gebhart/patrepeval huggingface dataset:
Structure-activity relationships of 8-styrylxanthines as A2-selective adenosine antagonists (1993)

A series of substituted 8-styryl derivatives of 1,3,7-alkylxanthines was synthesized as potential A2-selective adenosine receptor antagonists, and the potency at rat brain A1- and A2-receptors was studied in radioligand binding experiments. At the xanthine 7-position, only small hydrophobic substituents were tolerated in receptor binding. 7-Methyl analogues were roughly 1 order of magnitude more selective for A2 versus A1 receptors than the corresponding 7-H analogues. 1,3-Dimethylxanthine derivatives tended to be more selective for A2-receptors than the corresponding 1,3-diallyl, diethyl, or dipropyl derivatives. Substitutions of the phenyl ring at the 3-(monosubstituted) and 3,5-(disubstituted) positions were favored. 1,3, 7-Trimethyl-8-(3-chlorostyryl)xanthine was a moderately potent (Ki vs [3H]CGS 21680 was 54 nM) and highly A2-selective (520-fold) adenosine antagonist. 1,3,7-Trimethyl-8-[(3-carboxy-1-oxopropyl)amino] styryl]xanthine was highly A2-selective (250-fold) and of enhanced water solubility (max 19 mM). 1,3-Dipropyl-7-methyl-8-(3,5-dimethoxystyryl) xanthine was a potent (Ki = 24 nM) and very A2-selective (110-fold) adenosine antagonist.
Dental depth profilometric diagnosis of pit and fissure caries using frequency-domain infrared photothermal radiometry and modulated laser luminescence (2004)

Non-intrusive, non-contacting frequency-domain photothermal radiometry (FD-PTR or PTR) and frequency-domain luminescence (FD-LUM or LUM) have been used with 659-nm and 830-nm laser sources to detect artificial and natural sub-surface defects in human teeth. Fifty-two human teeth were examined with simultaneous measurements of PTR and LUM with the 659-nm laser and compared to conventional diagnostic methods including continuous (dc) luminescence (DIAGNOdent), visual inspection and radiographs. To compare each method, sensitivities and specificities were calculated by using histological observations as the gold standard. With the combined criteria of four PTR and LUM signals (two amplitudes and two phases), it was found that the sensitivity of this method was much higher than any of the other methods used in this study, whereas the specificity was comparable to that of dc luminescence diagnostics. Therefore, PTR and LUM, as a combined technique, has the potential to be a reliable tool to diagnose early pit and fissure caries and could provide detailed information about deep lesions with its depth profilometric character. Also, from the experiments with the teeth having natural or aritficial defect, some depth profilometric characteristics were confirmed. The major findings are (i) PTR is sensitive to very deep (>5 mm) defects at low modulation frequencies (5 Hz). Both PTR and LUM amplitudes exhibit a peak at tooth thicknesses ca. 1.4 - 2.7 mm. Furthermore the LUM amplitude exhibits a small trough at ca. 2.5~3.5 mm; (ii) PTR is sensitive to various defects such as a deep carious lesion, a demineralized area, and a crack while LUM exhibits low sensitivity and spatial resolution.
Establishment of macrocyclic lactone resistant Dirofilaria immitis isolates in experimentally infected laboratory dogs (2014)

Strains of Dirofilaria immitis suspected of lack of efficacy (LOE) to macrocyclic lactone (ML) preventive drugs have been increasingly reported in dogs by practicing veterinarians since 2005 in the Lower Mississippi Delta region. If proven, and not controlled in the early stages, the emergence of ML drug resistance threatens to become a widespread problem in the US that may limit the effectiveness of current preventive drug treatment methods. To validate practice reports, a statewide survey of Louisiana veterinarians was done to define the extent of the problem and identify focal `hotspots’ of reported ML LOEs using Geographic Information Systems (GIS) methods. The present study then utilized microfilariae (Mf) from two canine field cases from different state locations that fit criteria for a high index of suspicion of LOE against heartworms by ML drugs. Blood containing Mf from the canine field cases was used to infect and produce L3 in Aedes aegypti for experimental infection of two groups of dogs, each of which contained two laboratory dogs, one treated with prophylactic ivermectin (12 μg/kg) monthly for 6 months at twice the label dose (6 μg/kg), and one untreated control. Both treated and untreated dogs from Group I and Group II developed patent D. immitis infections by 218 DPI and 189 DPI, respectively, as evidenced by a positive occult heartworm antigen test and microfilaremia by the Knott’s test. Mf counts gradually increased post-patency in test and control dogs. Infective larvae raised from microfilariae from the treated Group I dog were used to successfully establish a second generation isolate, confirming heritability of resistance in the face of a monthly ivermectin challenge dose of 24 μg/kg, given monthly for 3 months. These experimental infection studies provide in vivo evidence of the existence of ML drug resistance in dogs infected by D. immitis L3 from suspect field LOE cases in the Lower Mississippi Delta. Results encourage further work on mechanisms underlying the emergence of ML resistance in D. immitis and development of evidence-based resistance management strategies for heartworm preventives in order to extend the useful life of current drugs.
Boron-coated straw detectors: A novel approach for helium-3 neutron detector replacement (2010)

US efforts to equip key points of entry with large area neutron detectors to intercept Special Nuclear Materials (SNM) have been undermined by a critical shortage of <sup xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">3</sup> He gas. Yearly demand for <sup xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">3</sup> He in US security applications alone is roughly 22,000 liters, exceeding current world supply. Neutron science, safeguards, defense, and other applications that depend on <sup xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">3</sup> He detectors have been severely limited as a result. Alternative neutron detection technologies with large sensitive areas, low gamma sensitivity, and low cost are needed to ensure the long term viability of US detection and interdiction capabilities. We propose a technology based on closely-packed arrays of long, 4 mm diameter, aluminum or copper tubes (straws), internally coated with a thin layer of <sup xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">10</sup> B-enriched boron carbide, as a ready replacement for <sup xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">3</sup> He in a variety of detection applications. The high abundance of boron on Earth and low <sup xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">10</sup> B enrichment cost give boron-coated straw (BCS) technology key advantages over <sup xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">3</sup> He detectors. We review three BCS detector configurations including: a large-area neutron-imaging panel, a long range monitor, and a detector module for portal monitors. The imaging panel has 1100 aluminum straws, each 1 m long and 4 mm in diameter. It offers a sensitive area of 1 m <sup xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">2</sup> , 3D spatial resolution of 7×4×4 mm <sup xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">3</sup> , and can sustain count rates up to 200,000 cps for each of its 22 readout channels without significant loss in resolution. The long-range monitor has 1100 copper straws of similar dimensions and has been subjected to rigorous environmental testing. Finally, the portal monitor design adopts the outer dimensions of currently deployed <sup xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">3</sup> He-based designs, but takes advantage of the small straw diameter to achieve more uniform distribution of neutron converter throughout the moderating material.
Compact Ambient Pressure Pyroelectric Ion Source for Mass Spectrometry (2007)

We present the construction and implementation of a compact, low-power ambient pressure pyroelectric ionization source. The source comprises a z-cut lithium niobate or lithium tantalate crystal with an attached resistive heater mounted in front of the atmospheric pressure inlet of an ion trap mass spectrometer. Positive and negative ion formation alternately results from thermally cycling the crystal over a narrow temperature range. Ionization of 1,1,1,3,3,3−hexafluoro-2-propanol or benzoic acid results in the observation of the singly deprotonated species and their clusters in the negative ion mass spectrum. Ionization of triethylamine or triphenylamine with the source results in observation of the corresponding singly protonated species of each in the positive ion mass spectrum. Although processes in which ion formation occurs directly on the highly charged crystal surface may contribute to the observed signal, ion formation appears to result mainly from electrical discharges occurring on the surface of the crystal, from one z face to another. This dielectric breakdown originates from the high electric fields generated at the surface of pyroelectric crystals when they are thermally cycled by as little as 30 K from ambient temperature. Ion formation is largely unaffected by contamination of the crystal faces. This robust source might prove particularly useful in applications where unattended operation in harsh environments, long service lifetimes, and durability are desirable characteristics.
Plasma sweeper. [Patents] (1982)

A device is described for coupling RF power (a plasma sweeper) from RF power introducing means to a plasma having a magnetic field associated therewith comprises at least one electrode positioned near the plasma and near the RF power introducing means. Means are described for generating a static electric field at the electrode directed into the plasma and having a component substantially perpendicular to the plasma magnetic field such that a non-zero vector cross-product of the electric and magnetic fields exerts a force on the plasma causing the plasma to drift.
Iterative Conversion of Cyclin Binding Groove Peptides into Druglike CDK Inhibitors with Antitumor Activity (2014)

The cyclin groove is an important recognition site for substrates of the cell cycle cyclin dependent kinases and provides an opportunity for highly selective inhibition of kinase activity through a non-ATP competitive mechanism. The key peptide residues of the cyclin binding motif have been studied in order to precisely define the structure-activity relationship for CDK kinase inhibition. Through this information, new insights into the interactions of peptide CDK inhibitors with key subsites of the cyclin binding groove provide for the replacement of binding determinants with more druglike functionality through REPLACE, a strategy for the iterative conversion of peptidic blockers of protein-protein interactions into pharmaceutically relevant compounds. As a result, REPLACE is further exemplified in combining optimized peptidic sequences with effective N-terminal capping groups to generate more stable compounds possessing antitumor activity consistent with on-target inhibition of cell cycle CDKs. The compounds described here represent prototypes for a next generation of kinase therapeutics with high efficacy and kinome selectivity, thus avoiding problems observed with first generation CDK inhibitors.
Fabrication and Individual Addressing of STT-MRAM Bit Array With 50 nm Full Pitch (2022)

Spin-transfer torque (STT) magnetic random access memory (MRAM) is gaining commercial traction in low-density embedded and standalone memories, but the available market opportunities would grow exponentially if STT-MRAM could approach dynamic random access memory (DRAM) bit density. Of course, achieving DRAM density will require, among other things, demonstrating the ability to pattern MRAM bits at an extremely tight pitch. Here, an experimental demonstration of fabrication and electrical testing of a STT-MRAM bit array are reported. By optimizing the hard mask and ion beam etching (IBE) processes, MRAM bit arrays with a full pitch down to 50 nm are fabricated, in which the bits are individually tested using a novel bottom-point-contact method.
Non-zero dispersion shifted fiber with low dispersion slope (1999)

A new non-zero-dispersion-shifted fiber design is presented. These fibers, with low dispersion slope of 0.03 ps/nm/sup 2/-km and small negative dispersion from 1530 to 1620 nm, are ideal transmission medium for use in broad band DWDM systems.
Distinct Polyphosphoinositide Binding Selectivities for Pleckstrin Homology Domains of GRP1-like Proteins Based on DiglycineVersus Triglycine Motifs (2000)

GRP1 and the related proteins ARNO and cytohesin-1 are ARF exchange factors that contain a pleckstrin homology (PH) domain thought to target these proteins to cell membranes through binding polyphosphoinositides. Here we show the PH domains of all three proteins exhibit relatively high affinity for dioctanoyl phosphatidylinositol 3,4,5-triphosphate (PtdIns(3,4,5)P(3)), with K(D) values of 0.05, 1.6 and 1.0 micrometer for GRP1, ARNO, and cytohesin-1, respectively. However, the GRP1 PH domain was unique among these proteins in its striking selectivity for PtdIns(3,4, 5)P(3) versus phosphatidylinositol 4,5-diphosphate (PtdIns(4,5)P(2)), for which it exhibits about 650-fold lower apparent affinity. Addition of a glycine to the Gly(274)-Gly(275) motif in GRP1 greatly increased its binding affinity for PtdIns(4,5)P(2) with little effect on its binding to PtdIns(3,4,5)P(3), while deletion of a single glycine in the corresponding triglycine motif of the ARNO PH domain markedly reduced its binding affinity for PtdIns(4,5)P(2) but not for PtdIns(3,4,5)P(3). In intact cells, the hemagglutinin epitope-tagged PH domain of GRP1 was recruited to ruffles in the cell surface in response to insulin, as were full-length GRP1 and cytohesin-1, but the PH domain of cytohesin-1 was not. These data indicate that the unique diglycine motif in the GRP1 PH domain, as opposed to the triglycine in ARNO and cytohesin-1, directs its remarkable PtdIns(3,4,5)P(3) binding selectivity.
Deciphering 3D Human Sphygmopalpation Pulse Patterns using “X-ray” Images Acquired from Tactile Robotic Fingers (2021)

ABSTRACT Sphygmopalpation at specific locations of human wrists has been used as a medical measurement technique in China since the Han Dynasty (202 BC - 220 AD); it is now generally accepted that traditional Chinese medicine (TCM) doctors are able to decipher 28 types of basic pulse patterns using their fingertips. This TCM technique of examining individual arterial pulses by palpation has undergone an upsurge recently in popularity as a low-cost and non-invasive diagnostic technique for monitoring patient health status. We have developed a pulse sensing platform for studying and digitalizing arterial pulse patterns via a TCM approach. This platform consists of a robotic hand with three fingers for pulse measurement and an artificial neural network (ANN) together with pulse signal preprocessing for pulse pattern recognition. The platforms previously reported by other research groups or marketed commercially exhibit one or more of the following imperfections: a single channel for data acquisition, low sensitivity and rigid sensors, lack of control of the applied pressure, and in many reported works, lack of an intelligent data analysis system. The platform presented here features up to three-dimensional (3D) tactile sensing channels for recording data and uses highly sensitive capacitive MEMS (microelectromechanical systems) flexible sensing arrays, pressure-feedback-controlled robotic fingers, and machine learning algorithms. We also proposed a methodology of obtaining “X-ray” image of pulse information constructed based on the sensing data from 3 locations and 3 applied pressures (i.e., mimicking TCM doctors), which contains all arterial pulse information in both spatial and temporal spans, and which could be used as an input to a deep learning algorithm. By applying our developed platform and algorithms, 3 types of consistent pulse patterns, i.e., “Hua” , “Xi” , and “Chen” , as described by TCM doctors”, could be identified in a selected group of 3 subjects who were diagnosed by TCM practitioners. We have shown the classification rates is 98.7% in training process and 84.2% in testing result for these 3 basic pulse patterns. The high classification rate of the developed platform could lead to further development of a high-level artificial intelligence system incorporating knowledge from TCM – the robotics finger system could become a standard clinical equipment for digitalizing and visualizing human arterial pulses
Star-Structured High-Order Heterogeneous Data Co-clustering Based on Consistent Information Theory (2006)

Heterogeneous object co-clustering has become an important research topic in data mining. In early years of this research, people mainly worked on two types of heterogeneous data (denoted by pair-wise co-clustering); while recently more and more attention was paid to multiple types of heterogeneous data (denoted by high- order co-clustering). In this paper, we studied the high- order co-clustering of objects with star-structured interrelationship, i.e., there is a central type of objects that connects the other types of objects. Actually, this case could be a very good model for many real-world applications, such as the co-clustering of Web images, their low-level visual features, and the surrounding text. We used a tripartite graph to represent the interrelationships among different objects, and proposed a consistent information theory which generates an effective algorithm to obtain the co-clusters of different types of objects. Experiments on a Web image show that our proposed algorithm is a better choice compared with previous work on heterogeneous object co-clustering.
High‐lysine corn produced by the combination of enhanced lysine biosynthesis and reduced zein accumulation (2005)

Corn is one of the major crops in the world, but its low lysine content is often problematic for animal consumption. While exogenous lysine supplementation is still the most common solution for today's feed corn, high-lysine corn has been developed through genetic research and biotechnology. Reducing the lysine-poor seed storage proteins, zeins, or expressing a deregulated lysine biosynthetic enzyme, CordapA, has shown increased total lysine or free lysine content in the grains of modified corn plants, respectively. Here, by combining these two approaches through genetic crosses, the total lysine content has more than doubled in F1 progeny. We also observe a synergy between the transgenic zein reduction and the enhanced lysine biosynthesis by CordapA expression. The zein reduction plants are found to accumulate higher levels of aspartate, asparagine and glutamate, and therefore, provide excess precursors for the enhanced lysine biosynthesis.
Flexible Composite Piezoelectric Sensors (1984)

The piezoelectric properties of several different composites with 0-3 connectivity are reviewed. In these composites a piezoelectric ceramic powder such as PbZr1-,Tix03 (PZT), PbTi03 or Pbl-xBixTil-TFex03 is used as a filler in a polymer matrix. The values of hydrostatic voltage coefficient ih of these composites are higher than the corresponding properties of single phase materials. Composites with PbTi03 or (Pb.Bi)(Ti.Fe)03 as fillers have higher piezoelectric voltage coefficients than PZTpolymer composites because of the greater anisotropy and lower dielectric constants of these systems. By adding a small amount of carbon to the piezoelectric composite, poling can be carried out at much lower voltages and shorter poling times, making it possible to mass produce the composites. Fabrication of 0-3 composites is a
General Reconstruction of Laplacian Pyramid and its Dual Frame Solutions (2007)

The Laplacian pyramid (LP) is a useful tool in image processing and computer vision. It provides an overcomplete signal representation, thus can be treated as a frame operator. In this paper, we first propose a lifting-based factorization for the LP decomposition. Based on such lifting factorization, a parameterization reconstruction algorithm is presented to characterize all synthesis banks yielding the perfect reconstruction property. Compared with other LP reconstruction algorithms in the literature, our proposed reconstruction contains much less number of parameters - the reduction is M times for an LP with the decimation factor of M. For the proposed reconstruction algorithm, noise analysis of the LP is carried out, and the closed-form solutions of the dual frame for any LP are also presented.
Towards a systematic design of novel endogenous peptide‐based antiangiogenic approaches (2008)

To date the quest for the experimental identification of angiogenesis inhibitors has been an empirical time‐consuming process. Selected proteins were proteolytically processed by proteases and the cleaved fragments were tested for their antiangiogenic potency. In this study we introduced a systematic computational and experimental methodology that enabled us to identify and classify novel putative endogenous inhibitors of angiogenesis. The novels peptides are derived from various protein families including thrombospondins, and CXC chemokines, type IV collagen fibrils, as well as coagulation factors, and various kringle‐containing proteins. Testing their activity in vitro in suppressing the proliferation and migration of endothelial cells provided proof of principle for the validity of the computational method. By performing receptor neutralization studies we identified receptors that the novel peptides bind. Using the receptor binding information we designed peptide combinatorial therapeutic strategies. In some cases the combinatorial targeting of specific receptors identified strong synergism. Based on the results from the in vitro screening, we tested the ability of the peptides to suppress angiogenesis in in vivo assays including the subcutaneous basement‐membrane‐extract filled angioreactors assay, the corneal micro‐pocket angiogenesis assay and tumor xenograft models.
microRNAs and the regulation of glucose and lipid metabolism (2007)

Over recent years, metabolic disorders such as type 2 diabetes have finally become recognized as a major challenge to global health. The attention of scientists therefore has to focus on improving our understanding of the molecular mechanisms behind these diseases and towards the design of new drug therapy strategies. The pathophysiology of diabetes is undoubtedly complex, oftentimes characterized by varying states of insulin resistance and impaired beta-cell function; however, the identification of new pathways is constantly improving our understanding of the disease. We and others have recently shown that microRNAs (miRNAs) can play a role in insulin secretion and glucose homostasis. Thus, in this review, we will discuss the potential role of miRNAs in type 2 diabetes and related metabolic diseases.