7‐AMINO‐CEPH‐3‐EM‐4‐CARBONSAEURE (1975)

Abstract Durch Ozonolyse der Methylen‐cephamsäureester (I) werden die Hydroxyester (I.I) erhalten; aus (IIa) werden die Verbindungen (III) bzw. ‐ über das Derivat (IVa) und sein Acetat (IVb)‐(V) [angegebene Ausbeute bezogen auf (IVa)] gewonnen.
Maintenance therapy for AML: are we there yet? (2019)

Curiously, in null neutrophils only CD32specific antibodies could block trogocytosis, suggesting that in the absence of FcgRIIIB, FcgRIIA can promote trogocytosis.
Fonctions d'exces et contributions de groupes appliquees au calcul des equilibres liquide-vapeur de systemes polaires ou non polaires sous haute pression (1989)

Dans le but d'elaborer un modele predictif applicable au calcul des equilibres liquide-vapeur a haute pression pour des systemes polaires et non polaires, trois equations d'etat (dont srk et pr) sont associees a une matrice unifac dependante de la temperature. La fonction d'exces impliquee (l'energie libre d'exces a compacite constante) differant notablement de l'enthalpie libre d'exces a pression constante, trois nouvelles matrices unifac (une pour chaque equation d'etat) ont ete developpees pour quatorze groupes fonctionnels incluant les alcanes, les aromatiques, les alcanols, les phenols, les alcanones et quelques gaz incondensables. La representation des equilibres liquide-vapeur a basse pression est aussi bonne qu'avec le modele conventionnel unifac pour la phase liquide, l'avantage sur ce dernier residant dans l'extension jusqu'au point critique du domaine de validite sans deterioration observable des resultats
ChemInform Abstract: An Iridium Based Mercury Ultramicroelectrode. Fabrication and Characterization. (1991)

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.
Development of Risk Assessment System for Steel and Iron Works (2009)

Steel and iron works have place many hazard or risk factor as a high temperature material, a high place, and so on. Accordingly, steel and iron works need system for risk assessment. In this paper, we development of risk assessment system for steel and iron works. In case study applied at the steel enterprise. The resultant, we can discovery that an human factor is an important question form risk assessment.
Stepwise Synthesis, Structures, and Reactivity of Mono-, Di-, and Trimetallic Metal Complexes with a 6π + 6π Quinonoid Zwitterion (2004)

The benzoquinonemonoimine N,N'-dineopentyl-2-amino-5-alcoholate-1,4-benzoquinonemonoiminium [C(6)H(2)(NHCH(2)t-Bu)(2)(O)(2)] 6, which is a rare example of an organic zwitterion being more stable than its canonical form, is best described as constituted of two chemically connected but electronically not conjugated 6pi electron subunits. The two successive acidities of 6 allow the preparation of mono-, di-, and trimetallic complexes in which the control of the pi-system delocalization becomes possible. Reaction of 6 with NaOt-Bu results in monodeprotonation of one N-H function, and the isolated sodium salt 9, which is stable under N(2), reacts with chloride-bridged Pd(II) homodimetallic complexes, [AuCl(PPh(3))] or trans-[NiCl(Ph)(PPh(3))(2)], to afford the monometallic complexes 10-15 in which the pi-system is localized. A second in situ deprotonation of the remaining N-H amino function of 10 with NaH followed by reaction with [Pd(8-mq)(mu-Cl)](2) (8-mq = orthometalated 8-methylquinoline) affords the homodimetallic complex 17 in which the pi-system of the quinonoid ligand is delocalized between the two metal centers. Deprotonation of both N-H amino functions of the square-planar complex trans-[Ni(N,O)(2)] 15 with NaH and reaction with [Pd(8-mq)(mu-Cl)](2) affords the heterotrimetallic (Pd, Ni, Pd) complex 18 in which the pi-system of the two quinonoid ligands is delocalized between the three metal centers. The crystal structures of the monometallic complexes 10 and 13 and of the dipalladium complex 17 are reported and consequences of metal coordination discussed. Complex 15 was tested in catalytic ethylene oligomerization with AlEtCl(2) as cocatalyst.
Long-Term Monitoring of Wind Farms Using Big Data Approach (2016)

There is a trend to build wind turbines in large wind farms and in the near future to operate such a farm as an integrated power production plant. Predictability of individual turbine behaviour is key in such a strategy. In order to minimize the influence on the balance of the electricity grid it is necessary to have stable electricity production by each of the turbines. Hence all turbines should be available for operation when needed, which puts significant constraints on owner operators. Failure of turbine subcomponents should be avoided. This requires planning in advance of all necessary maintenance actions such that they can be performed during low wind and low electricity demand periods. Therefore, it is necessary to anticipate upcoming component failures, such that spare parts can be ordered and are available for maintenance personnel during the optimal weather and market windows. In order to obtain the insights to predict component failure, it is necessary to have an integrated clean dataset spanning all turbines of the wind farm for a sufficiently long period of time. This paper describes the requirements and challenges related to such a dataset based on experience acquired during years of monitoring offshore wind farms. Furthermore, it suggests a big data based approach for an integrated no-sql data-storage and data-analytics platform to tackle these challenges. In addition a failure prognosis approach using the integrated dataset is proposed to detect failure initiation in the bearings of gearboxes and generators, which are vital parts of wind turbines.
Integridad y equidad electoral: El uso de las franjas en los medios de comunicación durante las campañas electorales (2015)

Hace un recorrido por la legislación y jurisprudencia electoral argentina. Puntualmente analiza el tema de la regulación del acceso de los medios de comunicación en el proceso electoral. Se analiza la jurisprudencia producida por la Cámara Nacional Electoral en materia de publicidad y campañas electorales, así como algunos fallos de la Corte Interamericana de Derechos Humanos sobre la equidad en los procesos de elecciones
Modèles de diffusion ultrasonore pour la caractérisation de l'agrégation érythrocytaire. (2013)

National audience
Transcriptional Cross-Regulation of the Catechol and Protocatechuate Branches of the β-Ketoadipate Pathway Contributes to Carbon Source-Dependent Expression of the Acinetobacter sp. Strain ADP1 pobA Gene (2003)

Transcriptional control of carbon source preferences by Acinetobacter sp. strain ADP1 was assessed with a pobA::lacZ fusion during growth on alternative substrates. The pobA-encoded enzyme catalyzes the first step in the degradation of 4-hydroxybenzoate, a compound consumed rapidly as a sole carbon source. If additional aromatic carbon sources are available, 4-hydroxybenzoate consumption is inhibited by unknown mechanisms. As reported here, during growth on aromatic substrates, pobA was not expressed despite the presence of 4-hydroxybenzoate, an inducer that normally causes the PobR regulator to activate pobA transcription. Growth on organic acids such as succinate, fumarate, and acetate allowed higher levels of pobA expression. In each case, pobA expression increased at the end of the exponential growth phase. Complex transcriptional regulation controlled 4-hydroxybenzoate catabolism in multisubstrate environments. Additional studies focused on the wild-type preference for benzoate consumption prior to 4-hydroxybenzoate consumption. These compounds are degraded via the catechol and protocatechuate branches of the beta-ketoadipate pathway, respectively. Here, mutants were characterized that degraded benzoate and 4-hydroxybenzoate concurrently. These mutants lacked the BenM and CatM transcriptional regulators that normally activate genes for benzoate catabolism. A model is presented in which BenM and CatM prevent pobA expression indirectly during growth on benzoate. These regulators may affect pobA expression by lowering the PcaK-mediated uptake of 4-hydroxybenzoate. Consistent with this model, BenM and CatM bound in vitro to an operator-promoter fragment controlling the expression of several pca genes, including pcaK. These studies provide the first direct evidence of transcriptional cross-regulation between the distinct but analogous branches of the beta-ketoadipate pathway.
Thermally assisted MRAMs: ultimate scalability and logic functionalities (2013)

International audience
Variation of lung volume after fixation when measured by immersion or Cavalieri method (2003)

Organ volume is a critical parameter in morphometric analysis. The special problems of the lung as a nonsolid organ are overcome by tracheal instillation of fixatives at a constant airway pressure (P(aw)). Lung volume can change significantly after fixation as P(aw) change. To determine the variation of lung volume after fixation, we measured the volume of intact fixed lungs by serial immersion in saline (V(imm)) at selected time points, compared with measurements obtained by point counting [Cavalieri Principle (V(cav))] after tissue sectioning to release P(aw). V(imm) was systematically higher than V(cav) by 25% in dog lungs and 13% in guinea pig lungs (P = 0.0003 between species). This size-dependent variability reflects residual elastic recoil, refolding and/or crumpling of alveolar septa after fixation. V(imm) remained 14% higher than V(cav) in dog lungs even after pressure release. V(cav)/V(imm) was systematically lower in the upper than the lower strata of the same lung. We conclude that V(cav) measured on lung slices after relaxation of P(aw) more precisely represents the state of the tissue to be used for subsequent morphometric analysis, particularly for large lungs.
Biopolymeric Anticorrosion Coatings from Cellulose Nanofibrils and Colloidal Lignin Particles (2021)

This study presents a process for preparation of cellulose-lignin barrier coatings for hot-dip galvanized (HDG) steel by aqueous electrophoretic deposition. Initially, a solution of softwood kraft lignin and diethylene glycol monobutyl ether was used to prepare an aqueous dispersion of colloidal lignin particles (CLPs) <i>via</i> solvent exchange. Analysis of the dispersion showed that it comprised submicron particles (<i>D</i> = 146 nm) with spherical morphologies and colloidal stability (ζ-potential = -40 mV). Following successful formation, the CLP dispersion was mixed with a suspension of TEMPO-oxidized cellulose nanofibers (TOCN, 1 and 2 g·L<sup>-1</sup>) at a fixed volumetric ratio (1:1, TOCN-CLPs), and biopolymers were deposited onto HDG steel surfaces at different potentials (0.5 and 3 V). The effects of these variables on coating formation, dry adhesion, and electrochemical properties (3.5% NaCl) were investigated. The scanning electron microscopy results showed that coalescence of CLPs occurs during the drying of composite coatings, resulting in formation of a barrier layer on HDG steel. The scanning vibrating electrode technique results demonstrated that the TOCN-CLP layers reduced the penetration of the electrolyte (3.5% NaCl) to the metal-coating interface for at least 48 h of immersion, with a more prolonged barrier performance for 3 V-deposited coatings. Additional electrochemical impedance spectroscopy studies showed that all four coatings provided increased levels of charge transfer resistance (<i>R</i><sub>ct</sub>)-compared to bare HDG steel-although coatings deposited at a higher potential (3 V) and a higher TOCN concentration provided the maximum charge transfer resistance after 15 days of immersion (13.7 <i>cf.</i> 0.2 kΩ·cm<sup>2</sup> for HDG steel). Overall, these results highlight the potential of TOCN-CLP biopolymeric composites as a basis for sustainable corrosion protection coatings.
Impaired Channel Targeting and Retinal Degeneration in Mice Lacking the Cyclic Nucleotide-Gated Channel Subunit CNGB1 (2005)

Cyclic nucleotide-gated (CNG) channels are important mediators in the transduction pathways of rod and cone photoreceptors. Native CNG channels are heterotetramers composed of homologous A and B subunits. In heterologous expression systems, B subunits alone cannot form functional CNG channels, but they confer a number of channel properties when coexpressed with A subunits. To investigate the importance of the CNGB subunits in vivo, we deleted the CNGB1 gene in mice. In the absence of CNGB1, only trace amounts of the CNGA1 subunit were found on the rod outer segment. As a consequence, the vast majority of isolated rod photoreceptors in mice lacking CNGB1 (CNGB1-/-) failed to respond to light. In electroretinograms (ERGs), CNGB1-/- mice showed no rod-mediated responses. The rods also showed a slow-progressing degeneration caused by apoptotic death and concurred by retinal gliosis. Cones were primarily unaffected and showed normal ERG responses up to 6 months, but they started to degenerate in later stages. At the age of approximately 1 year, CNGB1-/- animals were devoid of both rods and cones. Our results show that CNGB1 is a crucial determinant of native CNG channel targeting. As a result of the lack of rod CNG channels, CNGB1-/- mice develop a retinal degeneration that resembles human retinitis pigmentosa.
Spot activity of LQ Hydra from photometry between 1988 and 2011 (2012)

Aims. We investigate the spot activity of the young magnetically active main sequence star LQ Hya. Our aims are to identify possible active longitudes, estimate the differential rotation, and study long and short term changes in the activity.
Energy and Exergy Analyses of a New Combined Cycle for Producing Electricity and Desalinated Water Using Geothermal Energy (2014)

A new combined cogeneration system for producing electrical power and pure water is proposed and analyzed from the viewpoints of thermodynamics and economics. The system uses geothermal energy as a heat source and consists of a Kalina cycle, a LiBr/H2O heat transformer and a water purification system. A parametric study is carried out in order to investigate the effects on system performance of the turbine inlet pressure and the evaporator exit temperature. For the proposed system, the first and second law efficiencies are found to be in the ranges of 16%–18.2% and 61.9%–69.1%, respectively. For a geothermal water stream with a mass flow rate of 89 kg/s and a temperature of 124 °C, the maximum production rate for pure water is found to be 0.367 kg/s.
Bacterial muramy dipeptide differently affect IL-6 and VEGF production in pituitary folliculostellate TtT/GF cells through NOD1 and NOD2 receptors (2007)

The follicullostellate (FS) cells of the pituitary share properties with dendritic cells and also with macrophages. A subset of FS cells express MHC class I and MHC class II molecules and also several lymphoid and lymphatic markers. FS cells were further found to be a source of growth factors such as basic fibroblast growth factor (bFGF), vascular endothelial growth factors (VEGF), as well as cytokines such as leukaemia inhibitor factor (LIF) and interleukin-6 (IL-6). We have found that FS cells express Toll-like receptor 4 (Tlr4), a key component of the innate immune system. Bacterial lipopolysaccharide (LPS), the ligand of Tlr4, stimulated the release of IL-6 from FS cells which then enhanced ACTH secretion in corticotropes. Recently, nucleotide-binding oligomerization domain (NOD) proteins, NOD1 and NOD2 were found to represent an intracellular component of the innate immune system. The ligand of NOD2 is muramyl dipeptide (MDP), a component of bacterial cell-wall peptidoglycan present in most gram-positive and –negative bacteria. We have studied, whether the folliculostellate TtT/GF cell line expresses functional active NODs. By RT-PCR we could demonstrated the presence of NOD1 and NOD2 transcripts in FS cells. Moreover, NOD2 protein expression was increased in FS cells after 24 hours stimulation with MDP. We also observed significantly enhanced IL-6 secretion in the supernatant of FS cell cultures after stimulation with MDP whereas the production of vascular endothelial growth factor (VEGF-A) was strongly suppressed. Our preliminary data suggest that MDP-induced and NOD-mediated effects on IL-6 and VEGF-A secretion by FS cells may play a role in modulating pituitary function during bacterial infections.
Poly-ADP-Ribose Polymerase as a Therapeutic Target in Pediatric Diffuse Intrinsic Pontine Glioma and Pediatric High-Grade Astrocytoma (2015)

Pediatric high-grade astrocytomas (pHGA) and diffuse intrinsic pontine gliomas (DIPG) are devastating malignancies for which no effective therapies exist. We investigated the therapeutic potential of PARP1 inhibition in preclinical models of pHGA and DIPG. PARP1 levels were characterized in pHGA and DIPG patient samples and tumor-derived cell lines. The effects of PARP inhibitors veliparib, olaparib, and niraparib as monotherapy or as radiosensitizers on cell viability, DNA damage, and PARP1 activity were evaluated in a panel of pHGA and DIPG cell lines. Survival benefit of niraparib was examined in an orthotopic xenograft model of pHGA. About 85% of pHGAs and 76% of DIPG tissue microarray samples expressed PARP1. Six of 8 primary cell lines highly expressed PARP1. Interestingly, across multiple cell lines, some PARP1 protein expression was required for response to PARP inhibition; however, there was no correlation between protein level or PARP1 activity and sensitivity to PARP inhibitors. Niraparib was the most effective at reducing cell viability and proliferation (MTT and Ki67). Niraparib induced DNA damage (γH2AX foci) and induced growth arrest. Pretreatment of pHGA cells with a sublethal dose of niraparib (1 μmol/L) before 2 Gy of ionizing radiation (IR) decreased the rate of DNA damage repair, colony growth, and relative cell number. Niraparib (50 mg/kg) inhibited PARP1 activity in vivo and extended survival of mice with orthotopic pHGA xenografts, when administered before IR (20 Gy, fractionated), relative to control mice (40 vs. 25 days). Our data provide in vitro and in vivo evidence that niraparib may be an effective radiosensitizer for pHGA and DIPG.
Subsurface precision machining of glass substrates by innovative lasers (2003)

At very high laser intensities, achieved with modern, diode-pumped solid state lasers having high beam quality and high pulse power, even transparent materials such as glass can be easily machined with high efficiency and precision. Examples are given by the subsurface engraving, the cutting and the drilling of glass, where the physical effect of nonlinear absorption in transparent media is used. This enables machining processes and results which are not feasible with any other tool known before.
Structures of Bombyx mori and Samia cynthia Ricini Silk Fibroins Studied with Solid‐State NMR (2004)

Abstract For Abstract see ChemInform Abstract in Full Text.
Disease-controlling effect of a novel fungicide pyribencarb against Botrytis cinerea (2010)

Pyribencarb, methyl {2-chloro-5-[(E)-1-(6-methyl-2-pyridylmethoxyimino)ethyl]benzyl}carbamate, is a novel fungicide having excellent activity against a wide range of plant pathogenic fungi, especially gray mold diseases caused by Botrytis cinerea. Pyribencarb exhibited not only a preventive effect but also a curative effect. When spraying was performed 48 hr after inoculation (after visible symptoms appeared), pyribencarb also showed strong inhibitory activity against lesion development by cucumber gray mold that was significantly superior to its preventive activity. Experiments in the greenhouse demonstrated good translaminar, rain fastness and residual activities, resulting in pyribencarb's high performance in the field. Pyribencarb was effective to control eggplant gray mold and kidney bean gray mold at 100–200 μg/ml in field trials.
A Gram‐Scale Batch and Flow Total Synthesis of Perhydrohistrionicotoxin (2010)

The total synthesis of the spiropiperidine alkaloid (-)-perhydrohistrionicotoxin (perhydro-HTX) 2 has been accomplished on a gram scale by employing both conventional batch chemistry as well as microreactor techniques. (S)-(-)-6-Pentyltetrahydro-pyran-2-one 8 underwent nucleophilic ring opening to afford the alcohol 10, which was elaborated to the nitrone 13. Protection of the nitrone as the 1,3-adduct of styrene and side-chain extension to the unsaturated nitrile afforded a precursor 17, which underwent dipolar cycloreversion and 1,3-dipolar cycloaddition to give the core spirocyclic precursor 18 that was converted into perhydro-HTX 2. The principal steps to the spirocycle 18 have successfully been transferred into flow mode by using different types of microreactors and in a telescoped fashion, allowing for a more rapid access to the histrionicotoxins and their analogues by continuous processing.