gebhart/patrepeval huggingface dataset:
Discovery and Optimization of 4,5-Diarylisoxazoles as Potent Dual Inhibitors of Pyruvate Dehydrogenase Kinase and Heat Shock Protein 90 (2014)

Upregulation of pyruvate dehydrogenase kinase (PDHK) has been observed in a variety of cancers. Inhibition of PDHK offers an attractive opportunity for the development of novel cancer therapies. To obtain novel PDHK inhibitors, we took advantage of the homology of the ATP-binding pocket between Heat Shock Protein 90 (HSP90) and PDHK, and utilized 4,5-diarylisoxazole based HSP90 inhibitor for structural design. Our efforts led to the identification of 5k that inhibited PDHK1 with an IC50 value of 17 nM, which, however, showed marginal cellular activity. Further structural optimization resulted in compound 11a with improved cellular activity which could effectively modulate the metabolic profile of cancer cells and lead to the inhibition of cancer cell proliferation, evidenced by the increased oxidative phosphorylation and decreased glycolysis and associated oxidative stress. Our results suggested 11a as an excellent lead compound and a favorable biological tool to further evaluate the therapeutic potential of PDHK and HSP90 dual inhibitors in the treatment of cancer.
Mast cell function in prostate inflammation, fibrosis, and smooth muscle cell dysfunction (2021)

Intraurethral inoculation of mice with uropathogenic <i>Escherichia coli</i> (CP1) results in prostate inflammation, fibrosis, and urinary dysfunction, recapitulating some but not all of the pathognomonic clinical features associated with benign prostatic hyperplasia (BPH) and lower urinary tract symptoms (LUTS). In both patients with LUTS and CP1-infected mice, we observed increased numbers and activation of mast cells and elevated levels of prostate fibrosis. Therapeutic inhibition of mast cells using a combination of a mast cell stabilizer, cromolyn sodium, and the histamine 1 receptor antagonist cetirizine di-hydrochloride in the mouse model resulted in reduced mast cell activation in the prostate and significant alleviation of urinary dysfunction. Treated mice showed reduced prostate fibrosis, less infiltration of immune cells, and decreased inflammation. In addition, as opposed to symptomatic CP1-infected mice, treated mice showed reduced myosin light chain-2 phosphorylation, a marker of prostate smooth muscle contraction. These results show that mast cells play a critical role in the pathophysiology of urinary dysfunction and may be an important therapeutic target for men with BPH/LUTS.<b>NEW & NOTEWORTHY</b> LUTS-associated benign prostatic hyperplasia is derived from a combination of immune activation, extracellular matrix remodeling, hyperplasia, and smooth muscle cell contraction in prostates of men. Using a mouse model, we describe the importance of mast cells in regulating these multiple facets involved in the pathophysiology of LUTS. Mast cell inhibition alleviates both pathology and urinary dysfunction in this model, suggesting the potential for mast cell inhibition as a therapeutic that prevents and reverses pathology and associated symptomology.
Neuronal ceroid lipofuscinosis in Merino sheep (2002)

NCL in Merino sheep is a subunit c-storing disease, clinically and pathologically similar to NCL in South Hampshire sheep. We propose that the disease in both breeds represents mutation at the same gene locus in chromosomal region OAR7q13-15.
Diabetes-enhanced Inflammation and Apoptosis—Impact on Periodontal Pathology (2006)

Diabetes, particularly type 2 diabetes, is a looming health issue with many ramifications. Because diabetes alters the cellular microenvironment in many different types of tissues, it causes myriad untoward effects, collectively referred to as 'diabetic complications'. Two cellular processes affected by diabetes are inflammation and apoptosis. This review discusses how diabetes-enhanced inflammation and apoptosis may affect the oral environment. In particular, dysregulation of tumor necrosis factor and the formation of advanced glycation products, both of which occur at higher levels in diabetic humans and animal models, potentiate inflammatory responses and induce apoptosis of matrix-producing cells. The enhanced loss of fibroblasts and osteoblasts through apoptosis in diabetics could contribute to limited repair of injured tissue, particularly when combined with other known deficits in diabetic wound-healing. These findings may shed light on diabetes-enhanced risk of periodontal diseases.
Effect of Gate Metal Electrode on Chemical Bonding State in Metal/Pr-Oxide/Ge Gate Stack Structure (2012)

We investigated the effect of the oxidation-reduction character of metal electrode on the chemical bonding state in metal/Pr-oxide/Ge gate stack structure. The binding energy of the Pr-oxide peak increases with the formation of a metal electrode with the strong reduction character, indicating the change in the valence state of Pr from tetravalent to trivalent. The intensity of the Ge oxide peak changes depending on metal species. It is suggested that some amount of Ge oxide is reduced in the sample with the metal film with the strong reduction character. Therefore, the oxidation-reduction character of metal electrode affects on not only the change in the Pr valence state in oxide film but also the interfacial reaction at the Pr-oxide/Ge interface for metal/Pr-oxide/Ge gate stack structures. These results suggest that a selection of gate metal species with basing on an oxidation-reduction character is quite important since it affects not only the dielectric constant of high-k films but also the interfacial chemical bonding structures in metal/high-k/Ge gate stack structures.
Three-Dimensional Deformable-Model-Based Localization and Recognition of Road Vehicles (2011)

We address the problem of model-based object recognition. Our aim is to localize and recognize road vehicles from monocular images or videos in calibrated traffic scenes. A 3-D deformable vehicle model with 12 shape parameters is set up as prior information, and its pose is determined by three parameters, which are its position on the ground plane and its orientation about the vertical axis under ground-plane constraints. An efficient local gradient-based method is proposed to evaluate the fitness between the projection of the vehicle model and image data, which is combined into a novel evolutionary computing framework to estimate the 12 shape parameters and three pose parameters by iterative evolution. The recovery of pose parameters achieves vehicle localization, whereas the shape parameters are used for vehicle recognition. Numerous experiments are conducted in this paper to demonstrate the performance of our approach. It is shown that the local gradient-based method can evaluate accurately and efficiently the fitness between the projection of the vehicle model and the image data. The evolutionary computing framework is effective for vehicles of different types and poses is robust to all kinds of occlusion.
Bacteria Absorption-Based Mn2P2O7–Carbon@Reduced Graphene Oxides for High-Performance Lithium-Ion Battery Anodes (2016)

The development of freestanding flexible electrodes with high capacity and long cycle-life is a central issue for lithium-ion batteries (LIBs). Here, we use bacteria absorption of metallic Mn(2+) ions to in situ synthesize natural micro-yolk-shell-structure Mn2P2O7-carbon, followed by the use of vacuum filtration to obtain Mn2P2O7-carbon@reduced graphene oxides (RGO) papers for LIBs anodes. The Mn2P2O7 particles are completely encapsulated within the carbon film, which was obtained by carbonizing the bacterial wall. The resulting carbon microstructure reduces the electrode-electrolyte contact area, yielding high Coulombic efficiency. In addition, the yolk-shell structure with its internal void spaces is ideal for sustaining volume expansion of Mn2P2O7 during charge/discharge processes, and the carbon shells act as an ideal barrier, limiting most solid-electrolyte interphase formation on the surface of the carbon films (instead of forming on individual particles). Notably, the RGO films have high conductivity and robust mechanical flexibility. As a result of our combined strategies delineated in this article, our binder-free flexible anodes exhibit high capacities, long cycle-life, and excellent rate performance.
Adaptive Semiparametric Language Models (2021)

We present a language model that combines a large parametric neural network (i.e., a transformer) with a non-parametric episodic memory component in an integrated architecture. Our model uses extended short-term context by caching local hidden states -- similar to transformer-XL -- and global long-term memory by retrieving a set of nearest neighbor tokens at each timestep. We design a gating function to adaptively combine multiple information sources to make a prediction. This mechanism allows the model to use either local context, short-term memory, or long-term memory (or any combination of them) on an ad hoc basis depending on the context. Experiments on word-based and character-based language modeling datasets demonstrate the efficacy of our proposed method compared to strong baselines.
A systematic review of biomarkers associated with maternal infection in pregnant and postpartum women (2021)

Findings suggest that certain biomarkers have diagnostic value when maternal infection is suspected, but also confirms limitations in this population.
A simple Qt based comparison program for ITK and VTK images. (2010)

This document describes a project that can compare many images simultaneously in a synchronized manner. Such an application can be used in any ITK/VTK image processing pipelines; the programmer can use it to quickly visualize and compare intermediate results of used filters within the pipeline.The goals of this project are two folds: (i) to be integrated in gdb pretty debuggers (for visual debugging of ITK pipelines), and, (ii) to provide a visual comparison widget for image-to-image plugins (ITK or VTK based filters). This project is part of the Gofigure2 development effort, an open-source, cross-platform application for visualizing, processing and analyzing of multidimensional microscopy data.
Structure-antigastrin activity relationships of new (R)-4-benzamido-5-oxopentanoic acid derivatives (1992)

New (R)-4-benzamido-5-oxopentanoic acid derivatives were synthesized by a stereoconservative procedure and evaluated in vitro for their capacity to inhibit the binding of [125I](BH)-CCK-8 to either rat peripheral (CCK-A) or central (CCK-B) CCK receptors, or the binding of [3H]pentagastrin to rabbit gastric glands, as well as to inhibit, in vivo, the acid secretion induced by pentagastrin infusion in the perfused rat stomach. The parent compound of this series (lorglumide) is the first nonpeptidic, potent and selective antagonist of the CCK-A receptor. Chemical manipulations of the structure of lorglumide led to the discovery of selective antagonists of the CCK-B/gastrin receptors. Structure-activity relationships are discussed. Some of these new derivatives exhibit different affinities with rabbit gastric gland cells and rat cortex membranes, suggesting that the stomach gastrin receptor (arbitrarily termed CCK-B1 receptor) is not as closely related to the CCK central receptor (termed CCK-B2) as previously hypothesized. The antigastric activity of the most potent compound of the series, i.e. (R)-4-(3,5-dichlorobenzamido)-5-(8-azaspiro[4.5]decan- 8-yl)-5-oxopentanoic acid (compound 28, CR 2194) was further evaluated in vivo: in the first hour after administration the compound inhibits acid secretion induced by pentagastrin infusion, in both cat and dog (in the cat with gastric fistula and in the dog with Heidenhain pouch), with ID50s (mg/kg) of 15.5 (iv) (cat), 8.7 (IV) (dog) and 24.2 (oral) (Heidenhain dog). The characteristics of CR 2194, that is, the selectivity for the gastrin receptor, the simple nonpeptidic molecular structure, and the activity after oral administration, indicate that this compound is a useful tool in the study of the biological effects of gastrin and a potential agent for diagnostic or therapeutic use.
Health Implications of Obesity (1985)

Obesity, the excessive storage of energy in the form of fat, is clearly associated with hypertension, hypercholesterolemia, diabetes (Type II), certain cancers, and other medical problems.
Modal Identities for Elastic Bodies, With Application to Vehicle Dynamics and Control (1980)

It is a standard procedure to analyze a flexible vehicle in terms of its vibration frequencies and mode shapes. However, the entire mode shape is not needed per se, but two integrals of the mode shape, pi and hi, which correspond to the momentum and angular momentum in Mode i. Together with the natural frequencies ωi, these modal parameters satisfy several important identities, 25 of which are derived in this paper. Expansions in terms of both “constrained” and “unconstrained” modes are considered. A simple illustrative example is included. The paper concludes with some remarks on the theoretical and practical utility of these results, and several potential extensions to the theory are suggested.
Joint 3D Estimation of Objects and Scene Layout (2011)

We propose a novel generative model that is able to reason jointly about the 3D scene layout as well as the 3D location and orientation of objects in the scene. In particular, we infer the scene topology, geometry as well as traffic activities from a short video sequence acquired with a single camera mounted on a moving car. Our generative model takes advantage of dynamic information in the form of vehicle tracklets as well as static information coming from semantic labels and ge-ometry (i.e., vanishing points). Experiments show that our approach outperforms a discriminative baseline based on multiple kernel learning (MKL) which has ac-cess to the same image information. Furthermore, as we reason about objects in 3D, we are able to significantly increase the performance of state-of-the-art object detectors in their ability to estimate object orientation. 1
The KI-ASIC Dataset (2023)

&lt;p&gt;We present a novel dataset captured from a BMW X5 test carrier within the German research project KI-ASIC for use in radar sensor development and autonomous driving research. Our work aims at providing a blueprint for the process of creating labeled datasets for the development of neural networks for pattern recognition in radar data in the automotive environment. With a variety of different sensor types such as wide angle color cameras, a high-resolution color stereo camera, an Ouster OS1-64 laser scanner and three novel Infineon radar sensors, we recorded over 100,000 scenes of real traffic scenarios as well as defined test scenarios with a frequency of 10 Hz. The scenarios in real traffic contain inner-city situations, but also scenes from rural areas with static and dynamic objects. Besides, the defined test scenarios are based on the NCAP scenarios and focus mostly on turning, overtaking and follow-up maneuvers. The data from the different sensors is calibrated, synchronized and timestamped including raw and rectified information. Our dataset also contains labels for all detected objects from a defined class list with distance and angle properties. &lt;/p&gt;
IQGAP1 regulates ERK1/2 and AKT signalling in the heart and sustains functional remodelling upon pressure overload (2011)

These data demonstrate, for the first time, a key role for the scaffold protein IQGAP1 in integrating hypertrophy and survival signals in the heart and regulating long-term left ventricle remodelling upon pressure overload.
Dipentaerythritol‐Derived Hyperbranched Polyurethane Elastomers and Their Applications in Flexible Strain Sensors (2022)

Abstract Polyurethane (PU) elastomers have great potential to work as flexible substrates in electronic materials. In this work, hyperbranched PU elastomers are designed and prepared utilizing dipentaerythritol, isophorone diisocyanate, and polytetrahydrofuran as the monomers. The mechanical properties and transparency of the PU elastomers are regulated by the molar ratio of hydroxyl group to isocyanate group (OH/NCO). High tensile strength (26 MPa) and elongation at break (&gt;600%) are achieved. Furthermore, PU elastomer composites are developed by introducing graphene into the surface of PU elastomers. PU elastomer composites are further utilized in assembling flexible strain sensors, which achieve a gauge factor (GF) of 170 in the strain range of 0–75% and a GF of 549 in the strain range of 75–225%. The response time is as low as 140 ms and at least 1000 reversible sensing cycles are successfully conducted. Utilizing such flexible sensors, monitoring of various human motions, including biceps motion, finger bending, knee joint bending, elbow bending, and vocal cord vibration, are demonstrated. Overall, this work not only develops a new kind of PU elastomer with hyperbranched structure but also provides candidate materials for flexible sensors and other flexible electronic devices.
Franchising- A way to supersize a business? (2006)

Extract: When you next visit your favourite McDonalds, Hungry Jacks or KFC - please ponder the complex legal and economic structures that lurk behind the colourful clowns and dearly-departed Southern USA gentlemen. Many of these places are franchises. Have you ever wondered why a Big Mac is fundamentally the same whether you purchase it in Parramatta or Cairns or why the stores look the same wherever you go? Perhaps you work for a franchise. It is worthwhile to understand what franchising is because for many of the activities we undertake every day - and I am not only talking about convenience food - we will be provided with goods and services by someone employed by a franchise. But not all the stores you think might be franchises have gone with that model.
Cultivating Microalgae in Desert Conditions: Evaluation of the Effect of Light-Temperature Summer Conditions on the Growth and Metabolism of Nannochloropsis QU130 (2021)

Temperature and light are two of the most crucial factors for microalgae production. Variations in these factors alter their growth kinetics, macromolecular composition and physiological properties, including cell membrane permeability and fluidity. The variations define the adaptation mechanisms adopted by the microalgae to withstand changes in these environmental factors. In the Qatar desert the temperature varies widely, typically between 10° and 45 °C There are also wide variations in light intensity, with values of over 1500 μmolhν.m−2s−1 in summer. A study of the effects of these thermal and light fluctuations is therefore essential for large-scale outdoor production systems, especially during the summer when temperature and light fluctuations are at their highest. The aim of this work is to study the impact of temperature and light intensity variations as encountered in summer period on the Nannochloropsis QU130 strain, which was selected for its suitability for outdoor cultivation in the harsh conditions of the Qatar desert. It was carried out using lab-scale photobioreactors enabling simulation of both constant and dynamic temperature and light regimes. Biomass productivity, cell morphology and biochemical compositions were examined first in constant conditions, then in typical outdoor cultivation conditions to elucidate the adjustments in cell function in respect of fluctuations. The dynamic light and temperature were shown to have interactive effects. The application of temperature cycles under constant light led to a 13.6% increase in biomass productivity, while a 45% decrease was observed under light and temperature regimes due to the combined stress. In all cases, the results proved that N. sp. QU130 has a high level of adaptation to the wide fluctuations in light and temperature stress. This was shown through its ability to easily change its physiology (cell size) and metabolic process in response to different cultivation conditions.
NIMG-82. PREDICTING ISOCITRATE DEHYDROGENASE GENOTYPE IN GLIOMAS USING FET PET RADIOMICS (2017)

BACKGROUND: We investigated the potential of O-(2-[(18)F]fluoroethyl)-L-tyrosine (FET) PET textural features compared with static and dynamic FET PET parameters for preoperative differentiation of IDH-mutated (mut) from IDH-wild type (wt) gliomas. METHODS: Eighty-four glioma patients underwent dynamic FET PET imaging prior to histological confirmation on a stand-alone PET scanner (56 patients; 31 GBM-wt, 3 GBM-mut, 10 AA-wt, 7 AA-mut, 2 AII-mut, 3 ODGII-mut) or a high-resolution hybrid PET/MR scanner (28 patients; 15 GBM-wt, 2 GBM-mut, 1 AA-wt, 7 AA-mut, 1 ODGIII-mut, 1 AII-wt, 1 AII-mut). The IDH genotype was assessed by immunohistochemistry or direct sequencing (if immunohistochemistry was negative). Maximum and mean tumor-to-brain ratios (TBR(max/mean)) of FET uptake were determined and time-activity curves of FET uptake were used to evaluate the dynamic PET parameters time-to-peak (TTP) and slope (slope of linear regression line evaluated 20-50 min post-injection). Additionally, 39 textural parameters were calculated using the software LifeX. The diagnostic accuracy for IDH genotype prediction by FET PET was evaluated using ROC analyses using neuropathological results of IDH analysis as reference. In order to further increase the diagnostic accuracy, parameters were combined using linear logistic regression. Data of each scanner type were analyzed separately. RESULTS: Independent of scanner type, diagnostic accuracies of slope, TBR(mean) and TBR(max) were similar (range, 75-80%). Ten textural features showed an accuracy ranging from 71-79% independent of scanner type. For both PET scanners the combined analysis increased the diagnostic accuracy (84% and 93%, respectively). CONCLUSIONS: The combination of static and dynamic FET PET parameters with radiomics derived from textural feature analysis leads to a high diagnostic accuracy to predict IDH genotype of cerebral gliomas.
Determining the accuracy of gestation feed drops (2008)

Objective: To determine the accuracy of three different types of gestation feed drops. Materials and methods: Econo, Accu, and Ultra feed drops (Automated Production Systems, Assumption, Illinois) were attached to feed lines at three angles (90Ëš, 75Ëš, and 60Ëš). Feed was collected and weighed at settings of 2, 4, 6, 8, and 10 lb (0.9, 1.8, 2.7, 3.6, and 4.65 kg) for the Econo and Accu feed drops and 2, 4, 6, and 8 lb for the Ultra feed drops. Results: There was a drop type Ã— angle Ã— feed level interaction (P < .01) for the feed settings versus the actual amount dropped. At 90Ëš, the relationship between the feeder setting (x) and actual quantity of feed dropped was best described by the regression equation (1.156x + 0.244) for the Econo, (1.010x + 0.072) for the Accu, and (1.009x + 0.231) for the Ultra feed drops. At 75Ëš, the regression equations were (1.014x â€“ 0.139) for the Econo, (0.997x + 0.057) for the Accu, and (1.005x + 0.156) for the Ultra feed drops. At 60Ëš, the regression equations were (0.689x â€“ 0.076) for the Econo, (0.989x â€“ 0.249) for the Accu, and (0.951x + 0.026) for the Ultra feed drops. Implications: The type of feed drop and its angle relative to the feed line influences the amount of feed dispensed at a feeder setting. The Accu and Ultra feed drops more accurately dispense the correct amount of feed than the Econo feed drops.; Journal of Swine Health and Production; 16; Swine Day, 2008, Kansas State University, Manhattan, KS, 2008