gebhart/patrepeval huggingface dataset:
AQW051, a novel, potent and selective nicotinic acetylcholine receptor α7 partial agonist: Pharmacological characterisation and Phase I evaluation in healthy subjects (2014)

Activation of the nicotinic acetylcholine receptor (nAChR) α7 is considered as an attractive target for the treatment of cognitive impairment associated with neurological disorders. Here we describe the novel nAChR α7 agonist AQW051 as a promising drug candidate for this indication. In vitro, AQW051 bound with very high affinity to nAChR α7 and displayed considerably lower potency for other human nAChRs subtypes including α4β2, α3β4 and α1β1γδ receptors, as well as 5 HT3 receptors when tested functionally as an antagonist. Furthermore, AQW051 did not display agonistic activity at these other receptors. Similarly, AQW051 showed low binding activity at a wide panel of neurotransmitter receptors, transporters and kinases. Demonstrating that AQW051 is a potent, partial and selective agonist of nAChR α7. In vivo, AQW051 demonstrated good oral bioavailability and rapid penetration into the rodent brain. AQW051 administered over a broad dose range facilitated learning/memory performance in the object recognition and social recognition test in mice and the water maze experiment in aged rats. Clinically, AQW051 was well tolerated in healthy young and elderly volunteers, with an adverse event (AE) profile comparable with placebo. No serious adverse events (SAEs) were reported and all AEs were either mild or moderate in severity. Once daily oral administration of AQW051 resulted in continuous exposure and a 2-3 fold accumulation compared with steady state was achieved by one week; exposure was not affected by a light meal. Taken together, these data support further development of AQW051 as a cognitive-enhancing agent.
Use of transformation to construct antigenic hybrids of the class 1 outer membrane protein in Neisseria meningitidis (1993)

The class 1 protein of Neisseria meningitidis is an important component of candidate outer membrane vaccines against meningococcal meningitis. This porin protein contains two variable regions which determine subtype specificity and provide binding sites for bactericidal monoclonal antibodies. To determine the contribution of each of these variable regions in the induction of bactericidal antibodies, a set of isogenic strains differing only in their class 1 epitopes was constructed. This was done by transformation of meningococcal strain H44/76 with cloned class 1 genes and selection of the desired epitope combinations in a colony blot with subtype-specific monoclonal antibodies. When used for the immunization of mice, outer membrane complexes induced bactericidal antibodies only against meningococcal strains sharing at least one of their class 1 epitopes. The results demonstrate that the P1.2 and P1.16 epitopes, normally located in the fourth exposed loop of the protein, efficiently induce bactericidal antibodies independently of the particular sequence in the first variable region. The P1.5 and P1.7 epitopes, normally located in the first exposed loop, were found to induce lower bactericidal titers. Hybrid class 1 outer membrane proteins were constructed by inserting oligonucleotides encoding the P1.7 and P1.16 epitopes into the porA gene. In this way, we obtained a set of strains which carry the P1.5 epitope in loop 1, P1.2 in loop 4, and P1.7 and P1.16 (separately or in combination) in either loop 5 or loop 6. The additional epitopes were found to be exposed at the cell surface. Outer membrane complexes from several of these strains were found to induce a bactericidal response in mice against the inserted epitopes. These results demonstrate that it is feasible to construct meningococcal strains carrying multivalent class 1 proteins in which multiple subtype-specific epitopes are present in different cell surface-exposed loops.
Techniques for the Dry Transfer of Epitaxial Graphene onto Arbitrary Substrates (2010)

Epitaxial graphene (EG) grown on the carbon-face of SiC has been shown to exhibit high carrier mobilities, in comparison to other growth techniques amenable to wafer-scale graphene fabrication. The transfer of large area (>mm2) graphene films to substrates amenable for specific applications is desirable. We demonstrate the dry transfer of EG from the C-face of 4H-SiC onto SiO2, GaN and Al2O3 substrates via two approaches using either 1) thermal release tape or 2) a spin-on, chemically-etchable dielectric. We will report on the impact that these transfer processes has upon the electrical properties of the transferred EG films.
A Method for Estimating the Mechanical Properties of a Solid Material Subjected to Significant Compressional Forces - Part I: Numerical Theoretical Solution for a Single Thick Plate (2003)

Abstract : 13 ABSTRACT (Maximum 200 words) This report develops a technique for measuring (or estimating) the complex frequency-dependent dilatational and shear wavenumbers of a single slab of material subjected to large static compressional forces, The method employs two transfer functions that are obtained by vibrating the mass-loaded material in both the vertical and horizontal directions, Once this process is accomplished, the transfer functions are merged with a theoretical model and displayed as analytical surfaces from which the dilatational and shear wavenumbers can be identified and estimated, These wavenumbers are then combined to determine complex dilatational wavespeed, complex shear wavespeed, complex Lamb constants, complex Young's modulus, complex shear modulus, and complex Poisson's ratio,
Transfer switches for high performance contiguous-disk magnetic bubble devices (1982)

New transfer switches for 4-μm period ion-implanted contiguous-disk bubble devices are reported. Bubbles are translated through the major loop during WRITE-line transfer so that the data appear at the detector-after transfer from the storage loops-in the same order as they are written into the chip. Bias field margins of ∼8 percent have been obtained at drive field frequencies in the range of 100-400 kHz, making the designs particularly suitable for high performance (that is, short access time, high data rate) applications. Long-term testing has shown that such components can be operated over many cycles with only a modest degradation in bias margin of 0.5 Oe per decade.
Small Molecule Antagonists of the Nuclear Androgen Receptor for the Treatment of Castration-Resistant Prostate Cancer (2016)

After a high-throughput screening campaign identified thioether 1 as an antagonist of the nuclear androgen receptor, a zone model was developed for structure-activity relationship (SAR) purposes and analogues were synthesized and evaluated in a cell-based luciferase assay. A novel thioether isostere, cyclopropane (1S,2R)-27, showed the desired increased potency and structural properties (stereospecific SAR response, absence of a readily oxidized sulfur atom, low molecular weight, reduced number of flexible bonds and polar surface area, and drug-likeness score) in the prostate-specific antigen luciferase assay in C4-2-PSA-rl cells to qualify as a new lead structure for prostate cancer drug development.
Loaded Transducer Fpr Downhole Drilling Component (2005)

A robust transmission element for transmitting information between downhole tools, such as sections of drill pipe, in the presence of hostile environmental conditions, such as heat, dirt, rocks, mud, fluids, lubricants, and the like. The transmission element maintains reliable connectivity between transmission elements, thereby providing an uninterrupted flow of information between drill string components. A transmission element is mounted within a recess proximate a mating surface of a downhole drilling component, such as a section of drill pipe. To close gaps present between transmission elements, transmission elements may be biased with a "spring force," urging them closer together.
High Temperature Compression Properties of Ni<sub>3</sub>(Si,Ti) Based Intermetallic Compounds (2014)

High temperature compression properties of Al-, Cr-or Nb-added Ni 3 (Si,Ti) based intermetallic compounds were investigated by uni-axial compression test and microstructural observation. The Al-or Cr-added Ni 3 (Si,Ti) alloys after homogenization heat treatment exhibited a two-phase microstructure consisting of L1 2 and Ni-solid solution phases. The Nb-added Ni 3 (Si,Ti) alloy after homogenization heat treatment exhibited a triple-phase microstructure consisting of G-phase with D8a structure and Ni-solid solution phase in the L1 2 matrix. The volume fraction of Ni-solid solution phase increased in order of Cr-, Nb-and Al-added Ni 3 (Si,Ti) alloys. The Cr-added Ni 3 (Si,Ti) alloy was deformable at high strain rate, while the Nb-added one was deformable at low strain rate. It can be considered that the deformability of Ni 3 (Si,Ti) at high temperature is closely correlated with volume fraction of Ni-solid solution phase and recrystallization behavior.
Mining Software Revision History Using Advanced Social Network Analysis (2012)

In this paper, we propose a novel method to investigate relationship between the files that are committed together by applying advanced social network analysis to a "network" of source files that are committed together. The source files constitute the nodes of the network and an edge is created between files which are committed together in the same revision. We present our findings with recommendations on how mining revision histories from a social network analysis perspective can be used to build inferences on change propagation, evaluate impact analysis, and extract cross-programming-language relationships. We performed empirical analysis on revision histories of a well-known open-source web application testing system, 'Selenium' and results are reported.
Equivalence of VSSO and VSVO Kalman Channel Estimators in Doubly-Selective OFDM Systems—A Theoretical Perspective (2011)

Vector state-vector observation (VSVO) , and vector state-scalar observation (VSSO) are two types of Kalman estimators that can be used for channel estimation in doubly-selective OFDM systems over wide-sense stationary uncorrelated-scattering (WSSUS) channels. It was shown in that the VSSO Kalman channel estimator resulted in over 90% complexity savings compared to the VSVO Kalman channel estimator and this was achieved without any loss of performance. This inevitably raises the question whether the VSSO and VSVO Kalman channel estimators are computationally equivalent? We attempt to answer this question in this letter and theoretically show the equivalence of the VSSO and VSVO Kalman channel estimator for WSSUS channels.
Piston-Driven Fluid Ejectors In Silicon Mems (2005)

A surface-micromachined fluid-ejection apparatus is disclosed which utilizes a piston to provide for the ejection of jets or drops of a fluid (e.g. for ink-jet printing). The piston, which is located at least partially inside a fluid reservoir, is moveable into a cylindrical fluid-ejection chamber connected to the reservoir by a microelectromechanical (MEM) actuator which is located outside the reservoir. In this way, the reservoir and fluid-ejection chamber can be maintained as electric-field-free regions thereby allowing the apparatus to be used with fluids that are electrically conductive or which may react or break down in the presence of a high electric field. The MEM actuator can comprise either an electrostatic actuator or a thermal actuator.
Selective stimulation of the hypoglossal nerve: a fine approach to treating obstructive sleep apnea (2002)

Isolated activation of the tongue protrusor muscles is the current technique for treating obstructive sleep apnea (OSA) via functional electrical stimulation. Recent studies, however, have shown marked improvements in upper airway (UAW) patency by co-activating the tongue protrudor and retractor muscles. As such, selective stimulation of the hypoglossal (XII) nerve with a single implantable device presents an attractive alternative for treating OSA. In order to demonstrate the feasibility of such a device, the maximum achievable stimulation selectivity of the Flat Interface Nerve Electrode (FINE) was investigated. The beagle XII nerve was stimulated with an implanted FINE, while the corresponding neural and muscular responses were recorded. The overall performance of the FINE, as defined by the selectivity index (SI), showed a high degree of selectivity at both the fascicular and muscular levels: 0.91 /spl plusmn/ 0.05 (n = 5) and 0.85 /spl plusmn/ 0.03 (n = 4), respectively. The results clearly demonstrate the feasibility of the FINE for selective stimulation of the XII nerve and UAW muscles.
On the temperature assignment problem and the use of confidence textures in the creation of 3D thermograms (2015)

In infrared thermography, the temperature measured by a thermal imaging device varies with the position and orientation of the camera with respect to an object's surface. 3D thermography has hence the potential to depict the surface temperature of objects with higher fidelity than conventional 2D thermography. So far the problem of assigning temperature values that correspond to the same surface but were obtained from different perspectives has been addressed by simply overwriting previous values with new values or by averaging the measured values according to a weighted averaging scheme. A new approach to map temperature values onto a 3D model is proposed that results in a more faithful representation of an object's real surface temperature in form of a 3D thermogram. Temperature values are assigned in real time to the 3D model taking into consideration the observation conditions under which they were measured. These conditions are also made available to the user in form of textured 3D models, where the texture color depicts the level of confidence associated to the thermal measurements. These textures provide useful additional information about the 3D thermogram. The new approach is especially helpful in the real-time generation of 3D thermograms as the user gets live feedback on the quality of the thermal model being generated.
An oligopeptide transport gene from Candida albicans (1997)

A Candida albicans oligopeptide transport gene, OPT1, was cloned from a C. albicans genomic library through heterologous expression in the Saccharomyces cerevisiae di-/tripeptide transport mutant PB1X-9B. When transformed with a plasmid harbouring OPT1, S. cerevisiae PB1X-9B, which did not express tetra-/pentapeptide transport activity under the conditions used, was conferred with an oligopeptide transport phenotype, as indicated by growth on the tetrapeptide Lys-Leu-Leu-Gly, sensitivity to toxic tetra- and pentapeptides, and an increase in the initial uptake rate of the radiolabelled tetrapeptide Lys-Leu-Gly-[3H]Leu. The level of oligopeptide transport was found to be influenced in the heterologous host by the source of nitrogen used for growth. The entire 3.8 kb fragment containing the oligopeptide transport activity was sequenced and an ORF of 2349 nucleotides containing a 58 nucleotide intron was identified. The deduced protein product of 783 amino acid residues contained 12 hydrophobic regions suggestive of a membrane transport protein. Sequence comparisons revealed that similar proteins are encoded by genes from S. cerevisiae and Schizosaccharomyces pombe and that OPT1 is not a member of the ABC or PTR membrane transport families.
CRISPR-Cpf1 correction of muscular dystrophy mutations in human cardiomyocytes and mice (2017)

Duchenne muscular dystrophy (DMD), caused by mutations in the X-linked dystrophin gene (<i>DMD</i>), is characterized by fatal degeneration of striated muscles. Dilated cardiomyopathy is one of the most common lethal features of the disease. We deployed Cpf1, a unique class 2 CRISPR (clustered regularly interspaced short palindromic repeats) effector, to correct <i>DMD</i> mutations in patient-derived induced pluripotent stem cells (iPSCs) and <i>mdx</i> mice, an animal model of DMD. Cpf1-mediated genomic editing of human iPSCs, either by skipping of an out-of-frame <i>DMD</i> exon or by correcting a nonsense mutation, restored dystrophin expression after differentiation to cardiomyocytes and enhanced contractile function. Similarly, pathophysiological hallmarks of muscular dystrophy were corrected in <i>mdx</i> mice following Cpf1-mediated germline editing. These findings are the first to show the efficiency of Cpf1-mediated correction of genetic mutations in human cells and an animal disease model and represent a significant step toward therapeutic translation of gene editing for correction of DMD.
Human embryonic stem cells: A potential source for cellular therapy (2004)

Many degenerative human diseases reflect damage to cells that are not normally repaired or replaced, such as diabetes, Parkinson's disease, hepatic failure and congestive heart failure. Preliminary studies in animals and humans have suggested that these diseases may be treatable by transplantation of healthy cells. Such cells may be obtained by in vitro culture of embryonic stem cells, which are capable of differentiating into many cell types. This review discusses applicative approaches for the derivation, maintenance and safety of human embryonic stem (hES) cells as well as ethical concerns surrounding their possible source for cellular therapy. hES cells offer broad application in cellular therapy; however, this review specifically emphasizes on cardiovascular repair, generation and characterization of hES cell-derived cardiomyocytes, vascular progenitors and differentiation of derivatives.
Overshadow (2008)

Commodity operating systems entrusted with securing sensitive data are remarkably large and complex, and consequently, frequently prone to compromise. To address this limitation, we introduce a virtual-machine-based system called Overshadow that protects the privacy and integrity of application data, even in the event of a total OScompromise. Overshadow presents an application with a normal view of its resources, but the OS with an encrypted view. This allows the operating system to carry out the complex task of managing an application's resources, without allowing it to read or modify them. Thus, Overshadow offers a last line of defense for application data. Overshadow builds on multi-shadowing, a novel mechanism that presents different views of "physical" memory, depending on the context performing the access. This primitive offers an additional dimension of protection beyond the hierarchical protection domains implemented by traditional operating systems and processor architectures. We present the design and implementation of Overshadow and show how its new protection semantics can be integrated with existing systems. Our design has been fully implemented and used to protect a wide range of unmodified legacy applications running on an unmodified Linux operating system. We evaluate the performance of our implementation, demonstrating that this approach is practical.
Uptake of one and two molecules of CO<sub>2</sub> by the molybdate dianion: a soluble, molecular oxide model system for carbon dioxide fixation (2014)

Herein we report the finding that molybdate absorbs not just one but two equivalents of CO<sub>2</sub> (the second, reversibly) together with complete characterization including single-crystal X-ray diffraction studies of the resulting mono- and dicarbonate complexes.
Synthesis and Properties of Star HPMA Copolymer Nanocarriers Synthesised by RAFT Polymerisation Designed for Selective Anticancer Drug Delivery and Imaging (2015)

High-molecular-weight star polymer drug nanocarriers intended for the treatment and/or visualisation of solid tumours were synthesised, and their physico-chemical and preliminary in vitro biological properties were determined. The water-soluble star polymer carriers were prepared by the grafting of poly(amido amine) (PAMAM) dendrimers by hetero-telechelic N-(2-hydroxypropyl)methacrylamide (HPMA) copolymers, synthesised by the controlled radical Reversible Addition Fragmentation chain Transfer (RAFT) polymerisation. The well-defined star copolymers with Mw values ranging from 2 · 10(5) to 6 · 10(5) showing a low dispersity (approximately 1.2) were prepared in a high yield. A model anticancer drug, doxorubicin, was bound to the star polymer through a hydrazone bond, enabling the pH-controlled drug release in the target tumour tissue. The activated polymer arm ends of the star copolymer carrier enable a one-point attachment for the targeting ligands and/or a labelling moiety. In this study, the model TAMRA fluorescent dye was used to prove the feasibility of the polymer carrier visualisation by optical imaging in vitro. The tailor-made structure of the star polymer carriers should facilitate the synthesis of targeted polymer-drug conjugates, even polymer theranostics, for simultaneous tumour drug delivery and imaging.
Oil production by fermentation of lactose and the effect of temperature on the fatty acid composition1 (1978)

Abstract Strains of the yeasts Candida curvata and Trichosporon cutaneum were isolated that were able to ferment the lactose of cheese whey and ultrafiltered whey permeate to produce oil. Rapid fermentation rates and lactose utilization were achieved by the G curvata strains. The fermentation was more efficient on permeate than whey, because the organisms used whey protein very poorly. Methods of extracting the oil were compared, and the best results were obtained by sequential extraction with methanol and benzene or by ethanol and hexane. The fatty acid composition of the yeasts varied with the growth temperature, fermentation time, and medium. The oil was rich in 18:1, 16:0, and 18:0. The process is a technically feasible means of using whey permeate.
Pulse dynamics in optical fibers with random dispersion (2001)

Wo consider pulse propagation in an optical fiber link with/without dispersion management in the presence of random variation of chromatic dispersion. We propose a technique to stabilize pulse deterioration due to this dispersion randomness.
Large field-of-view and high resolution free-form head-mounted display (2010)

It is challenging to design a large field of view (FOV) and low F-number optical system, especially an eyepiece for head-mounted displays (HMD), which also demands compactness in size, lightness in weight and a large exit pupil distance. In this paper, we describe a novel design of a wide FOV free-form eyepiece by tiling multiple wedge-shaped free-form prisms. We compared our tiling method using the novel free-form prism eyepieces with a traditional tiling approach and the drawbacks of the traditional tiling method are analyzed. We further present a successive approximation method for designing a freeform surface and compare the accuracy of several surface conversion methods. An example design was also demonstrated.
“Polyaniline”: Interconversion of Metallic and Insulating Forms (1985)

Abstract “Polyaniline” has been synthesized in various forms both chemically and electrochemically in aqueous media. The qulnoid-benzenoid-diimine form, an insulator, is doped by dilute aqueous protonic acids to the metallic regime ([sgrave] = 5 ohm−1cm−1; compressed pellet) to give the corresponding iminium salt. This represents a new type of p-doping phenomenon in a conducting polymer. Both these forms are stable in the presence of air and/or water. The doping process is reversed by treatment with aqueous alkali. Cyclic voltammetry studies in an aqueous electrolyte show excellent reversibility between selected reduced and oxidized forms of polyaniline.
Optical arithmetic/logic unit based on residue arithmetic and symbolic substitution (1988)

There has been difficulty in achieving a fully parallel, digital optical adder or multiplier. The primary obstacle is the carry operation inherent in any fixed-radix number system. The concepts of residue number representation and symbolic substitution can be combined to produce a parallel optical arithmetic/logic unit.