gebhart/patrepeval huggingface dataset:
Structure-Based Discovery of a Novel Angiotensin-Converting Enzyme 2 Inhibitor (2004)

Angiotensin-converting enzyme 2 (ACE2) is considered an important therapeutic target for controlling cardiovascular diseases and severe acute respiratory syndrome (SARS) outbreaks. Recently solved high-resolution crystal structures of the apo-bound and inhibitor-bound forms of ACE2 have provided the basis for a novel molecular docking approach in an attempt to identify ACE2 inhibitors and compounds that block SARS coronavirus spike protein-mediated cell fusion. In this study, approximately 140 000 small molecules were screened by in silico molecular docking. In this structure-activity relation study, the molecules with the highest predicted binding scores were identified and assayed for ACE2 enzymatic inhibitory activity and for their ability to inhibit SARS coronavirus spike protein-mediated cell fusion. This approach identified N-(2-aminoethyl)-1 aziridine-ethanamine as a novel ACE2 inhibitor that also is effective in blocking the SARS coronavirus spike protein-mediated cell fusion. Thus, the molecular docking approach resulting in the inhibitory capacity of N-(2-aminoethyl)-1 aziridine-ethanamine provides an attractive small molecule lead compound on which the development of more effective therapeutic agents could be developed to modulate hypertension and for controlling SARS infections.
Microencapsulation – A Novel Approach in Drug Delivery: A Review (2012)

The review of Microencapsulation is a well-established dedicated to the preparation, properties and uses of individually encapsulated novel small particles, as well as significant improvements to tried-and-tested techniques relevant to micro and nano particles and their use in a wide variety of industrial, engineering, pharmaceutical, biotechnology and research applications. Its scope extends beyond conventional microcapsules to all other small particulate systems such as self-assembling structures that involve preparative manipulation. The review covers encapsulation materials, physics of release through the capsule wall and / or desorption from carrier, techniques of preparation, many uses to which microcapsules are put.© 2011 IGJPS. All rights reserved.
Cryptanalysis of Microsoft's point-to-point tunneling protocol (PPTP) (1998)

The Point-t&Point Meting Protocol (PPTP) is used to secure PPP connection over TCP/R ~. h this paper we ansdyze Microsoft's Windows NT implm entation of PPTP. We show how to break both the chWenge/r=ponse authentication protocol (Microsoft C~P) and the RC4 encryption protocol (MPPE), as weU x how to attack the control channel in Microsoft's implementation. Th=e attacks do not nec-tiy break PPTP, but ody Microsoft's implementation of the prt ocol.
Ultrasound as visual feedback in speech habilitation: Exploring consultative use in rural British Columbia, Canada (2008)

Ultrasound has shown promise as a visual feedback tool in speech therapy. Rural clients, however, often have minimal access to new technologies. The purpose of the current study was to evaluate consultative treatment using ultrasound in rural communities. Two speech-language pathologists (SLPs) trained in ultrasound use provided consultation with ultrasound in rural British Columbia to 13 school-aged children with residual speech impairments. Local SLPs provided treatment without ultrasound before and after the consultation. Speech samples were transcribed phonetically by independent trained listeners. Eleven children showed greater gains in production of the principal target /[image omitted]/ after the ultrasound consultation. Four of the seven participants who received more consultation time with ultrasound showed greatest improvement. Individual client factors also affected outcomes. The current study was a quasi-experimental clinic-based study. Larger, controlled experimental studies are needed to provide ultimate evaluation of the consultative use of ultrasound in speech therapy.
Helical rail glider launcher (1982)

The electromagnetic acceleration group at MIT has undertaken to build an electric glider launcher. The launcher features a mobile helical rail accelerator and power supply. It will launch a 6 foot radio-controlled glider for an overall range of several miles. This device is a prototype for a larger system that will provide a launch platform for munition and supply loaded gliders and a wide variety of RPV's. A 6 meter helical rail launcher has been constructed and is being tested. It is a twin boom device designed to accelerate a 5 kg glider to 100 m/s at 100 g's acceleration.
IEEE 802.11ah: Advantages in standards and further challenges for sub 1 GHz Wi-Fi (2012)

The rapid developments in Internet-of-Things (IoT) and Machine-to-Machine (M2M) communication make it necessary to design communication systems operating in different wireless spectrum as an alternative to highly congested wireless access systems. In addition, the deployment of wireless smart meter devices is ramping up and it is expected that such devices will flood the market in the near future competing for the same wireless spectrum. The IEEE 802.11ah standardization task group is developing a global Wireless LAN (WLAN) standard that will allow wireless access using carrier frequencies below 1 GHz in the ISM (Industrial, Scientific, and Medical) band and will help Wi-Fi-enabled devices to get guaranteed access for short-burst data transmissions, such as meter data. In addition to exploiting the underutilized sub 1 GHz spectrum the improved coverage range allows new applications to emerge such as wide area based sensor networks, sensor backhaul systems and potential Wi-Fi off-loading functions. This paper summarizes the IEEE 802.11ah standardization activities in progress and discusses advantages and challenges in the design of physical layer (PHY) and media access control (MAC) schemes in the sub 1 GHz band.
Francisella tularensis LPS induces the production of cytokines in human monocytes and signals via Toll-like receptor 4 with much lower potency than E. coli LPS (2006)

Francisella tularensis is a virulent Gram-negative intracellular pathogen. To address the signaling routes involved in the response of host cells to LPS from F. tularensis live vaccine strain (LVS), experiments were performed in transiently transfected 293 cells. Induction of kappaB-driven transcriptional activity by 2.5 mug ml(-1) F. tularensis LPS isolated by phenol-water and ether-water extraction, was observed in cells transfected with Toll-like receptor (TLR) 4 and MD-2, although CD14 was required for optimal induction. Conversely, TLR2, TLR2/TLR1 or TLR2/TLR6 transfected cells did not show kappaB-driven transcriptional activity in the presence of F. tularensis LPS. In human monocytic cells, F. tularensis LPS activated extracellular signal-regulated kinases and the production of pro-inflammatory proteins. Concentrations of 5-10 mug ml(-1) F. tularensis LPS elicited a similar pattern of mRNA and protein induction than 0.1 mug ml(-1) E. coli LPS, including the expression of CXC chemokines (IL-8, Gro and IFN-gamma-inducible protein-10); CC chemokines (monocyte chemoattractant protein-1 and -2, macrophage-derived chemoattractant, macrophage inflammatory protein-1alpha and -1beta and RANTES (regulated upon activation, normal T cell expressed and secreted) and pro-inflammatory cytokines (IL-6 and tumor necrosis factor alpha). Altogether, these data indicate that LPS from F. tularensis LVS signals via TLR4 at higher concentrations than those required for E. coli LPS, which may explain the inflammatory reaction and the low endotoxic response associated to vaccination with LVS in humans.
Separability of Very Noisy Mixed States and Implications for NMR Quantum Computing (1999)

We give a constructive proof that all mixed states of $N$ qubits in a sufficiently small neighborhood of the maximally mixed state are separable (unentangled). The construction provides an explicit representation of any such state as a mixture of product states. We give upper and lower bounds on the size of the neighborhood, which show that its extent decreases exponentially with the number of qubits. The bounds show that no entanglement appears in the physical states at any stage of present NMR experiments. Though this result raises questions about NMR quantum computation, further analysis would be necessary to assess the power of the general unitary transformations, which are indeed implemented in these experiments, in their action on separable states.
Eigen design of quadrature mirror filters (2002)

The paper presents a method for the design of quadrature mirror filters. A new frequency weighted stopband energy function is introduced, which leads to considerable flexibility in the design process. Unlike other techniques which involve searches and nonlinear optimization, the formulation reduces the design equations to an eigenvector problem. The resulting filters are regular and have additional desirable properties as discussed in the paper. Also considered is application to pyramidal coding of images, which together with DPCM and PCM, leads to high compression ratios.< <ETX xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">></ETX>
The Use of Direct Current in Induction Electron Accelerators (1945)

The application of a direct-current bias in the magnetic circuit of induction accelerators is described. In its simplest form this bias reduces power consumption to approximately 30 percent; in especially designed machines a reduction of the weight to 50 percent or less is an additional advantage. A machine with a closed central core is discussed and the use of orbit contraction by saturation over a range of x-ray energies is described.
Transient Extracellular Glutamate Events in the Basolateral Amygdala Track Reward-Seeking Actions (2012)

The ability to make rapid, informed decisions about whether or not to engage in a sequence of actions to earn reward is essential for survival. Modeling in rodents has demonstrated a critical role for the basolateral amygdala (BLA) in such reward-seeking actions, but the precise neurochemical underpinnings are not well understood. Taking advantage of recent advancements in biosensor technologies, we made spatially discrete near-real-time extracellular recordings of the major excitatory transmitter, glutamate, in the BLA of rats performing a self-paced lever-pressing sequence task for sucrose reward. This allowed us to detect rapid transient fluctuations in extracellular BLA glutamate time-locked to action performance. These glutamate transients tended to precede lever-pressing actions and were markedly increased in frequency when rats were engaged in such reward-seeking actions. Based on muscimol and tetrodotoxin microinfusions, these glutamate transients appeared to originate from the terminals of neurons with cell bodies in the orbital frontal cortex. Importantly, glutamate transient amplitude and frequency fluctuated with the value of the earned reward and positively predicted lever-pressing rate. Such novel rapid glutamate recordings during instrumental performance identify a role for glutamatergic signaling within the BLA in instrumental reward-seeking actions.
Whole blood assay for trypsin activity using polyanionic focusing gel electrophoresis (2010)

The measurement of trypsin activity directly in blood is important for the development of novel diagnostics and for biomedical research. Presently, most degradative enzyme assays require sample preparation, making them time consuming, costly, and less accurate. We recently demonstrated a simple and rapid electrophoretic assay for the measurement of trypsin activity directly in whole blood. This assay utilizes a charge-changing fluorescent peptide substrate that produces a positively charged fluorescent product fragment upon cleavage by the target enzyme. This fragment is then rapidly separated from whole blood by electrophoresis and quantified with a fluorescent detector. In this study, we demonstrate that polyanionic poly-L-glutamic acid-doped polyacrylamide gels can focus the fluorescent cleavage product and markedly improve the LODs of the assay. A LOD of 2 pg in 6 microL (0.3 ng/mL) in whole human blood was achieved after a 1-h reaction of enzyme and substrate followed by 10 min of electrophoresis. This is 50- to 200-fold better than the estimated reference levels for trypsin (15-60 ng/mL) in blood. This straightforward technique now allows for the rapid measurement of clinically relevant levels of trypsin activity in microliter volumes of whole blood, providing a useful tool for the development of novel point-of-care diagnostics.
Impacts of fluorouracil‐metabolizing enzymes on the outcomes of patients treated with S‐1 alone or S‐1 plus cisplatin for first‐line treatment of advanced gastric cancer (2009)

A phase III trial of S-1 plus cisplatin (SP) versus S-1 alone, for first-line treatment of advanced gastric cancer (SPIRITS trial), has shown that overall survival was better in patients treated with SP than with S-1 alone. In the present retrospective biomarker study, we aimed to develop a methodology to identify the patients with advanced gastric cancer who would respond better to S-1 alone than SP. We studied 120 patients who received S-1 alone or SP for first-line chemotherapy for advanced gastric cancer, and quantitatively evaluated mRNA levels of thymidylate synthase (TS), thymidine phosphorylase (TP), orotate phosphoribosyltransferase (OPRT), dihydropyrimidine dehydrogenase, vascular endothelial growth factor-A, and epidermal growth factor receptor in paraffin-embedded specimens of primary tumors. Multivariate survival analysis in patients who received S-1 monotherapy (66 patients) demonstrated that low TP expression (hazard ratio: 2.55 (95% CI: (1.33 to 4.89)), low TS (2.71 (1.36 to 5.37)), and high OPRT (0.33 (0.13 to 0.86)) were significant predictors of long overall survival. In patients with lower expression of both TP and TS (n = 23) than their cutoff values, the S-1 alone group (n = 15) had longer overall survival than the SP group (n = 8; median overall survival, 18.2 months vs. 9.4 months), whereas the frequency of overall adverse events in the S-1 alone group tended to be lower than that in SP group. Our results suggest that these biomarkers are useful for selection of patients with advanced gastric cancer in whom treatment with S-1 alone will yield survival benefit.
Wireless surface acoustic wave chemical sensor for simultaneous measurement of <inline-formula><math display="inline" overflow="scroll"><mrow><mi mathvariant="normal">C</mi><msub><mi mathvariant="normal">O</mi><mn>2</mn></msub></mrow></math></inline-formula> and humidity (2009)

A 440-MHz wireless and passive surface acoustic wave (SAW) microsensor was developed for simultaneous measurement of CO2 and relative humidity (RH). The developed SAW microsensor was composed of SAW reflective delay lines structured by an interdigital transducer (IDT) and several shorted grating reflectors, CO2, and water vapor-sensitive films. A theoretical model was established to predict the response mechanism of the polymer-coated SAW gas sensor. Infusion of CO2 into the chamber and humidity changes induced large phase shifts in the reflection peaks. Good linearity and repeatability were observed in the CO2 concentration of 0~400 ppm and 20~80% RH. The obtained sensitivity was ~2° ppm−1 for CO2 detection and 7.45°/%RH for humidity sensing. Temperature and humidity effects were also investigated during the sensitivity evaluation process.
Rowe, Thomas ( c. 1657–1705) (2000)

Rowe, Thomas Thomas Rowe was born in London and died there on 18 August 1705 from injuries sustained following a seizure which threw him from his horse. He was buried at Bunhill Fields. Thomas was the oldest son of John Rowe (1627–77), minister of an Independent church which met in Westminster Abbey
Covalent Binding of Tea Catechins to Protein Thiols: The Relationship between Stability and Electrophilic Reactivity (2010)

In this study, we investigated the relationship between the stability of catechins and their electrophilic reactivity with proteins. The stability of catechins was evaluated by HPLC analysis. Catechol-type catechins were stable in a neutral buffer, but pyrogallol-type catechins, such as (-)-epigallocatechin gallate (EGCg), were unstable. The electrophilic reactivity of catechins with thiol groups in a model peptide and a protein was confirmed by both mass spectrometry and electrophoresis/blotting with redox-cycling staining. In a comparison of several catechins, pyrogallol-type catechins had higher reactivity with protein thiols than catechol-type catechins. The instability and reactivity of EGCg were enhanced in an alkaline pH buffer. The reactivity of EGCg was reduced by antioxidants due to their ability to prevent EGCg autoxidation. These results indicate that the instability against oxidation of catechins is profoundly related to their electrophilic reactivity. Consequently, the difference in these properties of tea catechins can contribute to the magnitude of their biological activities.
Purification and Properties of a New Cathepsin from Rat Liver1 (1978)

1) A lysosomal protease, a new cathepsin that inactivates glucose-6-phosphate dehydrogenase [EC 1.1.1.49] and some other enzymes and differs from cathepsin B [EC 3.4.22.1] was purified about 2,200-fold from crude extracts of rat liver by cell-fractionation, freezing and thawing, acetone treatment, gel filtration, and DEAE Sephadex and CM-Sephadex column chromatographies. 2) The new cathepsin was markedly activated by the thiol-reagent, 2-mercaptoethanol and inhibited by monoiodoacetate. 3) The molecular weight of the new cathepsin was found by Sephadex G-75 column chromatography to be 22,000, which is smaller than that of cathepsin B. 4) The optimum pH of the enzyme for inactivation of glucose-6-phosphate dehydrogenase was pH 5.0--5.5. The enzyme was unstable in alkali and on heat treatment. 5) The rates of inactivation of glucose-6-phosphate dehydrogenase, apo-ornithine aminotransferase [EC 2.6.1.13], apo-tyrosine aminotransferase [EC 2.6.1.5], apo-cystathionase [EC 4.4.1.1], glucokinase [EC 2.7.1.2], glyceraldehyde-3-phosphate dehydrogenase [EC 1.2.1.12], and malate dehydrogenase [EC 1.1.1.37] by the new cathepsin were higher than those by cathepsin B. However aldolase [EC 4.1.2.13] was inactivated more rapidly by cathepsin B than by the new cathepsin. Lactate dehydrogenase [EC 1.1.1.27], glutamate dehydrogenase [EC 1.4.1.2] and alcohol dehydrogenase [EC 1.1.1.1] were not inactivated by either cathepsin. Unlike cathepsin B, the new cathepsin scarcely hydrolyzes N-substituted derivatives of arginine.
‘Streptomyces nanchangensis’, a producer of the insecticidal polyether antibiotic nanchangmycin and the antiparasitic macrolide meilingmycin, contains multiple polyketide gene clusters (2002)

Several independent gene clusters containing varying lengths of type I polyketide synthase genes were isolated from 'Streptomyces nanchangensis' NS3226, a producer of nanchangmycin and meilingmycin. The former is a polyether compound similar to dianemycin and the latter is a macrolide compound similar to milbemycin, which shares the same macrolide ring as avermectin but has different side groups. Clusters A-H spanned about 133, 132, 104, 174, 122, 54, 37 and 59 kb, respectively. Two systems were developed for functional analysis of the gene clusters by gene disruption or replacement. (1) Streptomyces phage phiC31 and its derived vectors can infect and lysogenize this strain. (2) pSET152, an Escherichia coli plasmid with phiC31 attP site, and pHZ1358, a Streptomyces-Escherichia coli shuttle cosmid vector, both carrying oriT from RP4, can be mobilized from E. coli into NS3226 by conjugation. pHZ1358 was shown to be generally useful for generating mutant strains by gene disruption and replacement in NS3226 as well as in several other Streptomyces strains. A region in cluster A (approximately 133 kb) seemed to be involved in nanchangmycin production because replacement of several DNA fragments in this region by an apramycin resistance gene [aac3(IV)] gave rise to nanchangmycin non-producing mutants.
Vasoactive intestinal peptide inhibits human small-cell lung cancer proliferation <i>in vitro</i> and <i>in vivo</i> (1998)

Small-cell lung carcinoma (SCLC) is an aggressive, rapidly growing and metastasizing, and highly fatal neoplasm. We report that vasoactive intestinal peptide inhibits the proliferation of SCLC cells in culture and dramatically suppresses the growth of SCLC tumor-cell implants in athymic nude mice. In both cases, the inhibition was mediated apparently by a cAMP-dependent mechanism, because the inhibition was enhanced by the adenylate cyclase activator forskolin and the phosphodiesterase inhibitor 3-isobutyl-1-methylxanthine in proportion to increases in intracellular cAMP levels, and the inhibition was abolished by selective inhibition of cAMP-dependent protein kinase. If confirmed in clinical trials, this antiproliferative action of vasoactive intestinal peptide may offer a new and promising means of suppressing SCLC in human subjects, without the toxic side effects of chemotherapeutic agents.
Super‐resolution musculoskeletal <scp>MRI</scp> using deep learning (2018)

DeepResolve was capable of resolving high-resolution thin-slice knee MRI from lower-resolution thicker slices, achieving superior quantitative and qualitative diagnostic performance to both conventionally used and state-of-the-art methods.
A Simple and Sensitive Method of Monitoring Crack and Load in Compact Fracture Mechanics Specimens Using Strain Gages (1979)

Abstract The calibrated strain on the back face (the face opposite that from which the slot is machined) of compact tension (CT) and T-type wedge-opening-loading (WOL) specimens provides a method for measuring crack length when the load is known or for measuring load when the crack length is known. The method is simple, reliable, sensitive, and inexpensive. A good correlation was achieved between strain measurements on a CT specimen and values computed from a two-dimensional finite element analysis. The method has good potential for developing into a more sensitive crack length measurement technique than has previously been achieved. Calibration tables and graphs are reproduced that describe the relationship between crack length, back-face strain, and load for CT and T-type WOL specimens of any size and thickness and for any linear elastic material. The method has several advantages over the closely related crack opening displacement (COD) technique for some test situations and these are described. In particular, the back-face strain increases linearly with crack length for constant stress intensity conditions except for very deep cracks in CT specimens. The overall characteristics render the technique ideal for incorporation into computerized/automated crack growth testing. For constant back-face strain, the stress intensity was shown to decrease with increase in crack length for both CT and T-type WOL specimens. This decrease is more pronounced than for corresponding constant COD testing and this provides a good technique for obtaining threshold fatigue or stress corrosion conditions.
Novel augmentation ileocystoplasty technique to manage non‐compliant bladders in the presence of obstructed megaureters: The “fez procedure” (2015)

The "fez procedure" represents a versatile and successful surgical option for these selected patients, as it offers improved bladder capacity/compliance, resolution of ureteral obstruction and vesicoureteral reflux, preservation of the renal function, control of urinary tract infections and urinary continence, and acceptable morbidity.