gebhart/patrepeval huggingface dataset:
Design, Selection, and Characterization of Thioflavin-Based Intercalation Compounds with Metal Chelating Properties for Application in Alzheimer’s Disease (2009)

Metal chelation is considered a rational therapeutic approach for interdicting Alzheimer's amyloid pathogenesis. At present, enhancing the targeting and efficacy of metal-ion chelating agents through ligand design is a main strategy in the development of the next generation of metal chelators. Inspired by the traditional dye Thioflavin-T, we have designed new multifunctional molecules that contain both amyloid binding and metal chelating properties. In silico techniques have enabled us to identify commercial compounds that enclose the designed molecular framework (M1), include potential antioxidant properties, facilitate the formation of iodine-labeled derivatives, and can be permeable through the blood-brain barrier. Iodination reactions of the selected compounds, 2-(2-hydroxyphenyl)benzoxazole (HBX), 2-(2-hydroxyphenyl)benzothiazole (HBT), and 2-(2-aminophenyl)-1H-benzimidazole (BM), have led to the corresponding iodinated derivatives HBXI, HBTI, and BMI, which have been characterized by X-ray diffraction. The chelating properties of the latter compounds toward Cu(II) and Zn(II) have been examined in the solid phase and in solution. The acidity constants of HBXI, HBTI, and BMI and the formation constants of the corresponding ML and ML2 complexes [M = Cu(II), Zn(II)] have been determined by UV-vis pH titrations. The calculated values for the overall formation constants for the ML2 complexes indicate the suitability of the HBXI, HBTI, and BMI ligands for sequestering Cu(II) and Zn(II) metal ions present in freshly prepared solutions of beta-amyloid (Abeta) peptide. This was confirmed by Abeta aggregation studies showing that these compounds are able to arrest the metal-promoted increase in amyloid fibril buildup. The fluorescence features of HBX, HBT, BM, and the corresponding iodinated derivatives, together with fluorescence microscopy studies on two types of pregrown fibrils, have shown that HBX and HBT compounds could behave as potential markers for the presence of amyloid fibrils, whereas HBXI and HBTI may be especially suitable for radioisotopic detection of Abeta deposits. Taken together, the results reported in this work show the potential of new multifunctional thioflavin-based chelating agents as Alzheimer's disease therapeutics.
Recombinant Sendai Virus Vector Induces Complete Remission of Established Brain Tumors through Efficient Interleukin-2 Gene Transfer in Vaccinated Rats (2005)

The present results show that the recombinant nontransmissible SeV vector provides efficient in vivo gene transfer that induces significant regression of the established brain tumors and suggest that it will be a safe and useful viral vector for the clinical practice of glioma gene therapy.
Crystal structure analysis of inclusion crystals with tetrapodal host molecules (2008)

Sessions 6 1 angles in the heterocyclic ring.
Enabling SCMA long codewords with a parallel SCMA coding scheme (2015)

Fifth generation (5G) wireless networks require massive connectivity with a large number of devices and ask for non-orthogonal multiple access which has been proposed as a paradigm shift of physical layer technologies. Among all the existing non-orthogonal technologies where the number of users can be larger than the spreading factor, recently proposed sparse code multiple access (SCMA) is shown to achieve a better link performance. However, the message passing algorithm (MPA) is used in SCMA decoding. And the decoding complexity of SCMA is very high and is increasing exponentially as the dimensions of the codebook increase. From this point of view, implementing SCMA long codewords in a real hardware environment with the high complexity MPA is intractable. A scheme to reduce the decoding complexity of SCMA is essential. In this paper, we propose a parallel SCMA system which can be called SCMA hierarchical coding to come through SCMA long codewords. We try to break the process of the encoding and decoding of a long SCMA codeword into several processes of encoding and decoding of short codewords. We also analyze the tradeoff between the performance and the decoding complexity of the parallel SCMA system. The simulation results show that the parallel SCMA system can greatly reduce the decoding complexity of SCMA long codewords while still keeping higher capacity and lower block error rate compared to long term evolution (LTE) and low density signature (LDS) respectively.
Production of hyaluronic acid derivative microfibers with controlled dimension as potential drug delivery system (2015)

n.a.
Final Report on Key Comparison CCM.P-K7 in the range 10 MPa to 100 MPa of hydraulic gauge pressure (2005)

NRC publication: Yes
1.51-GHz nanocrystalline diamond micromechanical disk resonator with material-mismatched isolating support (2004)

The first CVD nanocrystalline diamond micromechanical disk resonator with material-mismatched stem has been demonstrated at a record frequency of 1.51 GHz with an impressive Q of 11,555, which is more than 7X higher than demonstrated in a previous 1.14-GHz polysilicon disk resonator, and which achieves a frequency-Q product of 1.74/spl times/10/sup 13/ that now exceeds the 1/spl times/10/sup 13/ of some of the best quartz crystals. In addition, a 1.27-GHz version with a Q in the excess of 12,000 exhibits a measured motional resistance of only 100 k/spl Omega/ with a dc-bias voltage of 20 V, which is more than 34X lower than measured on a pure polysilicon counterpart at 1.14 GHz. At 498 MHz, Q's up to 55,300 in vacuum and 35,550 in air have been demonstrated, both of which set frequency-Q product records at 2.75/spl times/10/sup 13/ (vacuum) and 1.77/spl times/10/sup 13/ (air).
Homogeneous alignment of nematic liquid crystals by ion beam etched surfaces (1979)

A wide range of ion beam etch parameters capable of producing uniform homogeneous alignment of nematic liquid crystals on SiO2 films are discussed. The alignment surfaces were generated by obliquely incident (angles of 5 to 25 deg) argon ions with energies in the range of 0.5 to 2.0 KeV, ion current densities of 0.1 to 0.6 mA sq cm and etch times of 1 to 9 min. A smaller range of ion beam parameters (2.0 KeV, 0.2 mA sq cm, 5 to 10 deg and 1 to 5 min.) were also investigated with ZrO2 films and found suitable for homogeneous alignment. Extinction ratios were very high (1000), twist angles were small ( or = 3 deg) and tilt-bias angles very small ( or = 1 deg). Preliminary scanning electron microscopy results indicate a parallel oriented surface structure on the ion beam etched surfaces which may determine alignment.
Oridonin induced apoptosis through Akt and MAPKs signaling pathways in human osteosarcoma cells (2007)

Previous studies have shown that oridonin, a diterpenoid isolated from Rabdosia rubescens, was able to inhibit proliferation and induce apoptosis in several cell types. But the mechanisms remain poorly understood. In this study, we investigated the apoptosis-inducing effect and mechanisms of action of oridonin in human osteosarcoma cells. Our results demonstrated that oridonin induced concentration- and time-dependent suppression of proliferation and activation of apoptosis in U2OS, MG63 and SaOS-2 osteosarcoma cell lines. Oridonin induced the release of cytochrome c accompanied by activation of caspase-9, caspase-3 and cleavage of poly(ADP-ribose) polymerase (PARP). These events were all inhibited by z-VAD-fmk, a universal inhibitor of caspases. Oridonin treatment dephosphorylated constitutively active AKT, FOXO transcription factor, and glycogen synthase kinase 3 (GSK3). In addition, oridonin decreased the phosphorylation of ERK and increased the phosphorylation of p38 MAPK and JNK. Furthermore, oridonin treatment down-regulated the expression of the inhibitor of apoptosis protein(IAP) in osteosarcoma cells. All together, our results suggested that oridonin is able to inactivate Akt and ERK and activate p38 MAPK and JNK signalling pathways in osteosarcoma cells causing the suppression of proliferation and induction of mitochondria- and caspase-dependent apoptosis.
Paradoxical Increase in Methicillin-Resistant Staphylococcus aureus Acquisition Rates Despite Barrier Precautions and Increased Hand Washing Compliance during an Outbreak of Severe Acute Repiratory Syndrome (2005)

10.1086/427150
Ondansetron and metoclopramide as second-line antiemetics in women with nausea and vomiting in pregnancy: the EMPOWER pilot factorial RCT (2021)

This project was funded by the National Institute for Health Research (NIHR) Health Technology Assessment programme and will be published in full in <i>Health Technology Assessment</i>; Vol. 25, No. 63. See the NIHR Journals Library website for further project information.
Flow effects in epitaxial autodoping (1980)

A quantitative model has been developed to account for the flow effects in epitaxial autodoping for chemical-vapor-deposited films. Analytical expressions are derived for the autodoping variations along and against the direction of flow arising from a diffusion stripe in the substrate. These expressions relate the maximum concentration in the lateral autodoping peak to the distance from the autodoping source and to the carrier gas velocity. Experimental verification of the model is obtained for arsenic autodoping in silicon epitaxial films, which indicates that boundary layer effects are not predominant in the autodoping phenomenon. The analysis also yields a value of 2.5 cm2/sec for the arsenic vapor diffusivity in hydrogen at 1150 °C.
Absence of J/pi/, T = 0/+/, 1 level excitations in residual nuclei from /pi /+ or -/,2N/ reactions (1981)

Gamma-ray spectra taken in prompt coincidence with incident 180-MeV pi/+/, 220-MeV pi/-/ and 0-MeV pi/-/ on the self-conjugate targets C-12 and S-32 reveal that the cross sections/yields are equal to or near zero for production of the J/pi/,T = 0/+/, 1 levels of the odd Z, odd N nuclei resulting from np removal. It is thought that the 0-MeV pi/-/ results can be explained by selection rules governing one-step quasi-free interactions but that the delta(1232) region results cannot. This indicates that there may be additional restrictions upon the pion absorption mechanism.
Content aware routing: A content oriented traffic engineering (2013)

Content transfer, e.g. video transfer, is now becoming major traffic in the current Internet. Content transfer originally has a content oriented feature of “wherever content is retrieved, users only take care of what content they obtain”. Conventional traffic engineering aims to obtain optimal routes for traffic between ingress and egress router pairs, which has “location oriented feature, i.e. where to connect”. With content oriented feature of user demand for content traffic, traffic engineering can be changed towards content oriented routing design. In this paper, we propose a novel content oriented traffic engineering, named CAR (Content Aware Routing). In CAR, routes are designed for content and egress router pair, i.e. content traffic towards a receiver-side router. Content demand can be flexibly distributed to multiple servers(repositories) providing the same content, which means content can be obtained from anywhere. With numerical examples by linear programming formulation, we comparatively evaluate CAR with comparing with combination of CDN and traffic engineering, i.e. location oriented designs. Numerical results show that CAR improves maximum link utilization significantly with slight increase of network resource usage.
Quantitative Translation of Microfluidic Transporter in Vitro Data to in Vivo Reveals Impaired Albumin-Facilitated Indoxyl Sulfate Secretion in Chronic Kidney Disease (2019)

Indoxyl sulfate (IxS), a highly albumin-bound uremic solute, accumulates in chronic kidney disease (CKD) due to reduced renal clearance. This study was designed to specifically investigate the role of human serum albumin (HSA) in IxS renal secretion via organic anion transporter 1 (OAT1) in a microfluidic system and subsequently apply quantitative translation of <i>in vitro</i> data to predict extent of change in IxS renal clearance in CKD stage IV relative to healthy. Conditionally immortalized human proximal tubule epithelial cells overexpressing OAT1 were incubated with IxS (5-200 μM) in the HSA-free medium or in the presence of either HSA or CKD-modified HSA. IxS uptake in the presence of HSA resulted in more than 20-fold decrease in OAT1 affinity (K<sub>m,u</sub>) and 37-fold greater <i>in vitro</i> unbound intrinsic clearance (CL<sub>int,u</sub>) versus albumin-free condition. In the presence of CKD-modified albumin, K<sub>m,u</sub> increased four-fold and IxS CL<sub>int,u</sub> decreased almost seven-fold relative to HSA. Fold-change in parameters exceeded differences in IxS binding between albumin conditions, indicating additional mechanism and facilitating role of albumin in IxS OAT1-mediated uptake. Quantitative translation of IxS <i>in vitro</i> OAT1-mediated CL<sub>int,u</sub> predicted a 60% decrease in IxS renal elimination as a result of CKD, in agreement with the observed data (80%). The findings of the current study emphasize the role of albumin in IxS transport via OAT1 and explored the impact of modifications in albumin on renal excretion via active secretion in CKD. For the first time, this study performed quantitative translation of transporter kinetic data generated in a novel microfluidic <i>in vitro</i> system to a clinically relevant setting. Knowledge gaps and future directions in quantitative translation of renal drug disposition from microphysiological systems are discussed.
3-D-Laser-Based Scene Measurement and Place Recognition for Mobile Robots in Dynamic Indoor Environments (2012)

Active environment perception and autonomous place recognition play a key role for mobile robots to operate within a cluttered indoor environment with dynamic changes. This paper presents a 3-D-laser-based scene measurement technique and a novel place recognition method to deal with the random disturbances caused by unexpected movements of people and other objects. The proposed approach can extract and match the Speeded-Up Robust Features (SURFs) from bearing-angle images generated by a self-built rotating 3-D laser scanner. It can cope with the irregular disturbance of moving objects and the problem of observing-location changes of the laser scanner. Both global metric information and local SURF features are extracted from 3-D laser point clouds and 2-D bearing-angle images, respectively. A large-scale indoor environment with over 1600 m <sup xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">2</sup> and 30 offices is selected as a testing site, and a mobile robot, i.e., SmartROB2, is deployed for conducting experiments. Experimental results show that the proposed 3-D-laser-based scene measurement technique and place recognition approach are effective and provide robust performance of place recognition in a dynamic indoor environment.
Effect of p‐Cyclodextrin Complexation on the Photochemical and Photosensitizing Properties of Tolmetin: A Steady‐State and Time‐Resolved Study (1999)

The effects of beta-cyclodextrin complexation on the photochemical and photosensitizing properties of tolmetin have been investigated. Absorption, emission, circular dichroism and NMR measurements were used to characterize the host-guest complex. Nanosecond laser flash photolysis and steady-state photolysis experiments were performed to clarify the photoreactivity of the drug in the macrocycle. The decarboxylation of the drug is markedly reduced upon inclusion and the rate constants of the decay of the transient intermediates involved in tolmetin photodecomposition were slowed down due to their incorporation in the hydrophobic cavity. This also influenced the distribution of the stable photoproducts. A remarkable cyclodextrin-mediated protection against the tolmetin-photoinduced damage on biological substrates was observed. A rationale for these biological effects is provided.
Phase Conjugated Andreev Backscattering in Two-Dimensional Ballistic Cavities (1997)

We have experimentally investigated transport in two-dimensional ballistic cavities connected to a point contact and to two superconducting electrodes with a tunable macroscopic phase difference. The point contact resistance oscillates as a function of the phase difference in a way which reflects the ballistic nature of the transport in the cavity. We interpret our results in terms of a semiclassical model that relies on the properties of the phase conjugated trajectories on which a hole traces the path of the electron back to the emitting point contact. This model provides quantitative predictions (with no fitting parameters) as well as a clear physical picture.
PBFT Algorithm for Internet of Things (2022)

Due to the limited computing and storage capabilities of IoT devices, it is difficult to meet the computing needs of the Practical Byzantine Fault Tolerance (PBFT) algorithm. And the traditional PBFT algorithm is difficult to meet the throughput required by this system due to the prolonged consensus time. In order to solve the above problems, this paper proposes an improved PBFT algorithm, First, the node roles are divided, and only the consensus node role participates in the consensus, which reduces the communication overhead in the consensus process and makes enterprises of various strengths suitable for joining the system. Secondly, a scoring mechanism is added to improve the node selection and replacement method according to the points obtained by the nodes, and effectively eliminate Byzantine nodes, select a reliable node as the master node to the greatest extent, reduce the frequency of view change, and improve the speed of node change. Finally, the execution process of the consensus protocol is optimized, the communication complexity is reduced from O(N^2) to O(N), and the overall efficiency of the system is improved.
Studies of Silylfurans, Furylsilanes, and Silylthiophenes:  Structure of 2,5-Disilylthiophene (1999)

2-Silyl- and 2,5-disilylfuran (2-H3SiC4H3O, 2,5-(H3Si)2C4H2O) have been obtained from furan by lithiation with tBuLi, followed by treatment with H3SiBr at very low temperatures (−196 to −80 °C) in diethyl ether, as distillable liquids (bp 72 and 108 °C, respectively). Di-2-furyl- and tri-2-furylsilane ((2-C4H3O)nSiH4-n, n = 2, 3) are the products of the reaction of 2-furyllithium with Si(OMe)4, followed by reduction using LiAlH4 in diethyl ether/tetrahydrofuran. The methoxysilane precursors (2-C4H3O)nSi(OMe)4-n (n = 2, 3) have also been isolated. The analogous reactions of (MeO)4Si with equivalent quantities of (a) lithiated thiophenes and (b) LiAlH4 gave 2-silyl- and 2,5-disilylthiophene. Comprehensive NMR data have been compiled for all compounds, and the composition was confirmed by mass spectrometry. The crystal and molecular structure of 2,5-disilylthiophene has been determined by low-temperature “in situ” single-crystal X-ray diffraction, and ab initio calculations (MP2/6-31G*) have been carried out for this compound and the corresponding disilylfuran. The experimental and theoretical results are in excellent agreement and show that there are no silicon-induced irregularities as compared to methylated furans or thiophenes. Minor conformational differences can be ascribed to packing forces in the crystal. Low-temperature solution NMR experiments have shown that there is no aggregation via intermolecular donor−acceptor interactions in these systems.
Caffeine interferes with morphine-induced hyperactivity but not analgesia. (1984)

In C57BL/6 mice caffeine antagonized morphine-induced hyperactivity. This effect was most evident when caffeine was used in doses that slightly increased locomotor activity. Given at the same dose caffeine did not affect morphine-induced analgesia. Two possibilities of explanation of this effect are discussed: action of caffeine on dopaminergic mechanisms responsible for morphine-induced running fit through its effect on cyclic AMP level, and a direct action of caffeine on delta opiate receptors involved in the stimulatory effect of morphine.
Proceedings of the Third Workshop on Software Foundations for Data Interoperability (SFDI2019+), October 28, 2019, Fukuoka, Japan (2019)

This volume contains the papers presented at the Third Workshop on Software Foundations for Data Interoperability (SFDI2019+) held on October 28, 2019, in Fukuoka, co-located with the 11th Asia-Pasific Symposium on Internetware (Internetware 2019). One regular paper and six short papers have been accepted for presentation, each of which has its unique ideas and/or interesting results on interoperability of autonomic distributed data. Moreover, SFDI2019+ featured two keynote talks by Hiroyuki Seki (Nagoya University) and Zinovy Diskin (McMaster University), which introduce concepts and directions novel to the series of SFDI workshops so far.
How Much Do Modifications to Transformer Language Models Affect Their Ability to Learn Linguistic Knowledge? (2022)

Recent progress in large pretrained language models (LMs) has led to a growth of analyses examining what kinds of linguistic knowledge are encoded by these models. Due to computational constraints, existing analyses are mostly conducted on publicly-released LM checkpoints, which makes it difficult to study how various factors during training affect the models' acquisition of linguistic knowledge. In this paper, we train a suite of small-scale Transformer LMs that differ from each other with respect to architectural decisions (e.g., self-attention configuration) or training objectives (e.g., multi-tasking, focal loss). We evaluate these LMs on BLiMP, a targeted evaluation benchmark of multiple English linguistic phenomena. Our experiments show that while none of these modifications yields significant improvements on aggregate, changes to the loss function result in promising improvements on several subcategories (e.g., detecting adjunct islands, correctly scoping negative polarity items). We hope our work offers useful insights for future research into designing Transformer LMs that more effectively learn linguistic knowledge.
ChemInform Abstract: AN EFFICIENT METHOD FOR CONVERTING 17‐OXO‐ INTO 17‐ACETYL STEROIDS (1975)

Abstract Umsetzung des Östrons (I) mit dem Isocyanid (II) liefert ein trennbares Gemisch der Nitrile (III); die Reaktion von (III) mit CH 3 Li führt zu dem Epirnerengemisch (IV), aus dem durch Umkristallisieren das 17β‐Acetyl‐östratrien (IVb) isoliert wird; dieses kann auch direkt aus (IIIa) und CH 3 Li dargestellt werden.