gebhart/patrepeval huggingface dataset:
Development of Dual-Acting Agents for Thromboxane Receptor Antagonism and Thromboxane Synthase Inhibition. 3. Synthesis and Biological Activities of Oxazolecarboxamide-Substituted ω-Phenyl-ω-(3-pyridyl)alkenoic Acid Derivatives and Related Compounds (1998)

A novel series of oxazolecarboxamide-substituted omega-phenyl-omega-(3-pyridyl)alkenoic acid derivatives was discovered as potent dual-acting agents to block the TXA2 receptor and to inhibit the thromboxane synthase (TRA/TSI). Synthesis, structure-activity relationship (SAR), and in vitro and in vivo pharmacology of this series of compounds are described. Modification of the series revolved around the oxazole moiety to increase the hydrophilicity of the compounds and to correlate the biological activity with lipophilicity of the compounds. The most potent in the series was (E)-7-[4-[4-[[(4-cyclohexylbutyl)amino]carbonyl]-2-oxazolyl] phenyl]-7 -(3-pyridyl)hept-6-enoic acid (14) with Kd = 9.9 +/- 0.4 nM for the thromboxane receptor antagonism and IC50 = 55.0 +/- 17.9 nM for thromboxane synthase inhibition. The compound 14 was a selective TRA/TSI which exhibited desirable characteristics for oral activity, "shunt" effect to elevate PGI2 level, and absence of agonist activity.
Exceptionally Stable Fluorous Emulsions for the Intravenous Delivery of Volatile General Anesthetics (2012)

Hemifluorinated dibranched polymers can be used to generate exceptionally stable sevoflurane nanoemulsions, as required of formulations intended for clinical use. IV delivery of the emulsion in rats resulted in induction of anesthesia with rapid onset and smooth and rapid recovery.
Spectrum sensing for OFDM systems employing pilot tones (2009)

OFDM spectrum sensing algorithms are presented in this paper. The proposed spectrum sensing algorithms are based on Time-Domain Symbol Cross-Correlation (TDSC-MRC and TDSC-NP methods) and can be applied to all existing wireless OFDM systems. The statistical behaviors of the TDSCbased spectrum sensors are explicitly analyzed. The sensing performances of the TDSC-based spectrum sensors in terms of misdetection probability are derived in detail. In addition, the spectrum sensing method employing the Cyclic Prefix of the OFDM modulated signals (CP method) is described for comparison purposes. The DVB-T Standard [5] is adopted as an application example to illustrate the proposed spectrum sensing algorithms. Simulation results show that the TDSC-MRC method outperforms the CP method for all values of CP ratio considered. The TDSC methods have the advantage that the detection performances are the same for different CP ratios, while the detection performance of the CP method degrades dramatically when the CP ratio becomes small. From simulation results, for a sensing time of 50 ms, the TDSC-MRC method can achieve misdetection probabilities of 0.1 and 0.01 with respect to a false alarm probability of 0.01 for SNR values of -20.5 dB and -19.5 dB, respectively.
Strategy for Detection and Differentiation of <i>Coxiella bumetii</i> Strains Using the Polymerase Chain Reactionaa (1990)

A method for the rapid detection of Coxiella burnetii and differentiation between strains that cause endocarditis and those that cause acute Q fever is based on the observation that the different strains contain unique plasmid sequences. This method employs the polymerase chain reaction (PCR) and requires knowledge of specific DNA sequences in the region (target) of DNA to be amplified. To detect and differentiate between C. burnetii isolates, two sets of primers are required. The first set was derived from a fragment of plasmid QpH1 which has been detected in all C. burnetii isolates. A second PCR reaction was conducted using primers specific for DNA sequences that are shared only by QpRS plasmid-containing strains of C. burnetii. The first reaction detects the presence of C. burnetii. The second PCR is necessary to determine whether the isolate contains DNA sequences associated with strains causing chronic disease. These procedures detect as few as one to ten organisms.
Repeaterless 10.7-Gb/s DPSK Transmission Over 304 km of SSMF Using a Coherent Receiver and Electronic Dispersion Compensation (2008)

Record repeaterless transmission of differential phase-shift keying (DPSK) at 10.7 Gb/s over 304 km of standard single-mode fiber (SSMF) is demonstrated using a coherent optical receiver and electronic dispersion compensation. This is the longest repeaterless 10-Gb/s transmission over SSMF in the absence of Raman amplifiers. The high receiver sensitivity and the high tolerance to nonlinearities of DPSK allow us to overcome a total link loss of 58 dB with a 3-dB system margin. Coherent detection enables linear electrical dispersion compensation and avoids the use of optical dispersion compensation.
Self-calibrating Approach for Non-Contact Electrical Doping Profiling (2005)

We present a self‐calibrating version of non‐contact electrical doping profiling that is a refinement of our method based on monitoring of the decays of two voltages during the collapse of deep depletion. Small signal ac‐photovoltage, appropriately calibrated, provides a measure of the depletion capacitance, CD, while the corresponding depletion layer voltage, V, is obtained using a vibrating Kelvin probe. Deep depletion is created by a pulse of corona charge placed on the wafer surface. Doping depth profile is calculated from the set of C‐V data obtained from two voltage decays. The in‐situ self‐calibration is introduced in order to obtain, for each measurement, a constant that relates the ac‐photovoltage and the depletion capacitance. This constant depends on the condition of the wafer surface, and therefore, is not universal. Self‐calibration is realized by corona charging up to the avalanche breakdown limit and using the breakdown voltage relation to the dopant concentration. Application of the method is illustrated using epitaxial silicon wafers.
Preclinical and Clinical Experience with a Doxorubicin-Liposome Preparation (1990)

Entrapment of doxorubicin in liposomes results in increased drug concentrations in liver and spleen and decreased uptake by the heart muscle. these pharmacologic changes can be exploited to reduce the drug's toxicity and increase its therapeutic index in selected neoplastic conditions. We review here our preclinical and phase I clinical data with liposome-associated doxorubicin. these studies, together with preliminary observations on the pharmacokinetics of the liposome-associated drug and on the imaging of radiolabeled vesicles in patients, suggest that the maximal tolerated dosage is significantly increased over that of the free drug and that the reticuloendothelial system is responsible for the rapid and dominant pathway of liposome clearance. the implications of various pharmacologic aspects of liposome behavior in the circulation are also discussed.
Microfluidic Pumping Based on Traveling-Wave Dielectrophoresis (2009)

This article presents a microfluidic pumping approach using traveling-wave dielectrophoresis (twDEP) of microparticles. With this approach, the flow is generated directly in the microfluidic devices by inducing strong electromechanical effects in the fluid using integrated microelectrodes. The fluidic driving mechanisms due to the particle–fluid and particle–particle interactions under twDEP are analyzed, and the induced flow field is obtained from numerical simulations. Experimental measurements of the flow velocity in a prototype DEP micropumping device show satisfactory agreement with the numerical predications. Results from this work indicate that the DEP-induced micropumping scheme holds great promise for devising versatile, self-contained microscale fluidic delivery systems.
Secreted amyloid-β precursor protein functions as a GABA <sub>B</sub> R1a ligand to modulate synaptic transmission (2019)

Amyloid-β precursor protein (APP) is central to the pathogenesis of Alzheimer's disease, yet its physiological function remains unresolved. Accumulating evidence suggests that APP has a synaptic function mediated by an unidentified receptor for secreted APP (sAPP). Here we show that the sAPP extension domain directly bound the sushi 1 domain specific to the γ-aminobutyric acid type B receptor subunit 1a (GABA<sub>B</sub>R1a). sAPP-GABA<sub>B</sub>R1a binding suppressed synaptic transmission and enhanced short-term facilitation in mouse hippocampal synapses via inhibition of synaptic vesicle release. A 17-amino acid peptide corresponding to the GABA<sub>B</sub>R1a binding region within APP suppressed in vivo spontaneous neuronal activity in the hippocampus of anesthetized Thy1-GCaMP6s mice. Our findings identify GABA<sub>B</sub>R1a as a synaptic receptor for sAPP and reveal a physiological role for sAPP in regulating GABA<sub>B</sub>R1a function to modulate synaptic transmission.
Graphene's Role in Emerging Trends of Capacitive Energy Storage (2021)

Technological breakthroughs in energy storage are being driven by the development of next-generation supercapacitors with favorable features besides high-power density and cycling stability. In this innovation, graphene and its derived materials play an active role. Here, the research status of graphene supercapacitors is analyzed. Recent progress is outlined in graphene assembly, exfoliation, and processing techniques. In addition, electrochemical and electrical attributes that are increasingly valued in next-generation supercapacitors are highlighted along with a summary of the latest research addressing chemical modification of graphene and its derivatives for future supercapacitors. The challenges and solutions discussed in the review hopefully will shed light on the commercialization of graphene and a broader genre of 2D materials in energy storage applications.
Providing grades and feedback for student summaries by ontology-based information extraction (2012)

Automatic grading systems for summaries and essays have been studied for years. Most commercial and research implementations are based in statistical methods, such as Latent Semantic Analysis (LSA), which can provide high accuracy on similarity between the essay and the graded or standard essays, but they can offer very limited feedback. In the present work, we propose a novel method to provide both grades and meaningful feedback for student summaries by Ontology-based Information Extraction (OBIE). We use ontological concepts and relationships to create extraction rules to identify correct statements. Based on ontology constraints (e.g., disjointness between concepts), we define patterns that are logically inconsistent with the ontology to create rules to extract incorrect statements. Experiments show that the grades given to 18 student summaries on Ecosystems by OBIE are correlated to human gradings. OBIE also provide meaningful feedback on the errors those students made in their summaries.
Nonlinear optical isolators based on high-reflectivity Brillouin mirrors and their application to advanced lasers (1992)

A new type of optical isolator, the nonlinear isolator (NLI), was developed to replace polarization sensitive isolation devices in pulsed, solid state laser systems. The NLI was based on a high-reflectivity, stimulated Brillouin scatter (SBS) mirror configured as a Newtonian telescope. Transmission through the NLI was found to be limited to the SBS threshold power. Input powers tested were 50 to 100 times the threshold power. The NLI was operated in a 10-Hz repetition rate laser without introducing noticeable far-field distortion. Partial pulse compression could occur in the NLI. A single triple-pass phase-conjugated YAG amplifier that incorporated the NLI, plus a 2-mJ SLM oscillator, produced 0.83-J pulses of 2.5-ns duration.
Transient event detection in spectral envelope estimates for nonintrusive load monitoring (1995)

This paper describes the theoretical foundation and prototype implementation of a power system transient event detector for use in a nonintrusive load monitor (NILM). The NILM determines the operating schedule of the major electrical loads in a building from measurements made at the electric utility service entry. The transient event detector extends the applicability of the NILM to challenging commercial and industrial sites. A spectral preprocessor for use in the transient event detector is introduced first. Then, the transient event detection algorithm is developed. The performance of the algorithm is illustrated with results from a prototype event detector.< <ETX xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">></ETX>
Generation of PSA-ACT-Specific Monoclonal Antibodies and Their Application in a Sandwich Immunoassay (1999)

The prostate-specific antigen (PSA) immunoassay is an important tool for the detection and monitoring of prostate cancer. PSA exists in serum mainly as complexes with serine protease inhibitors including alpha1 antichymotrypsin (ACT) and alpha2 macroglobulin (MG). PSA-MG complex is not detected by the existing PSA immunoassays since MG (720 kDa) sequesters PSA and masks the antibody binding sites. Existing immunoassays for quantitation of total serum PSA measure PSA-ACT (CPSA) and free PSA (FPSA), which comprise the major and minor components of total PSA, respectively. Monoclonal antibodies (MAb) specific for CPSA alone were generated using a unique immunogen prepared by blocking the major antigenic determinants on FPSA and ACT. The blocked immunogen greatly enhanced the frequency of hybridomas reactive against the CPSA complex. CPSA prototype immunoassays were established using anti-CPSA (PX1G359) or anti-ACT (AC1A212) MAb as tracer MAb and anti-PSA (PSA399) MAb as capture MAb. The complex-selective MAbs demonstrated minimal cross-reactivity with Cathepsin-G (CG) ACT (CG-ACT), ACT or FPSA. CG-ACT complex interfered with the accuracy of initial prototype assays specific for CPSA measurement and caused over-recovery (1 to 3 ng/mL, with 40 to 180 ng/mL range of CG-ACT in serum) of apparent CPSA values. Addition of 0.4% NP-40 and 0.1% 0.088 micron microparticles in clinical specimens eliminated this interference. Specimens from 39 prostate cancer (PCa) patients and 44 benign prostatic hyperplasia (BPH) patients were analyzed with the PX1G359 CPSA assay. In this study, the area under the curve (AUC) values for ROC analysis of total PSA (CPSA+FPSA), FPSA to total PSA ratio (f/t), and FPSA to CPSA ratio (f/c) were 0.357, 0.634, and 0.624, respectively. In a second study using AC1A212 CPSA assay, where specimens from 16 PCa patients and 48 BPH patients were tested, the AUC values for total PSA, f/t and f/c ratios were 0.62, 0.785, and 0.732, respectively. Using the CPSA assay with minimal interference our studies are consistent with previous CPSA data showing that the f/t PSA ratio remains superior to the f/c PSA ratio in differentiating PCa and BPH diseases. Complex PSA by itself or as ratio with free or total PSA does not provide any advantage over the established method of FPSA to total PSA ratio.
Stereocontrolled Synthesis of (<i>E,Z</i>)-Dienals <i>via</i> Tandem Rh(I)-Catalyzed Rearrangement of Propargyl Vinyl Ethers (2013)

A novel Rh(I)-catalyzed approach to functionalized (E,Z) dienals has been developed via tandem transformation where a stereoselective hydrogen transfer follows a propargyl Claisen rearrangement. Z-Stereochemistry of the first double bond suggests the involvement of a six-membered cyclic intermediate whereas the E-stereochemistry of the second double bond stems from the subsequent protodemetalation step giving an (E,Z)-dienal.
Cross-talk between the two-component regulatory systems NodVW and NwsAB of<i>Bradyrhizobium japonicum</i> (1994)

The protein products of the Bradyrhizobium japonicum gene pairs nodVW and nwsVW are members of the bacterial two-component regulatory systems. While NodW and NwsB exhibit all of the characteristics of the response-regulator class, NodV and NwsA contain the conserved domain of the sensor-kinase family. Overexpression of the nwsB gene results in complementation of the nodulation defect of a nodW mutant. We report here that the NwsB protein, unlike the overproduced NodW protein, requires NodV or NwsA for its function. This shows that cross-talk occurs between NwsAB and NodVW, in that NodV appears to activate NwsB.
Enzymatic Properties and Substrate Specificity of the Trehalose Phosphorylase from Caldanaerobacter subterraneus (2011)

A putative glycoside phosphorylase from Caldanaerobacter subterraneus subsp. pacificus was recombinantly expressed in Escherichia coli, after codon optimization and chemical synthesis of the encoding gene. The enzyme was purified by His tag chromatography and was found to be specifically active toward trehalose, with an optimal temperature of 80°C. In addition, no loss of activity could be detected after 1 h of incubation at 65°C, which means that it is the most stable trehalose phosphorylase reported so far. The substrate specificity was investigated in detail by measuring the relative activity on a range of alternative acceptors, applied in the reverse synthetic reaction, and determining the kinetic parameters for the best acceptors. These results were rationalized based on the enzyme-substrate interactions observed in a homology model with a docked ligand. The specificity for the orientation of the acceptor's hydroxyl groups was found to decrease in the following order: C-3 > C-2 > C-4. This results in a particularly high activity on the monosaccharides d-fucose, d-xylose, l-arabinose, and d-galactose, as well as on l-fucose. However, determination of the kinetic parameters revealed that these acceptors bind less tightly in the active site than the natural acceptor d-glucose, resulting in drastically increased K(m) values. Nevertheless, the enzyme's high thermostability and broad acceptor specificity make it a valuable candidate for industrial disaccharide synthesis.
Acute demyelinating optic neuritis (2002)

Acute demyelinating optic neuritis associated with multiple sclerosis (MS) is the most common cause of inflammation of the optic nerve. The Optic Neuritis Treatment Trial (ONTT) has provided important clinical data on the use of corticosteroids, and demonstrated that patients with characteristic inflammatory lesions within the brain on magnetic resonance imaging had a greater chance of developing clinically definite MS (CDMS). The current approach to patients with optic neuritis has been modified by the results of the Controlled High-Risk Subjects Avonex Multiple Sclerosis Prevention Study (CHAMPS). Patients with an initial clinical episode of demyelination (optic neuritis, incomplete transverse myelitis, or brain-stem/cerebellar syndrome) and at least two characteristic demyelinating lesions within the brain were randomized to receive interferon beta-1a or placebo after initial treatment with intravenous corticosteroids. At the 3-year point patients treated with interferon beta-1a showed a 50% less risk of CDMS. The results of this study have set the standard for patients with a first bout of demyelinating optic neuritis.
A subsurface flexible plastic enclosure for the in situ study of short term microbiological and chemical dynamics1 (1984)

A simple nonmetallic device is described which allows the gentle enclosure of a few hundred liters of water from discrete depths in flexible plastic bags for in situ time‐series studies. The disposable bags close without rigid moving parts, remain in situ, and are pump‐sampled from the surface. The system can be deployed at sea and used for radiotracer experiments.
Mu transpososome activity-profiling yields hyperactive MuA variants for highly efficient genetic and genome engineering (2017)

The phage Mu DNA transposition system provides a versatile species non-specific tool for molecular biology, genetic engineering and genome modification applications. Mu transposition is catalyzed by MuA transposase, with DNA cleavage and integration reactions ultimately attaching the transposon DNA to target DNA. To improve the activity of the Mu DNA transposition machinery, we mutagenized MuA protein and screened for hyperactivity-causing substitutions using an in vivo assay. The individual activity-enhancing substitutions were mapped onto the MuA-DNA complex structure, containing a tetramer of MuA transposase, two Mu end segments and a target DNA. This analysis, combined with the varying effect of the mutations in different assays, implied that the mutations exert their effects in several ways, including optimizing protein-protein and protein-DNA contacts. Based on these insights, we engineered highly hyperactive versions of MuA, by combining several synergistically acting substitutions located in different subdomains of the protein. Purified hyperactive MuA variants are now ready for use as second-generation tools in a variety of Mu-based DNA transposition applications. These variants will also widen the scope of Mu-based gene transfer technologies toward medical applications such as human gene therapy. Moreover, the work provides a platform for further design of custom transposases.
A Statistical Deterministic Approach to Hurricane Risk Assessment (2006)

Hurricanes are lethal and costly phenomena, and it is therefore of great importance to assess the long-term risk they pose to society. Among the greatest threats are those associated with high winds and related phenomena, such as storm surges. Here we assess the probability that hurricane winds will affect any given point in space by combining an estimate of the probability that a hurricane will pass within some given radius of the point in question with an estimate of the spatial probability density of storm winds. To assess the probability that storms will pass close enough to a point of interest to affect it, we apply two largely independent techniques for generating large numbers of synthetic hurricane tracks. The first treats each track as a Markov chain, using statistics derived from observed hurricane-track data. The second technique begins by generating a large class of synthetic, time-varying wind fields at 850 and 250 hPa whose variance, covariance, and monthly means match NCEP–NCAR reanalysis data and whose kinetic energy follows an ω−3 geostrophic turbulence spectral frequency distribution. Hurricanes are assumed to move with a weighted mean of the 850- and 250-hPa flow plus a “beta drift” correction, after originating at points determined from historical genesis data. The statistical characteristics of tracks generated by these two means are compared. For a given point in space, many (~104) synthetic tracks are generated that pass within a specified distance of a point of interest, using both track generation methods. For each of these tracks, a deterministic, coupled, numerical simulation of the storm's intensity is carried out, using monthly mean upper-ocean and potential intensity climatologies, together with time-varying vertical wind shear generated from the synthetic time series of 850- and 250-hPa winds, as described above. For the case in which the tracks are generated using the synthetic environmental flow, the tracks and the shear are generated using the same wind fields and are therefore mutually consistent. The track and intensity data are finally used together with a vortex structure model to construct probability distributions of wind speed at fixed points in space. These are compared to similar estimates based directly on historical hurricane data for two coastal cities.