gebhart/patrepeval huggingface dataset:
Injectable Coacervate Hydrogel for Delivery of Anticancer Drug-Loaded Nanoparticles in vivo (2018)

In this study, bortezomib (BTZ, a cytotoxic water-insoluble anticancer drug) was encapsulated in micellar nanoparticles having a catechol-functionalized polycarbonate core through a pH-sensitive covalent bond between phenylboronic acid (PBA) in BTZ and catechol, and these drug-loaded micelles were incorporated into hydrogels to form micelle/hydrogel composites. A series of injectable, biodegradable hydrogels with readily tunable mechanical properties were formed and optimized for sustained delivery of the BTZ-loaded micelles through ionic coacervation between PBA-functionalized polycarbonate/poly(ethylene glycol) (PEG) "ABA" triblock copolymer and a cationic one having guanidinium- or thiouronium-functionalized polycarbonate as "A" block. An in vitro release study showed the pH dependence in BTZ release. At pH 7.4, the BTZ release from the micelle/hydrogel composite remained low at 7%, whereas in an acidic environment, ∼85% of BTZ was released gradually over 9 days. In vivo studies performed in a multiple myeloma MM.1S xenograft mouse model showed that the tumor progression of mice treated with BTZ-loaded micelle solution was similar to that of the control group, whereas those treated with the BTZ-loaded micelle/hydrogel composite resulted in significant delay in the tumor progression. The results demonstrate that this hydrogel has great potential for use in subcutaneous and sustained delivery of drug-loaded micelles with superior therapeutic efficacy.
Pyruvate fuels mitochondrial respiration and proliferation of breast cancer cells: effect of monocarboxylate transporter inhibition (2012)

Recent studies have highlighted the fact that cancer cells have an altered metabolic phenotype, and this metabolic reprogramming is required to drive the biosynthesis pathways necessary for rapid replication and proliferation. Specifically, the importance of citric acid cycle-generated intermediates in the regulation of cancer cell proliferation has been recently appreciated. One function of MCTs (monocarboxylate transporters) is to transport the citric acid cycle substrate pyruvate across the plasma membrane and into mitochondria, and inhibition of MCTs has been proposed as a therapeutic strategy to target metabolic pathways in cancer. In the present paper, we examined the effect of different metabolic substrates (glucose and pyruvate) on mitochondrial function and proliferation in breast cancer cells. We demonstrated that cancer cells proliferate more rapidly in the presence of exogenous pyruvate when compared with lactate. Pyruvate supplementation fuelled mitochondrial oxygen consumption and the reserve respiratory capacity, and this increase in mitochondrial function correlated with proliferative potential. In addition, inhibition of cellular pyruvate uptake using the MCT inhibitor α-cyano-4-hydroxycinnamic acid impaired mitochondrial respiration and decreased cell growth. These data demonstrate the importance of mitochondrial metabolism in proliferative responses and highlight a novel mechanism of action for MCT inhibitors through suppression of pyruvate-fuelled mitochondrial respiration.
Odd-order-frequency-multiple-generation technique (1976)

A technique is described that enables the odd-order frequency multiples of a sinusoidal voltage to be generated. The circuit uses analogue multipliers and op. amps., but no tuned-circuit components. Practical results are presented and fundamental limitations of the technique are discussed.
[Prognostic factors in ruptured intracranial aneurysm. Significance of the temperature curve]. (1990)

This report concerns 130 consecutive patients admitted as emergencies for ruptured intracranial aneurysms. The poorer the patient's clinical condition, the longer the time elapsed before surgery (14 days on average). While awaiting surgery, 4.6 per cent of the patients rebled and 5.4 per cent deteriorated due to vasospasm. The 14 patients who had shown no symptom since the rupture remained asymptomatic until surgery, while the clinical status of the other 116 patients improved in 36.3 per cent, remained unchanged in 53.4 per cent and deteriorated in 10.3 per cent (3 per cent of whom died). After a one year follow-up, 58 per cent of the 126 patients operated upon had resumed all their previous activities; 10.3 per cent were autonomous but had been unable to resume their professional activities normally; 8.7 per cent were dependent and 20.5 per cent had died of neurological complications and/or sequelae (2.4 per cent had died of intercurrent diseases). An analysis of prognostic factors showed that the outcome was not significantly influenced by the site of the aneurysms, the patient's sex or age, or a past history of systemic arterial hypertension, but it was narrowly dependent (P less than 0.001) upon the clinical status at the time of surgery, the amount of extravasated blood at CT or the degree of vasospasm at angiography. The greater the size of the haematoma and the degree of vasosplasm, the more the clinical status was affected (P less than 0.01). In addition, the clinical status was found to be particularly poor when hyperthermia was present (P less than 0.01), and the outcome was worse in patients who were operated upon during the ascending phase of fever (P less than 0.05). Thus, a careful examination of the temperature curve might be of help in the choice of the optimal time for surgery.
ARTMAP: a self-organizing neural network architecture for fast supervised learning and pattern recognition (2002)

The authors present a neural network architecture, called ARTMAP, that autonomously learns to classify arbitrarily many, arbitrarily ordered vectors into recognition categories based on predictive success. This supervised learning system is built up from a pair of adaptive resonance theory modules that are capable of self-organizing stable recognition categories in response to arbitrary sequences of input patterns. Tested on a benchmark machine learning database in both online and offline simulations, the ARTMAP system learned orders of magnitude more quickly, efficiently, and accurately than alternative algorithms, and achieves 100% accuracy after training on less than half the input patterns in the database. It achieves these properties by using an internal controller that conjointly maximizes predictive generalization and minimizes predictive error by linking predictive success to category size on a trial-by-trial basis, using only local operations.< <ETX xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">></ETX>
Merkel Cell Carcinomas Arising in Autoimmune Disease Affected Patients Treated with Biologic Drugs, Including Anti-TNF (2017)

<b>Purpose:</b> The purpose of this investigation was to characterize Merkel cell carcinomas (MCC) arisen in patients affected by autoimmune diseases and treated with biologic drugs.<b>Experimental Design:</b> Serum samples from patients with MCC were analyzed for the presence and titer of antibodies against antigens of the oncogenic Merkel cell polyomavirus (MCPyV). IgG antibodies against the viral oncoproteins large T (LT) and small T (ST) antigens and the viral capsid protein-1 were analyzed by indirect ELISA. Viral antigens were recombinant LT/ST and virus-like particles (VLP), respectively. MCPyV DNA sequences were studied using PCR methods in MCC tissues and in peripheral blood mononuclear cells (PBMC). Immunohistochemical (IHC) analyses were carried out in MCC tissues to reveal MCPyV LT oncoprotein.<b>Results:</b> MCPyV DNA sequences identified in MCC tissues showed 100% homology with the European MKL-1 strain. PBMCs from patients tested MCPyV-negative. Viral DNA loads in the three MCC tissues were in the 0.1 to 30 copy/cell range. IgG antibodies against LT/ST were detected in patients 1 and 3, whereas patient 2 did not react to the MCPyV LT/ST antigen. Sera from the three patients with MCC contained IgG antibodies against MCPyV VP1. MCC tissues tested MCPyV LT-antigen-positive in IHC assays, with strong LT expression with diffuse nuclear localization. Normal tissues tested MCPyV LT-negative when employed as control.<b>Conclusions:</b> We investigated three new MCCs in patients affected by rheumatologic diseases treated with biologic drugs, including TNF. A possible cause-effect relationship between pharmacologic immunosuppressive treatment and MCC onset is suggested. Indeed, MCC is associated with MCPyV LT oncoprotein activity. <i>Clin Cancer Res; 23(14); 3929-34. ©2017 AACR</i>.
Mechanical work and efficiency in treadmill running at aerobic and anaerobic thresholds (1990)

Mechanical work, mechanical power, energy consumption and mechanical efficiency were studied in constant-speed treadmill running of 5 min at seven different exercises around aerobic (AerT) and anaerobic (AnT) thresholds. The true efficiency of concentric (positive) mechanical work and gross efficiency of the whole body in seven male subjects were calculated. The total mechanical work was calculated from film through the translational, potential and rotational energy states as the sum of the changes of all the mechanical energy states in all body segments allowing energy transfer between segments and from energy state to state. The total energy consumption was measured by combining aerobic and anaerobic energy production in resting and working conditions. When the speed of the treadmill was increased from the velocity of 10 km h-1 (2.8 m s-1) to 22 km h-1 (6.1 m s-1), the concentric mechanical work per one step increased from 129 +/- 45 J to 228 +/- 82 J (P less than 0.01). Oxygen consumption increased from 2.22 +/- 0.27 1 min-1 to 4.47 +/- 0.24 1 min-1. The amount of blood lactate increased from 0.94 +/- 0.53 mmol l-1 at the lowest speed to 9.90 +/- 2.89 mmol l-1 at the highest speed (P less than 0.001). The true efficiency of concentric work decreased from 74 +/- 14% to 56 +/- 8% (P less than 0.05). At the speed of the AerT, the economy of running, the vertical rise of different body segments and mechanical efficiency of positive work were high. The highest gross efficiency was found at the running speed between the AerT and AnT.
Software engineering tools (2005)

Automated tools play an important role in the promotion and adoption of software engineering methods and processes. The development of these tools is itself a significant software engineering task, requiring a considerable investment of time and resources. There are a large number of different kinds of automated software engineering tools, variously known as Computer Aided Software Engineering (CASE), Computer Aided Method Engineering (CAME), Integrated Project Support Environment (IPSE), Software Engineering Environment (SEE), and metaCASE tools. Although these tools differ in the particular methods, activities, and phases of the software development cycle to which they are applied, constructors of these tools often face similar implementation issues. Decisions about host computing platform, implementation language, conformance with standards and reference models, choice of repository, integration and interoperability mechanisms, and user interface style have to be made. This mini-track is based around the experience reports of researchers and practitioners actively involved in software engineering tool development.
Hybrid Bridge Structures Made of Frp Composite and Concrete (2017)

Despite many advantages over the conventional construction materials, the contemporary development of FRP composites in bridge engineering is limited due to high initial cost, low stiffness (in case of glass fibers) and sudden composite failure mode. In order to reduce the given limitations, mixed (hybrid) solutions connecting the FRP composites and conventional construction materials, including concrete, have been tested in many countries for 20 years. Shaping the hybrid structures based on the attributes of particular materials, aims to increase stiffness and reduce cost without losing the carrying capacity, lightness and easiness of bridges that includes such hybrid girders, and to avoid the sudden dangerous failure mode. In the following article, the authors described examples of hybrid road bridges made of FRP composite and concrete within the time of 20 years and presented the first Polish hybrid FRP-concrete road bridge. Also, the directions of further research, necessary to spread these innovative, advanced and sustainable bridge structures were indicated.
A superfamily of archaeal, bacterial, and eukaryotic proteins homologous to animal transglutaminases (1999)

Computer analysis using profiles generated by the PSI-BLAST program identified a superfamily of proteins homologous to eukaryotic transglutaminases. The members of the new protein superfamily are found in all archaea, show a sporadic distribution among bacteria, and were detected also in eukaryotes, such as two yeast species and the nematode Caenorhabditis elegans. Sequence conservation in this superfamily primarily involves three motifs that center around conserved cysteine, histidine, and aspartate residues that form the catalytic triad in the structurally characterized transglutaminase, the human blood clotting factor XIIIa'. On the basis of the experimentally demonstrated activity of the Methanobacterium phage pseudomurein endoisopeptidase, it is proposed that many, if not all, microbial homologs of the transglutaminases are proteases and that the eukaryotic transglutaminases have evolved from an ancestral protease.
Pharmacological studies on prostanoid receptors in the rabbit isolated saphenous vein: a comparison with the rabbit isolated ear artery (1996)

1. In isolated ring preparations of the rabbit saphenous vein, prostaglandin E2 (PGE2) caused well-defined, stable and concentration-dependent relaxations of KCl contracted tissues with a mean potency (p[A50]) of 9.39. 2. The prostanoid EP-receptor agonists, PGE1, 11-deoxy PGE1, 16,16-dimethyl PGE2 and misoprostol were all full agonists in this preparation. The EP2-receptor selective agonists, butaprost and AH13205, and the EP1/EP3-receptor selective agonist, sulprostone, also relaxed this tissue but were at least 300 times less potent than PGE2. 3. Prostaglandin D2 (PGD2), the DP-receptor agonist, BW245C, and the IP-receptor agonist, cicaprost, caused concentration-dependent relaxations of the rabbit saphenous vein but were at least 60 times less potent than PGE2. 4. The selective EP4-receptor antagonist, AH23848B (30 microM), antagonized the PGE2 concentration-effect (E/[A]) curves yielding a pA2 estimate of 4.96. The EP1/DP-receptor antagonist, AH6809 (10 microM), had no effect on the location of PGE2 E/[A] curves. 5. The stable thromboxane A2-mimetic, U46619, elicited concentration-dependent contractions of the rabbit saphenous vein (p[A50] = 8.01) however, PGE2 and prostaglandin F2 alpha (PGF2 alpha) were unable to produce a contractile response. The response to U46619 was competitively antagonized by the TP-receptor antagonist, GR32191B, yielding a pKB estimate of 7.08. 6. In the rabbit isolated ear artery, PGE2, misoprostol and AH13205 relaxed tissues pre-contracted with phenylephrine. PGE2 (p[A50] = 7.04) and misoprostol were equipotent, whereas AH13205 was some 40 fold less potent. AH23848B (30 microM) and AH6809 (1 and 10 microM) caused no significant shift in the location of PGE2 E/[A] curves. 7. These data suggest that the rabbit isolated saphenous vein contains prostanoid, EP-, DP-, IP- and TP-receptors. Based on antagonist affinity information and agonist potency orders, the rabbit saphenous vein contains an inhibitory prostanoid EP-receptor different from that in the rabbit ear artery, but comparable to the recently described EP4-receptor.
Optical pattern recognition in motion acquired scenes using a binary joint transform correlation (1997)

Abstract The problem of detecting patterns in moved scenes is analysed. The correlation when the input scene presents a relative motion with respect to the recording system image is studied analytically and an original method for detecting patterns by means of a binary joint transform correlator is presented. The method is based on the compensation of the sign errors introduced in the joint power spectrum by the transfer function of the degradation. Two alternatives to determine the sign of the transfer function are demonstrated: the first is based on an algorithm to extract information from the Fourier spectrum of the blurred image and the second method determines the sign errors by post-processing the correlation. Digital simulations and optical results are provided.
Synthesis, Topoisomerase I Inhibitory Activity, and in Vivo Evaluation of 11-Azacamptothecin Analogs (1995)

A series of analogs based on a novel template, 11-aza-(20S)-camptothecin, were obtained from total synthesis and tested as potential anticancer drugs in the topoisomerase I enzyme cleavable complex assay. The parent compound 11-aza-(20S)-camptothecin (8) was derived from a Friedlander condensation between the known aminopyridine derivative 3-(3-amino-4-picolylidene)-p-toluidine and optically active tricyclic ketone 7. Compound 8 had activity approximately twice that of (20S)-camptothecin in the calf thymus topoisomerase I cleavable complex assay. Compounds were prepared wherein the 11-aza nitrogen atom was quaternized as either the corresponding N-oxide or methyl iodide. Compounds with quaternized N-11 showed improved water solubility and were equipotent to the clinically investigated camptothecin analog topotecan in the cleavable complex assay. These compounds were evaluated in vivo in nude mice bearing HT-29 human colon carcinoma xenografts. The analog 11-aza-(20S)-camptothecin 11-N-oxide was found to significantly retard tumor growth when compared to untreated controls. Finally, 7,10-disubstituted 11-azacamptothecin analogs were synthesized using Pd(0) coupling reactions of 10-bromo-7-alkyl-11-aza-(20S)-camptothecins 19 and 20, which in turn were available from a Friedlander condensation of the novel bromopyridine derivatives 17a and 17b with 7. Among the 10-substituted series, a number of analogs displayed extremely high in vitro potency against topoisomerase I and improved aqueous solubility. A significant number of the compounds were found to be active in whole cell cytotoxicity assays and several were evaluated in nude mice bearing the HT-29 tumor xenografts. The most effective of these proved to be (S)-11-aza-7-ethyl-10-(aminohydroximinomethyl)camptothecin trifluoracetic acid salt (27), a potent topoisomerase I inhibitor which demonstrated excellent efficacy in both short term and in extended in vivo assays. A comparison between in vitro enzyme data and in vivo data from nude mouse studies in other compounds in this series revealed a poor overall correlation between topoisomerase inhibition in vitro and antitumor efficacy in vivo.
Reduced postoperative infections with an immune‐enhancing nutritional supplement (1999)

Compared with standard formula, perioperative nutritional supplementation with Impact significantly reduced the incidence of infectious complications. The length of hospitalization was significantly prolonged in patients with postoperative infections, suggesting potential cost savings with the use of immune-enhancing formulas such as Impact.
The status and perspectives of metal oxide thin-film transistors for active matrix flexible displays (2011)

The purpose of this paper is to give an overview of the state-of-the-art of metal oxide thin-film transistors (TFTs). First, the question of how to achieve high-performance oxide TFTs is addressed, including the exploration of new channel materials, the realization of low-resistance ohmic contacts and the implementation of high-k dielectric materials as the gate insulator. The electrical instability of the oxide TFTs is also discussed, which is critical for their application in flexible backplane electronics: special attention is given to the understanding of the degradation mechanism of oxide TFTs against bias thermal stress (BTS) and light illuminated BTS. Finally, the recent application of oxide TFTs in active matrix displays, such as electronic paper, liquid crystal displays and organic light-emitting diodes, is addressed.
Selective effects of serotonergic psychoactive agents on gastrointestinal functions in health (2003)

This study evaluated the effects of serotonergic psychoactive agents on gastrointestinal functions in healthy human subjects. Participants received one of four regimens in a randomized, double-blind manner: buspirone, a 5-HT(1A) receptor agonist (10 mg twice daily); paroxetine, a selective serotonin reuptake inhibitor (20 mg daily); venlafaxine-XR, a selective serotonin and norepinephrine reuptake inhibitor (75 mg daily); or placebo for 11 days. Physiological testing performed on days 8-11 included scintigraphic assessment of gastrointestinal and colonic transit, the nutrient drink test, and assessment of the postprandial change in gastric volume. Fifty-one healthy adults (40 females, 11 males) participated in this study. No effects on gastric emptying or colonic transit were identified with any agent. Small bowel transit of a solid meal was accelerated by paroxetine. Buspirone decreased postprandial aggregate symptom and nausea scores. Venlafaxine-XR increased the postprandial change in gastric volume. Buspirone, paroxetine, and venlafaxine-XR affect upper gastrointestinal functions in healthy humans. These data support the need for clinical and physiological studies of these agents in functional gastrointestinal disorders.
Radioactive and Photoelectric <i>p-n</i> Junction Power Sources (1954)

An electrical power source can be made by exposing a p-n junction to radioactivity or light, so that the junction field separates electron-hole pairs produced by the radiation. Expressions for maximum power, optimum load resistance, and efficiency are derived from an equivalent circuit and rectification theory. Power and efficiency increase with source current Ig of separated charges and zero-bias junction resistance. Ig increases with energy and intensity of radiation, but is limited by self-absorption in the radioactive isotopes. Estimates of attainable power and efficiency for silicon cells are 3·10−3 watt cm−2 and 15 percent for solar radiation, averaged, allowing for night, weather, and varying angle of incidence; and 3·10−4 watt cm−2 and 8 percent, for beta radiation from Sr90–Y90 of activity 32 Curie/g. However, lattice defects produced by Sr90–Y90 beta radiation impair cell performance by increasing electron-hole recombination. A theoretical estimate of threshold energy for radiation damage in silicon is about 0.3 Mev, about half the experimental value reported for germanium. Avoiding radiation damage by annealing, by absorbers, and by use of less energetic isotopes is discussed. The Y90 beta spectrum is given; it is used in estimating damage rates in germanium, which are high, and efficiencies obtainable with absorbers, which are low. Theory and experiment are compared for Sr90–Y90 cells of silicon and of germanium.