gebhart/patrepeval huggingface dataset:
Synthesis of New Carboxylesterase Inhibitors and Evaluation of Potency and Water Solubility (2001)

Carboxylesterases are essential enzymes in the hydrolysis and detoxification of numerous pharmaceuticals and pesticides. They are vital in mediating organophosphate toxicity and in activating many prodrugs such as the chemotherapeutic agent CPT-11. It is therefore important to study the catalytic mechanism responsible for carboxylesterase-induced hydrolysis, which can be accomplished through the use of potent and selective inhibitors. Trifluoromethyl ketone (TFK)-containing compounds are the most potent esterase inhibitors described to date. The inclusion of a thioether moiety beta to the carbonyl further increased TFK inhibitor potency. In this study, we have synthesized the sulfone analogues of a series of aliphatic and aromatic substituted thioether TFKs to evaluate their potency and solubility properties. This structural change shifted the keto/hydrate equilibrium from <9% hydrate to >95% hydrate, forming almost exclusively the gem-diol. These new compounds were evaluated for their inhibition of carboxylesterase activity in three different systems, rat liver microsomes, commercial porcine esterase, and juvenile hormone esterase in cabbage looper (Trichoplusia ni) hemolymph. The most potent inhibitor of rat liver carboxylesterase activity was 1,1,1-trifluoro-3-(decane-1-sulfonyl)-propan-2,2-diol, which inhibited 50% of the enzyme activity (IC(50)) at 6.3 +/- 1.3 nM and was 18-fold more potent than its thioether analogue. However, the sulfone derivatives were consistently poorer inhibitors of porcine carboxylesterase activity and juvenile hormone esterase activity, with IC(50) values ranging from low micromolar to millimolar. The compound 1,1,1-trifluoro-3-(octane-1-sulfonyl)-propan-2,2-diol was shown to have a 10-fold greater water solubility than its thioether analogue, 1,1,1-trifluoro-3-octylsulfanyl-propan-2-one (OTFP). These novel compounds provide further evidence of the differences between esterase orthologs, suggesting that additional development of esterase inhibitors may ultimately provide a battery of ortholog and/or isoform selective inhibitors analogous to those available for other complex enzyme families with overlapping substrate specificity.
The Correlation between Residual Prostatic Volume Ratio and Parameters of Prostate Volume and Clinical Parameters before and after Transurethral Resection of Prostate in BPH (2001)

to be poorly correlated with other clinical parameters used to assess benign prostate hyperplasia (BPH), including international prostate symptom score(IPSS), peak flow rate(Qmax) and amount of postvoid residuals(PVR). 6) The purpose of this study was to determine
Copper at ancient Kerma: A diachronic investigation of alloys and raw materials (2022)

This paper describes the first comprehensive study of metal artefacts found at ancient Kerma, Sudan. Covering a period of several millennia, it investigates the development of copper alloy recipes as well as metal provenance through the trace element and lead isotope ratio analysis of forty-eight sampled objects. These include grave goods as well as production waste related to large-scale bronze casting performed at Kerma. This study is part of a wider evaluation of copper alloy production at Kerma through targeted workshop excavation, materials analysis, and experimental archaeology. The analytical results illustrate the gradual and flexible transition from arsenical copper to tin bronze alloys over time, in a pattern similarly observed in ancient Egypt. Trace element distributions and lead isotope ratios for copper used at Kerma are comparable to those of contemporary Egyptian artefacts too. These findings indicate the exploitation of ores similar to those mined at the Sinai Peninsula, although copper ore deposits in Nubia remain poorly characterized and thus difficult to identify as source candidates. Nonetheless, it can be suggested that metal provisioning networks along the Nile Valley likely overlapped to varying degrees over time. These results provide an important contribution to the mapping of technological exchanges that took place between ancient Egypt and Nubia.
Nifedipine Prevents Changes in Nitric Oxide Synthase mRNA Levels Induced by Cyclosporine (2000)

Cyclosporine toxicity mainly affects kidney and liver function. We have previously shown that cyclosporine nephrotoxicity alters kidney nitric oxide synthase mRNA pattern of expression. To determine if nitric oxide synthase expression changes are mediated directly by cyclosporine or by secondary hemodynamic alterations induced by cyclosporine, we evaluated if these effects are tissue specific and if nifedipine-induced vasodilation prevents these alterations. Uninephrectomized Wistar rats treated for 7 days with olive oil, cyclosporine (30 mg/kg), nifedipine (3 mg/kg), and nifedipine+cyclosporine were studied. In vehicle and cyclosporine groups, the gene expression of the neuronal, inducible, and endothelial nitric oxide synthases in cerebellum, heart, intestine, liver, renal cortex, and medulla was evaluated. The administration of cyclosporine was associated with nephrotoxicity and hepatotoxicity, increased endothelial nitric oxide synthase mRNA levels in renal cortex and liver, and a decrease in inducible nitric oxide synthase and neuronal nitric oxide synthase in renal medulla. The mRNA levels of the 3 nitric oxide synthase isoforms were not affected in any other tissue. Nifedipine did not alter nitric oxide synthase expression in the control group but prevented changes associated with cyclosporine. These results suggest that cyclosporine-induced changes in the pattern of expression of the nitric oxide synthases may be secondary to its hemodynamic effects.
Effects of light treatment on circadian rhythmicity in seasonal affective disorder (1992)

Summary Twelve outpatients with seasonal affective disorder were treated by 1-h morning bright light exposure for 5 days. The light treatment intervention produced a significant phase advance of self-rated sleepiness rhythm, a significant decrease of the mean level of subjective sleepiness, and a significant reduction of depression scores. No significant objective circadian rhythm phase shift nor amplitude changes would account for the antidepressant effect.
Pyramidal Inversion (1970)

Abstract Pyramidal inversion is discussed from the point of view of recent theoretical and experimental investigations in an attempt to provide a unified description of this process. Quantum mechanical studies of pyramidal molecules indicate that the origin of the inversion barrier may be dependent on the degree of angular constraint. Effects due to the electronegativity of substituents on the inversion center, to the presence of adjacent lone pairs, and to inclusion of d‐type functions in the basis set are discussed. The utility and limitations of molecular orbital calculations, vibrational spectroscopy, microwave spectroscopy, direct kinetic measurements, and dynamic nuclear magnetic resonance (DNMR) spectroscopy as means for determining barriers to pyramidal inversion are discussed in context with a review of the highlights of experimental observations on the subject. Ambiguities that arise in the interpretation of barriers determined by DNMR are explored in detail. Factors that affect the magnitude of inversion barriers are discussed separately in four broad categories: steric effects; effects of conjugation (including (p–d) π conjugation) and hyperconjugation; effects of angular constraint; and effects of heteroatomic substitution. In the last category, critical reference is made to the question of electronegativity vs. lone pair‐lone pair repulsions, the problem of rotation vs. inversion, and the role of d orbitals.
Statistical signal characterization-new help for real-time processing (2003)

The author presents and explains statistical signal characterization (SSC), a technique by which certain easily measured time and amplitude attributes of a signal may be extracted and used to calculate a set of SSC parameters. It is shown how the SSC parameter extraction and statistical analysis processes can be accomplished at considerable savings in computational burden, compared to waveform processing through conventional Fourier methods. The SSC technique is applied to some selected problems within the fields of signal identification and association (or discrimination), and to conventional waveform parameter (amplitude, frequency, phase) extraction. General examples are presented to clarify the use of the technique. Specific examples in radar processing, medical waveform analysis, and seismology are given. Discussions on combining SSC with more conventional processing methods, to arrive at an optimal system design for a particular application, are presented.< <ETX xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">&gt;</ETX>
Supplemental Table S2. Primers from Activation of Wnt/β-Catenin in Ewing Sarcoma Cells Antagonizes EWS/ETS Function and Promotes Phenotypic Transition to More Metastatic Cell States (2023)

&lt;p&gt;Supplemental table S2. qRT-PCR primer sequences.&lt;/p&gt;
JXTA: Java P2P Programming (2002)

(NOTE: Each chapter concludes with a Summary.) Introduction. 1. What is P2P? Defining Peer-To-Peer. Defining P2P. P2P Concepts. Applications for P2P. Key P2P Issues. Technologies Related to P2P. 2. Overview of JXTA. JXTA Defined. JXTA Concepts. JXTA Protocols. Peers and Groups. Advertisements. Pipe Binding Protocol. Resolver. Rendezvous Protocol. JXTA Identifiers. 3. JXTA Protocols. Protocol and API. JXTA Goals. JXTA Peer and Java. Overview of the JXTA Protocols API. Summary of Java API for JXTA Protocols. Where JXTA Applications Begin. The Peer. Starting JXTA. Peer Discovery Protocol API. Peer Resolver Protocol API. Peer Information Protocol. Peer Membership Protocol. Pipe Binding Protocol API. Peer Endpoint Protocol. 4. JXTA Shell. Why Shell? Installation and Troubleshooting. Shell Commands. Using the Shell. Adding Shell Commands. 5. JXTA ping Command. ping. Command Overview. Project Overview. Requirements. Design Approach. Implementation. Install. Test. Further Improvements to Ping. 6. Working with Groups. Importance of Peer Groups. Importance of Peer Group Management. Types of Peer Group Management. Peer Membership Management. 7. JXTA Content Manager Service (CMS). An Overview. How CMS Works. A Simple CMS Example. Overall Design. Initializing the Content Manager. Searching for Content. 8. JXTA and Security. Importance of Security. Security is Multifaceted. Security Attacks in P2P Networks. JXTA Platform Security. JXTA Security Requirements. The Cryptographic Toolkit. Security Issues and Solutions. Trust in P2P systems. P2P Security Models. 9. Synchronizing Data Between Peers. Designing a PDA Organizer for JXTA. Design Considerations. Group Security and Associations. Class Design. 10. JXTA Chess: Game Programming. Running JXTA Chess. Overview of the Classes. 11. JXTA Explorer. Designing an Advertisement Explorer. Design Overview. The Explorer Class. PeerDiscoveryThread Class. AdvertisementTreeCellRenderer Class. Running Explorer. Appendix A. The Project JXTA Community. Contributing to a Project. Submitting a New Project. JXTA.ORG Development Environment. jxta.org Projects. Details on Select Projects. Commercial Projects. Appendix B. XML Primer. XML Basics. Self-Describing. Strong Typing and Syntax Validation. Problems with XML. Index.
Effect of diltiazem on 2,4‐D‐induced myotonia in rats (1989)

Myotonia is characterized by prolonged contraction (delay in onset of relaxation) of skeletal muscle fibers with characteristic electromyographic findings. Calcium channel blocking drugs may be expected to reduce myotonia, should they promote the onset of relaxation in a contracted skeletal muscle. This study was aimed at evaluating the effect of diltiazem, a calcium channel blocking agent, on myotonia induced by 2,4-dichlorophenoxyacetic acid (2,4-D). In rat diaphragm, exposed to 2.5 mM 2,4-D in a tissue bath, myotonia was quantified by documenting the contraction time in response to direct stimulation with supramaximal electric stimuli. At the peak of myotonia, different concentrations of diltiazem were added to the tissue bath and the effect on evoked contraction studied over a period of 6 minutes. A concentration of 5 x 10(-5) M was found to be the most effective, causing a decrease in contraction time of more than 90% in 3 minutes in 100% of specimens (n = 7). The above findings raise the possibility of using diltiazem as an antimyotonic agent.
Indoor real-time 3D reconstruction of crash-tested car cabins (2010)

The main contribution of the paper is to propose a novel system for real-time measurement of the inside of crashed and non-crashed car cabins. The proposed system consists of a multi-camera system and a probe equipped with a camera and line laser module, both designed to enable the fast and easy acquisition of the car cabin from its inside. The main tasks of the development were first of all the accurate estimation of the location of the handheld probe, as well as its orientation in real-time by guaranteeing its almost free motion and rotation inside the cabin. Furthermore, the calibration of the system, the estimation of target's 3D coordinates - based on laser stripe projection and processing corresponding camera images - and finally the point-cloud processing can also be considered as main tasks to be performed. In the course of the development of these methods the main restriction was to keep the complexity as low as possible in order to guarantee the real-time functionality.
Inhibiting the Inhibitor of the Inhibitor: Blocking PKC-θ to Enhance Regulatory T Cell Function (2010)

Protein kinase C (PKC-theta), one of many PKC isoforms expressed in T cells, is important for the activation of mature effector T cells. During T cell activation, PKC-theta is recruited to the interface between the T cell and the activating cellular interaction partner, the antigen-presenting cell or a synthetic substitute thereof. New evidence establishes that PKC-theta function differs in regulatory T cells, a T cell subset that suppresses the function of effector T cells. In regulatory T cells, PKC-theta inhibits their function and, intriguingly, is sequestered from the activating cellular interface. This finding raises several questions of general interest. Does PKC-theta function overlap with that of other PKC family members? What are the functionally critical distinctions in the similar signaling systems of effector and regulatory T cells? Does the divergent localization of PKC-theta in regulatory T cells drive function?
MR-Sialographie: Optimierung und Bewertung ultraschneller Sequenzen mit paralleler Bildgebung und oraler Stimulation (2005)

Ziel: Die Optimierung einer schnellen Sequenz zur MR-Sialographie sowie der Vergleich der entwickelten Sequenz vor und nach oraler Stimulation. Des Weiteren sollten parallele und nicht parallele Bildakquisitionstechniken verglichen werden. Material und Methoden: 27 gesunde Probanden wurden an einem 1,5-T-System mit einer axialen und schräg sagittalen Single-Shot-Turbo-Spin-Echo-Sequenz (ss-TSE) mit einer Akquisitionszeit von 2,8 s mit und ohne parallele Bildakquisitionstechnik sowie vor und nach oraler Stimulation untersucht. Die Beurteilbarkeit der Ausführungsgänge der Glandulae parotideae und der Glandulae submandibulares wurde seitengetrennt anhand einer Skala von 1 - 5 von vier Auswertern unabhängig voneinander visuell eingestuft. Die statistische Auswertung erfolgte mittels einer ANOVA mit Post-hoc-Test. Die Bewertung der Observerübereinstimmung wurde mit einer Intraclass-Korrelation vorgenommen. Ergebnisse: Sämtliche Ganganteile der großen Speicheldrüsen konnten mit der entwickelten Technik mit einer hochsignifikanten Intraclass-Korrelation von 0,9475 zwischen den Auswertern dargestellt werden. Der Mittelwert der subjektiven Einschätzung aller ausgewerteten Ganganteile lag bei 2,26 (Standardabweichung [SD] ± 1,09). Nach Gabe des Sialogogums wurde die Darstellbarkeit signifikant besser bewertet als ohne Stimulation (p < 0,001; η2 = 0,049), während die Ausführungsgänge mittels paralleler Bildakquisitionstechnik signifikant schlechter bewertet wurden (p < 0,001; η2 = 0,013). Schlussfolgerung: Mittels der angewendeten ss-TSE ist eine gute Darstellung der Ausführungsgänge der großen Speicheldrüsen ohne notwendige Nachbearbeitung möglich. Zur Verbesserung der Ergebnisse sollte vor einer MR-Sialographie ein orales Stimulans appliziert werden.
Phase-error analysis and elimination for nonsinusoidal waveforms in Hilbert transform digital-fringe projection profilometry (2009)

The nonlinear intensity response of a digital fringe-projection-profilometry (FPP) system causes the captured fringe patterns to be nonsinusoidal waveforms, which results in phase error and therefore measurement error. The theoretical analysis of the phase error due to the nonsinusoidal waveforms in Hilbert transform FPP is performed. Based on the derived phase-error expression, a cubic spline-smoothing method is proposed to eliminate the nonsinusoidal phase error. Experiments show that the proposed algorithm can be used for effective phase-error elimination in practical Hilbert transform FPP.
Pulse-skipping power factor correction control schemes for AC/DC power converters (2013)

Power factor correction (PFC) is a must nowadays for many power supply applications. Recently, there has been a trend to cut down the overall cost even at the expense of the input harmonic current performance, as long as it meets the minimum requirement. There was a strategy reported, the so-called pulse-skipping PFC converter to achieve the goal mentioned above. In this strategy, there are two power stages used, like a conventional PFC circuit, but only one feedback control IC to provide gate drive signals to the main switches of the two stages. The frontstage boost converter is set to always operate in discontinuous conduction mode to achieve acceptable power factor. The second stage is a flyback converter. The gate drive signal to the flyback converter is derived with a conventional PWM strategy, but a pulse-skipping technique is applied to the aforementioned gatedrive signal to drive the boost converter stage. This control strategy can reduce the switching losses of the front stage, manage the interlink bulk capacitor voltage to stay within reasonable range, and may keep the input harmonic current performance in acceptable range. This paper presents the results of theoretical investigation of such a strategy. Mathematical analyses are conducted to reveal the complicated relationships for design purpose. Simulations are performed to verify the mathematical results. The conclusions indicate that there are advantages of such an approach for applications where hold-up time is not required, such as a driver circuit for LED lighting.
3D cell nuclei segmentation based on gradient flow tracking (2007)

The proposed algorithm is able to segment closely juxtaposed or touching cell nuclei obtained from 3D microscopy imaging with reasonable accuracy.
Automating Postsilicon Debugging and Repair (2008)

Due to increasing semiconductor design complexity, more errors are escaping presilicon verification and being discovered only after manufacturing. As an alternative to traditional manual chip repair, the authors propose the FogClear methodology, which automates the postsilicon debugging process and thereby reduces IC development time and costs.
Cell cycle-dependent deacetylation of telomeric histone H3 lysine K56 by human SIRT6 (2009)

SIRT6 is a member of the Sir2 (Silent Information Regulator-2) family of genes, which regulate fundamental processes in aging and lifespan control in multiple organisms.1-3 SIRT6 deficiency in mice results in genomic instability, metabolic defects, and degenerative phenotypes associated with aging.1 Previously, we showed that SIRT6 deacetylates lysine 9 on the N-terminal tail of histone H3 (H3K9Ac) to modulate telomeric chromatin and gene expression.2,3 Here, we identify a second substrate of SIRT6 at chromatin, lysine 56 on the globular core of histone H3 (H3K56Ac). We show that SIRT6 deacetylates H3K56Ac in vitro and in cells, and identify a physiologic role for this activity in maintaining dynamic changes of H3K56 acetylation levels at telomeric chromatin over the cell cycle. Together, these findings provide the first analysis of how H3K56Ac levels are dynamically regulated at human telomeres in response to a mammalian SIRT.
Comparative clinicopathological study of primary CNS diffuse large B-cell lymphoma and intravascular large B-cell lymphoma (2009)

Primary CNS diffuse large B-cell lymphoma (CNS DLBCL) is confined to the CNS, and constitutes a distinct entity. In the present study a series of 40 Japanese patients with CNS DLBCL who presented with neurological, but not systemic symptoms, was reviewed. Median survival was 18.7 months. CD5, CD10, Bcl-6, MUM-1, and Bcl-2 were positive in 30%, 10%, 84%, 100%, and 93% of patients, respectively. All CD10-negative patients had non-germinal center B-cell type. There was no significant difference in survival among the immunophenotypic subgroups. CNS DLBCL appeared to be homogenous as a group, which prompted the comparison with another distinct extranodal entity, intravascular large B-cell lymphoma (IVLBCL) in Japanese patients. CNS DLBCL patients did not differ in age, sex, or immunophenotype, including CD5 positivity, from IVLBCL patients, but were significantly less likely to have poor prognostic parameters than IVLBCL patients: the international prognostic index score was low or low-intermediate in 86% of CNS DLBCL patients and high or high-intermediate in 98% of IVLBCL patients. Notably, despite this difference, their survival curves almost overlapped. The present study highlights the issue of clinical distinctiveness of aggressive extranodal lymphomas, the peculiar migration and localization of which should be further clarified.
Extending the golden hour for Zone 1 resuscitative endovascular balloon occlusion of the aorta: Improved survival and reperfusion injury with intermittent versus continuous resuscitative endovascular balloon occlusion of the aorta in a porcine severe truncal hemorrhage model (2018)

Intermittent REBOA can maintain supraceliac hemorrhage control while decreasing distal ischemia in a swine model. Prolonged survival times, decreased acidosis, and lower resuscitation requirements indicate that this technique could potentially extend Zone 1 REBOA deployment times. Schedules based on MAP may be superior to time-based regimens.
Synthesis of Quinoxaline 1,4-Dioxides from Benzofuroxan Proceeds Not in, But on Zeolite (2003)

Quinoxaline synthesis using Na-zeolite A as a catalyst to proceeds in a better yield than that using zeolite X. The pore diameter of zeolite X is large enough to allow the benzofuroxan derivatives access to cages, therefore part of benzofuroxan is adsorbed in the internal surface of zeolite X. Whereas the windows to the cages of Na-zeolite A are too small to allow the benzofuroxan derivatives access to the cages, therefore all the benzofuroxan is adsorbed on the external surface of zeolite. The reactions of benzofuroxans with benzoylacetone was catalyzed by zeolite proceed not in, but on zeolite.
Novel organic scintillators for neutron detection (2010)

In this paper we report on novel organic scintillators in the form of single crystals for neutron detection. In particular, we focus on 9,10-Diphenylanthracene, Tetraphenylbutadiene, and Lithium-Salicylate, grown from solution.