gebhart/patrepeval huggingface dataset:
Structural Investigation of the 7-Chloro-3-hydroxy-1H-quinazoline-2,4-dione Scaffold to Obtain AMPA and Kainate Receptor Selective Antagonists. Synthesis, Pharmacological, and Molecular Modeling Studies (2006)

In this paper, the study of new 7-chloro-3-hydroxy-1H-quinazoline-2,4-dione derivatives, designed as AMPA and kainate (KA) receptor antagonists, is reported. Some derivatives bear different carboxy-containing alkyl chains on the 3-hydroxy group, while various heterocyclic rings or amide moieties are present at the 6-position of other compounds. Binding data at Gly/NMDA, AMPA, and high-affinity KA receptors showed that the presence of the free 3-hydroxy group is of paramount importance for a good affinity at all three investigated receptors, while introduction of some 6-heterocyclic moieties yielded AMPA-selective antagonists. The most significant result was the finding of the 6-(2-carboxybenzoylamino)-3-hydroxy-1H-quinazolin-2,4-dione 12, which possesses good affinity for high-affinity and low-affinity KA receptors (Ki=0.62 microM and 1.6 microM, respectively), as well as good selectivity. To rationalize the trend of affinities of the reported derivatives, an intensive molecular modeling study was carried out by docking compounds to models of the Gly/NMDA, AMPA, and KA receptors.
Design of sensors for three dimensional optical and electrical measurements in myocardial tissue (2002)

Cardiac mapping of activation and repolarization is currently limited by the lack of robust sensors for making electrical and optical measurements in three-dimensional myocardium. The paper describes potential designs for such sensors and discusses design, fabrication, application, and validation issues.
The overexpression ofOsNAC9alters the root architecture of rice plants enhancing drought resistance and grain yield under field conditions (2012)

Drought conditions limit agricultural production by preventing crops from reaching their genetically predetermined maximum yields. Here, we present the results of field evaluations of rice overexpressing OsNAC9, a member of the rice NAC domain family. Root-specific (RCc3) and constitutive (GOS2) promoters were used to overexpress OsNAC9 and produced the transgenic RCc3:OsNAC9 and GOS2:OsNAC9 plants. Field evaluations over two cultivating seasons showed that grain yields of the RCc3:OsNAC9 and the GOS2:OsNAC9 plants were increased by 13%-18% and 13%-32% under normal conditions, respectively. Under drought conditions, RCc3:OsNAC9 plants showed an increased grain yield of 28%-72%, whilst the GOS2:OsNAC9 plants remained unchanged. Both transgenic lines exhibited altered root architecture involving an enlarged stele and aerenchyma. The aerenchyma of RCc3:OsNAC9 roots was enlarged to a greater extent than those of GOS2:OsNAC9 and non-transgenic (NT) roots, suggesting the importance of this phenotype for enhanced drought resistance. Microarray experiments identified 40 up-regulated genes by more than threefold (P < 0.01) in the roots of both transgenic lines. These included 9-cis-epoxycarotenoid dioxygenase, an ABA biosynthesis gene, calcium-transporting ATPase, a component of the Ca(2+) signalling pathway involved in cortical cell death and aerenchyma formation, cinnamoyl CoA reductase 1, a gene involved in lignin biosynthesis, and wall-associated kinases¸ genes involved in cell elongation and morphogenesis. Interestingly, O-methyltransferase, a gene necessary for barrier formation, was specifically up-regulated only in the RCc3:OsNAC9 roots. Such up-regulated genes that are commonly and specifically up-regulated in OsNAC9 transgenic roots may account for the altered root architecture conferring increased drought resistance phenotype.
Adaptive slit beam shaping for direct laser written waveguides (2012)

We demonstrate an improved method for fabricating optical waveguides in bulk materials by means of femtosecond laser writing. We use an LC spatial light modulator (SLM) to shape the beam focus by generating adaptive slit illumination in the pupil of the objective lens. A diffraction grating is applied in a strip across the SLM to simulate a slit, with the first diffracted order mapped onto the pupil plane of the objective lens while the zeroth order is blocked. This technique enables real-time control of the beam-shaping parameters during writing, facilitating the fabrication of more complicated structures than is possible using nonadaptive methods. Waveguides are demonstrated in fused silica with a coupling loss to single-mode fibers in the range of 0.2 to 0.5 dB and propagation loss <0.4 dB/cm.
Efficacy of N-Acetylcysteine on Endometriosis-Related Pain, Size Reduction of Ovarian Endometriomas, and Fertility Outcomes (2023)

Oral NAC improves endometriosis-related pain and the size of endometriomas. Furthermore, it decreases Ca125 serum levels and may improve fertility in patients with endometriosis.
Mechanism of cytochrome P-450 catalysis. Mechanism of N-dealkylation and amine oxide deoxygenation (1985)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTMechanism of cytochrome P-450 catalysis. Mechanism of N-dealkylation and amine oxide deoxygenationLeo T. Burka, F. Peter Guengerich, Randolf J. Willard, and Timothy L. MacdonaldCite this: J. Am. Chem. Soc. 1985, 107, 8, 2549–2551Publication Date (Print):April 1, 1985Publication History Published online1 May 2002Published inissue 1 April 1985https://pubs.acs.org/doi/10.1021/ja00294a057https://doi.org/10.1021/ja00294a057research-articleACS PublicationsRequest reuse permissionsArticle Views707Altmetric-Citations89LEARN ABOUT THESE METRICSArticle Views are the COUNTER-compliant sum of full text article downloads since November 2008 (both PDF and HTML) across all institutions and individuals. These metrics are regularly updated to reflect usage leading up to the last few days.Citations are the number of other articles citing this article, calculated by Crossref and updated daily. Find more information about Crossref citation counts.The Altmetric Attention Score is a quantitative measure of the attention that a research article has received online. Clicking on the donut icon will load a page at altmetric.com with additional details about the score and the social media presence for the given article. Find more information on the Altmetric Attention Score and how the score is calculated. Share Add toView InAdd Full Text with ReferenceAdd Description ExportRISCitationCitation and abstractCitation and referencesMore Options Share onFacebookTwitterWechatLinked InRedditEmail Other access optionsGet e-Alertsclose Get e-Alerts
Cooperative Intelligence - A Humane Perspective (2020)

In this contribution, we outline our concept of cooperation between humans and intelligent systems which we denote as cooperative intelligence. We argue from a human perspective and emphasize the advantages of keeping the human in the loop rather than targeting autonomous systems. Our focus is respecting human values such as retaining competences, sharing experiences, and self-esteem. We discuss process-oriented requirements for intuitive cooperation like joint goals and shared intentions and social dimensions like empathy, relations, and trust. Finally, we suggest that cooperative intelligence can be facilitated by integrating interaction episodes across multiple system embodiments and instances, achieving the best holistic service with regard to personal preferences and needs.
Supplementary Figure 8 from Canonical Wnt Signaling Is Required for Pancreatic Carcinogenesis (2023)

&lt;p&gt;PDF file - 1428K, Supplemental Figure 8. Wnt/β-catenin signaling regulates PanIN survival.&lt;/p&gt;
The effect of normal and calcium bicarbonate rich water replacement after sauna on muscle behaviour [L'effetto della reidratazione, dopo sauna, con acqua normale e ricca di bicarbonato di calcio sul comportamento muscolare] (2003)

Aim. The present investigation was undertaken to study if the different fluid replacement (normal vs calcium bicarbonate rich water) could influence heavy cycling performance and explosive power. The purpose of the present study is to compare the effect of water replacement during sauna bath using 2 different types of water intake: Normal vscalcium rich bicarbonate and very low sodium concentration (Sangemini, Italy) on muscle mechanical behaviour. Methods. A group of 27 healthy and moderately active students, 19 males and 8 females, randomly assigned in 2 groups have performed the same test protocol in 2 sessions. After 5 minutes of warming up on an electro-magnetically-braked cycle ergometer at 50 W for males and 35 W for females, and free revolutions per minute, and 3 minutes of static stretching the subjects performed a counter movement jump (CMJ) and after a modified Wingate test on the cycle ergometer for 60 s. The Wingate test started from 0 rpm and the torque was set at 0.7 Nm/kg body weight for the males and 0.67 Nm/kg body weight for the females. Mechanical power, synchronised with electromyography (EMG) analysis from the mm Vastus lateralis and medialis and Lactate (mM/L) were measured. In the 2nd session the subjects took first a Finnish sauna bath at 90Â° and 100% humidity. After sauna the subjects drunk water from a bottle ad libitum, and 1 hour after the sauna performed the 2nd test with the same protocol than in the 1st session. The Group A (Control group) took a normal water while the Group B (Experimental group) took a calcium bicarbonate rich water. Results. In the jumping performance the group treated with calcium water bicarbonate showed a significantly increase of height of the centre of gravity (31,6Â±7,12 cm vs 32,3Â±7,42 cm p<0,05) while the control group (33,6Â±6,5 cm vs 32,0Â±5,6 cm, p=n.s.) was negatively affected by normal water after the sauna bath. Average power, average power/body mass ratio, and EMGrms, no statistically significant differences were founded in both groups. The group treated with calcium water bicarbonate showed a decrease of lactate production post treatment test (12,3Â±1,9 mM/L vs 10,6Â±2,1 mM/L, p<0,05) while no difference was noted in the control group (11,9Â±1,8 mM/L vs 11,4Â±2,0 mM/L, p=n.s.). Also significant differences was found in the maximal lactate and the average power ratio. Conclusions. It seems that the supplement of calcium bicarbonate rich water could effect positively the negative effect of elevated (H+) on Ca2+ binding mechanism. This is a simple suggestions which, however cannot explain why the experimental subjects drinking calcium bicarbonate rich water developed lower blood [Lac-]. On basis of the present results it can be suggested that drinking calcium bicarbonate rich water helps the athletes to perform strenuous work by reducing the blood [Lac-] accumulation.
miR-34c-3p Regulates Protein Kinase A Activity Independent of cAMP by Dicing prkar2b Transcripts in Theileria annulata-Infected Leukocytes (2023)

MicroRNAs (miRNAs) are small noncoding RNAs that can play critical roles in regulating various cellular processes, including during many parasitic infections. Here, we report a regulatory role for miR-34c-3p in cAMP-independent regulation of host cell protein kinase A (PKA) activity in <i>Theileria annulata</i>-infected bovine leukocytes. We identified <i>prkar2b</i> (cAMP-dependent protein kinase A type II-beta regulatory subunit) as a novel miR-34c-3p target gene and demonstrate how infection-induced upregulation of miR-34c-3p repressed PRKAR2B expression to increase PKA activity. As a result, the disseminating tumorlike phenotype of <i>T. annulata</i>-transformed macrophages is enhanced. Finally, we extend our observations to Plasmodium falciparum-parasitized red blood cells, where infection-induced augmentation in miR-34c-3p levels led to a drop in the amount of <i>prkar2b</i> mRNA and increased PKA activity. Collectively, our findings represent a novel cAMP-independent way of regulating host cell PKA activity in infections by <i>Theileria</i> and <i>Plasmodium</i> parasites. <b>IMPORTANCE</b> Small microRNA levels are altered in many diseases, including those caused by parasites. Here, we describe how infection by two important animal and human parasites, Theileria annulata and Plasmodium falciparum, induce changes in infected host cell miR-34c-3p levels to regulate host cell PKA kinase activity by targeting mammalian <i>prkar2b</i>. Infection-induced changes in miR-34c-3p levels provide a novel epigenetic mechanism for regulating host cell PKA activity independent of fluxes in cAMP to both aggravate tumor dissemination and improve parasite fitness.
On the specialization of online program specializers (1993)

Abstract A common technique for improving the speed of program specialization is to specialize the program specializer itself on the program to be specialized, creating a custom program generator . Much research has been devoted to the problem of generating efficient program generators, which do not perform reductions at program generation time which could instead have been performed when the program generator was constructed. The conventional wisdom holds that only program specializers using binding-time approximations can be specialized into such efficient program generators. This paper argues that this is not the case, and demonstrates that the specialization of a nontrivial online program specializer similar to the original ‘naive MIX’ can indeed yield an efficient program generator. The key to our argument is that, while the use of binding-time information at program generator generation time is necessary for the construction of an efficient custom specializer, the use of explicit binding-time approximation techniques is not. This allows us to distinguish the problem at hand (i.e. the use of binding-time information during program generator generation) from particular solutions to that problem (i.e. offline specialization). We show that, given a careful choice of specializer data structures, and sufficiently powerful specialization techniques, binding-time information can be inferred and utilized without explicit approximations. This allows the construction of efficient, optimizing program generators from online program specializers.
System and method of forming nanostructured ferritic alloy (2023)

A system for mechanical milling and a method of mechanical milling are disclosed. The system includes a container, a feedstock, and milling media. The container encloses a processing volume. The feedstock and the milling media are disposed in the processing volume of the container. The feedstock includes metal or alloy powder and a ceramic compound. The feedstock is mechanically milled in the processing volume using metallic milling media that includes a surface portion that has a carbon content less than about 0.4 weight percent.
NY-ESO-1 as a predictive marker for neoadjuvant chemotherapy in stage IIIa non-small cell lung cancer (NSCLC). (2011)

10576 Background: The use of neoadjuvant chemotherapy in stage IIIa NSCLC is controversial with trials consistently failing to demonstrate a significant benefit. The ability to identify chemoresponsive tumors should aid clinical trial design and outcome. Cancer-Testis antigens (CTAg), such as MAGE A3, are currently being investigated as immunotherapeutic targets in the adjuvant setting. CTAgs are expressed in over 50% of both squamous cell and adenocarcinomas but restricted to testis in normal tissues. Since CTAgs have been proposed as markers of drug-resistant stem-like cells, we investigated their expression and association with chemosensitivity. Methods: Stage IIIa patients treated with neoadjuvant chemotherapy at the Austin Hospital (AH) Melbourne and Weill Cornell Medical College (WCMC) New York were investigated. Preoperative mediastinal lymphadenectomy tissues were stained for a panel of CTAgs including NY-ESO-1, MAGE-A, MAGE-C1/CT7, GAGE and CT45 by immunohistochemistry. DNA was isolated from paraffin sections from the WCMC dataset and mutationally profiled using Sequenom’s MassArray platform. Molecular results were correlated to clinical characteristics, chemoresponsiveness (defined as pathological down-staging of TNM status), progression free and overall survival (OS). Results: 95 patients (WCMC: 70, AH: 25) were studied. Staining for one or more CTAgs was positive in 50% of samples regardless of histology. NY-ESO-1 was expressed in 33% of samples. DNA was isolated from 63/70 WCMC samples. Mutations were seen predominantly in the EGFR (5/63) and KRAS (8/63) genes. CTAg expression occurred independent to KRAS mutant tumors. NY-ESO-1 expression occurred independent to EGFR and KRAS mutations and was significantly associated with chemosensitivity in both datasets (Chi square p=0.010). Improved OS was only seen in the AH dataset (HR 0.36; 95% CI 0.14-0.96, p=0.04). Conclusions: Expression of NY-ESO-1 predicts response to neoadjuvant chemotherapy in stage IIIa NSCLC. Expression occurred independent of common mutations but in both adenocarcinoma and squamous cell carcinoma. Given their immunogenicity, immunological mechanisms for these responses are being investigated.
Component embedding platform for thin profile SiP, POP and fan-out WLP (2015)

While component embedding technologies have reached maturity and are used for high volume manufacturing, the industry is looking for new ways to exploit the possibilities it enables. Growing interest in embedding is introducing new challenges, requiring further innovation and pushing development of solutions that offer cost efficient and robust manufacturing processes for novel product designs. High quality and high yield production processes are essential for all embedding technologies, but it is equally important to have a flexible supply solution, which lowers the barrier for adoption and enables short cycle time from early product concept to prototyping and manufacturing. The Power Overlay (POL) technology has been developed to improve product performance and miniaturization using a direct microvia and polyimide (PI) based interconnection technology. The POL is a platform of packaging technology solutions for wide application area. Different POL adaptations and target applications will be briefly reviewed in this paper. A new Ultra-Thin WLPOL process has been developed and will be presented in the paper. The technology feasibility for sub 200μm fan-out WLP package has been demonstrated using 6×6mm, 90×9mm, 10×10mm, and 12×12mm package configurations.
Defect dynamics and coarsening dynamics in smectic-Cfilms (1992)

We study the dynamics of defects generated in free-standing films of liquid crystals following a thermal quench from the smectic-A phase to the smectic-C phase. The defects are type-1 disclinations, and the strain field between defect pairs is confined to 2\ensuremath{\pi} walls. We compare our observations with a phenomenological model that includes dipole coupling of the director field to an external ordering field. This model is able to account for both the observed coalescence dynamics and the observed ordering dynamics. In the absence of an ordering field, our model predicts the defect density \ensuremath{\rho} to scale with time t as \ensuremath{\rho} ln\ensuremath{\rho}\ensuremath{\propto}${\mathit{t}}^{\mathrm{\ensuremath{-}}1}$. When the dipole coupling of the director field to an external ordering field is included, both the model and experiments show the defect coarsening proceeds as \ensuremath{\rho}\ensuremath{\propto}${\mathit{e}}^{\mathrm{\ensuremath{-}}\mathrm{\ensuremath{\alpha}}\mathit{t}}$ with the strain field confined to 2\ensuremath{\pi} walls. The external ordering field most likely arises from the director's tendency to align with edge dislocations within the liquid-crystal film.
Correction of Wall Adhesion Effects in Batch Settling of Strong Colloidal Gels (2014)

The batch settling test is widely used to estimate the compressive rheology of strongly flocculated colloidal suspensions, in particular the compressive yield strength and hydraulic permeability. Recently it has been discovered that wall adhesion effects in these tests may be significantly greater than previously appreciated, which can introduce unbounded errors in the estimation of these rheological functions. Whilst a methodology to solve the underlying static problem and correct for wall adhesion effects has been developed, this method is quite complex and unwieldy, involving solution of a 2D hyper-elastic constitutive model for strong colloidal gels. In this paper we develop a highly simplified 1D visco-plastic approximation to the hyper-elastic model which admits analytic expressions for the equilibrium solids concentration profile and bed height. These expressions facilitate robust estimation of the compressive yield and wall adhesion strength via nonlinear regression of experimental data in the presence of small measurement errors.
ChemInform Abstract: On the Protein Kinase C Pharmacophore: Synthesis and Biological Activity of 4‐Hydroxylated Analogues of Ingenol. (1995)

Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.
Characterization of Flow in Intravenous Catheters (1986)

The pressure-flow (P-F) relationship in intravenous catheters is shown to be represented by the predictive model P = RLF + RTF2. The pressure loss due to F, calculated from experimental data, was found to equal the expected Poiseuille laminar flow loss. Pressure loss due to F2 was found to be the sum of turbulent P losses due to entrance length flow disturbance, kinetic energy at the outflow, and minor shape change losses. Analysis of the flow capabilities of intravenous catheters can be used to evaluate suitability for specific intravenous infusion needs.
Crowd-sensing driving environments using headway dynamics (demo paper) (2022)

In this paper, we develop a set of normalized spatial temporal properties from which to assess road performance and detect abnormal traffic stream environments. Data is provided by non-instrumented retail vehicle telemetry data, which captures timestamps, GPS locations, and velocity provided every 3 seconds. Open Street Map (OSM) roadways are subdivided into 500-meter segments. Vehicles traveling across those segments are crowd-sensed every 15 minutes. The demonstration compares two traffic streams over the same segments and time periods exactly two weeks apart and illustrates the effectiveness of the approach. The novelty includes methods to create comparable spatial temporal frames and properties by transformations of telemetry data into driver experiences. The outcome of our approach generates a space time grid of cells from which to detect, describe, and diagnose traffic environments.
Quantitative measurements of intraocular structures including subretinal microinjection bleb volumes using intraoperative optical coherence tomography (Conference Presentation) (2020)

Microscope-integrated optical coherence tomography (MIOCT) systems allow for 4D visualization of thin, semi-transparent structures during ophthalmic microsurgery. While these visualizations have greatly increased the information available to surgeons, new surgical techniques, such as subretinal injections of gene therapies, would benefit from quantitative measurements of structures imaged using OCT. Calibration of true scan dimensions in OCT is complicated by inter-patient ocular variability as well as poor control of scanner-patient alignment. We introduce novel measurement techniques for calibration and de-warping of OCT imagery which allows for accurate measurement of intraocular structures including subretinal microinjection bleb volumes in the ocular posterior segment.
Ion-pair separation via selective inclusion/segregation processes (2009)

Segregation of iodide ions—via trifurcated halogen bonding to diiodoperfluoroalkanes—within fluorous layers consisting of 1D networks, provides the driving force for the isolation, in the solid state, of the first alkylammonium–calix[5]arene 1 : 1 endo-cavity complex.