gebhart/patrepeval huggingface dataset:
Phase I dose finding study of AZD8931, an inhibitor of EGFR, HER2, and HER3 signaling, alone or in combination with paclitaxel in Japanese patients. (2013)

e13501 Background: AZD8931 is an equipotent, reversible inhibitor of signaling by EGFR, HER2 and HER3. Methods: This open-label, multiple-dose cohort study (NCT01003158) was conducted in Japan to evaluate the safety, tolerability and PK of ascending doses of AZD8931 alone (starting dose 40 mg bd) in patients (pts) with advanced solid malignancies and AZD8931 in combination with paclitaxel (P; 90 mg/m 2 on days 1, 8 and 15 of a 28-day cycle) in pts with advanced breast cancer. Results: Between Jan 2010 and Apr 2012,17 pts were treated; 11 with AZD8931 monotherapy (40/60/80 mg bd [n=3/4/4]) and 6 with AZD8931 40 mg bd plus P. Median (range) duration of exposure to AZD8931 was 42.5 (22–238) and 79.5 (53–244) days for monotherapy and combination therapy, respectively. No DLTs were observed (in the DLT evaluation period) and therefore the MTD was not confirmed for AZD8931 alone or with P. The most frequent AEs (all grades) with AZD8931 monotherapy were diarrhea, paronychia, rash pustule and dry skin (each n=8) and with combination therapy were diarrhea, stomatitis, rash, alopecia, epistaxis and neutropenia (each n=4). Throughout the study grade ≥3 AEs were reported for 1, 2 and 4 pts in the 40 mg, 60 mg and combination groups, respectively. One serious AE was reported each in the 40 mg (grade 3 intervertebral disc protrusion) and combination (grade 2 infectious pneumonia) groups; neither was considered related to study treatment. One pt in the combination therapy part discontinued due to an AE of grade 1 pneumonia. AZD8931 was rapidly absorbed (median t max 1–2 hours), well distributed, had moderate clearance (31–39 L/h) and a t ½ of 12 hours. There was no suggestion of a PK interaction between AZD8931 and P. One pt on AZD8931 80 mg bd (primary stomach cancer) and another receiving AZD8931 plus P (advanced breast cancer) had an unconfirmed and confirmed PR, respectively (duration of responses 42 and 172 days, respectively) demonstrating preliminary efficacy. Conclusions: Although a MTD was not confirmed for AZD8931, based on overall incidence of AEs of rash and diarrhea in the 80 mg group, doses up to 60 mg bd as monotherapy and 40 mg bd combined with P are the recommended doses for evaluation in Japanese pts. Clinical trial information: NCT01003158.
Altered Ethanolamine Plasmalogen and Phosphatidylethano-lamine Concentrations in Serum of Patients with Bipolar Disorder (P08-117-19) (2019)

Growing evidence has suggested that metabolic alterations of plasmalogen ethanolamine (PlsEtn) are implicated in neuropsychiatric diseases. However, few studies examined the association of peripheral blood PlsEtn levels with bipolar disorder (BP). In this study, we measured serum PlsEtn and phosphatidylethanolamine (PtdEtn) levels in patients with BP and healthy controls. We investigated the relationships between serum PlsEtn and PtdEtn levels, diagnosis, symptom severity and medication status. Subjects were 40 patients with BP (DSM-IV) and 40 healthy controls matched for age, sex, and ethnicity (Japanese). Informed consent was obtained from each subject. Serum levels of PlsEtn and PtdEtn were determined by liquid chromatography/tandem mass spectrometry. Serum PlsEtn were significantly lower in patients with BP compared with controls (P = 0.017). Serum PtdEtn levels were significantly lower in patients with a BP type I (n = 12) versus patients with BP type II (n = 24) diagnosis (P = 0.011). In the BP patients, symptom severity did not correlate with serum PlsEtn or PtdEtn levels. Low serum PlsEtn might be involved in the pathophysiology of BP. PtdEtn might be related differently with BP I and BP II. This study was supported by an Intramural Research Grant for Neurological and Psychiatric Disorders by the National Center of Neurology and Psychiatry (H.K.).
Evaluation of experimental permanent-magnet brushless motor utilizing new magnetic material for stator core teeth (2005)

We prepared motors with experimental cores using a soft magnetic composite and an amorphous metal and evaluated their performance. We measured the magnetic and motor characteristics, such as iron loss, when the new materials were used in the stator core teeth. The amorphous metal was found to have very high permeability and low iron loss, whereas the soft magnetic composite had low permeability and had a comparable iron loss as low-grade magnetic steel. The soft magnetic composite had the added benefits of being able to form a three-dimensional shape and having relatively low core loss in high frequency conditions. The magnetic properties we measured were able to predict the motor characteristics with high accuracy based on numerical and finite-element-method analysis.
Mesenchymal stem cells protect from hypoxia-induced alveolar epithelial-mesenchymal transition (2015)

Administration of bone marrow-derived human mesenchymal stem cells (hMSC) reduces lung inflammation, fibrosis, and mortality in animal models of lung injury, by a mechanism not completely understood. We investigated whether hMSC would prevent epithelial-mesenchymal transition (EMT) induced by hypoxia in primary rat alveolar epithelial cell (AEC). In AEC cultured on semipermeable filters, prolonged hypoxic exposure (1.5% O2 for up to 12 days) induced phenotypic changes consistent with EMT, i.e., a change in cell morphology, a decrease in transepithelial resistance (Rte) and in the expression of epithelial markers [zonula occludens-1 (ZO-1), E-cadherin, AQP-5, TTF-1], together with an increase in mesenchymal markers [vimentin, α-smooth muscle actin (α-SMA)]. Expression of transcription factors driving EMT such as SNAIL1, ZEB1, and TWIST1 increased after 2, 24, and 48 h of hypoxia, respectively. Hypoxia also induced TGF-β1 mRNA expression and the secretion of active TGF-β1 in apical medium, and the expression of connective tissue growth factor (CTGF), two inducers of EMT. Coculture of AEC with hMSC partially prevented the decrease in Rte and in ZO-1, E-cadherin, and TTF-1 expression, and the increase in vimentin expression induced by hypoxia. It also abolished the increase in TGF-β1 expression and in TGF-β1-induced genes ZEB1, TWIST1, and CTGF. Finally, incubation with human recombinant KGF at a concentration similar to what was measured in hMSC-conditioned media restored the expression of TTF-1 and prevented the increase in TWIST1, TGF-β1, and CTGF in hypoxic AEC. Our results indicate that hMSC prevent hypoxia-induced alveolar EMT through the paracrine modulation of EMT signaling pathways and suggest that this effect is partly mediated by KGF.
Adaptive coding of hyperspectral imagery (1999)

Two systems are presented for compression of hyperspectral imagery. These systems utilize adaptive classification, trellis-coded quantization, and optimal rate allocation. In the first system, DPCM is used for spectral decorrelation, while an adaptive wavelet-based coding scheme is used for spatial decorrelation. The second system uses DPCM in conjunction with an adaptive DCT-based coding scheme. In each system, entropy-constrained trellis-coded quantization (ECTCQ) is used to quantize the transform coefficients. Entropy-constrained codebooks are designed for generalized Gaussian distributions by using a modified version of the generalized Lloyd algorithm. The wavelet-based system compresses an AVIRIS hyperspectral test sequence at 0.118 bits/pixel/band, while retaining an average peak signal-to-noise ratio (PSNR) of 41.24 dB. The DCT-based system achieves the same bit rate with an average PSNR of 40.72 dB.
Synthesis of 7‐Cyano‐ and 7‐Acetamido‐indoles via Cyanocarbonation/Hydrogenation of 7‐Formyl Indole. (2003)

Abstract For Abstract see ChemInform Abstract in Full Text.
GPU virtualization on VMware's hosted I/O architecture (2009)

Modern graphics co-processors (GPUs) can produce high fidelity images several orders of magnitude faster than general purpose CPUs, and this performance expectation is rapidly becoming ubiquitous in personal computers. Despite this, GPU virtualization is a nascent field of research. This paper introduces a taxonomy of strategies for GPU virtualization and describes in detail the specific GPU virtualization architecture developed for VMware's hosted products (VMware Workstation and VMware Fusion). We analyze the performance of our GPU virtualization with a combination of applications and microbenchmarks. We also compare against software rendering, the GPU virtualization in Parallels Desktop 3.0, and the native GPU. We find that taking advantage of hardware acceleration significantly closes the gap between pure emulation and native, but that different implementations and host graphics stacks show distinct variation. The microbenchmarks show that our architecture amplifies the overheads in the traditional graphics API bottlenecks: draw calls, downloading buffers, and batch sizes. Our virtual GPU architecture runs modern graphics-intensive games and applications at interactive frame rates while preserving virtual machine portability. The applications we tested achieve from 86% to 12% of native rates and 43 to 18 frames per second with VMware Fusion 2.0.
Chapter V: The Lactose Repressor (1970)

The repressor for the lactose operon has been the paradigm for negative control. The Jacob and Monod (1961) hypothesis proposed that control genes would make repressors which would turn off other genes. Regulatory genes, as distinct from “structural” genes, were to make substances that could directly affect a rate-determining step in the synthesis of the functional products of other specific genes. This rate-determining step defines a target for the control: a specific point of interaction for the controlling substance. Such a target, named an “operator,” could be a specific point on a DNA molecule. The binding of a substance to the region of the DNA molecule that serves as an initiation point for the synthesis of messenger RNA clearly could block (or affect or enhance) the synthesis of that messenger. Alternatively, the target for control could be a region on a messenger RNA molecule. The binding of a control substance to such a messenger could easily be imagined to block the attachment of ribosomes and hence the synthesis of proteins. The term “bind” simply supplies a specific physical picture. As far as any genetic arguments are concerned, any biochemical process that leads to the same result would serve. The control substance could modify bases, achieving the same ends through a chemical alteration of structure. The isolation of several repressors (Gilbert and Muller-Hill, 1966; Ptashne, 1967a; Riggs and Bourgeois, 1968; Pirrotta and Ptashne, 1969) and the demonstration that the operator is a region on a DNA molecule to which they bind...
Remote Sensing of Alpha and Beta Sources - Modeling Summary (2005)

Evaluating the potential for optical detection of the products of interactions of energetic electrons or other particles with the background atmosphere depends on predictions of change in atmospheric concentrations of species which would generate detectable spectral signals within the range of observation. The solar blind region of the spectrum, in the ultra violet, would be the logical band for outdoor detection (see Figure 1). The chemistry relevant to these processes is composed of ion-molecule reactions involving the initially created N{sub 2}{sup +} and O{sub 2}{sup +} ions, and their subsequent interactions with ambient trace atmospheric constituents. Effective modeling of the atmospheric chemical system acted upon by energetic particles requires knowledge of the dominant mechanism that exchange charge and associate it with atmospheric constituents, kinetic parameters of the individual processes (see e.g. Brasseur and Solomon, 1995), and a solver for the coupled differential equations that is accurate for the very stiff set of time constants involved. The LLNL box model, VOLVO, simulates the diel cycle of trace constituent photochemistry for any point on the globe over the wide range of time scales present using a stiff Gear-type ODE solver, i.e. LSODE. It has been applied to problems such as tropospheric and stratospheric nitrogen oxides, stratospheric ozone production and loss, and tropospheric hydrocarbon oxidation. For this study we have included the appropriate ion flux.
Comparison of adaptive array processing schemes for land mine detection using hyperspectral imagery (2005)

Adaptive techniques for detecting small or difficult targets in the midst of high noise and/or clutter have a rich history in the radar array processing community. However, the utility of these schemes is only beginning to be realized for multichannel electro-optical techniques, specifically hyperspectral imaging (HSI). The data products generated by hyperspectral sensors differ greatly from those of radar and sonar arrays, yet recent studies using HSI data have offered promising results for modified versions of common adaptive detectors. In this paper, we compare a series popular adaptive detection schemes applied to HSI data for the task of land mine detection. Experiments using real hyperspectral image cubes, not simulations, are performed with data from both the visible-SWIR and LWIR regions. Results are presented for different mine types in a variety of scenes.
α3β1 Integrin-TargetingPolymersomal Docetaxel as an Advanced Nanotherapeutic for NonsmallCell Lung Cancer Treatment (2020)

Docetaxel\n(DTX) widely used for treating nonsmall cell lung cancer\n(NSCLC) patients is associated with dose-limiting side effects, especially\nneurotoxicity and myelosuppression. Here, we have developed cyclic\ncNGQGEQc peptide-directed polymersomal docetaxel (cNGQ-PS-DTX) as\na targeted and multifunctional formulation for NSCLC. cNGQ-PS-DTX\ncarrying 8.1 wt % DTX had a size of 93 nm, neutral surface charge,\nhigh stability, and glutathione-triggered DTX release behavior. Cytotoxicity\nstudies demonstrated a clearly better antitumor activity of cNGQ-PS-DTX\nin α&lt;sub&gt;3&lt;/sub&gt;β&lt;sub&gt;1&lt;/sub&gt; integrin overexpressing\nA549 human lung cancer cells than free DTX and nontargeted PS-DTX.\ncNGQ-PS-DTX showed a remarkably high tolerability (over 8 times better\nthan free DTX) and slow elimination in mice. Importantly, cNGQ-PS-DTX\nexhibited greatly improved tumor accumulation and higher suppression\nof subcutaneous and orthotopic A549 xenografts as compared to PS-DTX\nand free DTX controls. α&lt;sub&gt;3&lt;/sub&gt;β&lt;sub&gt;1&lt;/sub&gt; integrin-targeting\npolymersomal docetaxel emerges as an advanced nanotherapeutic for\nNSCLC treatment.
ChemInform Abstract: ORGANISCHE SCHWEFELVERBINDUNGEN 61. MITT. RK. VON DIARYLDIAZOMETHANEN MIT O,O′‐DIALKYLXANTHOGENSAEUREANHYDRIDEN (1970)

Abstract Das Diazomethan (I) reagiert mit den Xanthogensäureanhydriden (II) zu den Thiiranen (III) (82‐84% Ausbeute), die sich in der Wärme in die Thionessigsäuren (IV) umlagern.
Appendix E: Background Information (2010)

This appendix contains sections titled: Commonly Used Equations Acronyms Electromagnetic Spectrum Periodic Table Symbols for Elements International System of Units (SI Units) Unit Prefixes Greek Alphabet Fundamental Constants List of Symbols ]]>
Improved Fermentative Hydrogen Production with the Addition of Calcium-Lignosulfonate-Derived Biochar (2019)

This study investigated the roles of calcium lignosulfonate (CL) and its derived biochar (BC) in biohydrogen production. CL was pyrolyzed at 250 °C to produce BC, and the main characteristics of the two materials were compared. A series of anaerobic processes were carried out at 54 ± 1 °C, and the results suggested that CL remarkably lowered the H2 yield compared with that obtained with CL-derived BC. The highest H2 yield (262 mL/g glucose) was obtained at 20 g/L, corresponding to an increase of 50.9%, whereas the lowest H2 yield (110 mL/g glucose) occurred at 20 g/L and was 36.4% lower than that in the control group (173 mL/g glucose, without CL and BC). The CL-derived BC exhibited more pore structures than CL, providing more attachment sites for anaerobes. In addition, the high potassium, calcium, and magnesium contents and low sulfur dosage enhanced the microbial activity and process stability.
Sequence and tissue distribution of the human integrin α8 subunit: a β1-associated α subunit expressed in smooth muscle cells (1995)

Integrins are a major family of cell adhesion molecules involved in cell-cell and cell-extracellular matrix interactions. Each integrin is a heterodimeric glycoprotein composed of an alpha and a beta subunit. We now report the cDNA sequence and distribution of a new human integrin alpha subunit. This sequence is 78% identical to the previously reported chicken alpha 8 integrin sequence. Thus, we have designated this subunit as human alpha 8. By northern blot analysis, an alpha 8 probe detects two mRNA species of approximately 6.5 and 4.0 kb in neuroglioma H4 cells. An anti-alpha 8 polyclonal antibody precipitates a protein complex containing the beta 1 subunit associated with the putative alpha 8 subunit, which has an apparent molecular mass of 180 kDa (non-reduced) or 155 kDa and 25 kDa (reduced). Immunohistochemistry with anti-alpha 8 polyclonal antibody in adult rat tissues shows prominent staining in vascular and visceral smooth muscle. In addition, the antibody strongly stained kidney mesangial cells and a cell type in the alveolar wall of the lungs, most likely corresponding to alveolar myofibroblasts. These results suggest that in adult mammalian tissues, alpha 8 is predominantly expressed in smooth muscle and smooth muscle-like contractile cells.
Sterol and Fatty Acid Metabolism inFusarium oxysporum (1977)

The effects of temperatures ranging from 10°C to 35°C on sterol and fatty acid production and hydroxymethylglutaryl CoA reductase (EC 1.1,1.34, HMGCoA reductase) activity have been examined. Growth, based on dry weight, was maximal at 25°C to 30°C. Sterol production and the reductase activity were highest at 15°C after 28~32 hr incubation when the total fatty acids were minimal. Fatty acid unsaturation generally increased with decrease in temperature.
Role of a Guanine Nucleotide Regulatory Protein in Exocrine Pancreatic Secretion (1989)

We have recently shown that F- can mimic the actions of cholecystokinin (CCK) on amylase release, Ca2+ mobilization and inositol phosphate generation in pancreatic acinar cells. We have concluded, therefore, that pancreatic CCK receptors may be coupled to the activation of polyphosphoinositide hydrolysis by a guanine nucleotide regulatory protein (N protein), which seems to be sensitive to F-. In the present study, in order to further characterize this N protein coupled to pancreatic CCK receptors, we have examined the effects of bacterial toxins, pertussis toxin (PT) and cholera toxin (CT) on both CCK- and NaF-induced cellular responses in isolated rat pancreatic acini. Neither PT or CT pretreatment of acini affected both CCK- and NaF-stimulated increases in intracellular Ca2+ concentration monitored by quin2. Furthermore, pretreatments of acini with PT and CT didn't alter the effects of CCK on inositol phosphate generation in acini. Similarly, NaF-induced inositol phosphate generation was not changed by these toxin treatments. However, pretreatment procedures employed in this study were considered to catalyze complete ADP-ribosylation of alpha-subunit of the stimulatory (Ns) and inhibitory (Ni) N protein. These results, therefore, strongly suggest that a N protein coupling pancreatic CCK receptors to the breakdown of polyphosphoinositide may be distinct from Ns or Ni like protein.
Sub-10 μHz/√Hz Measurement Instrumentation for 140-dB DR Frequency-Modulated MEMS Sensors (2022)

The field of frequency-modulated (FM) microelectromechanical system (MEMS) sensors is emerging as an alternative to conventional amplitude-modulated (AM) architectures, especially because of new application requirements on extended full-scale and low noise, which turn into a wide dynamic range (DR). As a consequence, a need for characterization tools dedicated to this novel class of transducers is arising. This work presents the development of the key building blocks of an instrument for the characterization of FM sensors, including an integrated circuit and external board-level components. In the instrument design, the focus is set on versatility in terms of input range frequencies and on guaranteeing a DR in the order of 140 dB. The instrument core is based on a frequency-to-digital converter, implemented through a type-II phase-locked loop with a differentiator implementing a period meter. Low-quantization noise is obtained using a high-frequency (100 MHz) time reference, while versatility is guaranteed at the same time by having programmable parameters within the integrated circuit. The instrument is tested across the 27–260-kHz input range and demonstrates sub-10- <inline-formula xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink"> <tex-math notation="LaTeX">$\mu \text {Hz}/\sqrt {\text {Hz}}$ </tex-math></inline-formula> frequency noise density in the range from 10 to 100 Hz offset from the carrier and up to 100-Hz full scale. The instrument is available for testing and used by whoever is interested in its features.
Synthesis of 188Re-labelled long chain alkyl diaminedithiol for therapy of liver cancer (2002)

Radioisotope-labelled lipiodol has been used in the therapy of liver cancer. Recently a lipiodol solution of 188Re-labelled diaminedithiol (DD) has been reported to show a high uptake in the liver cancer. We synthesized long-chain alkyl DD derivatives to improve their uptake and retention in tissue. As the length of the alkyl chain increased, tissue uptake and retention also increased due to hydrophobic interaction with lipiodol. Among the synthesized compounds, the lipiodol solution of 188Re-HDD, the DD derivative with the longest side chain (C16), is a promising agent for therapy of liver cancer.
Taking computer vision aloft – archaeological three‐dimensional reconstructions from aerial photographs with photoscan (2011)

Abstract Structure from motion (SFM) algorithms are known for their ability to reconstruct a sparse point cloud of scenes that were imaged by a series of overlapping photographs. When complemented by stereo‐matching algorithms, detailed three‐dimensional models can be built from such photograph collections in a fully automated way. Since 2010, a computer vision software package called PhotoScan has been available from the Russian manufacturer AgiSoft LLC. Even though the programme has a straightforward and simple interface, state‐of‐the‐art SFM and other computer vision algorithms are implemented that enable PhotoScan to generate very dense and accurate three‐dimensional meshes of various (archaeological) settings captured in two‐dimensional imagery. Using a mixture of archaeological case studies, it will be shown that this low‐cost application produces excellent results from aerial imagery in a minimum of time with almost no effort needed. Because of its solid and uncomplicated operation, it looks like this application could become an essential part of the aerial archaeologist's toolkit. Copyright © 2011 John Wiley &amp; Sons, Ltd.