gebhart/patrepeval huggingface dataset:
Identification of the amino-acetonitrile derivative monepantel (AAD 1566) as a new anthelmintic drug development candidate (2008)

Anthelmintic resistance has become a global phenomenon in gastro-intestinal nematodes of farm animals, including multi-drug resistance against the three major classes of anthelmintics. There is an urgent need for an anthelmintic with a new mode of action. The recently discovered amino-acetonitrile derivatives (AADs) offer a new class of synthetic chemicals with anthelmintic activity. The evaluation of AADs was pursued applying in vitro assays and efficacy and tolerability studies in rodents, sheep, and cattle. Amongst various suitable compounds, AAD 1566 eliminated many tested pathogenic nematode species, both at larval and adult stages, at a dose of 2.5 mg/kg bodyweight in sheep and 5.0 mg/kg bodyweight in cattle. The same doses were sufficient to cure animals infected with resistant or multi-drug-resistant nematode isolates. These findings, complemented by the good tolerability and low toxicity to mammals, suggest that AAD 1566, monepantel, would be a suitable anthelmintic drug development candidate.
Estimating maximal measurable performance for automated decision systems from the characteristics of the reference standard. application to diabetic retinopathy screening (2014)

We investigate the maximal performance that can be measured for automated binary decision systems in terms of area under the ROC curve (AUC), against a reference standard provided by human readers. The goal is to determine the required characteristics of the reference standard to assess and compare automated decision systems with a given degree of confidence, or, to determine what degree of confidence can be obtained given the characteristics of the reference standard. We modeled the expected value of the AUC that can be measured for a perfect decision system, given a reference standard provided either by a single human reader or by multiple human readers (consensus, majority vote). The proposed model was applied to diabetic retinopathy screening in a dataset of 874 eye fundus examinations graded by three readers. The expected value of the AUC for a perfect decision system was estimated at 0.956 against a single human reader, and 0.990 against a `majority wins' vote of three human readers. The Iowa detection program has reached the maximal performance measurable by a single human reader (0.929, CI: [0.897-0.962]) and is close to the maximal performance measurable by a `majority wins' vote (0.955, CI: [0.939-0.972]).
Air cavity low-loss signal lines on bt substrates for high frequency chip-to-chip communication (2009)

Chip-to-chip communication across conventional printed circuit boards is limited to low frequencies (a few GHz), thus limiting the aggregate bandwidth without the use of optics. Low-loss, air insulated transmission lines can extend the frequency range of electrical circuitry on fiberglass-epoxy substrates (e.g. FR4 and BT). Described in this paper are electrical signal lines separated only by an airgap fabricated on BT substrates. The structures demonstrated greater than 46 percent reduction in capacitance and greater than 90 percent in loss tangent, which translates to substantially lower losses at high frequencies (10 GHz or greater). Attenuation in these structures have been simulated to be eight times lower than conventional microstrip lines. Air cavity signal lines are currently being integrated on multilayer BT substrates to demonstrate chip-to-chip communication using chips fabricated at the 65-nm node employing cross-talk cancellation techniques.
Development of an expert system for injection molding operations (1993)

Abstract To provide a computer assisted system in finding optimum conditions for injection molding operations, an Expert System based on Artificial Intelligence (AI) technique and knowledge or “know‐how” from many skilled injection molding operators has been developed. For the construction of this Expert System, we have originally applied a new method of “Multi‐dimensional Matrix” that represents the relationship between the parameters of each molding condition and expert's knowledge. In this article we describe an outline of the system and the process of converting expert knowledge into AI rules, and demonstrate some molded samples obtained using this Expert System. © 1993 by John Wiley &amp; Sons, Inc.
Design and Analysis of a Surface Micromachined Spiral-Channel Viscous Pump (2003)

A new viscous spiral micropump which uses the surface micromachining technology is introduced. The paper outlines the design of a spiral pump fabricated in five levels of polysilicon using Sandia’s Ultraplanar Multilevel MEMS Technology (SUMMiT), and presents an analytical solution of the flow field in its spiral channel. The pump characteristics are obtained experimentally for a scaled-up prototype and are found to be in good agreement with the results obtained using the analytical model.
Scalar relativistic effects on energies of molecules containing atoms from hydrogen through argon (2001)

Stationary direct perturbation theory is used to calculate a scalar relativistic correction to the species in the G3/99 test set. We observe that the relativistic energy almost always reduces atomization energies, electron affinities, and ionization potentials. Exceptions occur when s orbitals play a predominant role in the energy differences between reactants and products. The scalar relativistic energy, when added to G3 theory and the empirical parameters are reoptimized, gives slightly worse agreement with experiment.
EVIDENCE THAT GABAA RECEPTORS MEDIATE RELAXATION OF RAT DUODENUM BY ACTIVATING INTRAMURAL NONADRENERGIC‐NON‐CHOLINERGIC NEURONES (1984)

GABA produced rapid and transient relaxation of rat duodenum. Homotaurine (3-aminopropansulphonic acid) but not (+/-)-baclofen had a GABA-like effect. GABA-induced relaxation was almost completely inhibited by tetrodotoxin but was unaffected by atropine. Cross desensitization developed between GABA and homotaurine but not between GABA and (+/-)-baclofen. The concentration response curve to the relaxant effects of GABA was shifted to the right by both bicuculline and picrotoxin. However maximal relaxation was still produced by GABA in the presence of bicuculline but not in the presence of picrotoxin. GABA-induced relaxation was not affected by prazosin, yohimbine, propranolol or reserpine pretreatment. Field stimulation (0.1 Hz) of rat isolated duodenum in the presence of atropine and guanethidine produced relaxation similar to that produced by GABA. The ganglionic stimulant DMPP produced a similar effect. Neither Met-enkephalin, noradrenaline, 5-HT, histamine, VIP or arachidonic acid could be held responsible for GABA-induced neurogenic relaxation of rat duodenum. ATP produced relaxations which closely mimicked those produced by either GABA or field stimulation. Exposure to ATP desensitized responses to both GABA and field stimulation to about the same extent. ATP, GABA and field stimulation-induced relaxation was unaffected by either theophylline or indomethacin, but was significantly and selectively antagonized by apamin. In conclusion, GABA-induced relaxation of rat isolated duodenum is largely dependent upon activation of intra-mural nonadrenergic-noncholinergic neurones. The GABA receptor involved appears to be of the GABAA subtype. Circumstantial evidence is provided indicating that ATP might be the endogenous substance released by GABA.
MYC-driven synthesis of Siglec ligands is a glycoimmune checkpoint (2023)

The Siglecs (sialic acid-binding immunoglobulin-like lectins) are glycoimmune checkpoint receptors that suppress immune cell activation upon engagement of cognate sialoglycan ligands. The cellular drivers underlying Siglec ligand production on cancer cells are poorly understood. We find the <i>MYC</i> oncogene causally regulates Siglec ligand production to enable tumor immune evasion. A combination of glycomics and RNA-sequencing of mouse tumors revealed the <i>MYC</i> oncogene controls expression of the sialyltransferase <i>St6galnac4</i> and induces a glycan known as disialyl-T. Using in vivo models and primary human leukemias, we find that disialyl-T functions as a "don't eat me" signal by engaging macrophage Siglec-E in mice or the human ortholog Siglec-7, thereby preventing cancer cell clearance. Combined high expression of <i>MYC</i> and <i>ST6GALNAC4</i> identifies patients with high-risk cancers and reduced tumor myeloid infiltration. MYC therefore regulates glycosylation to enable tumor immune evasion. We conclude that disialyl-T is a glycoimmune checkpoint ligand. Thus, disialyl-T is a candidate for antibody-based checkpoint blockade, and the disialyl-T synthase ST6GALNAC4 is a potential enzyme target for small molecule-mediated immune therapy.
Fourier transform infrared investigation of the effects of irradiation on the 19 and 30°C phase transitions in polytetrafluoroethylene (1980)

Abstract Fourier transform infrared spectroscopy has been used in conjunction with differential scanning calorimetric measurements to investigate the nature of molecular degradation and its effect on the phase transition temperatures in irradiated polytetrafluoroethylene (PTFE). Both the 19 and 30°C transitions are observed to exhibit similar shifts to low temperatures upon irradiation. Infrared absorbance subtraction data from irradiated PTFE indicate a continual decrease in sample crystallinity accompanied by an increase in the number of free and bonded COOH groups with increasing dose consistent with molecular degradation by chain scission. By comparing infrared band intensities on a number of irradiated PTFE samples with those from short chain perfluoro n ‐alkanes, it was determined that the overall reduction in chain length caused by irradiation was primarily responsible for the observed reduction in both phase transition temperatures.
Comet assay as a reliable tool for genotoxic exposure and reproductive effect assessment in Gammarus fossarum (2009)

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Transport properties of some alternative refrigerants. (1993)

The paper presents a brief description of experimental techniques and equipment used for accurate measurement of thermal conductivities and viscosities of new fluorocarbon refrigerants over a range of temperatures and pressures. New experimental results are presented for selected refrigerants. Correlations were also developed that allow one to calculate transport properties or to estimate them with minimal experimental information. Measurements were done using a modified hot-wire and capillary-tube method.
DIAGNOSTIC MODE FOR EARLY DIAGNOSIS OF ACUTE AORTIC DISSECTION (2012)

Objectives To investigate the clinical manifestations, laboratory tests, imaging characteristics of acute aortic dissection (AD) patients, looking for a simple diagnostic mode for early accurate diagnosis of AD. Methods 156 cases of acute AD patients hospitalised in the hospital January 2005 to December 2011 were collected, clinical manifestations, laboratory tests, imaging data were analysed to explore the diagnostic mode for the early diagnosis of AD. Results According to the logistic regression equations and clinical practice to establish scoring models for the early diagnosis of AD. Score 5, predicts that the sensitivity of AD was 98.2%, specificity of 83.4%. Conclusions A diagnostic mode Containing sudden severe pain of abdominal, chest and (or) back, abnormal elevation of blood pressure, the blood pressure and (or) pulse inconsistent both sides, chest radiograph for aortic shadow and (or) mediastinal shadow widening, significantly higher D-dimer may significantly improve the early diagnosis of acute AD.
Radical, One-Step Approach to o-Chlorophenyl Thioethers from Xanthates. A Rapid Access to Vinylsilanes (2008)

Xanthates have been readily converted into o-chlorophenyl thioethers using a one-step procedure conducted under radical conditions. In some selected cases, these aryl thioethers were successfully oxidized to the corresponding sulfoxides and sulfenic acid elimination afforded the corresponding vinylsilanes.
dWFS: DISTRIBUTED WAVE FIELD SYNTHESIS (2006)

In this paper we consider the problem of using a network of sensor and actuator nodes, to synthesize a given desired wave field in a given medium – we refer to this problem as the distributed Wave Field Synthesis problem (dubbed dWFS). We formulate this problem as one of minimization of a quadratic function, subject to linear (and very sparse) constraints. This formulation results from a finite-element approximation of the underlying wave equation, which constrains the values that a field and the source that induces that field can take. We present a complete solution for a 1D vibration, although our solution method can be readily extended to any number of dimensions. Numerical simulations are included.
Space robotics - towards advanced mechatronic components and powerful telerobotic systems (2001)

Salmonellae, gram-negative bacteria, are facultative intracellular pathogens that cause a number of diseases in animals and humans. The poor penetration ability of antimicrobial agents limits their use in the treatment of intracellular bacterial infections. In this study, the cell-penetrating peptides (CPPs) bLFcin<sub>6</sub> and Tat<sub>11</sub> were separately conjugated to the antimicrobial peptide N2, and the antibacterial activity and pharmacodynamics of the CPPs-N2 conjugates were first evaluated against Salmonellae typhimurium in vitro and in macrophage cells. The cytotoxicity, cellular uptake and mechanism of cellular internalization of the CPPs-N2 conjugates were also examined in RAW264.7 cells. Similar to N2, CPPs-N2 have two reverse β-sheets and three loops. The minimal inhibitory concentration (MIC) of CPPs-N2 was approximately 2 μM, which was higher than that of N2 (0.8 μM). The dose-time curves and cytotoxicity assay showed that both peptide conjugates were more effective than N2 alone at concentrations ranging from 0.25 to 1 × MIC, and they exhibited low cytotoxicity (9.78%-13.54%) at 100 μM. After 0.5 h incubation, the cell internalization ratio of B6N2 and T11N2 exceeded 28.3% and 93.5%, respectively, which was higher than that of N2. The uptake of B6N2 and T11N2 was reduced by low temperature (82.1%-91.7%), chlorpromazine (35.7%-75.1%), and amiloride (26.0%-52.1%), indicating that macropinocytosis and clathrin-mediated endocytosis may be involved. Approximately 98.85% and 91.35% of bacteria were killed within 3 h by T11N2 and B6N2, respectively, which was higher than the percentage killed by N2 (69.74%). Compared with the bactericidal activity of N2 alone, the bactericidal activity of T11N2 and B6N2 was increased by 53.7%-99.6% and 85.3-85.8%, respectively. Both CPPs-N2 conjugates may be excellent candidates for novel antimicrobial agents to treat infectious diseases caused by intracellular pathogens.
Structural Characterization of Nitroxide-Terminated Poly(n-butyl acrylate) Prepared in Bulk and Miniemulsion Polymerizations (2002)

The structure of “living” poly(n-butyl acrylate) homopolymers prepared via nitroxide-mediated controlled radical polymerization in bulk and in miniemulsion at 112 °C was examined by SEC, NMR, and MALDI−TOF mass spectrometry in order to study the influence of chain transfer to polymer. The absence of detectable terminal unsaturation was confirmed by proton NMR. The branched structure was observed by 13C NMR. MALDI−TOF MS demonstrated that the majority of chains, even at high conversion, had the ideal structure with one initiator fragment and one nitroxide end group. From these results, we concluded that intramolecular chain transfer occurred (presumably by backbiting) and was the predominant mechanism throughout the polymerization at 112 °C.
Block Based Extra/Inter-Polating Prediction for Intra Coding (2007)

In this paper, we propose an efficient intra coding method. The method involves adding an extra/inter-polating prediction method to the conventional H.264/MPEG-4 AVC (H.264) intra prediction method. The proposal consists of two parts. One is to change the sub-block coding order in macroblock (MB). The bottom-right sub-block in MB is predicted using the reference pels on the upper and left side of the sub-block firstly. After that, the other sub-blocks are predicted using not only the reference pels on the upper and/or left side but also ones on the bottom and/or right side of each sub-block. The other part is to use an intra bidirectional prediction method which can use the interpolation of the prediction from upper/left pels and the prediction from bottom/right pels. Experimental results show that our method improves bit reduction by up to 7.7% at the same PSNR compared to H.264.
Stress Responses in Alfalfa (XXI. Activation of Caffeic Acid 3-O-Methyltransferase and Caffeoyl Coenzyme A 3-O-Methyltransferase Genes Does Not Contribute to Changes in Metabolite Accumulation in Elicitor-Treated Cell-Suspension Cultures) (1996)

Transcription of genes encoding L-phenylalanine ammonia-lyase (PAL), the first enzyme of the phenylpropanoid pathway, and caffeic acid 3-O-methyltransferase (COMT) and caffeoyl CoA 3-O-methyltransferase (CCOMT), enzymes involved in the synthesis of lignin and wall-esterified phenolic compounds, was strongly activated in elicitor-treated cell-suspension cultures of alfalfa (Medicago sativa L.). However, consequent changes in the extractable activities of COMT and CCOMT were small to nonexistent compared with a 15- to 16-fold increase in PAL activity. Only low levels of COMT and CCOMT transcripts were reflected in the total and polysomal RNA fractions compared with PAL transcripts. Elicited cell cultures did not accumulate lignin or the products of COMT and CCOMT in the soluble and wall-esterified phenolic fractions. In one alfalfa cell line in which elicitation resulted in very high PAL activity and increased deposition of methoxyl groups in the insoluble wall fraction, there was still no change in COMT and CCOMT activities. Overall, these results indicate that the initial gene transcription events in elicited cells may be less selective than the subsequent metabolic changes, highlighting the importance of posttranscriptional events in the control of phenylpropanoid biosynthesis.
Imatinib induces durable hematologic and cytogenetic responses in patients with accelerated phase chronic myeloid leukemia: results of a phase 2 study (2002)

Chronic myelogenous leukemia (CML) is caused by expression of the BCR-ABL tyrosine kinase oncogene, the product of the t(9;22) Philadelphia translocation. Patients with CML in accelerated phase have rapidly progressive disease and are characteristically unresponsive to existing therapies. Imatinib (formerly STI571) is a rationally developed, orally administered inhibitor of the Bcr-Abl kinase. A total of 235 CML patients were enrolled in this study, of whom 181 had a confirmed diagnosis of accelerated phase. Patients were treated with imatinib at 400 or 600 mg/d and were evaluated for hematologic and cytogenetic response, time to progression, survival, and toxicity. Imatinib induced hematologic response in 82% of patients and sustained hematologic responses lasting at least 4 weeks in 69% (complete in 34%). The rate of major cytogenetic response was 24% (complete in 17%). Estimated 12-month progression-free and overall survival rates were 59% and 74%, respectively. Nonhematologic toxicity was usually mild or moderate, and hematologic toxicity was manageable. In comparison to 400 mg, imatinib doses of 600 mg/d led to more cytogenetic responses (28% compared to 16%), longer duration of response (79% compared to 57% at 12 months), time to disease progression (67% compared to 44% at 12 months), and overall survival (78% compared to 65% at 12 months), with no clinically relevant increase in toxicity. Orally administered imatinib is an effective and well-tolerated treatment for patients with CML in accelerated phase. A daily dose of 600 mg is more effective than 400 mg, with similar toxicity.
The Hardness of Learning Access Control Policies (2023)

The problem of learning access control policies is receiving increasing attention in research. We contribute to the foundations of this problem by posing and addressing meaningful questions on computational hardness. Our work addresses learning access control policies in the context of three different models from the literature: the access matrix, and Role- and Relationship-Based Access Control (RBAC and ReBAC, respectively). Our underlying theory is the well-established notion of Probably Approximately Correct (PAC), with careful extensions for our setting. The data, or examples, a learning algorithm is provided in our setup is that related to access enforcement, which is the process by which a request for access to a resource is decided. For the access matrix, we pose a learning problem that turns out to be computationally easy, and another that we prove is computationally hard. We generalize the former result so we have a sufficient condition for establishing other problems to be computationally easy. With these results as the basis, we consider five learning problems in the context of RBAC, two of which turn out to be computationally hard. Finally, we consider four learning problems in the context of ReBAC, all of which turn out to be computationally easy. Every proof for a problem that is computationally easy is constructive, in that we propose a learning algorithm for the problem that is efficient, and probably, approximately correct. As such, our work makes contributions at the foundations of an important, emerging aspect of access control, and thereby, information security.
Validation of moulding productivity with two self-regulating melt pressure valves (2004)

A self-regulating melt pressure valve has been developed to proportion melt pressure relative to a control force without the need for a pressure transducer or a closed-loop controller. The lean and agile plastics injection moulding, realized through the use of multiple self-regulating melt pressure valves that provide independent zone-based control of the polymer melt pressure and flow rate, is characterized. The process productivity of a hot-runner injection moulding process with two self-regulating melt pressure valves is validated with respect to flexibility and clamp tonnage requirements. With respect to flexibility, the use of the two self-regulating valves provided the individual tuning of two cavities of varying geometry. The resulting mouldings could not be produced to specification without the self-regulating valves or changes in the mould design. Furthermore, the consistency (as measured by the standard deviation of part weights) of the moulded parts with the self-regulating melt pressure valves was at least twice the consistency of the moulded parts produced with conventional moulding. With respect to productivity, the independent profiling and time shifting of the melt pressure for each moulding zone with the self-regulating valves enabled a 20% reduction in clamp tonnage with no increase in cycle time and a 50% reduction in clamp tonnage requirement with an 8% increase in cycle time compared with conventional injection moulding.