gebhart/patrepeval huggingface dataset:
Synthetic chemotherapeutic agents. I. Synthesis of 2-substituted thiazolo(5,4-f)quinoline derivatives.(1). (1976)

By using 6-aminobenzothiazoles as starting meterial, a series of 2-substituted 6-ethyl-6, 9-dihydro-9-oxothiazolo [5, 4-f] quinoline-8-carboxylic acids has been prepared through successive steps of, e.g. condensation with diethyl ethoxymethylenemalonate, Gould-Jacobs reaction, N-alkylation and hydrolysis. These compounds were evaluated for antibacterial activities in vitro. The 2-chloro derivative (10d) showed nearly the same activity with nalidixic acid.
ON THE ROLE OF MOISTURE IN DEGRADATION OF CONCRETE STRUCTURES (2005)

Moisture is decisive for a large number of reaction, binding and transport processes in concrete affecting the durability, shrinkage and performance in various environments. Consequently, the role of moisture must be assessed and quantified in a diagnosis of concrete degradation by moisture measurements and a survey of environmental actions. The paper gives an over-view of the role of moisture in various degradation processes and some recommendations on the assessment of moisture in diagnosis of degradation.
Disruption of SF3B1 results in deregulated expression and splicing of key genes and pathways in myelodysplastic syndrome hematopoietic stem and progenitor cells (2014)

The splicing factor SF3B1 is the most commonly mutated gene in the myelodysplastic syndrome (MDS), particularly in patients with refractory anemia with ring sideroblasts (RARS). We investigated the functional effects of SF3B1 disruption in myeloid cell lines: SF3B1 knockdown resulted in growth inhibition, cell cycle arrest and impaired erythroid differentiation and deregulation of many genes and pathways, including cell cycle regulation and RNA processing. MDS is a disorder of the hematopoietic stem cell and we thus studied the transcriptome of CD34(+) cells from MDS patients with SF3B1 mutations using RNA sequencing. Genes significantly differentially expressed at the transcript and/or exon level in SF3B1 mutant compared with wild-type cases include genes that are involved in MDS pathogenesis (ASXL1 and CBL), iron homeostasis and mitochondrial metabolism (ALAS2, ABCB7 and SLC25A37) and RNA splicing/processing (PRPF8 and HNRNPD). Many genes regulated by a DNA damage-induced BRCA1-BCLAF1-SF3B1 protein complex showed differential expression/splicing in SF3B1 mutant cases. This is the first study to determine the target genes of SF3B1 mutation in MDS CD34(+) cells. Our data indicate that SF3B1 has a critical role in MDS by affecting the expression and splicing of genes involved in specific cellular processes/pathways, many of which are relevant to the known RARS pathophysiology, suggesting a causal link.
Family-Based Samples Can Play an Important Role in Genetic Association Studies (2008)

Over the past 2 decades, DNA samples from thousands of families have been collected and genotyped for linkage studies of common complex diseases, such as type 2 diabetes, asthma, and prostate cancer. Unfortunately, little success has been achieved in identifying genetic susceptibility risk factors through these considerable efforts. However, significant success in identifying common disease risk-associated variants has been recently achieved from genome-wide association studies using unrelated case-control samples. These genome-wide association studies are typically done using population-based cases and controls that are ascertained irrespective of their family history for the disease of interest. Few genetic association studies have taken full advantage of the considerable resources that are available from the linkage-based family collections despite evidence showing cases that have a positive family history of disease are more likely to carry common genetic variants associated with disease susceptibility. Herein, we argue that population stratification is still a concern in case-control genetic association studies, despite the development of analytic methods designed to account for this source of confounding, for a subset of single nucleotide polymorphisms in the genome, most notably those single nucleotide polymorphisms in regions involved with natural selection. We note that current analytic approaches designed to address the issue of population stratification in case-control studies cannot definitively distinguish between true and false associations, and we argue that family-based samples can still serve an invaluable role in following up findings from case-control studies.
5-Fluorouracil and Recombinant Alpha Interferon-2a in the Treatment of Advanced Colorectal Carcinoma: a Dose Optimization Study (1990)

A dose optimization study was carried out with the aim of identifying the maximally tolerated dose of recombinant alpha interferon-2a (raIFN-2a) in combination with 5-fluorouracil (5FU). 5FU was given at the dose of 750 mg/m2 over a 4-hour infusion on day 1- - greater than 5 followed by 750 mg/m2 weekly i.v. bolus. Recombinant aIFN-2a was started at 3 x 10(6) IU subcutaneously three times/week. 12 patients with advanced colorectal carcinoma were included in the study. 10 patients had previously received chemotherapy for advanced disease. Severe fatigue, most likely attributable to rIFN, was the dose-limiting toxicity. The dosage of raIFN-2a could not be further escalated above 12 x 10(6) IU. At this dose level all patients required dose reduction due to fatigue, fever, myalgia and severe reduction of performance status.
Study of istradefylline in patients with Parkinson's disease on levodopa with motor fluctuations (2008)

The objective of this study was to evaluate the efficacy, safety, and tolerability of istradefylline 20 mg once daily versus placebo as an adjunct to levodopa in subjects with Parkinson's disease (PD) who have motor fluctuations. Istradefylline (KW-6002) is an adenosine A(2A) receptor antagonist that in primate models of PD improves motor function without causing or worsening dyskinesia. This 12-week, multicenter, double-blind, placebo-controlled, randomized, Phase 3 study of istradefylline was conducted in subjects experiencing an average daily OFF time of at least 3 hours (116 randomized to istradefylline; 115 to placebo). All were on stable levodopa regimens; 90% were also on stable regimens of other anti-Parkinson's medications. Istradefylline-treated subjects had significant placebo-corrected reductions in daily OFF time from baseline to endpoint: 4.6% (P = 0.03) and 0.7 hours (P = 0.03). For ON time with troublesome dyskinesia, the changes between istradefylline and placebo were not significant. Istradefylline was well tolerated, with 6 (5.2%) istradefylline-treated and 7 (6.1%) placebo-treated subjects withdrawing from the study because of adverse events. Dyskinesia, lightheadedness, tremor, constipation, and weight decrease were reported more often with istradefylline than placebo. We conclude that istradefylline is well tolerated and significantly reduces OFF time as an adjunct to levodopa in PD subjects with motor fluctuations.
Photoinduced charge transfer in composites of conjugated polymers and semiconductor nanocrystals (2003)

Photoinduced electron transfer in composites of CdSe and InP nanocrystals (NC) with a conjugated polymer [2-methoxy-5-(3-,7-dimethyl-octyloxy)-1, 4-phenylene vinylene] (OC1C10-PPV) is studied by means of light-induced electron spin resonance (LESR), photoluminescence (PL) as well as quasi steady-state photoinduced absorption (PIA) spectroscopy. The quenching of PL, the occurrence of two new optical absorption bands, and the formation of light-induced paramagnetic species on the polymer chain are altogether interpreted as an electron transfer between a donor polymer and acceptor NC in the excited state. In particular the LESR provides evidence of an electron transfer rather than energy transfer due to an overlap of absorption and emission bands of NC and the conjugated polymer. The g-factor of the signal is consistent with the cationic origin of OC1C10-PPV radicals. Additionally, the LESR signal is sensitive to NC surface coating being smaller in blends with the tri-n-octylphosphine oxide-tri-n-octylphosphine (TOPO-TOP) coated CdSe surface and completely absent in blends with TOPO-TOP-InP. LESR probes predominantly positive polarons on the conjugated polymer chain generated at room temperature in the course of an electron transfer to NC. This is very different from the situation in blends of OC1C10-PPV with fullerenes, another promising photovoltaic acceptor, where the photogenerated cation and anion were both observed in the LESR. In PIA we found contributions of both polymer polarons and electrons on the NC. The recombination kinetics shows a broad distribution of lifetimes, which is characteristic for dispersive (diffusive) recombination processes with fractional power frequency dependence.
Shortcomings of short hairpin RNA-based transgenic RNA interference in mouse oocytes (2010)

We conclude that, the long RNA hairpin-based RNAi is more reliable and cost-effective and we recommend it as a method-of-choice when a gene is studied selectively in the oocyte.
Tumor Suppressor and Aging Biomarker p16INK4a Induces Cellular Senescence without the Associated Inflammatory Secretory Phenotype (2011)

Cellular senescence suppresses cancer by preventing the proliferation of cells that experience potentially oncogenic stimuli. Senescent cells often express p16(INK4a), a cyclin-dependent kinase inhibitor, tumor suppressor, and biomarker of aging, which renders the senescence growth arrest irreversible. Senescent cells also acquire a complex phenotype that includes the secretion of many cytokines, growth factors, and proteases, termed a senescence-associated secretory phenotype (SASP). The SASP is proposed to underlie age-related pathologies, including, ironically, late life cancer. Here, we show that ectopic expression of p16(INK4a) and another cyclin-dependent kinase inhibitor, p21(CIP1/WAF1), induces senescence without a SASP, even though they induced other features of senescence, including a stable growth arrest. Additionally, human fibroblasts induced to senesce by ionizing radiation or oncogenic RAS developed a SASP regardless of whether they expressed p16(INK4a). Cells induced to senesce by ectopic p16(INK4a) expression lacked paracrine activity on epithelial cells, consistent with the absence of a functional SASP. Nonetheless, expression of p16(INK4a) by cells undergoing replicative senescence limited the accumulation of DNA damage and premature cytokine secretion, suggesting an indirect role for p16(INK4a) in suppressing the SASP. These findings suggest that p16(INK4a)-positive cells may not always harbor a SASP in vivo and, furthermore, that the SASP is not a consequence of p16(INK4a) activation or senescence per se, but rather is a damage response that is separable from the growth arrest.
A New Vector Waveform Inversion Algorithm for Simultaneous Updating of Conductivity and Permittivity Parameters From Combination Crosshole/Borehole-to-Surface GPR Data (2010)

We have developed a new full-waveform groundpenetrating radar (GPR) multicomponent inversion scheme for imaging the shallow subsurface using arbitrary recording configurations. It yields significantly higher resolution images than conventional tomographic techniques based on first-arrival times and pulse amplitudes. The inversion is formulated as a nonlinear least squares problem in which the misfit between observed and modeled data is minimized. The full-waveform modeling is implemented by means of a finite-difference time-domain solution of Maxwell's equations. We derive here an iterative gradient method in which the steepest descent direction, used to update iteratively the permittivity and conductivity distributions in an optimal way, is found by cross-correlating the forward vector wavefield and the backward-propagated vectorial residual wavefield. The formulation of the solution is given in a very general, albeit compact and elegant, fashion. Each iteration step of our inversion scheme requires several calculations of propagating wavefields. Novel features of the scheme compared to previous full-waveform GPR inversions are as follows: 1) The permittivity and conductivity distributions are updated simultaneously (rather than consecutively) at each iterative step using improved gradient and step length formulations; 2) the scheme is able to exploit the full vector wavefield; and 3) various data sets/survey types (e.g., crosshole and borehole-to-surface) can be individually or jointly inverted. Several synthetic examples involving both homogeneous and layered stochastic background models with embedded anomalous inclusions demonstrate the superiority of the new scheme over previous approaches.
Detection of bacteria by hybridization of rRNA with DNA-latex and immunodetection of hybrids (1988)

A novel nucleic acid hybridization assay with a DNA probe immobilized on 1.25-micron-diameter latex particles was developed. Hybridization of the immobilized probe DNA with sample rRNA was complete in 10 to 15 min. Alkaline phosphatase-labeled anti-DNA-RNA was allowed to bind to the DNA-RNA hybrids on the latex particles. Then the latex was collected on a small glass fiber filter pad, and bound alkaline phosphatase was quantitated by reflectance rate measurement. The method detected a broad range of bacterial species and had a detection limit of 500 cells per assay. The assay was used to screen urine samples for bacteriuria and had a sensitivity of 96.2% compared with conventional culture at a decision level of greater than or equal to 10(4) CFU/ml. The hybridization method could have broad application to the detection of bacteria and viruses.
Comparison of the Biochemical and Kinetic Properties of the Type 1 Receptor Tyrosine Kinase Intracellular Domains (2002)

Epidermal growth factor receptor (EGFR), ErbB-2, and ErbB-4 are members of the type 1 receptor tyrosine kinase family. Overexpression of these receptors, especially ErbB-2 and EGFR, has been implicated in multiple forms of cancer. Inhibitors of EGFR tyrosine kinase activity are being evaluated clinically for cancer therapy. The potency and selectivity of these inhibitors may affect the efficacy and toxicity of therapy. Here we describe the expression, purification, and biochemical comparison of EGFR, ErbB-2, and ErbB-4 intracellular domains. Despite their high degree of sequence homology, the three enzymes have significantly different catalytic properties and substrate kinetics. For example, the catalytic activity of ErbB-2 is less stable than that of EGFR. ErbB-2 uses ATP-Mg as a substrate inefficiently compared with EGFR and ErbB-4. The three enzymes have very similar substrate preferences for three optimized peptide substrates, but differences in substrate synergies were observed. We have used the biochemical and kinetic parameters determined from these studies to develop an assay system that accurately measures inhibitor potency and selectivity between the type 1 receptor family. We report that the selectivity profile of molecules in the 4-anilinoquinazoline series can be modified through specific aniline substitutions. Moreover, these compounds have activity in whole cells that reflect the potency and selectivity of target inhibition determined with this assay system.
Evaluation and Validation of a Real-Time Polymerase Chain Reaction Assay for Rapid Identification ofBacillus anthracis (2002)

To the Editor: During the 2001 anthrax outbreak, we evaluated and validated a highly sensitive and specific three-target (two plasmid and one chromosomally located target) 5´ nuclease assay (real-time polymerase chain reaction [PCR]) for detection and identification of Bacillus anthracis. This PCR assay was successfully used to rapidly test hundreds of suspect isolates as well as screen environmental samples for the presence of B. anthracis throughout the 2001 anthrax outbreak. For the first time in an outbreak setting, a PCR assay was used to detect B. anthracis directly from clinical specimens, consequently becoming a part of the laboratory confirmation of anthrax. In this letter, we describe the evaluation of this assay on a diverse panel of bacterial isolates including isolates obtained throughout the outbreak. A supplement, which includes data on the use of this assay on environmental and clinical specimens, is online (available from http://www.cdc.gov/ncidod/EID/vol8no10/02-0393sup.htm).
Equilibria in Furfural-Water Systems under Increased Pressure and the Influence of Added Salts upon the Mutual Solubilities of Furfuraland Water (1948)

Liquid-vapour equilibrium data are reported for the furfural-water system at pressures of 6.17, 7.85, and 9.83 kg. per cm2. Under these pressures the system forms a homoazeotropic mixture differing only slightly in composition from the heteroazeotropic mixture formed at normal pressures. The data are checked by the calculation of activity coefficients. Abnormal activity coefficients are found for water in mixtures of high furfural content. The equation log10 P= -2209/T + 7.959 fits published data and that now reported for t'he vapour pressure of furfural over the range of pressures 100 to 6,000 mm. Hg. Changes in the mutual solubilities of furfural and water caused by the addition of metallic sulphates are determined. All the sulphates examined raised the critical solution temperat'ure, sodium sulphate being most effective. With magnesium sulphate there was a region of discontinuity, which may possibly be attributed to a change of phase or of hydration of magnesium sulphate. The velocities of reaction (decomposition or polymerization) of furfural in aqueous and in aqueous acidic medium at 180°C. are reported. The data are used to estimate the amount of furfural lost by such reactions in a commercial process for the production of furfural. It is considered that the use of metallic sulphat'es in the commercial prociuotion of furfural should not influence the yield appreciably.
Top-Gated Epitaxial Graphene FETs on Si-Face SiC Wafers With a Peak Transconductance of 600 mS/mm (2010)

In this letter, we present state-of-the-art performance of top-gated graphene n-FETs and p-FETs fabricated with epitaxial graphene layers grown on Si-face 6H-SiC substrates on 50-mm wafers. The current-voltage characteristics of these devices show excellent saturation with on-state current densities (I <sub xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">on</sub> ) of 0.59 A/mm at V <sub xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">ds</sub> = 1 V and 1.65 A/mm at V <sub xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">ds</sub> = 3 V. I <sub xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">on</sub> /I <sub xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">off</sub> ratios of 12 and 19 were measured at V <sub xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">ds</sub> = 1 and 0.5 V, respectively. A peak extrinsic g <sub xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">m</sub> as high as 600 mS/mm was measured at V <sub xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">ds</sub> = 3.05 V, with a gate length of 2.94 ¿m. The field-effect mobility versus effective electric field (E <sub xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">eff</sub> ) was measured for the first time in epitaxial graphene FETs, where record field-effect mobilities of 6000 cm <sup xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">2</sup> /V·s for electrons and 3200 cm <sup xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">2</sup> /V·s for holes were obtained at E <sub xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">eff</sub> ~ 0.27 MV/cm .
Superconducting qubit in a waveguide cavity with a coherence time approaching 0.1 ms (2012)

We report a superconducting artificial atom with a coherence time of ${T}_{2}^{*}=92$ $\ensuremath{\mu}$s and energy relaxation time ${T}_{1}=70$ $\ensuremath{\mu}$s. The system consists of a single Josephson junction transmon qubit on a sapphire substrate embedded in an otherwise empty copper waveguide cavity whose lowest eigenmode is dispersively coupled to the qubit transition. We attribute the factor of four increase in the coherence quality factor relative to previous reports to device modifications aimed at reducing qubit dephasing from residual cavity photons. This simple device holds promise as a robust and easily produced artificial quantum system whose intrinsic coherence properties are sufficient to allow tests of quantum error correction.
Electrostatic Layer-by-Layer Assembled Carbon Nanotube Multilayer Film and Its Electrocatalytic Activity for O2 Reduction (2004)

Multilayer films of shortened multiwalled carbon nanotubes (MWNTs) are homogeneously and stably assembled on glassy carbon electrodes with the layer-by-layer (LBL) method, based on electrostatic interaction of positively charged poly(diallyldimethylammonium chloride) and negatively charged and shortened MWNTs. The film assembly and electrochemical property as well as the electrocatalytic activity toward O2 reduction of the MWNT multilayer film are studied. Scanning electron microscopy, the quartz crystal microbalance technique, ultraviolet-visible-near-infrared spectroscopy, and cyclic voltammetry are used for characterization of film assembly. Experimental results revealed that film growth is uniform, almost with the same coverage of the MWNTs in each layer, and that the assembled MWNTs are mainly in the form of small bundles or single tubes on the electrodes. Electrochemical studies indicate that the LBL assembled MWNT films possess a remarkable electrocatalytic activity toward O2 reduction in alkaline media. This property, combined with the well-dispersed, porous and conductive features of the MWNT film illustrated with the LBL method, suggests the potential application of the MWNT film for constructing an efficient alkaline air electrode for energy conversions.
Single-Molecule Circuits with Well-Defined Molecular Conductance (2006)

We measure the conductance of amine-terminated molecules by breaking Au point contacts in a molecular solution at room temperature. We find that the variability of the observed conductance for the diamine molecule-Au junctions is much less than the variability for diisonitrile- and dithiol-Au junctions. This narrow distribution enables unambiguous conductance measurements of single molecules. For an alkane diamine series with 2-8 carbon atoms in the hydrocarbon chain, our results show a systematic trend in the conductance from which we extract a tunneling decay constant of 0.91 +/- 0.03 per methylene group. We hypothesize that the diamine link binds preferentially to undercoordinated Au atoms in the junction. This is supported by density functional theory-based calculations that show the amine binding to a gold adatom with sufficient angular flexibility for easy junction formation but well-defined electronic coupling of the N lone pair to the Au. Therefore, the amine linkage leads to well-defined conductance measurements of a single molecule junction in a statistical study.