gebhart/patrepeval huggingface dataset:
Overcoming the Low Oral Bioavailability of Deuterated Pyrazoloquinolinone Ligand DK-I-60-3 by Nanonization: A Knowledge-Based Approach (2021)

Poor water solubility of new chemical entities is considered as one of the main obstacles in drug development, as it usually leads to low bioavailability after administration. To overcome these problems, the selection of the appropriate formulation technology needs to be based on the physicochemical properties of the drug and introduced in the early stages of drug research. One example of the new potential drug substance with poor solubility is DK-I-60-3, deuterated pyrazoloquinolinone, designed for the treatment of various neuropsychiatric disorders. In this research, based on preformulation studies, nanocrystal technology was chosen to improve the oral bioavailability of DK-I-60-3. Nanocrystal dispersions stabilized by sodium lauryl sulfate and polyvinylpyrrolidone were prepared by modified wet media milling technique, with the selection of appropriate process and formulation parameters. The nanoparticles characterization included particle size and zeta potential measurements, differential scanning calorimetry, X-ray powder diffraction, dissolution and solubility study, and in vivo pharmacokinetic experiments. Developed formulations had small uniform particle sizes and were stable for three months. Nanonization caused decreased crystallite size and induced crystal defects formation, as well as a DK-I-60-3 solubility increase. Furthermore, after oral administration of the developed formulations in rats, two to three-fold bioavailability enhancement was observed in plasma and investigated organs, including the brain.
Ubiquitin Ligase HUWE1 Regulates Axon Branching through the Wnt/β-Catenin Pathway in a Drosophila Model for Intellectual Disability (2013)

We recently reported that duplication of the E3 ubiquitin ligase HUWE1 results in intellectual disability (ID) in male patients. However, the underlying molecular mechanism remains unknown. We used Drosophila melanogaster as a model to investigate the effect of increased HUWE1 levels on the developing nervous system. Similar to the observed levels in patients we overexpressed the HUWE1 mRNA about 2-fold in the fly. The development of the mushroom body and neuromuscular junctions were not altered, and basal neurotransmission was unaffected. These data are in agreement with normal learning and memory in the courtship conditioning paradigm. However, a disturbed branching phenotype at the axon terminals of the dorsal cluster neurons (DCN) was detected. Interestingly, overexpression of HUWE1 was found to decrease the protein levels of dishevelled (dsh) by 50%. As dsh as well as Fz2 mutant flies showed the same disturbed DCN branching phenotype, and the constitutive active homolog of β-catenin, armadillo, could partially rescue this phenotype, our data strongly suggest that increased dosage of HUWE1 compromises the Wnt/β-catenin pathway possibly by enhancing the degradation of dsh.
Tables for practical Wyner-Ziv coding of Laplacian sources (2009)

Many practical coding scenarios deal with sources with transform coefficients that are well modeled as Laplacians. For the Wyner-Ziv coding problem for such sources when correlated side-information is available at the decoder, the side-information is modeled as obtained by independent additive Laplacian or Gaussian innovation on the source. This paper deals with the optimal choice of encoding parameters for practical Wyner-Ziv coding in such scenarios, using the same quantizer family as in the regular codec to cover a range of rate-distortion trade-offs, given the variances of the source and innovation. Using our prior analysis of a general encoding model based on multi-level coset codes combining source and channel coding, we present comprehensive tables with optimal encoding parameters. These tables can be readily incorporated into a practical codec to read off the encoding parameters.
ChemInform Abstract: Synthetic Utility of 4‐Bromo‐2,3,5,6‐tetrafluoropyridine. (2008)

Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 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.
Tuning of conformational preorganization in model 2',5'- and 3',5'-linked oligonucleotides by 3'- and 2'-O-methoxyethyl modification (2003)

Conformational properties of trimeric and tetrameric 2',5'-linked oligonucleotides, 3'-MOE-A3(2',5') (1) and 3'-MOE-A4(2',5') (2), and their 3',5'-linked analogs, 2'-MOE-A3(3',5') (3) and 2'-MOE-A4(3',5') (4), were examined with the use of heteronuclear NMR spectroscopy. The temperature-dependent 3JHH, 3JHP and 3JCP coupling constants, acquired in the range of 273-343 K, gave insight into the conformation of sugar rings in terms of a two-state North <---> South (N <---> S) pseudorotational equilibrium and into the conformation of the sugar-phosphate backbone in the model antisense oligonucleotides 1-4. 2',5'-linked oligomers 3'-MOE-A3(2',5') (1) and 3'-MOE-A4(2',5') (2) show preference for N-type conformers and indication of A-type conformational features, which is prerequisite for antisense hybridization. The drive of N <---> S equilibrium in 1-4 has been rationalized with the competing gauche effects of 2'/3'-phosphodiester and 3'/2'-MOE groups, anomeric and steric effects. Furthermore, the pairwise comparisons of 3'-MOE with 3'-OH and 3'-deoxy 2',5'-linked adenine trimers emphasized the fine tuning of N <---> S equilibrium in 3'-MOE-A3(2',5') (1) and 3'-MOE-A4(2',5') (2) by the steric effects of 3'-MOE group and the possibility of water-mediated H-bonds with vicinal phosphodiester functionality. In full correspondence, the drive of N <---> S equilibrium towards N by 2'-MOE in 3',5'-linked analogs 2'-MOE-A3(3',5') (3) and 2'-MOE-A4(3',5') (4) is weaker in comparison with 3'-OH group in the corresponding ribo analogs. Beta(t), gamma+ and epsilon- rotamers are preferred in both 2',5'- and in 3',5'-linked oligonucleotides 1-4.
The interplay of software bloat, hardware energy proportionality and system bottlenecks (2011)

In large flexible software systems, bloat occurs in many forms, causing excess resource utilization and resource bottlenecks. This results in lost throughput and wasted joules. However, mitigating bloat is not easy; efforts are best applied where savings would be substantial. To aid this we develop an analytical model establishing the relation between bottleneck in resources, bloat, performance and power.
WCDMA and WLAN for 3G and beyond (2002)

The WCDMA air interface was initially designed to support a wide variety of services with different QoS requirements having a maximum bit rate of 2 Mb/s. In order to satisfy the future service and application needs several technical enhancements are being studied and standardized for WCDMA in 3GPP. Even with evolved WCDMA, there is a need for another public wireless access solution to cover the demand for data-intensive applications and enable smooth online access to corporate data services in hot spots. This need could be fulfilled by WLAN together with a high-data-rate cellular WCDMA system. WLAN offers an interesting possibility for cellular operators to offer additional capacity and higher bandwidths for end users without sacrificing the capacity of cellular users. The evolved WCDMA air interface will provide better performance and higher bit rates than basic WCDMA, based on first releases of the specifications. Eventually, evolution may not be the answer to all the needs, and come revolutionary concepts need to be considered. However, before some future wireless system can be regarded as belonging to 4G it must possess capabilities that by far exceed those of 3G systems like WCDMA. Judging from an application and services point of view, one distinguishing factor between 3G and 4G will still be the data rate. We could define that 4G should support at least 100 Mb/s peak data rates in full-mobility wide area coverage and 1 Gb/s in low-mobility local area coverage. Other possible characteristics of 4G need to be further studied.
Structure of Nodules Formed by Rhizobium Strain ANU289 in the Nonlegume Parasponia and the Legume Siratro (Macroptilium atropurpureum) (1984)

A study of root nodules produced by Rhizobium strain ANU289 in the legume siratro (Macroptilium atropurpureum) and the nonlegume Parasponia rigida showed that the legume nodule has a "typical" tropical legume nodule morphology: spherical determinate nodules with a peripheral vascular system. The invaded zone contains both infected hypertrophied cells and small uninfected starch-containing interstitial cells. All infected cells are at a comparable developmental stage. The bacteroids are packaged in the peribacteroid membrane that is of plant origin. Typically three to four bacteroids are found per enveloping membrane. The nonlegume nodule is a modified lateral root with multiple regions of apical meristematic activity; the nodule is indeterminate and has a centralized vascular system. Developmentally, the infected cells vary; the mature, fully infected cells are most distant from the meristem. The bacteroids are not released from the membrane-bound infection thread, which appears to develop into a lightly staining, thin-walled thread (the "fixation" thread) that contains numerous, loosely packed bacteroids, often with significant deposits of polybetahydroxybutyrate. The morphology of the bacteroids is similar in both nodule types, which are capable of high rates of acetylene reduction.
Virus-like particles of the Ty3 retrotransposon assemble in association with P-body components (2005)

Retroviruses and retrotransposons assemble intracellular immature core particles around a RNA genome, and nascent particles collect in association with membranes or as intracellular clusters. How and where genomic RNA are identified for retrovirus and retrotransposon assembly, and how translation and assembly processes are coordinated is poorly understood. To understand this process, the subcellular localization of Ty3 RNA and capsid proteins and virus-like particles was investigated. We demonstrate that mRNAs, proteins, and virus-like particles of the yeast Ty3 retrotransposon accumulate in association with cytoplasmic P-bodies, which are sites of mRNA translation repression, storage, and degradation. Deletions of genes encoding P-body proteins decreased Ty3 transposition and caused changes in the pattern of Ty3 foci, underscoring the biological significance of the association of Ty3 virus-like protein components and P-bodies. These results suggest the hypothesis that P-bodies may serve to segregate translation and assembly functions of the Ty3 genomic RNA to promote assembly of virus-like particles. Because Ty3 has features of a simple retrovirus and P-body functions are conserved between yeast and metazoan organisms, these findings may provide insights into host factors that facilitate retrovirus assembly.
Detection of "Solo Intervals" in Multiple Microphone Multiple Source Audio Applications (2011)

The papers at this Convention have been selected on the basis of a submitted abstract and extended precis that have been peer reviewed by at least two qualified anonymous reviewers. This convention paper has been reproduced from the author’s advance manuscript, without editing, corrections, or consideration by the Review Board. The AES takes no responsibility for the contents. Additional papers may be obtained by sending request and remittance to Audio
Automated quantification of renal fibrosis with Sirius Red and polarization contrast microscopy (2014)

Interstitial fibrosis is commonly measured by histology. The Masson trichrome stain is widely used, with semiquantitative scores subjectively assigned by trained operators. We have developed an objective technique combining Sirius Red staining, polarization contrast microscopy, and automated analysis. Repeated analysis of the same sections by the same operator (r = 0.99) or by different operators (r = 0.98) was highly consistent for Sirius Red, while Masson trichrome performed less consistently (r = 0.61 and 0.72, respectively). These techniques performed equally well when comparing sections from the left and right kidneys of mice. Poor correlation between Sirius Red and Masson trichrome may reflect different specificities, as enhanced birefringence with Sirius Red staining is specific for collagen type I and III fibrils. Combining whole-section imaging and automated image analysis with Sirius Red/polarization contrast is a rapid, reproducible, and precise technique that is complementary to Masson trichrome. It also prevents biased selection of fields as fibrosis is measured on the entire kidney section. This new tool shall enhance our search for novel therapeutics and noninvasive biomarkers for fibrosis.
Considerations for high-numerical aperture EUV lithography (2013)

With numerical apertures &gt; 0.4 there will be broad ranges of angles of incidence of light on masks for EUV systems with 4&times; lens reduction, leading to several undesirable consequences with current MoSi multilayers and tantalum-based absorbers. An option for reducing the range of incident angles is to increase the lens reduction, but this entails small field sizes with standard 6" mask form factors or necessitates the use of larger masks sizes. Small fields lead to a need for stitching or accepting substantially reduced throughput - a problem for a technology already challenged with respect to cost-of-ownership. The implementation of larger mask formats is straightforward but requires considerable investments in new tools for mask making. New absorbers may provide a solution for high-NA EUV lithography at 4&times; lens reduction, but much R&amp;D is required to demonstrate that this approach will work.
Reshaping EDA for power (2003)

Today's rising power densities have been widely cited as the foremost challenge to continued CMOS scaling. In fact, the current power crisis is reminiscent of the final days previous technologies, such as the once popular bipolar and NMOS technologies and even vacuum tubes. How CMOS technology will respond to the current power challenge to extend CMOS scaling to sub-90nm technology is an important question for designer and CAD tool developers alike. With aggressive scaling a number of new challenges have arisen, such as leakage control, heat removal and power supply distribution, that need to be addressed using new design techniques in conjunction with new CAD solutions.This panel brings together experts in circuit design and CAD tool development to discuss the current status of low-power design and provide opinions on what new EDA capabilities are most important in the power-constrained design era. For instance, how will power be distributed in a robust fashion in sub-90nm ICs, and what are the critical EDA analysis and optimization capabilities? What are the best techniques for leakage reduction, not only in standby modes, but also in the active mode? And how far will voltage scaling take us in attacking the dynamic power consumption issue? What will a power-centric design flow look like and how will it change the way we design ICs? The objective of the panel is to explore these issues and formulate a list of critical issues that need to be addressed by the EDA community to enable successful scaling of CMOS into the sub-90nm era.
Efficiency of microlens arrays for projection LCD (2002)

The properties relevant to the use of a microlens array in a projection LCD device are examined and discussed. In particular, the effect of the lens geometry, shape, focal length, cover glass thickness, and beam spread angle, are related to the optical performance as measured by the improvement in light transmission through the LCD. Experimental data suggest that the performance of a lens array with hexagonal cross-section and a focal length of 0.7 mm can lead to an 80% increase in the light through-put.< <ETX xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">&gt;</ETX>
Abstract 55: Use of a Novel Electrogram Filter to Visualise the Conduction Tissue Signals in the Ventricle in Sinus Rhythm and Arrhythmia: Canine Studies (2017)

Background: Conduction tissue in the ventricles is closely intertwined with myocardium. Owing to high velocity of conduction, there is near simultaneous activation , making it difficult to discern. Restricted sampling rates and limited dynamic range make real time signal processing challenging for these signals in routine recording systems. Objectives: We aimed to use novel signal processing techniques in a new system to isolate the conduction tissue signals from the rest of the myocardial activation. Methods: We used the PURE-EP™ (BioSig Technologies, MN) signal processing system to record endocardial and epicardial signals from 6 anesthetized canines in an acute study setting. A novel filter based on proprietary algorithms to isolate the high frequency signal was applied at sites where the electrogram signals were thought to have a conduction tissue component to them. . In addition, ventricular fibrillation (VF) was induced at the end of the experiment and signals were then recorded from the endocardium and the conduction system. Results: This filter was successfully able to isolate conduction tissue signals in the myocardium from those of the ventricular muscle. It did over sense atrial signals at the basal left ventricular septum owing to the high frequency components of the atrial signal at this location. When applied to epicardial signals, it did not pick up any conduction tissue signals. In VF, we could discern signals originating from the conduction system endocardially. (Figure 1) Conclusions: This filter can isolate conduction tissue signals from those of the myocardium and may prove to be a useful adjunct in mapping arrhythmias originating near the conduction system.
Thermal Management for the HEV Liquid-Cooled Electric Machine (2001)

&lt;div class="htmlview paragraph"&gt;The future of the Hybrid Electric Vehicle (HEV) is very promising for the automotive industry. In order to take a full advantage of this concept, a better thermal performance of the electric motor is required. In this study, Computational Fluid Dynamics (CFD) model was first verified through several prototypes testing and then is going to be used to execute a series of design of experiment via simulation. Based on the thermal studies in this paper, the integrated coolant jacket design has a better performance than that of separated one. The thermal performance of the stator with the 3M coating is better than the one with paper liner. In addition, using 3M coating reduces the packaging size of the stator.&lt;/div&gt;
A monolithic capacitive pressure sensor with pulse-period output (1980)

A batch-fabricated 2.8 × 3.4mm monolithic capacitive pressure sensor, replacing piezoresistive pressure transducers, employing on-chip (less than 10mm <sup xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">2</sup> ) circuitry, with current drain of 20μA operating at 2.5-20V, will be reported.
Fresnel rhombs as achromatic phase shifters for infrared nulling interferometry (2007)

We propose a new family of achromatic phase shifters for infrared nulling interferometry. These key optical components can be seen as optimized Fresnel rhombs, using the total internal reflection phenomenon, modulated or not. The total internal reflection indeed comes with a phase shift between the polarization components of the incident light. We propose a solution to implement this vectorial phase shift between interferometer arms to provide the destructive interference process needed to disentangle highly contrasted objects from one another. We also show that, modulating the index transition at the total internal reflection interface allows compensating for the intrinsic material dispersion in order to make the subsequent phase shift achromatic over especially broad bands. The modulation can be induced by a thin film of a well-chosen material or a subwavelength grating whose structural parameters are thoroughly optimized. We present results from theoretical simulations together with preliminary fabrication outcomes and measurements for a prototype in Zinc Selenide.
A Finitist's Manifesto: Do we need to Reformulate the Foundations of Mathematics? (2020)

There is a problem with the foundations of classical mathematics, and potentially even with the foundations of computer science, that mathematicians have by-and-large ignored. This essay is a call for practicing mathematicians who have been sleep-walking in their infinitary mathematical paradise to take heed. Much of mathematics relies upon either (i) the "existence'" of objects that contain an infinite number of elements, (ii) our ability, "in theory", to compute with an arbitrary level of precision, or (iii) our ability, "in theory", to compute for an arbitrarily large number of time steps. All of calculus relies on the notion of a limit. The monumental results of real and complex analysis rely on a seamless notion of the "continuum" of real numbers, which extends in the plane to the complex numbers and gives us, among other things, "rigorous" definitions of continuity, the derivative, various different integrals, as well as the fundamental theorems of calculus and of algebra -- the former of which says that the derivative and integral can be viewed as inverse operations, and the latter of which says that every polynomial over $\mathbb{C}$ has a complex root. This essay is an inquiry into whether there is any way to assign meaning to the notions of "existence" and "in theory'" in (i) to (iii) above.
Interferometric fiber sensor for high-speed railway pantograph monitoring (2008)

A new optical fiber sensor is proposed to monitor pantograph strain in high-speed railway. The sensor is based on a Michelson’s interferometer with a 3x3 coupler and employs standard 1550nm optical communications. The use optical fiber ensures excellent thermal and electrical insulation and allows non-invasive measures. A test rig simulating experimentally the pantograph-catenary contact force validates the sensor performance compared with standard electric sensors.
Radio frequency noise measurements and models for indoor wireless communications at 918 MHz, 2.44 GHz, and 4.0 GHz (2002)

The authors describe average and impulsive noise measurements inside several office buildings and retail stores. The receiver had a 70 dB dynamic range and operated at 918 MHz, 2.44 GHz, and 4.0 GHz with a nominal 40 MHz 3 dB RF bandwidth. Omni-directional and directional antennas were used to investigate the characteristics and sources of RF noise in indoor channels. Statistical analyses of the measurements are presented in the form of noise level distributions, amplitude probability distributions, pulse duration distributions, and interarrival time distributions. These analyses indicate that photocopiers, printers (line printers and cash register receipt printers), elevators, and microwave ovens are significant sources of impulsive noise in office and retail environments.< <ETX xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">&gt;</ETX>