gebhart/patrepeval huggingface dataset:
Data from First-in-Human Phase I Trial of Two Schedules of OSI-930, a Novel Multikinase Inhibitor, Incorporating Translational Proof-of-Mechanism Studies (2023)

&lt;div&gt;Abstract&lt;p&gt;&lt;b&gt;Purpose:&lt;/b&gt; OSI-930 is a novel, potent, oral small-molecule receptor tyrosine kinase inhibitor, predominantly against VEGF receptors (VEGFR), c-Kit, and platelet-derived growth factor receptors. A phase I trial was undertaken to determine safety, maximum-tolerated dose (MTD), pharmacokinetics, pharmacodynamics, and antitumor activity of OSI-930 in patients with advanced solid tumors.&lt;/p&gt;&lt;p&gt;&lt;b&gt;Experimental Design:&lt;/b&gt; OSI-930 was administered once or twice a day using a modified accelerated titration design. Pharmacokinetics and plasma soluble VEGFR2 (sVEGFR2) studies were undertaken. Dynamic contrast-enhanced MRI (DCE-MRI) and 2[18F]fluoro-2-deoxy-d-glucose-positron emission tomography (FDG-PET) MTD expansion cohorts were conducted.&lt;/p&gt;&lt;p&gt;&lt;b&gt;Results:&lt;/b&gt; Fifty-eight patients received OSI-930 in 2 schedules; once a day schedule: 12 patients at doses up to 1,600 mg without reaching MTD; twice a day schedule: 46 patients at 400 mg (&lt;i&gt;n&lt;/i&gt; = 7), 500 mg (&lt;i&gt;n&lt;/i&gt; = 31), and 600 mg (&lt;i&gt;n&lt;/i&gt; = 8). Dose-limiting toxicities were observed at 600 mg twice a day (&lt;i&gt;n&lt;/i&gt; = 3): G3 rash (&lt;i&gt;n&lt;/i&gt; = 2) and G4 γ-glutamyltransferase, establishing the MTD at 500 mg twice a day. Common G1–2 toxicities included fatigue, diarrhea, nausea, and rash. Antitumor responses were seen in 2 patients with advanced ovarian cancer [Response Evaluation Criteria in Solid Tumors (RECIST) partial response (PR) (&lt;i&gt;n&lt;/i&gt; = 1); GCIG CA125 response (&lt;i&gt;n&lt;/i&gt; = 1)]. Eleven of 19 heavily pretreated imatinib-resistant patients with gastrointestinal stromal tumors achieved RECIST stable disease (median duration: 126 days), with FDG-PET scans showing PRs in 4 of 9 patients. OSI-930 exposure increased with dose; substantial decreases in sVEGFR levels were observed with OSI-930 twice a day doses ≥400 mg, while DCE-MRI responses were shown in 4 of 6 patients.&lt;/p&gt;&lt;p&gt;&lt;b&gt;Conclusions:&lt;/b&gt; OSI-930 is safe and well tolerated, with pharmacokinetic–pharmacodynamic data supporting proof-of-mechanism with clinically relevant antitumor activity. &lt;i&gt;Clin Cancer Res; 19(4); 909–19. ©2012 AACR&lt;/i&gt;.&lt;/p&gt;&lt;/div&gt;
Effects of Porphyromonas gingivalis and Escherichia coli lipopolysaccharides on mononuclear phagocytes (1997)

The mononuclear phagocyte plays an important role in the regulation of microbe-induced inflammation, in part through its ability to secrete mediators, particularly cytokines, in response to microorganisms and their products. To evaluate the effects of the microbial flora associated with chronic adult periodontitis on cytokine induction, lipopolysaccharide (LPS) from the periodontopathogen Porphyromonas gingivalis was used to stimulate naive and phorbol ester-primed U937 monocytic cells, as well as elutriated human peripheral blood monocytes. We assessed the effect of this LPS, in comparison to that of LPS from Escherichia coli, on cell proliferation, cytokine induction, and surface expression of the LPS receptor CD14. P. gingivalis LPS stimulated proliferation of U937 cells at concentrations of greater than 1 ng/ml, while E. coli LPS inhibited proliferation. Phorbol myristic acid (PMA)-treated U937 cells and elutriated monocytes responded to E. coli LPS activation by producing tumor necrosis factor alpha (TNF-alpha) mRNA and protein; however, P. gingivalis LPS induced greater numbers of TNF-alpha mRNA-positive cells and higher (P < 0.05) levels of protein than did E. coli LPS. Both cell types expressed interleukin-1 beta (IL-1beta) mRNA and protein in response to either LPS treatment. Compared with E. coli LPS, P. gingivalis LPS induced significantly (P < 0.05) higher numbers of IL-1 mRNA-positive U937 cells and elutriated monocytes, as well as production of significantly more (P < 0.05) IL-1 protein by the monocytes. The PMA-treated U937 cells and the monocytes produced high levels of IL-1 receptor antagonist mRNA and protein which were only marginally affected by the LPS preparations. While E. coli LPS induced expression of CD 14 on the surface of PMA-primed U937 cells and monocytes, P. gingivalis LPS exhibited a significantly (P < 0.05) greater ability to enhance receptor levels. Our results indicate that P. gingivalis LPS can activate the mononuclear phagocyte for proliferation, cytokine production, and CD14 expression, providing evidence for the potential of this bacterial component to act as a critical regulatory factor in the chronic inflammatory response associated with periodontitis.
Role of microRNAs in vascular diseases, inflammation, and angiogenesis (2008)

The integrity of the endothelial monolayer is fundamental for the homoeostasis of the vascular system. Functional endothelial cells are also required for the growth of new blood vessels during neovascularization. Although multiple growth factors have been shown to regulate angiogenesis and vascular development, little is known about the complex upstream regulation of gene expression and translation. MicroRNAs (miRNAs) are an emerging class of highly conserved, non-coding small RNAs that regulate gene expression on the post-transcriptional level by inhibiting the translation of protein from mRNA or by promoting the degradation of mRNA. More than 500 human miRNAs have been identified so far, and increasing evidence indicates that miRNAs have distinct expression profiles and play crucial roles in various physiological and pathological processes such as cardiogenesis, haematopoietic lineage differentiation, and oncogenesis. Meanwhile, a few specific miRNAs that regulate endothelial cell functions and angiogenesis have been described. Let7-f, miR-27b, and mir-130a were identified as pro-angiogenic miRNAs. In contrast, miR-221 and miR-222 inhibit endothelial cell migration, proliferation, and angiogenesis in vitro by targeting the stem cell factor receptor c-kit and indirectly regulating endothelial nitric oxide synthase expression. Moreover, some miRNAs are involved in tumour angiogenesis such as the miR-17-92 cluster and miR-378. Early studies also indicate the contribution of specific miRNAs (e.g. miR-155, miR-21, and miR-126) to vascular inflammation and diseases. Thus, the identification of miRNAs and their respective targets may offer new therapeutic strategies to treat vascular diseases such as atherosclerosis, to improve neovascularization after ischaemia, or to prevent tumour progression.
FTC cracks down on spyware and PC hijacking, but not true lies (2005)

The US Federal Trade Commission (FTC) recently sued an Internet marketing organization to make it stop infecting consumers' PCs with spyware. According to the FTC, Seismic Entertainment Productions developed a scheme that seized control of PCs nationwide, infected them with spyware and other malicious software, bombarded them with a barrage of pop-up advertising for Seismic's clients, exposed the PCs to security risks, and caused them to malfunction, slow down, and, at times, crash. Seismic then offered to sell the victims an "antispyware" program to fix the computers, and stop the pop-ups and other problems that Seismic had caused.
Synthesis of new cyano‐substituted analogues of Tröger's bases from bromo‐derivatives. A stereochemical dependence of long‐range (nJHH, n = 4, 5, and 6) proton–proton and proton–carbon (nJCH, n = 1, 2, 3, 4, and 5) coupling constants of these compounds (2019)

A free-catalyst microwave-assisted cyanation of brominated Tröger's base derivatives (2a-f) is reported. The procedure is simple, efficient, and clean affording the nitrile compounds (3a-e, I) in very good yields. Complete assignment of <sup>1</sup> H and <sup>13</sup> C chemical shifts of 2a-f, I and 3a-d, I was achieved using gradient selected 1D nuclear magnetic resonance (NMR) techniques (1D zTOCSY, PSYCHE, DPFGSE NOE, and DEPT), homonuclear 2D NMR techniques (gCOSY and zTOCSY), and heteronuclear 2D NMR techniques (gHSQCAD/or pure-shift gHSQCAD, gHMBCAD, bsHSQCNOESY, and gHSQCAD-TOCSY) with adiabatic pulses. Determination of the long-range proton-proton coupling constants <sup>n</sup> J<sub>HH</sub> (n = 4, 5, 6) was accomplished by simultaneous irradiation of two protons at appropriate power levels. In turn, determined coupling constants were tested by an iterative simulation program by calculating the <sup>1</sup> H NMR spectrum and comparing it to the experimental spectrum. The excitation-sculptured indirect-detection experiment (EXSIDE) and <sup>1</sup> H-<sup>15</sup> N CIGARAD-HMBC (constant time inverse-detection gradient accordion rescaled heteronuclear multiple bond correlation) were applied for determination of long-range carbon-proton coupling constants <sup>n</sup> J<sub>CH</sub> (n = 2, 3, and 4) and for assignment of <sup>15</sup> N chemical shift at natural abundance, respectively. DFT/B3LYP optimization studies were performed in order to determine the geometry of 2c using 6-31G(d,p), 6-311G(d,p), and 6-311 + G(d,p) basis sets. For calculation of <sup>1</sup> H and <sup>13</sup> C chemical shifts, <sup>n</sup> J<sub>HH</sub> (n = 2, 3, 4, 5, and 6), and <sup>n</sup> J<sub>CH</sub> (n = 1, 2, 3, and 4) coupling constants, the GIAO method was employed at the B3LYP/6-31G(d,p), B3LYP/6-31+G(d,p), B3LYP/6-311+G(d,p), B3LYP/6-311++G(2d,2p), B3LYP/cc-pVTZ), and B3LYP/aug-cc-pVTZ) levels of theory. For the first time, a stereochemical dependence magnitude of the long-range <sup>n</sup> J<sub>HH</sub> (n = 4, 5, and 6) and <sup>n</sup> J<sub>CH</sub> (n = 1, 2, 3, 4, and 5) have been found in bromo-substituted analogues of Tröger's bases.
Human Motion Recognition With Limited Radar Micro-Doppler Signatures (2020)

The performance of deep learning (DL) algorithms for radar-based human motion recognition (HMR) is hindered by the diversity and volume of the available training data. In this article, to tackle the issue of insufficient training data for HMR, we propose an instance-based transfer learning (ITL) method with limited radar micro-Doppler (MD) signatures, alleviating the burden of collecting and annotating a large number of radar samples. ITL is a unique algorithm that consists of three interconnected parts, including DL model pretraining, correlated source data selection, and adaptive collaborative fine-tuning (FT). Any of the three components cannot be excluded; otherwise, the performance of the entire algorithm decreases. The experiments with a radar data set of six human motions show that ITL achieves state-of-the-art performance for HMR with limited training samples, outperforming several existing transfer learning approaches. Especially, when there are only 100 samples per person per class, ITL yields an F1 score of 96.7%. Last but not least, ITL is more generalized to human motion differences. Though adapted to recognize the persons’ motions in a small-scale target data set, ITL can also classify the persons’ motion data used for pretraining, achieving up to 11.0% F1 score enhancement over the conventional FT method.
Alcohol Extract of Neem (Azadirachta indica L.) Seed as Nitrification Inhibitor (1975)

After removal of the ethanol solvent, the extractive, which is rich in lipid associates, was incubated in soil with 200ppm NH4-N at rates of 5 to 30% of the NH4-N. NH4-N was supplied by ammonium sulphate and urea. Inhibition of nitrification depended on the amount of the seed extract applied and on time of incubation; application at 30% of the NH4-N was effective up to 75 days.
Plane‐wave attenuation anisotropy in orthorhombic media (2005)

We develop an analytic framework for describing the attenuation coefficients in orthorhombic media with orthorhombic attenuation. To take full advantage of the analogy between the Christoffel equations in the symmetry planes of orthorhombic and TI (transversely isotropic) media, we introduce a set of attenuation‐anisotropy parameters similar to the TI attenuation parameters , , and . This notation, based on the same principle as Tsvankin's velocity‐anisotropy parameters for orthorhombic media, leads to simple linearized equations for the symmetry‐plane attenuation coeficients of all three modes (, and ). The attenuation‐anisotropy parameters also allow us to simplify the P‐wave attenuation coeficient outside the symmetry planes under the assumption of weak attenuation and weak velocity and attenuation anisotropy. The approximate has the same form as the linearized phase‐velocity function, with Tsvankin's velocity parameters and replaced by the attenuation parameters and The simple expression for the coeficient and the reduction in the number of parameters responsible for P‐wave attenuation provide a basis for inverting attenuation measurements from orthorhombic media. The attenuation processing has to be preceded by anisotropic velocity analysis that can be performed (in the absence of pronounced velocity dispersion) using existing algorithms for nonattenuative media.
NIR‐FT Raman, FT‐IR and surface‐enhanced Raman scattering spectra, with theoretical simulations on chloramphenicol (2008)

Abstract Chloramphenicol (CLM), originally derived from the bacterium Streptomyces venezuelae , is an inhibitor of bacterial ribosomal peptidyl transferase activity. The near infrared Fourier transform (NIR‐FT) Raman, surface‐enhanced Raman spectroscopy (SERS) and Fourier transform infrared (FT‐IR) spectral analyses of CLM, a potential antibacterial drug for the treatment of typhoid fever, were carried out along with density functional computations. The vibrational spectral analysis reveals that the CH 2 asymmetric and symmetric stretching modes are shifted to higher wavenumbers than the computed values, owing to the electronic effects resulting from induction of methylene group with the adjacent electronegative atom. The lowering of CO stretching wavenumber is due to the presence of the strong electronegative atom, nitrogen, attached to the carbonyl carbon, causing large degree of molecular π‐electron delocalization and redistribution of electrons, which weakens the CO bond. The absence of a CH stretching vibration and the observed CH out‐of‐plane bending modes suggest that the CLM molecule may be adsorbed in a flat orientation with respect to the silver surface. Copyright © 2008 John Wiley &amp; Sons, Ltd.
Looking Abroad: Two Edinburgh Journals in the Early Nineteenth Century (2009)

The nineteenth century was a time when British culture, although increasingly insular in many ways, was also increasingly aware of a wide spread of world literature. New “discoveries” included writing from Germany, Northern and Eastern Europe, medieval Spain and the countries of the East. An important part in this exploration was played by the thriving new periodical literature, which found space both for translations of foreign works and for long reviews that often contained substantial translated passages. This field has yet to be fully explored; the present article focuses on two very different Edinburgh periodicals which occupied a central position in British literary culture, the Edinburgh Review and Blackwood's Edinburgh Magazine. An analysis of the content of these journals over two five-year periods during the first half of the century brings out the different approaches of an established review and a newly founded magazine, showing among other things Blackwood's interest in a great variety of foreign writing, ancient and modern, (above all from Germany) and in the process of translation, while the Edinburgh Review tends to concentrate on recent French culture.
Modeling gradual and rate dependent closing and opening of pores in porous materials under dynamic loading (2018)

Most models for dynamic deformation of porous materials assume that under compressive loading pore closure is instantaneous. Such an approach is sometime known as the snowplough model. But pore closing, as well as pore opening, is a relatively slow mechanical process that involves fracture, plastic flow and material motion on the mesoscale. As a result, a shock loaded porous material may become overstressed relative to its quasistatic pore closing/opening curves. It is then plausible to assume that when overstressed, the material state point tends to fall back onto the quasistatic curve (in the pressure-porosity plane) at a rate that is an increasing function of the amount of overstress. In this way the pore opening and closing processes become rate dependent. Here we develop and describe such a rate dependent pore opening/closing model. The model includes: 1) an equation of state for porous materials based on Herrmann’s assumptions; 2) the quasistatic opening/closing curves; 3) rate functions for overstress relaxation; and 4) strength reduction of the porous material. We implemented our model in a hydrocode, and we show examples of some uniaxial strain (planar impact) runs.
Visualisation and resolution of encoding conflicts in asynchronous circuit design (2003)

Synthesis of asynchronous circuits from signal transition graphs (STGs) involves resolution of state encoding conflicts by means of refining the STG specification. The refinement process is generally done automatically using heuristics. It often produces suboptimal solutions or sometimes fails to solve the problem. Thus manual intervention by the designer may be required. A framework is presented for an interactive refinement process aimed to help the designer. It is based on the visualisation of conflict cores, i.e. sets of transitions causing encoding conflicts, which are represented at the level of finite and complete prefixes of STG unfoldings.
Filter-embedded wavelength-division multiplexerfor hybrid-integrated transceiver based on silica-based PLC (1996)

A thin film filter-embedded wavelength-division multiplexer is designed for a hybrid-integrated WDM transceiver based on a silica-based PLC platform. A compact multiplexer with a low insertion loss of 1.1 dB and a low crosstalk of &lt;–50 dB is successfully fabricated.
Product Analysis from Direct Liquefaction of Several High-Moisture Biomass Feedstocks (1988)

Experimental results are reported for high-pressure liquefaction of high-moisture biomass. The feedstocks included macrocystis kelp, water hyacinths, spent grain from a brewery, grain sorghum field residue and napier grass. The biomass was processed in a batch autoclave as a ten weight percent slurry in water with sodium carbonate catalyst and carbon monoxide gas. Thirty-minute experiments were performed at 350°C with operating pressures ranging from 270 to 340 atmospheres. The oil products were collected by methylene chloride and acetone extractions. Oil yields ranged from 19 to 35 mass percent on a moisture and ash-free basis. The oil products contained from 9.9 to 16.7 percent oxygen with hydrogen to carbon atomic ratios from 1.36 to 1.61. Significant nitrogen content was noted in the oil product from those feedstocks containing nitrogen (kelp, hyacinth, spent grain). Chemical composition analysis by gas chromatography/mass spectrometry demonstrated many similarities between these products and wood-derived oils. The nitrogen components were found to be mainly saturated heterocyclics.
A Fractal-Based Circularly Polarized UHF RFID Reader Antenna (2014)

This letter presents the design of a coplanar waveguide (CPW) circularly polarized antenna for the central frequency 900 MHz, it comes in handy for radio frequency identification (RFID) short-range reading applications within the band of 902-928 MHz where the axial ratio of proposed antenna model is less than 3 dB. The proposed design has an axial-ratio bandwidth of 36 MHz (4%) and impedance bandwidth of 256 MHz (28.5%).
Percutaneous left atrial appendage transcatheter occlusion (PLAATO) for stroke prevention in atrial fibrillation: 2-year outcomes. (2009)

Ninety-seven percent of AF patients were successfully treated with PLAATO. After mechanical LAA occlusion, the 2-year risk of stroke in AF patients is markedly reduced. Therefore, this therapeutic concept is a clear alternative for patients with AF and contraindications for oral anticoagulation.
Low Threshold Channel Waveguide Laser in a Monocrystalline Nd:(Gd, Lu)2O3 Film (2009)

We report the first waveguide laser based on rare-earth sesquioxides. A structured Nd(0.5%):(Gd, Lu)2O3 film pumped at 820 nm showed lasing at 1.08 µm. The laser threshold was 0.8 mW, the preliminary slope efficiency 0.5 % and the maximum output power 1.8 mW.
Electrical-conductivity calculation in ab initio simulations of metals:Application to liquid sodium (1997)

We describe a calculation of the electrical conductivity in ab initio simulations of liquid sodium, using the Kubo-Greenwood formula for the optical conductivity and the molecular-dynamics scheme based on finite-temperature density functional theory. The effect of different Brillouin-zone samplings and that of the finite size of the system have been extensively studied at different temperatures. Close to the melting point, even with an adequate sampling of the Brillouin zone, our results exhibit a large discrepancy between theory and experiment. This is much reduced at higher temperatures. The possible reasons for this behavior are discussed.
Neurophysiological modulation of the subthalamic nucleus by pallidal stimulation in Parkinson's disease (2002)

Although these findings require confirmation, they suggest that the current theories of GPi DBS action, which do not include a GPi-STN modulation, are most likely incomplete.
Protective effects of a new stable, highly active SOD mimetic, M40401 in splanchnic artery occlusion and reperfusion (2001)

1. Splanchnic artery occlusion shock (SAO) causes an enhanced formation of reactive oxygen species (ROS), which contribute to the pathophysiology of shock. Here we have investigated the effects of M40401, a new S:,S:-dimethyl substituted biscyclohexylpyridine Mn-based superoxide dismutase mimetic (SODm, k(cat)=1.2x10(+9) M(-1) s(-1) at pH=7.4), in rats subjected to SAO shock. 2. Treatment of rats with M40401 (applied at 0.25, 2.5 or 25 microg kg(-1), 15 min prior to reperfusion), attenuated the mean arterial blood and the migration of polymorphonuclear cells (PMNs) caused by SAO-shock. M40401 also attenuated the ileum injury (histology) as well as the increase in the tissue levels of myeloperoxidase (MPO) and malondialdehyde (MDA) caused by SAO shock in the ileum. 3. Immunohistochemical analysis for nitrotyrosine revealed a positive staining in ileum from SAO-shocked rats. The degree of staining for nitrotyrosine was markedly reduced in tissue sections obtained from SAO-shocked rats which had received M40401. Reperfused ileum tissue sections from SAO-shocked rats showed positive staining for P-selectin and for anti-intercellular adhesion molecule (ICAM-1) in the vascular endothelial cells. M40401 treatment markedly reduced the intensity and degree of P-selectin and ICAM-1 in tissue sections from SAO-shocked rats. M40401 treatment significantly improved survival. 4. Additionally, the very high catalytic activity of this new mimetic (comparable to the native human Cu/Zn SOD enzyme and exceeding the activity of the human Mn SOD enzyme) translates into a very low dose ( approximately microg kg(-1)) required to afford protection in this SAO model of ischemia reperfusion injury. 5. Taken together, our results clearly demonstrate that M40401 treatment exerts a protective effect, and part of this effect may be due to inhibition of the expression of adhesion molecules and peroxynitrite-related pathways with subsequent reduction of neutrophil-mediated cellular injury.