gebhart/patrepeval huggingface dataset:
[18F]Fluorophenylazocarboxylates: Design and Synthesis of Potential Radioligands for Dopamine D3 and μ-Opioid Receptor (2017)

<sup>18</sup>F-Labeled building blocks from the type of [<sup>18</sup>F]fluorophenylazocarboxylic-<i>tert</i>-butyl esters offer a rapid, mild, and reliable method for the <sup>18</sup>F-fluoroarylation of biomolecules. Two series of azocarboxamides were synthesized as potential radioligands for dopamine D3 and the μ-opioid receptor, revealing compounds <b>3d</b> and <b>3e</b> with single-digit and sub-nanomolar affinity for the D3 receptor and compound <b>4c</b> with only micromolar affinity for the μ-opioid receptor, but enhanced selectivity for the μ-subtype in comparison to the lead compound AH-7921. A "minimalist procedure" without the use of a cryptand and base for the preparation of 4-[<sup>18</sup>F]fluorophenylazocarboxylic-<i>tert</i>-butyl ester <b>[</b><sup><b>18</b></sup><b>F]2a</b> was established, together with the radiosynthesis of methyl-, methoxy-, and phenyl-substituted derivatives (<b>[</b><sup><b>18</b></sup><b>F]2b-f</b>). With the substituted [<sup>18</sup>F]fluorophenylazocarbylates in hand, two prototype azocarboxylates radioligands were synthesized by <sup>18</sup>F-fluoroarylation, namely the methoxy azocarboxamide <b>[</b><sup><b>18</b></sup><b>F]3d</b> as the D3 receptor radioligand and <b>[</b><sup><b>18</b></sup><b>F]4a</b> as a prototype structure of the μ-opioid receptor radioligand. By introducing the new series of [<sup>18</sup>F]fluorophenylazocarboxylic-<i>tert</i>-butyl esters, the method of <sup>18</sup>F-fluoroarylation was significantly expanded, thereby demonstrating the versatility of <sup>18</sup>F-labeled phenylazocarboxylates for the design of potential radiotracers for positron emission tomography .
Heatsink-less Quasi 3-level flying capacitor inverter based on low voltage SMD MOSFETs (2017)

Outstanding efficiencies can be achieved by the utilization of the latest technology of low voltage, SMD-packaged Si- or GaN-based semiconductors. These devices allow a heatsink- and fan-less converter design, thus lightweight and high power density converters are typically derived. This paper investigates the advantages of using these relatively low cost SMD-packaged devices in medium power industrial applications. A Quasi 3-level Flying-Capacitor topology is proposed. A cost-performing map is presented in order to verify the benefits of designing this system with low voltage Si- or GaN-based MOSFETs against the latest 650 V IGBTs and 900 V SiC MOSFETs. Finally, a heatsink-less 3.3 kW single-phase inverter prototype implementing 150 V SMD-packaged Si MOSFETs was designed and successfully tested.
Scalable compression of multibeam echo sounder data (2017)

We propose a scalable lossy-compression method to enable acoustic data transmission through a narrow band channel (e.g. from an AUV), while still allowing for sufficiently good reconstruction on the receive station, which is adequate for other processing applications. Scalable coders are well-known in regular image compression, but they have not been applied yet to sonar backscatter data from multi-beam echo sounders (MBES). We achieve so by converting the backscatter samples acquired during a survey into one waterfall-image, which is an optimized representation of the MBES backscatter data. Each line of the image is assembled based on an auxiliary ping time-series obtained by consolidating the individual beam time-series into a single signal, spanning the space of all the responses of the multiple overlapping beams. Then, the ping time series are stacked, forming a monochrome image aligned by the center of the navigation, without any geodesic referencing. The assembled waterfall-image is then compressed using standard image compression algorithms. The distortion metric we use to evaluate quality is the mean absolute error (MAE) of samples among original and reconstructed ping time series as well as the MAE among the original multi-beam time series. However, the most important distortion metric in our opinion is the comparison of compositions of a mosaic image of the sea bottom surface among compressed and uncompressed data. Results indicate compression ratios of up to 200:1 at a lower but useful quality, while smaller ratios may yield mosaic images from compressed data that are virtually indistinguishable from the original. Thus, we have a scalable compression method that allows for a large range of compression ratios. From the highly compact preview version that an AUV could send to the surface to the accurate data that can be near-losslessly stored for future studies. The proposed algorithm is efficient and we are unaware of any similar work in the literature.
Instant Surface Reconstruction for Incremental SfM (2013)

We propose an instant reconstruction of 3D surface meshes for a set of images and their camera poses and sparse 3D points computed by structure from motion (SfM). We aim at the proposed method to be compati-ble with an incremental structure from motion system as it can immediately generate the 3D surface model seen from the latest view point recovered by SfM. The proposed method consists of four steps: reference and target image selection adaptive to so-far recovered sur-face models; triangular patch initialization by taking into account the scene structures; fast 3D pose estima-tion of each triangular patch using inverse composi-tional image alignment (ICIA); surface generation by robustly refining the 3D triangular patches and inte-grating into pieces of surface meshes. The surface re-construction results are shown on real image datasets of indoor as well as outdoor scenes and compared with the state of the art approach. 1
Investigation of Performance and Flow Field of a Centrifugal Compressor Under Negative Pre-Swirl (2015)

In the paper the effect of negative pre-swirl on the performance and the flow in a centrifugal compressor stage are investigated by both the experimental and numerical methods. The results show that, at a negative pre-swirl, whether the pressure ratio of compressor is increased or not is determined by the contest between the increased energy transfer and flow losses. At a large negative pre-swirl, the flow losses in the IGV and the impeller are increased obviously, which makes the pressure ratio and efficiency reduced dramatically. The further flow analysis show that, the enhanced separation area in the IGV and the depravation of the inlet flow condition of the impeller are the main sources of the losses, while there is almost no influence of the pre-swirl on the diffuser losses. Additionally, at a large negative pre-swirl there exist vortexes shedding from the separation region at impeller leading edge, which causes severe excited force on the impeller leading edge.
Metal Complexes of Azacrownethers in Molecular Recognition and Catalysis (review) (2002)

Reversible coordination of ligands or substrates with Lewis-basic groups to Lewis-acidic metal ion binding sites can provide the binding enthalpy and selectivity necessary for molecular recognition or catalysis. Metal complexes of functionalised azamacrocycles have proven to be particularly useful for this purpose. This review summarises the properties and applications of some recently published compounds of this kind, giving typical examples, but no comprehensive coverage of the field. With focus on molecular recognition, the binding of inorganic and organic anions to metal complex binding sites, changes of anion properties induced by the binding and the interaction of metal complexes with the polyanion DNA are discussed. The second part of the review focuses on catalysis mediated by azamacrocyclic Lewis-acidic metal binding sites leading to ester hydrolysis, redox catalysis or polymerisation.
Castor: Contextual IoT Time Series Data and Model Management at Scale (2018)

We demonstrate Castor, a cloud-based system for contextual IoT time series data and model management at scale. Castor is designed to assist Data Scientists in (a) exploring and retrieving all relevant time series and contextual information that is required for their predictive modelling tasks; (b) seamlessly storing and deploying their predictive models in a cloud production environment; (c) monitoring the performance of all predictive models in production and (semi-)automatically retraining them in case of performance deterioration. The main features of Castor are: (1) an efficient pipeline for ingesting IoT time series data in real time; (2) a scalable, hybrid data management service for both time series and contextual data; (3) a versatile semantic model for contextual information which can be easily adopted to different application domains; (4) an abstract framework for developing and storing predictive models in R or Python; (5) deployment services which automatically train and/or score predictive models upon user-defined conditions. We demonstrate Castor for a real-world Smart Grid use case and discuss how it can be adopted to other application domains such as Smart Buildings, Telecommunication, Retail or Manufacturing.
Day-Long Integrated Serum Insulin and C-Peptide Profiles in Patients With NIDDM: Correlation With Urinary C-Peptide Excretion (1988)

To determine whether non-insulin-dependent diabetes mellitus (NIDDM) is characterized by day-long hypoinsulinemia, we measured 24-h serum profiles for glucose, insulin, and C-peptide by use of a constant-rate blood-withdrawal technique in diabetic and control subjects fed isocaloric meals. When only lean subjects were considered, diabetic subjects (relative body weight 0.99 +/- 0.3) and control subjects (relative body weight 0.95 +/- 0.03) had similar 24-h integrated serum insulin concentrations (13.4 +/- 2.5 vs. 16.1 +/- 2.0 microU/ml, P NS) due to the offsetting effects of increased basal levels and decreased postprandial responses in NIDDM. In contrast, both basal and meal-stimulated insulin levels were decreased in obese NIDDM subjects (relative body weight 1.39 +/- 0.07) compared with obese control subjects (relative body weight 1.60 +/- 0.08), resulting in a 61% reduction in the 24-h integrated insulin value (18.7 +/- 1.5 vs. 48.4 +/- 13.7 microU/ml). Thus, the capacity to increase 24-h integrated serum insulin as a function of relative body weight was impaired in NIDDM subjects (r = 0.27, P NS) compared with control subjects (r = .70, P less than .01). In contrast, 24-h integrated C-peptide was decreased (P less than .01) in both lean (0.92 +/- 0.13 pM/ml) and obese (1.52 +/- 0.19 pM/ml) NIDDM patients compared with the respective control groups (1.50 +/- 0.13 and 3.03 +/- 0.44 pM/ml). The molar ratio of 24-h integrated C-peptide to insulin was diminished in lean but not obese NIDDM compared with control subjects. A 3-wk period of intensive insulin therapy led to normalization of the mean 24-h integrated insulin (but not integrated serum C-peptide) value in NIDDM compared with a control group that had an identical mean relative body weight. The 24-h urinary C-peptide measured on the same day as the serum profile was correlated (P less than .01) with both the 24-h integrated serum insulin (r = .69) and C-peptide (r = .67) concentrations in control subjects but not in NIDDM subjects (r = .20 and .04, respectively, P NS). Additionally, the urinary clearance of C-peptide was increased in NIDDM (38.1 +/- 7.8 vs. 20.4 +/- 1.7 ml/min in control subjects, P less than .05) and varied with treatment status (26.0 +/- 4.6 ml/min after insulin therapy).(ABSTRACT TRUNCATED AT 400 WORDS)
Decision of Robot's Movement by Means of Potential Field (1983)

In this paper a method of deciding robot's movement by means of potential field is proposed and simple simulations using it are shown. Especially two concepts, “State space for robots” and “Oval potential”, are unique.A robot which utilizes the proposed method has a potential field as what keeps informations about its surrounding situation. The field is formed in a space that represents the robot's state (state space) . And the robot's state that is a point in the space moves according to the potential distribution.The principal characteristics of this method are following.•As a robot's state is represented by a point, the decision of movement can be made simply.•And the oval potential is used for potential distribution, the robot's state moves successfully, the object is memorized by a little information and the calculation for the potential is easy.
A targeted immunotherapy approach for HER2/neu transformed tumors by coupling an engineered effector domain with interferon-γ (2017)

Despite substantial clinical progress with targeted therapies, current antibody-based approaches have limited efficacy at controlling HER2/neu-positive breast cancers, especially in the absence of chemotherapies. Previously, we showed that the combination of IFNγ and anti-HER2/neu antibody synergistically reduces tumor growth in an <i>in vivo</i> implanted mammary tumor model. Here, we report a recombinant approach to produce an anti-HER2/neu scFv and IFNγ fusion protein using an engineered effector domain (EED) scaffold. The new molecule induces <i>in vitro</i> apoptosis in an IFNγ receptor-dependent manner. At a very low dose in the <i>in vivo</i> xenografted tumor models, the new EED-IFNγ fusion protein demonstrates superior activity over the anti-HER2/neu antibody and is even active on tumors that are resistant to anti-HER2/neu antibody therapy. Examination of tumor infiltrated macrophages and lymphocytes reveals that the fusion protein can induce changes in tumor microenvironment to support immune reactivity against tumors. Our studies have defined a targeted immunotherapy approach for the treatment of cancers.
COVID-ARDS: A Vascular Endotype (2020)

COVID-19, the pandemic caused by the SARS-CoV-2 coronavirus can progress to pneumonia and Acute Respiratory Distress Syndrome (ARDS), resulting in an extraordinary level of ICU utilization and considerable mortality. Several pathophysiological features of COVID-19 associated ARDS are strikingly atypical, leading to the hypothesis that COVID-19 related ARDS represents a unique endotype of ARDS (1). With the caveat that studies are ongoing, and observations are preliminary, there appear to be striking differences in the pulmonary physiology of COVID-19 patients compared to the features of ARDS precipitated by other respiratory pathogens and viruses (e.g. influenza). These observations suggest that dysfunction of the pulmonary vasculature contributes to the pathogenesis of COVID-19-induced ARDS. We will highlight observations that implicate the lung microvasculature as a critical mediator of COVID-ARDS.
Drug-Loaded Polymeric Spherical Nucleic Acids: Enhancing Colloidal Stability and Cellular Uptake of Polymeric Nanoparticles through DNA Surface-Functionalization (2016)

Small-sized (∼65 nm) doxorubicin (Dox)-loaded polymeric nanoparticles (PNPs) were modified with oligonucleotides to form colloidally stable Dox-loaded polymeric spherical nucleic acid (Dox-PSNA) nanostructures in biological media. The nucleic acid shell facilitates the cellular uptake of Dox-PSNA, which results in in vitro cytotoxicity against SKOV3 cancer cells.
Low-energy physics in neutrino LArTPCs (2023)

Abstract In this paper, we review scientific opportunities and challenges related to detection and reconstruction of low-energy (less than 100 MeV) signatures in liquid argon time-projection chamber (LArTPC) neutrino detectors. LArTPC neutrino detectors designed for performing precise long-baseline oscillation measurements with GeV-scale accelerator neutrino beams also have unique sensitivity to a range of physics and astrophysics signatures via detection of event features at and below the few tens of MeV range. In addition, low-energy signatures are an integral part of GeV-scale accelerator neutrino interaction final-states, and their reconstruction can enhance the oscillation physics sensitivities of LArTPC experiments. New physics signals from accelerator and natural sources also generate diverse signatures in the low-energy range, and reconstruction of these signatures can increase the breadth of Beyond the Standard Model scenarios accessible in LArTPC-based searches. A variety of experimental and theory-related challenges remain to realizing this full range of potential benefits. Neutrino interaction cross-sections and other nuclear physics processes in argon relevant to sub-hundred-MeV LArTPC signatures are poorly understood, and improved theory and experimental measurements are needed; pion decay-at-rest sources and charged particle and neutron test beams are ideal facilities for improving this understanding. There are specific calibration needs in the low-energy range, as well as specific needs for control and understanding of radiological and cosmogenic backgrounds. Low-energy signatures, whether steady-state or part of a supernova burst or larger GeV-scale event topology, have specific triggering, DAQ and reconstruction requirements that must be addressed outside the scope of conventional GeV-scale data collection and analysis pathways. Novel concepts for future LArTPC technology that enhance low-energy capabilities should also be explored to help address these challenges.
GDNF promotes tubulogenesis of GFRα1-expressing MDCK cells by Src-mediated phosphorylation of Met receptor tyrosine kinase (2003)

Glial cell line-derived neurotrophic factor (GDNF) and hepatocyte growth factor (HGF) are multifunctional signaling molecules in embryogenesis. HGF binds to and activates Met receptor tyrosine kinase. The signaling receptor complex for GDNF typically includes both GDNF family receptor alpha1 (GFRalpha1) and Ret receptor tyrosine kinase. GDNF can also signal independently of Ret via GFRalpha1, although the mechanism has remained unclear. We now show that GDNF partially restores ureteric branching morphogenesis in ret-deficient mice with severe renal hypodysplasia. The mechanism of Ret-independent effect of GDNF was therefore studied by the MDCK cell model. In MDCK cells expressing GFRalpha1 but no Ret, GDNF stimulates branching but not chemotactic migration, whereas both branching and chemotaxis are promoted by GDNF in the cells coexpressing Ret and GFRalpha1, mimicking HGF/Met responses in wild-type MDCK cells. Indeed, GDNF induces Met phosphorylation in several ret-deficient/GFRalpha1-positive and GFRalpha1/Ret-coexpressing cell lines. However, GDNF does not immunoprecipite Met, making a direct interaction between GDNF and Met highly improbable. Met activation is mediated by Src family kinases. The GDNF-induced branching of MDCK cells requires Src activation, whereas the HGF-induced branching does not. Our data show a mechanism for the GDNF-induced branching morphogenesis in non-Ret signaling.
MALIGNANT FIBULA PATHOLOGY: 17 YEARS REVIEW (2003)

We discuss the management and outcome of 52 patients who presented with malignant tumours of the fibula over a 15-year period between1983 and 1998. The tumour type was Osteosarcoma (23 patients), Ewing’s sarcoma (16), Chondrosarcoma (11 – of which 10 low grade) and Malignant Fibrous Histiocytoma (2). We concentrate on the two most common frankly malignant groups: Osteosarcoma and Ewing’s. The male:female ratio of patients with Osteosarcoma was 11:12 and with Ewing’s Sarcoma was 11:5. Mean age for Osteosarcoma was 21. 5 years and for Ewing’s Sarcoma was 14. 2. The most common site of tumour was in the proximal fibula in both Osteosarcoma (19 / 23) and Ewing’s Sarcoma (10 / 16). The stage of disease at presentation was IIa or IIb in the majority of patients, with seven patients presenting with metastases. The current investigative procedures are Radiographs, Magnetic Resonance Imaging, Radioisotope Bone Scans, Computerised Tomography of the chest and needle biopsy whereas in the past CT of the lesion and open biopsy were common. Chemotherapy was administered as per protocol at the time of diagnosis and radiotherapy was given in selected cases. Surgery was performed on all but 3 patients, who were unfit and died. This consisted of local en bloc resection in 86. 3% and above knee amputation in 6. 8%. Whereas all the diaphyseal and distal lesions were completely excised, 9 out of 26 proximal lesions had a marginal excision, 4 of which had open biopsies. The common peroneal nerve was sacrificed in 50% of cases and this had no link to survival. The overall 5-year survival was 33% for Osteosarcoma and 40% for Ewing’s Sarcoma, with proximal lesions doing much worse than diaphyseal and distal lesions. Patients who had marginal excisions all died within 2. 5 years.
Large-scale Additive Manufacturing of Highly Exothermic Reactive Polymer Systems (2019)

Additive manufacturing (AM) of reactive polymer systems involves the deposition of materials at room temperature that either cure during printing through a chemically initiated reaction or require thermal initiation after printing. This presentation focuses on large-scale AM of chemically initiated thermosetting resins to characterize the effects of heat generation, temperature-dependent viscoelasticity, and crosslinking on the printing process. Real-time tracking of both temperature and cure fronts during the build process were investigated using infrared (IR) and optical vision systems in combination with selected material dyes. Heat generation within the previously-deposited layers was observed to cause significant reduction in the storage modulus (G’) and viscosity of newly-deposited layers, resulting in bead instabilities and failure of the print. Quantitative experimental observations on thin-wall structures suggest strategies for mitigating this failure mode through selection of print parameters and tailoring of viscoelastic properties of the feedstock resin.
A randomized phase II trial of sipuleucel-T with concurrent or sequential abiraterone acetate (AA) plus prednisone (P) in metastatic castrate-resistant prostate cancer (mCRPC). (2013)

5047^ Background: Sipuleucel-T and AA + P are FDA-approved for asymptomatic/minimally symptomatic mCRPC. Suppression of the androgen axis can be immunostimulatory and AA suppresses circulating androgen levels; AA plus sipuleucel-T may therefore be synergistic. However P used with AA, which may be immunosuppressive, has not been studied with concurrent sipuleucelET and could impair sipuleucel-T production and/or immunologic response. P11-3 (NCT01487863) is the 1 st study to evaluate the combination of sipuleucel-T and AA + P Methods: Patients (pts) with asymptomatic/minimally symptomatic mCRPC were randomized (1:1) to sipuleucel-T (3 infusions at approx 2-wk intervals) with up to 26 wks of AA + P (AA 1000mg QD + P 5mg BID) starting 1 day after the 1 st sipuleucel-T infusion (concurrent, arm A) or at 10 wks following the 1 st sipuleucel-T infusion (sequential, arm B). Endpoints included the effect of AA + P on product (sipuleucel-T) characteristics eg antigen presenting cell (APC) activation, measured as CD54 upregulation (primary endpoint), APC (measured as CD54 + cells) and total nucleated cell (TNC) counts, as well as safety and immunologic responses. Results: 31 pts in arm A and 32 pts in arm B completed sipuleucel-T treatment by the interim analysis (Nov 2012). Baseline characteristics were similar in the 2 arms. 60/63 pts received all 3 infusions of sipuleucel-T. No significant differences in median cumulative APC activation, APC count or TNC count were seen between the arms. Increased CD54 upregulation with the 2 nd and 3 rd treatments were indicative of a prime boost effect in both arms. Similar profiles of antigen-specific humoral and cellular immune responses were generated with no difference in magnitude of response between the arms (p&gt;0.05). The incidence of adverse events (AEs) and serious AEs was similar in both arms. Conclusions: These data suggest sipuleucel-T can be successfully manufactured during concurrent AA + P. Product potency and prime boost effect were similar to sipuleucel-T alone. Immune responses and AEs were similar in both arms. It is not known if sipuleucel-T will provide similar efficacy with concurrent or sequential AA + P. Clinical trial information: NCT01487863.