gebhart/patrepeval huggingface dataset:
Novel S1P<sub>1</sub> Receptor Agonists − Part 3: From Thiophenes to Pyridines (2013)

In preceding communications we summarized our medicinal chemistry efforts leading to the identification of potent, selective, and orally active S1P1 agonists such as the thiophene derivative 1. As a continuation of these efforts, we replaced the thiophene in 1 by a 2-, 3-, or 4-pyridine and obtained less lipophilic, potent, and selective S1P1 agonists (e.g., 2) efficiently reducing blood lymphocyte count in the rat. Structural features influencing the compounds’ receptor affinity profile and pharmacokinetics are discussed. In addition, the ability to penetrate brain tissue has been studied for several compounds. As a typical example for these pyridine based S1P1 agonists, compound 53 showed EC50 values of 0.6 and 352 nM for the S1P1 and S1P3 receptor, respectively, displayed favorable PK properties, and penetrated well into brain tissue. In the rat, compound 53 maximally reduced the blood lymphocyte count for at least 24 h after oral dosing of 3 mg/kg.
SlC30A8 Is a Major Target of Humoral Autoimmunity in Type 1 Diabetes and a Predictive Marker in Prediabetes (2008)

Type 1A diabetes (T1D) results from autoimmunity targeted at a limited number of molecules that are expressed in the pancreatic beta cell. Putative novel autoantigen candidates were identified from microarray expression profiling of human and rodent islet cells. The highest ranking candidate was Slc30A8 (zinc transporter 8; ZnT8), which was screened by radioimmunoprecipitation assays against new-onset T1D and prediabetic sera. Such assays detected 63% of subjects with new-onset diabetes, but fewer than 2% of controls, 3% of those with type 2 diabetes, and 10% of patients with other autoimmune disorders. ZnT8 autoantibodies were found, however, in 26% of T1D subjects previously classified as autoantibody-negative on the basis of existing markers (GADA, IA2 A, IAA, and ICA). We conclude that SLC30A8 provides an important additional and independent predictive marker for T1D.
Dopant concentration imaging in crystalline silicon wafers by band-to-band photoluminescence (2011)

In this work, we present two techniques for spatially resolved determination of the dopant density in silicon wafers. The first technique is based on measuring the formation rate of iron-acceptor pairs, which is monitored by band-to-band photoluminescence in low injection. This method provides absolute boron concentration images on p-type wafers, even if compensating dopants such as phosphorus are present, without reference to other techniques. The second technique is based on photoluminescence images of unpassivated wafers, where the excess carrier concentration is pinned by a high surface recombination rate. This rapid technique is applicable to either p- or n-type wafers, when the bulk carrier lifetime is much longer than the transit time to the surface. The relative sensitivities and advantages of the two techniques are discussed.
White Light Diffraction Phase Microscopy (wDPM) for quantitative phase imaging (2012)

We present white-light diffraction phase microscopy (wDPM) as a fast and sensitive quantitative phase imaging method and a successive derivatives based phase reconstruction method. We illustrate the utility of wDPM with measurements on live cells.
ChemInform Abstract: Development of a New Synthesis of 3‐(1H‐Tetrazol‐5‐yl)‐4(3H)‐quinazolinone, Sodium Salt via an Amidine Intermediate. (1989)

Abstract A new high‐yield one‐pot process is reported for the title compound (VI) via the amidine intermediate (IV).
Human Norovirus Neutralized by a Monoclonal Antibody Targeting the Histo-Blood Group Antigen Pocket (2018)

The emergence of new epidemic GII.4 norovirus variants is thought to be associated with changes in antigenicity and HBGA binding capacity. Here, we show that HBGA binding profiles remain unchanged between the 1974 and 2012 GII.4 variants, whereas these variants showed various levels of reactivity against a panel of GII.4 MAbs. We identified a MAb that bound at the HBGA pocket, blocked norovirus VLPs from binding to HBGAs, and neutralized norovirus virions in the cell culture system. Raised against a GII.4 2006 strain, this MAb was unreactive to a GII.4 1974 isolate but was able to neutralize the newer 2012 strain, which has important implications for vaccine design. Altogether, these new findings suggest that the amino acid variations surrounding the HBGA pocket lead to temporal changes in antigenicity without affecting the ability of GII.4 variants to bind HBGAs, which are known cofactors for infection.
The Galileo Integrity Concept (2004)

The Galileo system as specified is the most demanding Global Navigation Satellite System in terms of performance requirements on integrity, continuity, and availability. It has been shown by simulations that the performance of classical SBAS integrity concepts could not be sufficient due to Galileo’s required unavailability of integrity of 0.5% (cf. typical systems: 5% unavailability). Therefore, a new concept has been developed based on the classical approaches but with exploiting unused margins. The present paper outlines this Galileo high quality integrity concept and its impact on the overall System Design. After outlining the high-level architectural basics and system performance requirements the system alert mechanism and user integrity risk equations including the necessary assumptions to cope with the demanding Galileo performance requirements are presented. This user integrity concept for the decision to start a critical operation has an impact on the system allocations and the corresponding integrity and continuity allocation trees are presented. According to the presented concept the user integrity algorithm has to provide various functionalities which are outlined after the presentation of the overall concept. Finally the necessary key performance requirements to cope with the Galileo integrity, continuity, and availability specifications are presented, which have been derived by detailed service volume simulations.
Tracking both magnitude and direction of 2-D transverse motion with optical coherence tomography (2014)

We have developed and demonstrated a 2-D transverse motion tracking method that provides quantitative assessment of both direction and magnitude of motion using optical coherence tomography (OCT). This motion tracking method involves scanning the OCT beam circularly and processing the obtained three-dimensional data with novel algorithms.
Emphasizing the role of <scp>Wnt5a</scp> protein expression to predict favorable outcome after radical prostatectomy in patients with low‐grade prostate cancer (2012)

Abstract Wnt5a , a member of non‐canonical wingless‐related MMTV integration site family is a secreted glycoprotein that plays important roles in development and disease. Recent studies have shown that Wnt5a protein levels are up‐regulated in prostate cancer, but contrasting reports exist on the role of Wnt5a to predict outcome after radical prostatectomy in patients with localized prostate cancer. Our group has recently shown that preserved high protein expression of Wnt5a in prostate cancer is associated with longer relapse‐free time after radical prostatectomy. The present tissue microarray study emphasizes the role of Wnt5a protein expression in a different, well‐defined, and independent cohort consisting of 312 prostate cancer patients. Kaplan–Meier curves plotted between Wnt5a expression and time to biochemical recurrence revealed that in low‐grade prostate cancer, patients with preserved high‐ Wnt5a protein levels in their tumor cells have a lower risk of recurrence after radical prostatectomy compared to patients with low‐ Wnt5a protein expression. When Wnt5a protein expression was added to a Cox regression multivariate analysis, both Wnt5a protein expression and surgical margin status independently predict biochemical free survival. Herein we confirm Wnt5a positivity as a prognostic factor and show that preserved overexpression of Wnt5a protein is associated with increased time to biochemical recurrence in localized low‐grade prostate cancer patients after radical prostatectomy. Our results emphasize that Wnt5a can be used as a predictive biomarker, and favoring the view of Wnt5a as a future therapeutic target in prostate cancer patients with tumor cells displaying low expression of Wnt5a .
Bayesian Estimation and Control of Engine Knocking Level for Transient Operation (2021)

The contribution of this article is to propose a knock controller based on the estimation of the distribution quantile of the knock intensity measurements. Despite the quantile estimation randomness, the corrections undertaken by the controller are moderated by the level of confidence in the quantile estimation. This strategy offers a fast control ensuring a better compromise between the engine efficiency and the prevention of knock phenomenon. The design of the controller reduces the engine torque fluctuations and is suited for engine transient operations.
Global Offset Compensation for CNC Machine Tools Based on Workpiece Errors (2016)

Machine tool accuracy and repeatability is one of the most important considerations for manufacturing parts with the required quality for consistent performance in their assemblies. One of the most challenging areas has been the ability to quickly identify and evaluate the quasi-static and dynamic machine errors and apply the corresponding error models to compensate. Because there are many challenges associated with some methods, including the cost in design, analysis and control of precision machine tools, the compensation method has been the most effective approach to control part quality. This paper presents the development of a Global Offset compensation method utilizing the measurements of machined part(s). The Global Offset for a machine tool is estimated through a model while utilizing the computed deviation between the measured and nominal dimensions of the part. Examples are provided to demonstrate the capabilities of this new method.
Fire‐ and heat‐resistant adhesive resins based on maleimido and citraconimido substituted 1‐[(dialkoxyphosphinyl)methyl]‐2,4‐ and ‐2,6‐diaminobenzenes (1984)

Abstract A novel class of fire‐ and heat‐resistant bisimide resins was prepared by thermal polymerization of maleimido or citraconimido derivatives of 1‐[(dialkoxyphosphinyl)methyl]‐2,4‐ and ‐2,6‐diaminobenzenes (1). The neat bisimide resin prepared by curing 1‐[di(2‐chloroethoxyphosphinyl)methyl]‐2,4‐ and ‐2,6‐bismaleimidobenzene exhibited a limiting oxygen index 75% higher and smoke evolution about 30 times lower compared with the parent polymer obtained by curing m ‐phenylenebismaleimide. The char yield of cured bisimide resins at 700°C was 58–70% in a nitrogen atmosphere and 35–60% in air. An increase in formula weight between the imide groups slightly reduced the char yield. The polymer precursors were synthesized by reacting the phosphorus‐containing diamines (1) (1 mol) with maleic anhydride/citraconic anhydride (2 mol) or by reacting the monomaleimido derivative of (1) with benzophenone tetracarboxylic dianhydride/methylenebis(4‐phenylisocyanate) in a 2:1 mole ratio. The monomers were characterized by elemental analysis, Fourier‐transform–infrared (FT‐IR), proton nuclear magnetic resonance ( 1 H‐NMR) spectroscopy, and gas chromatography–mass spectroscopy (GC‐MS). Direct cleavage of the PC bond and inversion of the synthesis reaction may occur during their pyrolysis. The thermal polymerization of the monomers was investigated by differential scanning calorimetry (DSC). Biscitraconimides are thermally polymerized at a relatively lower temperature than the corresponding bismaleimides.
Effects of RF amplifier distortion on selective excitation and their correction by prewarping (1992)

In a magnetic resonance imaging system, an RF power amplifier is employed to boost an RF pulse to sufficient strength to excite the nuclear spins in a subject. The nonideal behavior of this amplifier distorts a selective-excitation pulse, and this distortion in turn degrades the slice profile. We have found two types of nonideal behavior particularly troublesome: nonlinearity and incidental phase modulation. One of their effects is the introduction of an unwanted "skirt" in the out-of-slice region of a slice profile. We present an effective method of correction in which a selective-excitation pulse is prewarped to compensate for the distortion.
Camera-Radar Fusion for 3-D Depth Reconstruction (2020)

We introduce and study the problem of camera-radar fusion for 3-D depth reconstruction. This problem is motivated by autonomous driving applications, in which we can expect to have access to both front-facing camera and radar sensors. These two sensors are complementary in several respects: the camera is a passive sensor measuring azimuth and elevation; the radar is an active sensor measuring azimuth and range. Fusing their measurements is therefore beneficial. Our fusion solution uses a modified encoder-decoder deep convolutional neural network. We train and evaluate this network on over 100 000 samples collected in highway environments. Our results demonstrate an improvement in reconstruction accuracy and robustness from fusing the two sensors.
Rapid and Quantitative Detection of Enzymatically Amplified HIV-1 DNA Using Chemiluminescent Oligonucleotide Probes (1990)

A hybridization protection assay (HPA) that uses acridinium ester (AE) labeled oligonucleotide probes which are specific for a conserved gag gene region of human immunodeficiency virus type 1 (HIV-1) was developed to measure the amount of HIV-1 nucleic acid. Hybridization of the single-stranded probes with their target HIV-1 sequences protected the chemiluminescent AE group from subsequent alkaline hydrolysis. The chemiluminescence from the residual AE could be easily quantitated in a luminometer. The entire process comprising template dissociation, hybridization, alkaline hydrolysis, and chemiluminescence measurement can be completed in less than one hour and does not require the separation of hybridized probe from unhybridized probe. We demonstrated that HPA could quantitatively measure the amount of DNA amplified by polymerase chain reaction. A comparative study using amplified DNA from the peripheral blood mononuclear cells (PBMC) of HIV seropositive and seronegative persons showed that HPA was as sensitive as the previous methods using 32P-labeled DNA probes.
The Study on the Ceramic Membrane Wastewater Reuse System with Pre-Ozonation and Coagulation (2013)

Abstract A new wastewater reuse system using ozonation, coagulation and MF ceramic membrane (0.1 μm) filtration was developed. The testing was performed using secondary effluent treated at the wastewater treatment plant (WWTP) in Tokyo, Japan. The volume of treated water by the pilot study equipment is about 90 m3/day. The combination of pre-ozonation and coagulation processes achieves continuous stable membrane filtration with flux of 4m3/m2/day (167 LMH). A stable membrane filtration could be maintained by controlling ozone dosing rate depending on secondary effluent (raw water) quality fluctuation. The COD (Mn) removal ratio in raw water was 50 to 60%, and the color removal ratio satisfied 80% or higher. The quality of the treated water that was obtained from our pilot study was better than the California's standards. Keywords: OzoneCoagulationCeramic MembraneWastewater ReuseTurbidityOrganic MatterColor
<i>Retracted</i>: RNAi‐mediated downregulation of urokinase plasminogen activator receptor and matrix metalloprotease‐9 in human breast cancer cells results in decreased tumor invasion, angiogenesis and growth (2007)

The serine protease urokinase-type plasminogen activator (uPA) plays a significant role in tumor cell invasion and metastasis when bound to its specific receptor, uPAR (also known as CD87). In addition to the uPA-uPAR system, matrix metalloproteinases (MMPs) are involved in tumor cell invasion and metastasis. In this study, we achieved specific inhibition of uPAR and MMP-9 using RNAi technology. We introduced small interfering RNA to downregulate the expression of uPAR and MMP-9 (pUM) in breast cancer cell lines (MDA MB 231 and ZR 75 1). In vitro angiogenesis studies indicated a decrease in the angiogenic potential of the treated cells; in particular, a remarkable decrease was observed in the cells treated with bicistronic construct (pUM) in comparision to the controls. Additionally, bicistronic construct inhibited the formation of capillary-like structures in in vivo models of angiogenesis. Similarly, the invasive potential and migration decreased dramatically when treated with the bicistronic construct as shown by matrigel invasion and migration assays. These results suggest a synergistic effect from the simultaneous downregulation of uPAR and MMP-9. We also assessed the levels of phosphorylated forms of MAPK, ERK and AKT signaling pathway molecules and found reduction in the levels of these molecules in cells treated with the bicistronic construct as compared to the control cells. Furthermore, targeting both uPAR and MMP-9 totally regressed orthotopic breast tumors in nude mice. In conclusion, our results provide evidence that the simultaneous downregulation of uPAR and MMP-9 using RNAi technology may provide an effective tool for breast cancer therapy.
A Novel Corolla-Irradiating Fiber Optic Probe For Laser Angioplasty (1988)

A novel fiber optic probe for laser angioplasty has been realized consisting of a cone fiber tip inserted in a quartz microcapsule. This capsule is sealed on the top by a toroidal shaped lens-structure which avoids the on-axis radiation and gives rise to a sharp corolla shaped beam. These characteristics should minimize the risk both of mechanical and laser perforation. Preliminary tests carried out on aorta segments from cadaver seem to confirm the expected advantages of the new fiber probe.
Interaction of <i>Francisella asiatica</i> with Tilapia ( <i>Oreochromis niloticus</i> ) Innate Immunity (2010)

Members of the genus Francisella are facultative intracellular bacteria that cause important diseases in a wide variety of animals worldwide, including humans and fish. Several genes that are important for intramacrophage survival have been identified, including the iglC gene, which is found in the iglABCD operon in the Francisella sp. pathogenicity island (FPI). In the present study, we examined the interaction of wild-type Francisella asiatica and a Delta iglC mutant strain with fish serum and head kidney-derived macrophages (HKDM). Both the wild-type and the mutant strains were resistant to killing by normal and heat-inactivated sera. The wild-type F. asiatica is able to invade tilapia head kidney-derived macrophages and replicate vigorously within them, causing apoptosis and cytotoxicity in the macrophages at 24 and 36 h postinfection. The Delta iglC mutant, however, is defective for survival, replication, and the ability to cause cytotoxicity in HKDM, but the ability is restored when the mutant is complemented with the iglC gene. Uptake by the HKDM was mediated partially by complement and partially by macrophage mannose receptors, as demonstrated by in vitro assays. Light and electron microscopy analysis of the infected macrophages revealed intracellular bacteria present in a tight vacuole at 2 h postinoculation and the presence of numerous bacteria in spacious vacuoles at 12 h postinfection, with some bacteria free in the cytoplasm.
Preliminary design for a maglev development facility (1992)

A preliminary design was made of a national user facility for evaluating magnetic-levitation (maglev) technologies in sizes intermediate between laboratory experiments and full-scale systems. A technical advisory committee was established and a conference was held to obtain advice on the potential requirements of operational systems and how the facility might best be configured to test these requirements. The effort included studies of multiple concepts for levitating, guiding, and propelling maglev vehicles, as well as the controls, communications, and data-acquisition and -reduction equipment that would be required in operating the facility. Preliminary designs for versatile, dual 2-MVA power supplies capable of powering attractive or repulsive systems were developed. Facility site requirements were identified. Test vehicles would be about 7.4 m (25 ft) long, would weigh form 3 to 7 metric tons, and would operate at speeds up to 67 m/s (150 mph) on a 3.3-km (2.05-mi) elevated guideway. The facility would utilize modular vehicles and guideways, permitting the substitution of levitation, propulsion, and guideway components of different designs and materials for evaluation. The vehicle would provide a test cell in which individual suspension or propulsion components or subsystems could be tested under realistic conditions. The system would allow economical evaluation of integrated systems under varying weather conditions and in realistic geometries.
Detecting O‐GlcNAc using in vitro sulfation (607.1) (2014)

O‐GlcNAc glycosylation, the covalent attachment of N‐acetylglucosamine to serine and threonine residues of proteins, is a post‐translational modification that shares many features with protein phosphorylation. O‐GlcNAc is essential for cell survival and plays important roles in many biological processes (e.g., transcription, translation, cell division) and human diseases (e.g., diabetes, Alzheimer’s disease, cancer). However, detection of O‐GlcNAc is challenging. Here, a method for O‐GlcNAc detection using in vitro sulfation with two GlcNAc‐specific sulfotransferases, CHST2 and CHST4, and the radioisotope 35 S is described. Sulfation on free GlcNAc is first demonstrated, and then on O‐GlcNAc residues of peptides as well as nuclear and cytoplasmic proteins. It is also demonstrated that the sulfation on O‐GlcNAc is sensitive to OGT and OGA treatment. The labeled samples are separated on SDS‐PAGE and visualized by autoradiography. Overall, the method is sensitive, specific and convenient
Objective quality evaluation measure of symmetric and asymmetric distorted stereoscopic images (2012)

An objective quality evaluation measure of asymmetric and symmetric distorted stereoscopic images is proposed. In the measure, stereoscopic features are first extracted from left and right images by using singular value decomposition. Then, the relationship between the stereoscopic features and subjective scores is established by using support vector regression. Finally, the objective evaluation scores are tested on symmetric and asymmetric databases. Experimental results show that the proposed measure is more effective in quantifying image quality, compared with other two relevant quality evaluation measures.
Facile fabrication and formation mechanism of aluminum nanowire arrays (2019)

Anodized alumina membranes (AAMs) have proven effective at making vertically-oriented and well-ordered metal nanowire arrays, which are useful in plasmonics and electrochemistry. Here, we produced Al nanowires via directed AAM pore nucleation: a patterned oxide mask on a flat Al surface directed where pores did and did not form, the pores acting to oxidize Al around the sites without pores. This left Al nanowires embedded in the AAM, and produced freestanding Al nanowires after etching the AAM. The nanowire tops had two distinct contours, smooth bowls and flat rough surfaces-suggesting that nanowires with bowl tops result from slow pore development relative to pattern-nucleated pores, not pore blockage as prior literature suggests. The observed low porosity of ∼2%, as opposed to the more typical 10%, suggests pore nucleation in the electrolyte employed may need greater local variations in electric field or pH, possibly explaining the electrolyte's peculiar ability to make Al nanowires. Finally, a soft nano-imprint lithography process was developed here to pattern the mask without damaging the stamp, avoiding a stamp degradation problem in previous work that utilized hard nano-imprint lithography.