gebhart/patrepeval huggingface dataset:
An oxazole-based small-molecule Stat3 inhibitor induces Stat3 aggresome formation and antitumor cell effects (2008)

4872 Constitutive activation of STAT3 and STAT5, members of the Signal Transducer and Activator of Transcription (STAT) family of proteins, occurs with a high frequency in diverse human tumors. Several lines of evidence from studies with tumors and cell lines have indicated constitutive activation of STAT3 to be one of the molecular abnormalities leading to carcinogenesis and established a requirement for constitutively-active STAT3 for tumor maintenance and progression, thereby making STAT3 a valid cancer drug target. How aberrant STAT3 is regulated in tumor cells to meet the tumor-specific requirements, however, remains undefined. We present a novel small-molecule STAT3 dimerization inhibitor and describe the dynamics of the intracellular processing of activated STAT3 within the context of the biochemical and biological effects of the STAT3 inhibitor. S3I-M2001 is a newly synthesized oxazole-based peptidomimetic small-molecule that is designed to selectively disrupt STAT3 dimerization. Studies in vitro and in vivo reveal S3I-M2001 selectively abrogates constitutive activation of STAT3 signaling in tumor cells. Consequently, hyperactivated STAT3, which hitherto occurs as “dotlike” structures of nuclear bodies, undergoes an early aggregation into nonfunctional perinuclear aggresomes and a late-phase proteasome-mediated degradation in malignant cells treated with S3I-M2001. Furthermore, S3I-M2001 inhibited growth and survival of malignant cells harboring aberrant STAT3, in contrast to the minimal effect on non-STAT3 signaling pathways or cells that do not harbor aberrant STAT3. S3I-M2001 further inhibited STAT3-dependent malignant transformation, blocked the migration and invasion of mouse and human cancer cells harboring persistently activated STAT3, and repressed STAT3-dependent transcriptional regulation of tumor survival genes, such as Bcl-xL. Finally, S3I-M2001 inhibited growth of human breast tumor xenografts. Our studies together provide proof-of-concept for the anti-tumor cell activity of an oxazole-based peptidomimetic STAT3 dimerization inhibitor, which represents a major advance toward molecular-targeted therapies for tumors that harbor persistent STAT3 activity. Moreover, these studies are the first on intracellular STAT3 stability and processing following inhibition by a small molecule that has significant antitumor activity.
A Spray-Drying Method for Mass Production of Liposomes. (1991)

A spray-drying method for the mass production of liposomes was developed : lipids were dissolved in a volatile organic solvent such as chloroform in which, in some cases, a core material such as mannitol was additionally suspended, and the organic solution or suspension was then spray-dried. Addition of core material particles or the use of hydrogenated lecithins increased the recovery of the lipid mixture prepared by spray-drying. Since the obtained spray-dried product was very amorphous, it could be easily hydrated with an aqueous solution, and lipid vesicles (lisopomes) were spontaneously formed by agitating. These spray-dried (SD) liposomes were characterized in comparison with the traditional liposomes known as Bangham's liposomes.Incorporation of cholesterol into the SD-liposomal membrane was confirmed by differential scanning calorimetry and gel filtraiton chromatography. Incorporation of charged lipids was confirmed by the zeta potential of liposomes.The size distribution of the unextruded SD-liposomes was similar to that of Bangham's liposomes, and a more homogeneous size distribution could be obtained by the extrusion technique. When glucose and dextran were used as water-soluble model drugs, the encapsulation efficiency was 15-65% depending on the total lipid concentration. Increasing the practical surface area of the lipid mixture using a core material was considered to cause a noticeably high encapsulation efficiency of dextran into the SD-liosomes.This spray-drying method was found to be useful and valuable for the mass production of liposomes.
<i>Lateral organ boundaries 1</i> is a disease susceptibility gene for citrus bacterial canker disease (2014)

Citrus bacterial canker (CBC) disease occurs worldwide and incurs considerable costs both from control measures and yield losses. Bacteria that cause CBC require one of six known type III transcription activator-like (TAL) effector genes for the characteristic pustule formation at the site of infection. Here, we show that Xanthomonas citri subspecies citri strain Xcc306, with the type III TAL effector gene pthA4 or with the distinct yet biologically equivalent gene pthAw from strain XccA(w), induces two host genes, CsLOB1 and CsSWEET1, in a TAL effector-dependent manner. CsLOB1 is a member of the Lateral Organ Boundaries (LOB) gene family of transcription factors, and CsSWEET1 is a homolog of the SWEET sugar transporter and rice disease susceptibility gene. Both TAL effectors drive expression of CsLOB1 and CsSWEET1 promoter reporter gene fusions when coexpressed in citrus or Nicotiana benthamiana. Artificially designed TAL effectors directed to sequences in the CsLOB1 promoter region, but not the CsSWEET1 promoter, promoted pustule formation and higher bacterial leaf populations. Three additional distinct TAL effector genes, pthA*, pthB, and pthC, also direct pustule formation and expression of CsLOB1. Unlike pthA4 and pthAw, pthB and pthC do not promote the expression of CsSWEET1. CsLOB1 expression was associated with the expression of genes associated with cell expansion. The results indicate that CBC-inciting species of Xanthomonas exploit a single host disease susceptibility gene by altering the expression of an otherwise developmentally regulated gene using any one of a diverse set of TAL effector genes in the pathogen populations.
Diode-pumped laser action in a new broadly tunable crystal: Yb/sup 3+/:Sr/sub 3/Y(BO/sub 3/)/sub 3/ (2001)

Summary form only given. The first demonstration of laser action under diode-pumping is herein reported with a Yb:Sr/sub 3/Y (BO/sub 3/)/sub 3/ (Yb:SrYBO or Yb:BOYS) double-borate crystal: 0.9 W were obtained for 2.45 W of absorbed pump power. This new material exhibits a particularly broad emission spectrum (60 nm FWHM) and an unusually broad zero-phonon absorption linewidth (6 nm). The similarity with glasses is striking, although Yb:SrYBO has higher cross sections and presumably better thermal conductivity due to its crystalline structure. These features make this material potentially very attractive for tunable lasers around 1 /spl mu/m and directly diode-pumped femtosecond sources. One major interest is the broad absorption bandwidth at 975 nm, approximately 6 nm, which makes spectral linewidth specifications of high power diodes less demanding. The broad absorption and emission bands are supposed to be linked to vibronic transitions, Yb/sup 3+/-Yb/sup 3+/ pairs effects and multisite behavior. Moreover, a strong crystal field is experienced by the Yb/sup 3+/ ions within the lattice (the /sup 2/F/sub 7/2/ splitting of Yb/sup 3+/ is approximately 800 cm/sup -1/): this should lead to a very small lower laser level thermal population, and reduced reabsorption losses. Last but not least, it is a congruent melting crystal, whose growth was thus carried out by the Czochralski process, leading to high optical quality pieces.
Omnimagnet: An Omnidirectional Electromagnet for Controlled Dipole-Field Generation (2014)

An Omnimagnet is an omnidirectional electromagnet comprising a spherical ferromagnetic core inside of three orthogonal nested solenoids. It generates a magnetic dipole field with both a variable dipole-moment magnitude and orientation with no moving parts. The magnetic and physical properties (e.g., dipole moment, weight, resistance, and inductance) of any Omnimagnet are derived. These general relationships are used to design an optimal Omnimagnet subject to the constraints that it has the same dipole-moment per applied current in any direction, each solenoid has no quadrupole contribution to the magnetic field, and the spherical core size maximizes the strength of the resulting dipole field. This optimal design is analyzed using FEA tools and is verified to be dipole-like in nature. Finally, the optimal design is constructed and its utility is demonstrated by driving a helical capsule-endoscope mockup through a transparent lumen.
Online identification of hierarchical heavy hitters (2004)

In traffic monitoring, accounting, and network anomaly detection, it is often important to be able to detect high-volume traffic clusters in near real-time. Such heavy-hitter traffic clusters are often hierarchical (<i>ie</i>, they may occur at different aggregation levels like ranges of IP addresses) and possibly multidimensional (<i>ie</i>, they may involve the combination of different IP header fields like IP addresses, port numbers, and protocol). Without prior knowledge about the precise structures of such traffic clusters, a naive approach would require the monitoring system to examine all possible ombinations of aggregates in order to detect the heavy hitters, which can be proohibitive in terms of computation resources.
Self-assembled Messenger RNA Nanoparticles (mRNA-NPs) for Efficient Gene Expression (2015)

Although mRNA has several advantages over plasmid DNA when delivered into cells for gene expression, mRNA transfection is a very rare occurrence in gene delivery. This is mainly because of the labile nature of RNA, resulting in a low expression level of the desired protein. In this study, self-assembled mRNA nanoparticles (mRNA-NPs) packed with multiple repeats of mRNA were synthesized to achieve efficient gene expression. This approach required only a one-step process to synthesize particles with a minimal amount of plasmid DNA to produce the RNA transcripts via rolling circle transcription. Moreover, there are no concerns for cytotoxicity which can be caused by chemical condensates because mRNA-NPs are made entirely of mRNA. An examination of the cells transfected with the mRNA-NPs encoding the green fluorescence protein (GFP) confirmed that the mRNA-NPs can be used as a novel platform for effective gene delivery.
Steam gasification of brown coal impregnated with calcium hydroxide. (1986)

In the previous study it was found that the nickel catalyst impregnated on brown coals shows excellent activity in the gasification reaction. In this study more cheap catalyst, Ca (OH) 2, was used as starting material. The chemical state during the steam gasification was determined and the reactivity was determined in the temperature range from 600 to 800°C. Ion-exchanged Ca was transformed to finely dispersed CaCO3 upon pyrolysis and the extensive crystal growth of CaCO3 was observed during the course of steam gasification. Near the end of gasification CaCO3 was converted to CaO owing to the decrease of CO2 content in the atmosphere. About 2 wt% of Ca content was enough to enhance the reactivity of coal by a factor of 10 at 650°C. In order to obtain the same reaction rate, 750°C is necessary without catalyst. This catalytic effect was more significant when compared with the data for the Ca-catalyzed gasification of American low-rank coals.
Flame‐assisted flash sintering: A noncontact method to flash sinter coatings on conductive substrates (2017)

Abstract We present a novel and effective method for sintering ceramic coatings onto metallic substrates. This new technique, called Flame‐assisted flash sintering (FAFS), utilizes a flame as both a heating source and a conformal, current‐carrying top electrode to facilitate flash sintering. Using this method, Yttria‐stabilized Zirconia (8 mol% Y, 8YSZ) coatings are sintered onto stainless steel substrates to controlled degrees of porosity in rapid fashion. Flame‐assisted flash sintering utilizes a dynamic soft electrode for flash sintering and has commercial potential to sinter ceramic coatings on complex‐shaped substrates for a variety of applications including tribological or thermal protection coatings.
Online approach to performance fault localization for cloud and datacenter services (2017)

Automated detection and diagnosis of the performance faults in cloud and datacenter environments is a crucial task to maintain smooth operation of different services and minimize downtime. We demonstrate an effective machine learning approach based on detecting metric correlation stability violations (CSV) for automated localization of performance faults for datacenter services running under dynamic load conditions.
Highly accelerated multishot echo planar imaging through synergistic machine learning and joint reconstruction (2019)

Combination of ML and JVC-SENSE enabled navigator-free msEPI at higher accelerations than previously possible while using fewer shots, with reduced vulnerability to poor generalizability and poor acceptance of end-to-end ML approaches.
Cellular Internalization Mechanisms of Polyanhydride Particles: Implications for Rational Design of Drug Delivery Vehicles (2016)

Polyanhydride nanoparticles have emerged as a versatile delivery platform, due to their ability to encapsulate diverse drugs, immunogens, antibodies, and proteins. However, mechanistic studies on the effects of particle chemistry interactions with immune cells have yet to be described. Understanding the mechanism by which these particles are internalized by immune cells will enable rational selection of delivery vehicles for specific applications. In the present study, the internalization, mechanism(s) of uptake by monocytes, and intracellular fate of polyanhydride nanoparticles were evaluated using copolymers based on 1,6-bis(p-carboxyphenoxy)hexane (CPH), sebacic acid (SA), and 1,8-bis(p-carboxyphenoxy)3,6-dioxaoctane (CPTEG). The results showed that 20:80 CPH:SA and 20:80 CPTEG:CPH nanoparticles were internalized to a greater extent by monocytes as compared to the 50:50 CPH:SA and 50:50 CPTEH:CPH nanoparticles. Further, cytochalasin-D treatment of cells inhibited uptake of all the particles, regardless of chemistry, indicating that actinmediated uptake is the primary mechanism of cellular entry for these particles. The insights gained from these studies were used to identify lead nanoparticle formulations to enhance treatment of intracellular bacterial infections. The use of doxycycline-loaded nanoparticles exhibited enhanced therapeutic efficacy compared to soluble drug in treating monocyte monolayers infected with the virulent intracellular pathogen Brucella abortus. Altogether, these studies demonstrate how rational design and selection of nanoscale delivery platforms can be used for a wide spectrum of biomedical applications.
Solid-Supported Synthesis of a Peptide β-Turn Mimetic (2000)

[structure: see text]The solid-supported synthesis of a bicyclic diketopiperazine, a potential peptide beta-turn mimetic, is described. The Ugi reaction between the resin ester of alpha-N-Boc-diaminopropionic acid (an amine input), alpha-bromo acid, aldehyde, and isocyanide is the key step in the proposed protocol.
Comparing Sunflower Stearins with Cocoa Butter (2012)

Key Points High-oleic high-stearic sunflower mutant is one of the new commercial varieties of this oil crop that have been developed by breeding and mutagenesis from common sunflower lines. The oil extracted from this line contains high levels of stearic acid in a high-oleic background and could be a source of stearate-rich fats in the future. Dry fractionation is a process by which the triacylglycerols with a high degree of saturation of an oil or fat are selectively crystallized and separated from the liquid matrix without the addition of any solvent to yield a solid fraction enriched in saturated fatty acids and a liquid fraction richer in unsaturated fatty acids. This method is used for palm oil fractionation. Solvent fractionation involves the addition of solvent to oil as a step previous to its fractionation. The resulting micelle is fractionated by crystallization of the species of triacylglycerols with higher levels of saturated fatty acids. The resulting solid phase is separated from the liquid one and washed with fresh solvent. This method is more efficient than dry fractionation, although it requires higher operation costs. It is often used to obtain highly valuable stearate-rich butters from tropical fats. Stearin is the name given to the solid fraction obtained in the fractionation of an oil or fat. It contains higher levels of saturated fatty acids than the initial oil. Its characteristics and composition will depend on the composition of the initial oil and the method and conditions of fractionation. A cocoa butter equivalent is a vegetable fat or a mixture of vegetable fats with similar physical and chemical properties to those of cocoa butter. It has to be compatible in mixtures with cocoa butter and display similar polymorphism. Cocoa butter equivalents are produced by mixing stearate-rich tropical butters and fractions resulting from palm oil fractionation.
Predictive modeling of pattern-dependent etch effects in large-area fully-integrated 3D virtual fabrication (2014)

We present a predictive modeling approach for pattern-dependent etch processes implemented in a 3D virtual fabrication software platform. This technique combines long-range effects using design data and short-range effects using predictive 3D models of the design-technology interaction. For the first time, this type of pattern-dependent predictive capability is integrated into a full 3D virtual fabrication environment to enable fast accurate structural modeling of complex advanced technologies such as FinFETs, 3D memory and BEOL interconnect.
Quantum cascade lasers with blocking barriers in the active regions (2002)

Summary form only given. We report on a new design of GaInAs-AlInAs quantum cascade lasers (QCLs) improving the concept of Bragg reflectors by incorporating "blocking barriers" into the active regions. These barriers significantly enhance the confinement of electrons in the initial state of the laser transition by selectively blocking direct tunneling through the exit barrier (reducing the tunneling probability by a factor of 2). The high tunneling probability of electrons in the final state into the injector's miniband is maintained by reducing the total width of the exit barrier appropriately.
Thermoelectric generator. [liquid metal working fluid] (1977)

An improved thermoelectric generator is described having (1) enclosure means for a first reaction zone; (2) enclosure means for a second reaction zone; (3) a reaction zone separator which (a) separates and essentially completes enclosure of the two reaction zones and (b) comprises a cationically-conductive, solid electrolyte that is essentially impermeable to elemental alkali metal and compounds thereof and ionically conductive with respect to cations of the alkali metal; (4) alkali metal within the first reaction zone and in fluid communication with the solid electrolyte; (5) an electrode within the second reaction zone in electrical contact with the solid electrolyte and sufficiently porous to permit alkali metal vapor to pass therethrough; (6) conduction means for electron flow between the alkali metal within the first reaction zone and the electrode; (7) inlet means for introducing the alkali metal into the first reaction zone; and (8) temperature control means adapted to maintain a temperature in the first reaction zone at least 100/sup 0/C in excess of the lowest temperature in the second reaction zone. The improvement of the invention comprises employing as the electrode a porous film of a metal which has a melting point above about 1000/sup 0/C and which ismore » chemically inert to sodium, the film having been deposited on said reaction zone separator by chemical vapor deposition.« less
Immunological Probes of the Structure, Function, and Expression of Heterotrimeric GTP-Binding Proteins (1992)

G-proteins convey extracellular signals from cell surface receptors to diverse effectors such as enzymes of second messenger metabolism and ion channels. Receptor-effector coupling G-proteins are composed of three subunits, α, β, and γ, each separate gene products. Multiple forms of each type of subunit have been identified at the DNA and protein level (Gilman, 1987; Lochrie and Simon, 1988; Spiegel, 1987). Historically, α subunits were first identified by GTP affinity labeling and bacterial toxin-catalyzed ADP-ribosylation. These methods lack requisite specificity. Pertussis toxin, for example, is now known to covalently modify as many as six different Gα subunits (Gilman, 1987; Lochrie and Simon, 1988; Spiegel, 1987). Antibodies specific for G-protein subunits have proved to be powerful tools for studies of G-proteins. Both polyclonal (Gierschik et al., 1985, 1986c; Huff et al., 1985; Katada et al., 1987; Pines et al., 1985a; Roof et al., 1985) and monoclonal (Halpern et al., 1986; Hamm and Bownds, 1984; Navon and Fung, 1987, 1988; Tsai et al., 1987) antibodies have been raised against purified G-proteins. Antisera raised against purified G-holoproteins and subunits provided initial evidence for similarities (β subunits) and differences (α and γ subunits) between members of the G-protein family (Figure 11. 1). Immunochemical studies with such antisera suggested diversity in pertussis toxin substrates (Gierschik et al., 1986b), subsequently confirmed by cloning of cDNAs encoding multiple types of putative pertussis toxin substrate (Gilman, 1987; Lochrie and Simon, 1988; Spiegel, 1987).
Three New Alkaloids from the Marine Tunicate <i>Cystodytes violatinctus</i> (1998)

Three novel alkaloids, shermilamine D and E (1 and 2) and tintamine (3), two pyridoacridines (1 and 2), and one alkaloid possessing a new heterocyclic system have been isolated from the Indian Ocean tunicate Cystodytes violatinctus collected at the Mayotte Lagoon, Comoros Islands, northwest of Madagascar. The structures of all compounds were elucidated on the basis of spectroscopic data, mainly 1D and 2D NMR data.
Composition-dependent superconductivity in<mml:math xmlns:mml="http://www.w3.org/1998/Math/MathML" display="inline"><mml:mrow><mml:msub><mml:mrow><mml:mi mathvariant="normal">La</mml:mi></mml:mrow><mml:mrow><mml:mn>2</mml:mn><mml:mi mathvariant="normal">−</mml:mi><mml:mi mathvariant="normal">x</mml:mi></mml:mrow></mml:msub></mml:mrow></mml:math><mml:math xmlns:mml="http://www.w3.org/1998/Math/MathML" display="inline"><mml:mrow><mml:msub><mml:mrow><mml:mi mathvariant="normal">Sr</mml:mi></mml:mrow><mml:mrow><mml:mi mathvariant="normal">x</mml:mi></mml:mrow></mml:msub></mml:mrow></mml:math><mml:math xmlns:mml="http://www.w3.org/1998/Math/MathML" display="inline"><mml:mrow><mml:msub><mml:mrow><mml:mi mathvariant="normal">CuO</mml:mi></mml:mrow><mml:mrow><mml:mn>4</mml:mn><mml:mi mathvariant="normal">−</mml:mi><mml:mi mathvariant="normal">δ</mml:mi></mml:mrow></mml:msub></mml:mrow></mml:math> (1987)

We report the dependence of the superconducting critical temperature on x for a series of ${\mathrm{La}}_{2\mathrm{\ensuremath{-}}\mathrm{x}}$${\mathrm{Sr}}_{\mathrm{x}}$${\mathrm{CuO}}_{4\mathrm{\ensuremath{-}}\mathrm{\ensuremath{\delta}}}$ samples prepared under identical conditions. A strong peak in the fraction of the sample which is superconducting occurs near x=0.15, the composition which also gives the highest transition temperatures as measured by resistivity and the dc Meissner effect. Relatively high onset temperatures are observed, and we infer the presence of another, possibly metastable, material with a critical temperature substantially higher than that of bulk ${\mathrm{K}}_{2}$${\mathrm{NiF}}_{4}$ structure-type ${\mathrm{La}}_{2\mathrm{\ensuremath{-}}\mathrm{x}}$${\mathrm{Sr}}_{\mathrm{x}}$${\mathrm{CuO}}_{4\mathrm{\ensuremath{-}}\mathrm{\ensuremath{\delta}}}$.