gebhart/patrepeval huggingface dataset:
Discovery of a Novel Series of CRTH2 (DP2) Receptor Antagonists Devoid of Carboxylic Acids (2011)

Antagonism of the CRTH2 receptor represents a very attractive target for a variety of allergic diseases. Most CRTH2 antagonists known to date possess a carboxylic acid moiety, which is essential for binding. However, potential acid metabolites O-acyl glucuronides might be linked to idiosynchratic toxicity in humans. In this communication, we describe a new series of compounds that lack the carboxylic acid moiety. Compounds with high affinity (Ki < 10 nM) for the receptor have been identified. Subsequent optimization succeeded in reducing the high metabolic clearance of the first compounds in human and rat liver microsomes. At the same time, inhibition of the CYP isoforms was optimized, giving rise to stable compounds with an acceptable CYP inhibition profile (IC50 CYP2C9 and 2C19 > 1 μM). Taken together, these data show that compounds devoid of carboxylic acid groups could represent an interesting alternative to current CRTH2 antagonists in development.
An Experimental Digital Image Processor (1986)

A prototype digital image processor for enhancing photographic images has been built in the Research Laboratories at Kodak. This image processor implements a particular version of each of the following algorithms: photographic grain and noise removal, edge sharpening, multidimensional image-segmentation, image-tone reproduction adjustment, and image-color saturation adjustment. All processing, except for segmentation and analysis, is performed by massively parallel and pipelined special-purpose hardware. This hardware runs at 10 MHz and can be adjusted to handle any size digital image. The segmentation circuits run at 30 MHz. The segmentation data are used by three single-board computers for calculating the tonescale adjustment curves. The system, as a whole, has the capability of completely processing 10 million three-color pixels per second. The grain removal and edge enhancement algorithms represent the largest part of the pipelined hardware, operating at over 8 billion integer operations per second. The edge enhancement is performed by unsharp masking, and the grain removal is done using a collapsed Walsh-hadamard transform filtering technique (U.S. Patent No. 4549212). These two algo-rithms can be realized using four basic processing elements, some of which have been imple-mented as VLSI semicustom integrated circuits. These circuits implement the algorithms with a high degree of efficiency, modularity, and testability. The digital processor is controlled by a Digital Equipment Corporation (DEC) PDP 11 minicomputer and can be interfaced to electronic printing and/or electronic scanning de-vices. The processor has been used to process over a thousand diagnostic images.
ES4: Fusion of MEMS and circuits (2010)

In recent times, the market for sensor applications that use MEMS (accelerator, gas, pressure, etc.) has greatly expanded. In the future, MEMS devices are expected to provide innovations for new chip functions and to enable the “More than Moore” era.
Dynamic nature of the aortic regurgitant orifice area during diastole in patients with chronic aortic regurgitation. (1994)

The effective regurgitant orifice area decreases during diastole in patients with chronic aortic regurgitation. This phenomenon should be considered when evaluating aortic regurgitant severity.
YB‐1 is upregulated during prostate cancer tumor progression and increases P‐glycoprotein activity (2004)

We hypothesize that early in prostate cancer progression, increased expression of YB-1 may increase P-gp activity which may in turn lower androgen levels in the prostate tumor cells. Suppression of androgen levels may activate cell survival pathways and lead to an adaptive survival advantage of androgen independent prostate cancer cells following androgen ablation therapy.
Absent CNKSR2 causes seizures and intellectual, attention, and language deficits (2014)

Synaptic function is central to brain function. Understanding the synapse is aided by studies of patients lacking individual synaptic proteins. Common neurological diseases are genetically complex. Their understanding is likewise simplified by studies of less common monogenic forms. We detail the disease caused by absence of the synaptic protein CNKSR2 in 8 patients ranging from 6 to 62 years old. The disease is characterized by intellectual disability, attention problems, and abrupt lifelong language loss following a brief early childhood epilepsy with continuous spike-waves in sleep. This study describes the phenotype of CNKSR2 deficiency and its involvement in systems underlying common neurological disorders.
GNSS signal-based snow water equivalent determination for different snowpack conditions along a steep elevation gradient (2022)

Abstract. Snow water equivalent (SWE) can be measured using low-cost Global Navigation Satellite System (GNSS) sensors with one antenna placed below the snowpack and another one serving as a reference above the snow. The underlying GNSS signal-based algorithm for SWE determination for dry- and wet-snow conditions processes the carrier phases and signal strengths and additionally derives liquid water content (LWC) and snow depth (HS). So far, the algorithm was tested intensively for high-alpine conditions with distinct seasonal accumulation and ablation phases. In general, snow occurrence, snow amount, snow density and LWC can vary considerably with climatic conditions and elevation. Regarding alpine regions, lower elevations mean generally earlier and faster melting, more rain-on-snow events, and shallower snowpack. Therefore, we assessed the applicability of the GNSS-based SWE measurement at four stations along a steep elevation gradient (820, 1185, 1510 and 2540 m a.s.l.) in the eastern Swiss Alps during two winter seasons (2018–2020). Reference data of SWE, LWC and HS were collected manually and with additional automated sensors at all locations. The GNSS-derived SWE estimates agreed very well with manual reference measurements along the elevation gradient, and the accuracy (RMSE = 34 mm, RMSRE = 11 %) was similar under wet- and dry-snow conditions, although significant differences in snow density and meteorological conditions existed between the locations. The GNSS-derived SWE was more accurate than measured with other automated SWE sensors. However, with the current version of the GNSS algorithm, the determination of daily changes of SWE was found to be less suitable compared to manual measurements or pluviometer recordings and needs further refinement. The values of the GNSS-derived LWC were robust and within the precision of the manual and radar measurements. The additionally derived HS correlated well with the validation data. We conclude that SWE can reliably be determined using low-cost GNSS sensors under a broad range of climatic conditions, and LWC and HS are valuable add-ons.
Cryptographic Trust Management System Design Document (2010)

Deliverable for DOE NSTB Cryptographic Trust Management project. Design document to follow the Requirements document submitted in Sept 2009.
Tensile-Strained Germanium-on-Insulator Substrate Fabrication for\n Silicon-Compatible Optoelectronics (2011)

We present a method to fabricate tensile-strained germanium-on-insulator\n(GOI) substrates using heteroepitaxy and layer transfer techniques. The\nmotivation is to obtain a high-quality wafer-scale GOI platform suitable for\nsilicon-compatible optoelectronic device fabrication. Crystal quality is\nassessed using X-Ray Diffraction (XRD) and Transmission Electron Microscopy. A\nbiaxial tensile film strain of 0.16% is verified by XRD. Suitability for device\nmanufacturing is demonstrated through fabrication and characterization of\nmetal-semiconductor-metal photodetectors that exhibit photoresponse beyond 1.55\n{\\mu}m. The substrate fabrication process is compatible with complementary\nmetal-oxide-semiconductor manufacturing and represents a potential route to\nwafer-scale integration of silicon-compatible optoelectronics.\n
Long-term dopamine neurochemical monitoring in primates (2017)

Many debilitating neuropsychiatric and neurodegenerative disorders are characterized by dopamine neurotransmitter dysregulation. Monitoring subsecond dopamine release accurately and for extended, clinically relevant timescales is a critical unmet need. Especially valuable has been the development of electrochemical fast-scan cyclic voltammetry implementing microsized carbon fiber probe implants to record fast millisecond changes in dopamine concentrations. Nevertheless, these well-established methods have only been applied in primates with acutely (few hours) implanted sensors. Neurochemical monitoring for long timescales is necessary to improve diagnostic and therapeutic procedures for a wide range of neurological disorders. Strategies for the chronic use of such sensors have recently been established successfully in rodents, but new infrastructures are needed to enable these strategies in primates. Here we report an integrated neurochemical recording platform for monitoring dopamine release from sensors chronically implanted in deep brain structures of nonhuman primates for over 100 days, together with results for behavior-related and stimulation-induced dopamine release. From these chronically implanted probes, we measured dopamine release from multiple sites in the striatum as induced by behavioral performance and reward-related stimuli, by direct stimulation, and by drug administration. We further developed algorithms to automate detection of dopamine. These algorithms could be used to track the effects of drugs on endogenous dopamine neurotransmission, as well as to evaluate the long-term performance of the chronically implanted sensors. Our chronic measurements demonstrate the feasibility of measuring subsecond dopamine release from deep brain circuits of awake, behaving primates in a longitudinally reproducible manner.
PPARα Deficiency in Inflammatory Cells Suppresses Tumor Growth (2007)

Inflammation in the tumor bed can either promote or inhibit tumor growth. Peroxisome proliferator-activated receptor (PPAR)alpha is a central transcriptional suppressor of inflammation, and may therefore modulate tumor growth. Here we show that PPARalpha deficiency in the host leads to overt inflammation that suppresses angiogenesis via excess production of the endogenous angiogenesis inhibitor thrombospondin-1 and prevents tumor growth. Bone marrow transplantation and granulocyte depletion show that PPARalpha expressing granulocytes are necessary for tumor growth. Neutralization of thrombospondin-1 restores tumor growth in PPARalpha-deficient mice. These findings suggest that the absence of PPARalpha activity renders inflammatory infiltrates tumor suppressive and, thus, may provide a target for inhibiting tumor growth by modulating stromal processes, such as angiogenesis.
Charakterisierung und Einfluss des intraoperativen Gallengang- und Pankreasgang-Abstrich auf den postoperativen Verlauf nach Pankreaskopfresektion bei malignen Tumoren der periampullären Region (2018)

Bei Patienten mit Tumoren der periampullären Region besteht ein erhöhtes Risiko für einen Verschlussikterus und damit einer bakteriellen Kolonisation von Gallengang- und Pankreasgangsekret. Es liegen keine Studien vor, die die Art der bakteriellen Kolonisation differenzieren.
Quantum Annealing amid Local Ruggedness and Global Frustration (2019)

A recent Google study [Phys. Rev. X, 6:031015 (2016)] compared a D-Wave 2X quantum processing unit (QPU) to two classical Monte Carlo algorithms: simulated annealing (SA) and quantum Monte Carlo (QMC). The study showed the D-Wave 2X to be up to 100 million times faster than the classical algorithms. The Google inputs are designed to demonstrate the value of collective multiqubit tunneling, a resource available to D-Wave QPUs but not to simulated annealing. But the computational hardness in these inputs is highly localized in gadgets, with only a small amount of complexity coming from global interactions, meaning that the relevance to real-world problems is limited. In this study we provide a new synthetic problem class that addresses the limitations of the Google inputs while retaining their strengths. We use simple clusters instead of more complex gadgets and more emphasis is placed on creating computational hardness through frustrated global interactions like those seen in interesting real-world inputs. The logical problems used to generate these inputs can be solved in polynomial time [J. Phys. A, 15:10 (1982)]. However, for general heuristic algorithms that are unaware of the planted problem class, the frustration creates meaningful difficulty in a controlled environment ideal for study. We use these inputs to evaluate the new 2000-qubit D-Wave QPU. We include the HFS algorithm---the best performer in a broader analysis of Google inputs---and we include state-of-the-art GPU implementations of SA and QMC. The D-Wave QPU solidly outperforms the software solvers: when we consider pure annealing time (computation time), the D-Wave QPU reaches ground states up to 2600 times faster than the competition. In the task of zero-temperature Boltzmann sampling from challenging multimodal inputs, the D-Wave QPU holds a similar advantage as quantum sampling bias does not seem significant.
Chymotrypsin Inhibitory Triterpenoids from Silybum marianum. (2006)

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, please click on HTML or PDF.
Analog compressed sensing (2009)

A traditional assumption underlying most data converters is that the signal should be sampled at a rate exceeding twice the highest frequency. Practical signals often posses a sparse structure so that a large part of the bandwidth is not exploited. In this paper, we consider a framework for utilizing this sparsity in order to sample such analog signals at a low rate. By relying on results developed in the context of compressed sensing (CS) of finite-length vectors, we develop a general framework for low-rate sampling of signals in shift-invariant spaces. In contrast to the problems treated in the context of CS, here we explicitly consider sampling of analog signals for which no underlying finite-dimensional model exists.
Subcutaneous implantable cardioverter-defibrillator and drug-induced Brugada syndrome: the importance of repeat morphology analysis during ajmaline challenge (2015)

We report the case of a 65-year-old female without history of significant cardiovascular diseases, referred to our institution because of sudden cardiac arrest due to ventricular fibrillation. At the time of admission, no structural abnormality or coronary artery disease was documented. Her baseline ECG showed normal PR, QRS, and QT interval ( Panel A ) and signs of early repolarization …
Optimizing an Intermittent Stretch Paradigm Using ERK1/2 Phosphorylation Results in Increased Collagen Synthesis in Engineered Ligaments (2011)

Dynamic mechanical input is believed to play a critical role in the development of functional musculoskeletal tissues. To study this phenomenon, cyclic uniaxial mechanical stretch was applied to engineered ligaments using a custom-built bioreactor and the effects of different stretch frequency, amplitude, and duration were determined. Stretch acutely increased the phosphorylation of p38 (3.5±0.74-fold), S6K1 (3.9±0.19-fold), and ERK1/2 (2.45±0.32-fold). The phosphorylation of ERK1/2 was dependent on time, rather than on frequency or amplitude, within these constructs. ERK1/2 phosphorylation was similar following stretch at frequencies from 0.1 to 1 Hz and amplitudes from 2.5% to 15%, whereas phosphorylation reached maximal levels at 10 min of stretch and returned toward basal within 60 min of stretch. Following a single 10-min bout of cyclic stretch, the cells remained refractory to a second stretch for up to 6 h. Using the phosphorylation of ERK1/2 as a guide, the optimum stretch paradigm was hypothesized to be 10 min of stretch at 2.5% of resting length repeated every 6 h. Consistent with this hypothesis, 7 days of stretch using this optimized intermittent stretch program increased the collagen content of the grafts more than a continuous stretch program (CTL=3.1%±0.44%; CONT=4.8%±0.30%; and INT=5.9%±0.56%). These results suggest that short infrequent bouts of loading are optimal for improving engineered tendon and ligament physiology.
Biomass pyrolysis: Thermal decomposition mechanisms of furfural and benzaldehyde (2013)

The thermal decompositions of furfural and benzaldehyde have been studied in a heated microtubular flow reactor. The pyrolysis experiments were carried out by passing a dilute mixture of the aromatic aldehydes (roughly 0.1%-1%) entrained in a stream of buffer gas (either He or Ar) through a pulsed, heated SiC reactor that is 2-3 cm long and 1 mm in diameter. Typical pressures in the reactor are 75-150 Torr with the SiC tube wall temperature in the range of 1200-1800 K. Characteristic residence times in the reactor are 100-200 μsec after which the gas mixture emerges as a skimmed molecular beam at a pressure of approximately 10 μTorr. Products were detected using matrix infrared absorption spectroscopy, 118.2 nm (10.487 eV) photoionization mass spectroscopy and resonance enhanced multiphoton ionization. The initial steps in the thermal decomposition of furfural and benzaldehyde have been identified. Furfural undergoes unimolecular decomposition to furan + CO: C4H3O-CHO (+ M) → CO + C4H4O. Sequential decomposition of furan leads to the production of HC≡CH, CH2CO, CH3C≡CH, CO, HCCCH2, and H atoms. In contrast, benzaldehyde resists decomposition until higher temperatures when it fragments to phenyl radical plus H atoms and CO: C6H5CHO (+ M) → C6H5CO + H → C6H5 + CO + H. The H atoms trigger a chain reaction by attacking C6H5CHO: H + C6H5CHO → [C6H6CHO]* → C6H6 + CO + H. The net result is the decomposition of benzaldehyde to produce benzene and CO.
Advances in diode laser bar power and reliability for multi-kW disk laser pump sources (2020)

The industrial laser market has rapidly expanded over the past decade with the emergence of advanced high brightness solid state laser technology. Thin disk laser systems are important examples of these powerful tools enabling a range of high-end CW materials processing applications such as 2D sheet metal cutting and remote welding applications, and the rising demand for a range of demanding high-energy pulsed applications of high average power. Commercial applications with power in the range of 8 kW- 20 kW can be cost competitive using disk lasers in moderate volumes compared to more commoditized solid-state laser sources such as fiber lasers. Reduction in the cost structure of disk laser pump sources requires an increase in brightness, efficiency and power of diode lasers bars within. Here we show the development of thin disk laser pump modules from an original common cooler platform with ~180 W per laser bar to recently developed individually cooled laser bars each operating continuously over 300 W. We demonstrate pump modules utilizing these bars with total power of up to 2.4 kW at 940 nm. Cooling in such laser modules is provided by mounting laser bars on isolated laser coolers (ILASCO). The ILASCO cooler comprises a multi-layer structure of aluminum nitride and copper sheets that are designed to decouple the direct current path from the water cooling eliminate electro-corrosion and to maximize heat dissipation and match the thermal expansion of the diode laser bar. We demonstrate advances in the single quantum well InGaAs/AlGaAs laser epitaxy design and chip layout that enables high power operation at operating temperatures up to 80°C. We show increase in peak electro-optic efficiencies from 55% to over 60% at this temperature. With the application of advanced facet passivation technology, we demonstrate &gt;35 khr reliable operation in the application through accelerated aging tests.
Single-Conformation and Diastereomer Specific Ultraviolet and Infrared Spectroscopy of Model Synthetic Foldamers: α/β-Peptides (2009)

Resonant two-photon ionization (R2PI), UV hole-burning (UVHB), and resonant ion-dip infrared (RIDIR) spectroscopies have been used to record single-conformation infrared and ultraviolet spectra of three model synthetic foldamers with heterogeneous backbones, alpha/beta-peptides Ac-beta(3)-hAla-L-Phe-NHMe (betaalphaL), Ac-beta(3)-hAla-D-Phe-NHMe (betaalphaD), and Ac-L-Phe-beta(3)-hAla-NHMe (alphabetaL), isolated and cooled in a supersonic expansion. BetaalphaL and betaalphaD are diastereomers, differing only in the configuration of the alpha-amino acid residue; betaalphaL and alphabetaL contain the same residues, but differ in residue order. In all three alpha/beta-peptides the beta(3)-residue has S absolute configuration. UVHB spectroscopy is used to determine that there are six conformers of each molecule and to locate and characterize their S(0)-S(1) transitions in the origin region. RIDIR spectra in the amide NH stretch region reflect the number and strength of intramolecular H-bonds present. Comparison of the RIDIR spectra with scaled, harmonic vibrational frequencies and infrared intensities leads to definite assignments for the conformational families involved. C8/C7(eq) double-ring structures are responsible for three conformers of betaalphaL and four of betaalphaD, including those with the most intense transitions in the R2PI spectra. This preference for C8/C7(eq) double rings appears to be dictated by the C7(eq) ring of the alpha-peptide subunit. Three of the conformers of betaalphaL and betaalphaD form diastereomeric pairs (A/A', C/C', and G/G') that have nearly identical S(0)-S(1) origin positions in the UV and belong to the same conformational family, indicating no significant change associated with the change in chirality of the alpha-peptide subunit. However, betaalphaL favors formation of a C6/C5 conformer over C11, while the reverse preference holds in betaalphaD. Calculations indicate that the selective stabilization of the lowest-energy C11(g(+)) structure in betaalphaD occurs because this structure minimizes steric effects between the beta(2) methylene group and C=O(1). In the alpha/beta-peptide alphabetaL, two conformers dominate the spectrum, one assigned to a C5/C8 bifurcated double-ring, and the other to a C5/C6 double-ring structure. This preference for C5 rings in the alpha/beta-peptide occurs because the C5 ring is further stabilized by an amide NH...pi interaction involving an NH group on the adjacent amide, as it is in the alpha-peptides. Comparison of the NH stretch spectra of C8/C7(eq) structures in betaalphaL with their C7(eq)/C8 counterparts in alphabetaL shows that the central amide NH stretch is shifted to lower frequency by some 50-70 cm(-1) due to cooperative effects associated with the central amide accepting and donating a H-bond to neighboring amide groups. This swaps the ordering of the C8 and C7 NH stretch fundamentals in the two molecules.
On the preparation and structure of some trans-fused ureas: perhydro-trans-thieno[3,4-d]imidazol-2-one SS-dioxides (1972)

Reaction of trans-3,4-dibromotetrahydrothiophen dioxide with methylamine affords trans-tetrahydro-3 4-bis-(methylamino)thiophen dioxide. Reaction with phosgene then gave perhydro-1,3-dimethyl-trans-thieno-[3,4-d]imidazol-2-one SS-dioxide (3; R = Me), which was studied by X-ray crystallography. [Crystal data: a= 8.616(3), b= 15.280(5), c= 7.409(3)Åβ= 102.62(4)°, space group C2/c,Z= 4]. Ammonia gave a similar product. Piperidine also reacted with the dibromide to give the corresponding diamine, whereas pyridine afforded a novel pyridinium salt.
Clinical Course of Unilateral Moyamoya Disease (2021)

Church, Ephraim W MD; Bell-Stephens, Teresa E BSN, RN; Bigder, Mark G MD; Gummidipundi, Santosh MS; Han, Summer S PhD; Steinberg, Gary K MD, PhD
Research Trend on Broadcasting Systems, Broadcasting Facilities and Operations and Radio and Optical Fiber Transmission Systems (2017)

ては HDR (High Dynamic Range) があり，今後の動向が注 目される．