gebhart/patrepeval huggingface dataset:
Synthesis and evaluation of hydrogen peroxide sensitive tofacitinib prodrugs (2021)

Tofacitinib (CP-690,550), an approved Janus kinase (JAK) inhibitor, has been proven highly efficacious in treating rheumatoid arthritis (RA). Unfortunately, tofacitinib's clinical application has been limited by adverse side effects that arise from its pan-JAKs inhibition and ubiquitous biodistribution. In this study, we have examined whether a reactive oxygen species (ROS)-activated prodrug design could be applied to tofacitinib to potentially avoid its systemic JAK inhibition and thereby reduce its adverse effects. The prodrug strategy selected is based on ROS-labile 4-methylphenylboronic acid pro-moieties linked to the drugs via a carbamate linkage (prodrug 1) or a direct C–N bond (prodrug 2). Activation under pathophysiological concentrations of H2O2 was investigated and conversion to desired tofacitinib assessed. The most promising prodrug candidate, prodrug 2, was selected in agreement with relevant in vitro physicochemical assay and in silico predicted ADME properties. Selected candidate prodrug 2 showed a remarkable potency window compared to tofacitinib in an in vitro kinase assay against JAK1 and JAK3 kinases. Importantly, prodrug 2 displayed a similar pharmacokinetic profile to tofacitinib after single dose i.p. administration to DBA/1 mice. This study supports the promising applications of ROS-sensitive tofacitinib prodrugs. Their further development and applicability would enhance tofacitinib's therapeutic efficacy, and may provide an opportunity for future development of safer tofacitinib dosing regimens.
Measuring Abuse in Web Push Advertising (2020)

The rapid growth of online advertising has fueled the growth of ad-blocking software, such as new ad-blocking and privacy-oriented browsers or browser extensions. In response, both ad publishers and ad networks are constantly trying to pursue new strategies to keep up their revenues. To this end, ad networks have started to leverage the Web Push technology enabled by modern web browsers. As web push notifications (WPNs) are relatively new, their role in ad delivery has not been yet studied in depth. Furthermore, it is unclear to what extent WPN ads are being abused for malvertising (i.e., to deliver malicious ads). In this paper, we aim to fill this gap. Specifically, we propose a system called PushAdMiner that is dedicated to (1) automatically registering for and collecting a large number of web-based push notifications from publisher websites, (2) finding WPN-based ads among these notifications, and (3) discovering malicious WPN-based ad campaigns. Using PushAdMiner, we collected and analyzed 21,541 WPN messages by visiting thousands of different websites. Among these, our system identified 572 WPN ad campaigns, for a total of 5,143 WPN-based ads that were pushed by a variety of ad networks. Furthermore, we found that 51% of all WPN ads we collected are malicious, and that traditional ad-blockers and malicious URL filters are remarkably ineffective against WPN-based malicious ads, leaving a significant abuse vector unchecked.
Enantioselective Syntheses of Tetrahydroquinolines Based on Iridium‐Catalyzed Allylic Substitutions: Total Syntheses of (+)‐Angustureine and (–)‐Cuspareine (2011)

Abstract A protecting‐group‐free two‐step approach for the preparation of tetrahydroquinolines has been developed. The procedure involves a highly regio‐ and enantioselective intermolecular iridium‐catalyzed allylic amination followed by one‐pot hydroboration and intramolecular Suzuki–Miyaura cross‐coupling. This method was applied in total syntheses of the alkaloids (+)‐angustureine and (–)‐cuspareine.
A Novel Abandoned Object Detection System Based on Three-Dimensional Image Information (2015)

A new idea of an abandoned object detection system for road traffic surveillance systems based on three-dimensional image information is proposed in this paper to prevent traffic accidents. A novel Binocular Information Reconstruction and Recognition (BIRR) algorithm is presented to implement the new idea. As initial detection, suspected abandoned objects are detected by the proposed static foreground region segmentation algorithm based on surveillance video from a monocular camera. After detection of suspected abandoned objects, three-dimensional (3D) information of the suspected abandoned object is reconstructed by the proposed theory about 3D object information reconstruction with images from a binocular camera. To determine whether the detected object is hazardous to normal road traffic, road plane equation and height of suspected-abandoned object are calculated based on the three-dimensional information. Experimental results show that this system implements fast detection of abandoned objects and this abandoned object system can be used for road traffic monitoring and public area surveillance.
A THROMBOGENIC INDEX FOR BLOOD CONTACT MATERIALS (1977)

Roohk, H. V.; Nakamura, M.; Hill, R. L.; Hung, E. K.; Bartlett, R. H. Author Information
Neurotransmitter changes induced by methamphetamine in olfactory bulbectomy model rat of depression, an in vivo microdialysis study (2013)

The aim of this study was to elucidate the neurotransmitter changes in a rat model of depression by measuring levels of dopamine and its metabolites in the nucleus accumbens shell (NACs), which is typically involved in the drug of abuse acquisition mechanisms.
(−)-Englerin A-evoked Cytotoxicity Is Mediated by Na+ Influx and Counteracted by Na+/K+-ATPase (2016)

(-)-Englerin A ((-)-EA) has a rapid and potent cytotoxic effect on several types of cancer cell that is mediated by plasma membrane ion channels containing transient receptor potential canonical 4 (TRPC4) protein. Because these channels are Ca<sup>2+</sup>-permeable, it was initially thought that the cytotoxicity arose as a consequence of Ca<sup>2+</sup> overload. Here we show that this is not the case and that the effect of (-)-EA is mediated by a heteromer of TRPC4 and TRPC1 proteins. Both TRPC4 and TRPC1 were required for (-)-EA cytotoxicity; however, although TRPC4 was necessary for the (-)-EA-evoked Ca<sup>2+</sup> elevation, TRPC1 was not. TRPC1 either had no role or was a negative regulator of Ca<sup>2+</sup> entry. By contrast, both TRPC4 and TRPC1 were necessary for monovalent cation entry evoked by (-)-EA, and (-)-EA-evoked cell death was dependent upon entry of the monovalent cation Na<sup>+</sup> We therefore hypothesized that Na<sup>+</sup>/K<sup>+</sup>-ATPase might act protectively by counteracting the Na<sup>+</sup> load resulting from sustained Na<sup>+</sup> entry. Indeed, inhibition of Na<sup>+</sup>/K<sup>+</sup>-ATPase by ouabain potently and strongly increased (-)-EA-evoked cytotoxicity. The data suggest that (-)-EA achieves cancer cell cytotoxicity by inducing sustained Na<sup>+</sup> entry through heteromeric TRPC1/TRPC4 channels and that the cytotoxic effect of (-)-EA can be potentiated by Na<sup>+</sup>/K<sup>+</sup>-ATPase inhibition.
Experimental verification of accommodation-convergence conflict in viewing integral photography (2018)

We experimentally verified the depth perception and accommodation-convergence conflict in viewing integral photography. For comparison, the same measurements were performed with binocular stereoscopic images and real objects. First, the depth perception in viewing an integral three-dimensional (3D) target was measured at three display resolutions: 153, 229, and 458 ppi. The results showed that the depth perception was dependent on the display resolution. The results were also evaluated in a statistical test at a significance level of 5%. The results showed that the recognized depth perception ranges were 180, 240, and 330 mm when the display resolutions were 153, 229, and 458 ppi, respectively. The results were also analyzed in terms of image resolution. This suggested that depth perception occurred at over 1.0 cpd. The accommodation and convergence responses in viewing an integral 3D target displayed on a 3D display with 458 ppi were measured using PowerRef 3. The experimental results were evaluated with a multiple comparison test. It was found that 6 of the 10 observers did not have an accommodation-convergence conflict when viewing the integral 3D target inside and outside the depth of field. In conclusion, integral photography can provide a natural 3D image that looks like a real object.
Factor from Swamp Water Induces Hatching in Eggs of<i>Anopheles diluvialis</i>(Diptera: Culicidae) Mosquitoes (1999)

Journal Article Factor from Swamp Water Induces Hatching in Eggs of Anopheles diluvialis (Diptera: Culicidae) Mosquitoes Get access Truls Jensen, Truls Jensen 1Illinois Natural History Survey, University of Illinois, Champaign, IL 61820. Search for other works by this author on: Oxford Academic PubMed Google Scholar David A. Carlson, David A. Carlson 2Center for Medical, Agricultural, and Veterinary Entomology, USDA–ARS, Gainesville, FL, 32604. Search for other works by this author on: Oxford Academic PubMed Google Scholar Donald R. Barnard Donald R. Barnard 2Center for Medical, Agricultural, and Veterinary Entomology, USDA–ARS, Gainesville, FL, 32604. Search for other works by this author on: Oxford Academic PubMed Google Scholar Environmental Entomology, Volume 28, Issue 4, 1 August 1999, Pages 545–550, https://doi.org/10.1093/ee/28.4.545 Published: 01 August 1999 Article history Received: 22 July 1998 Accepted: 01 April 1999 Published: 01 August 1999
In Vivo Imaging of Retinal and Choroidal Morphology and Vascular Plexuses of Vertebrates Using Swept-Source Optical Coherence Tomography (2022)

In vivo characterization of retinal morphology and vasculature plexus of multiple species using SS-OCT and SS-OCTA imaging can increase the pool of species available as models of human retinal diseases.
SU-FF-T-67: A TG43 Methodology to Describe Iridium-Wires with Variable Length (2006)

The use of Iridium wire has a long history in the application of radiation therapy. A number of legacy systems still support the planning of this treatment. Newer brachytherapy planning systems currently rely on a methodology based on the recommendations of the AAPM task group no. 43 (TG43). The aim of this task group was to provide a framework for the application of point like (or near point like) brachytherapy sources. However, in clinical practice, the Iridium wires are cut to the needed length necessitating an description of sources with variable length. It is clear that the TG43 methodology implies a fixed source length. In this work we aim to provide an extension of the TG43 framework by allowing the length of a given source to vary. To this end monte carlo simulation (MCNPX2.6.0A) of Iridium sources of lengths between 1 and 14cm were performed. Dose distributions around the source in water and in vacuum (activity determination) were calculated. From this data we derived the activity, the dose rate constant and the radial function. The activity (Air Kerma measured at 1m distance) showed no variation as a function of the source length(L). The dose rate constant followed a relatively simple pattern which could be fit with a function of the form: . The radial dose rate could be fit with a function of the form . The radial function was subsequently obtained by taking the geometrical function into account. The variables A,B, C, and D showed smooth variation as a function of L. Allowing interpolation to predict radial functions of lengths for which no monte carlo simulations were available. We hope to extend this work to include the anisotropy terms in the near future.
Development of a novel hydrogel for skin regeneration (2014)

Skin lesions are traumatic events that lead to increased fluid loss, infections, scars formation and the appearance of immunocompromised regions. The loss of skin integrity can result in significant physiological imbalances and disability or even death. Skin functionality must be restored quickly in order to maintain homeostasis. Researchers have been developing new systems to accelerate the healing process. Although the many skin substitutes available in the market, there is none that promotes full restoration of the native structure of skin. Among the various materials used to cover the wound immediately after injury, hydrogels are the most studied. The hydrogels are made of a highly hydrophilic polymeric network forming a three dimensional structure very similar to the extracellular matrix, that allows cell growth. Moreover, hydrogels are biocompatible, biodegradable and have porous structures that allow cell internalization and proliferation within its structure and promote the diffusion of gases, nutrients and waste products. Currently, new hydrogels that respond to external stimuli such as pH, and temperature have been extensively studied in tissue engineering. Thus, the work plan of this master thesis had as main goal to produce a hydrogel composed of deacetylated chitosan and agarose, formed at body temperature (37°C), in order to verify their applicability in the treatment of wounds. The hydrogel structure was initially characterized by Fourier transform infrared spectroscopy. Its inner and surface morphology was characterized by scanning electron microscopy. Cellular adhesion and internalization into the porous structure of the hydrogel was visualized by confocal and scanning electron microscopy. The cytotoxicity profile of the hydrogel was characterized through cell viability assays, and the results obtained confirmed the biocompatibility of the hydrogel. The antimicrobial activity of the hydrogel was also evaluated and the results showed that the hydrogel inhibits the growth, at the surface, of the most common microorganism in skin infection. The results obtained demonstrated that this 3D network has the suitable properties for improving the healing process of cutaneous wounds.
&lt;title&gt;Multichannel laser vibrometer and its applications&lt;/title&gt; (1998)

A multi-channel laser measurement system based on a commercially available single-channel laser vibrometer has been developed to measure the vibrations of low mass flexible space structures. The first generation of the multi-channel laser vibrometer is bulk-optic based system with laser being switched by an acousto-optical modulator. To overcome some of its drawbacks, for instance, being physically large and cumbersome, requiring tedious alignment, the second generation of the system was developed which employs fiber-optic technique to distribute the laser signal to the desired fiber-optic laser head. The design of the fiber-optic switch minimizes the power loss of laser beam in such a way that the vibrometer can work in its optimal range. Both bulk-optic and fiber-optic multi-channel vibrometers were verified using accelerometers on a light weight communication satellite antenna reflector. The modal parameters of the reflector were identified using measured frequency response functions both from laser vibrometer and from accelerometers. The result show that the laser system gives virtually the same result as the accelerometers.
Learning more about the optimal anatomical position for deep brain stimulation in essential tremor patients: 3d visualisation of intraoperative stimulation test results (2017)

Poster
USP9X stabilizes XIAP to regulate mitotic cell death and chemoresistance in aggressive B‐cell lymphoma (2016)

The mitotic spindle assembly checkpoint (SAC) maintains genome stability and marks an important target for antineoplastic therapies. However, it has remained unclear how cells execute cell fate decisions under conditions of SAC-induced mitotic arrest. Here, we identify USP9X as the mitotic deubiquitinase of the X-linked inhibitor of apoptosis protein (XIAP) and demonstrate that deubiquitylation and stabilization of XIAP by USP9X lead to increased resistance toward mitotic spindle poisons. We find that primary human aggressive B-cell lymphoma samples exhibit high USP9X expression that correlate with XIAP overexpression. We show that high USP9X/XIAP expression is associated with shorter event-free survival in patients treated with spindle poison-containing chemotherapy. Accordingly, aggressive B-cell lymphoma lines with USP9X and associated XIAP overexpression exhibit increased chemoresistance, reversed by specific inhibition of either USP9X or XIAP. Moreover, knockdown of USP9X or XIAP significantly delays lymphoma development and increases sensitivity to spindle poisons in a murine Eμ-Myc lymphoma model. Together, we specify the USP9X-XIAP axis as a regulator of the mitotic cell fate decision and propose that USP9X and XIAP are potential prognostic biomarkers and therapeutic targets in aggressive B-cell lymphoma.
Assessment of heart rate variability in Boxers with arrhythmogenic right ventricular cardiomyopathy (2004)

Results suggest that persistently high sympathetic tone is not a consistent feature of ARVC. Differences in some HRV variables between Boxers without CHF and control dogs suggest that Boxers may have different autonomic control of heart rate, compared with that of clinically normal non-Boxer dogs. The usefulness of HRV analysis appears limited to Boxers with ARVC that have systolic dysfunction and CHF.
Pickering nano-emulsions stabilized by solid lipid nanoparticles as a temperature sensitive drug delivery system (2019)

Correction for 'Pickering nano-emulsions stabilized by solid lipid nanoparticles as a temperature sensitive drug delivery system' by Sidy Mouhamed Dieng et al., Soft Matter, 2019, DOI: 10.1039/c9sm01283d.
Ionizable Lipid Nanoparticle-Mediated Delivery of Plasmid DNA in Cardiomyocytes (2022)

Collectively, our results highlight the potential of LNPs as an efficient delivery vector for pDNA to cardiomyocytes. This study suggests that LNPs hold promise to improve gene therapy for treatment of cardiovascular disease.
Discovery (2010)

This chapter narrates the discovery of dendritic spines. It begins with Santiago Ramón y Cajal, a Spanish professor of Pathology and Histology, and his work entitled Estractura delos centros nerviosos de la aves (Structure of the Nervous Centers in Birds) and how he discovered the spines using the Golgi technique. Cajal defined “spine” on the spines of a rose bush, as it resembled one when he first investigated it in Purkinje cells.
Growth and Survival of Monarch Butterflies (Lepidoptera: Danaidae) After Exposure to Permethrin Barrier Treatments (2006)

We assessed the toxicity of permethrin residues from barrier treatments for mosquito control on monarch buttery (Danaus plexippus L.) larvae and adults. The motivation for this study was an absence of work on the effects of this commonly used insecticide on nontarget herbivorous insects and the fact that monarchs host plant, milkweed (Asclepias spp.), is often found in treated areas. In one experiment, larvae fed leaves from naturally growing milkweeds in operationally treated areas were much less likely to survive than control larvae, even when treated leaves were collected up to 21 d after spraying. In a second experiment, larvae fed leaves from potted milkweeds sprayed with 0.5 and 0.1% dilutions of the operational dose had lower survival and longer development times than control larvae. In a third experiment, ovipositing females did not discriminate against permethrintreated plants. Female survival in 0.66-m 3 cages with plants sprayed 1 d earlier was very low, whereas survival was greater if plants were assayed 8 or 15 d later. In a fourth experiment, neither frequent overhead watering (versus watering from below) nor outdoor sunlight (versus in a glasshouse) over a 14-d period lessened the toxicity of sprayed plants to larvae. These ndings indicate that monarch larvae and adults are likely to be killed if exposed to residues of permethrin after barrier treatments for mosquito control. Extent of mortality in a eld population of monarch butteries will depend, among other things, on the proportion of host plants that are treated in a given area.
Comparison of Magnetic Resonance Angiography and Digital Subtraction Angiography for Visualization of Lower Extremity Arteries (2001)

Objective vascular assessment is frequently required before microvascular reconstruction involving the lower extremities. The purpose of this study was to evaluate the reliability of magnetic resonance angiography (MRA) for preoperative assessment before free flap surgery. Five patients underwent preoperative MRA: one before fibula harvest for oromandibular reconstruction, and four before muscle free flap reconstruction of the lower extremity. In all patients, the tibioperoneal trunk, anterior tibial, posterior tibial, and peroneal arteries were well visualized to the ankle, including pathological occlusions. The radiographic findings were demonstrated at surgery and were confirmed to be accurate. These findings facilitated and guided the surgical procedure. This study strongly suggests the accuracy and surgical relevance of MRA before free flap surgery. MRA is desirable over angiography because of its noninvasive nature. It may also be better than ultrasonography because the latter is highly dependent on the technician (particularly in identifying the peroneal artery). MRA may likely replace angiography as the objective procedure of choice before microvascular surgery.
Two-Dimensional Air Exfiltration and Heat Transfer Through Fiberglass Insulation II. Comparisons between Simulations and Experiments (1997)

The two-dimensional, transient numerical model of heat and water vapor convection and diffusion during air exfiltration within fiberglass insulation, presented in Part I, is validated in Part II, with experimental data for temperature, moisture and frost accumulation, and heat flux. With a few exceptions, the simulation results and experimental data agree within the experimental uncertainty. Exfiltration airflow in the two-dimensional space showed strong entrance and exit effects for temperature, moisture and frost accumulation, and heat flux on the cold side. Between the entrance and exit, the temperature, mass accumulation, and heat flux showed characteristics similar to a boundary layer.
Micro instrumentation for characterizing thermoelectric properties of nanomaterials (2004)

A micro tool for evaluating thermoelectric properties of low-dimensional materials is developed. It is expected that a one-dimensional thermoelectric material exhibits superior thermoelectric properties and low thermal conductivity due to its inherent nanoscale structure. By using these superior properties, high efficient thermoelectric power transformation devices may be realized. In this study, we developed micro instrumentation fabricated by micromachining for the characterization of thermoelectric properties of low-dimensional materials. The device consists of freely suspended heating elements and built-in microthermocouple as a sensing element on the heating elements. A bundle of Bi2Te3 nanowire, which is prepared by a silicon template method, was positioned onto the microdevice by manipulation. Measurements of the electric conductivity, thermal conductivity and Seebeck coefficient of the Bi2Te3 bundle were performed to show the feasibility of this device for measurements of thermoelectric properties of nanomaterials.
<i>Arthrobacter scleromae</i>sp. nov. Isolated from Human Clinical Specimens (2005)

A gram-positive, coryneform bacterium was isolated from swollen scleromata of a dermatosis patient. An analysis of its phenotypic, chemotaxonomic, and genotypic characteristics showed that this bacterium is closely associated with Arthrobacter oxydans and Arthrobacter polychromogenes but that it belongs to a distinct species, for which the name Arthrobacter scleromae sp. nov. is proposed.
Endogenous Estrogens, Estrogen Metabolites, and Breast Cancer Risk in Postmenopausal Chinese Women (2016)

Lower urinary parent estrogen concentrations and more extensive 2-hydroxylation were each associated with reduced postmenopausal breast cancer risk in a low-risk nation. Markedly higher total estrogen/estrogen metabolite concentrations in postmenopausal United States women (Asian Americans) than in Shanghai women may partly explain higher breast cancer rates in the United States.