gebhart/patrepeval huggingface dataset:
Current state and outlook for drug repositioning anticipated in the field of ovarian cancer (2018)

Ovarian cancer is the seventh most common cancer and the eighth most common cause of cancer mortality in women. Although standard chemotherapy is the established treatment for ovarian cancer, the prognosis remains poor, and it is highly anticipated that new drugs will be developed. New drugs, such as humanized anti-vascular endothelial growth factor monoclonal antibodies and poly ADP-ribose polymerase inhibitors, are expected to improve clinical outcomes of ovarian cancer. However, long-term, costly research is required to develop such new drugs, and soaring national healthcare costs are becoming a concern worldwide. In this social context, drug repositioning, wherein existing drugs are used to develop drugs with new indications for other diseases, has recently gained attention. Because trials have already confirmed the safety in humans and the pharmacokinetics of such drugs, the development period is shorter than the conventional development of a new drug, thereby reducing costs. This review discusses the available basic experimental and clinical data on drugs used for other types of cancer for which drug repositioning is anticipated to repurpose the drug for the treatment of ovarian cancer. These include statins, which are used to treat dyslipidemia; bisphosphonate, which is used to treat osteoporosis; metformin, which is used to treat diabetes; non-steroidal anti-inflammatory drugs; ivermectin, an antiparasitic agent; and itraconazole, an anti-fungal agent. These drugs will play an important role in future drug repositioning strategies for ovarian cancer. Furthermore, drug repositioning is anticipated to extend not only to ovarian cancer treatment but also to ovarian cancer prevention.
Comparison of nalbuphine and fentanyl as intravenous analgesics for medically compromised patients undergoing oral surgery. (1992)

This study compared the efficacy and side effects of equianalgesic doses of nalbuphine and fentanyl as intravenous (IV) analgesics for medically compromised patients undergoing oral surgery with local anesthesia. A total of 24 inpatients scheduled for oral surgery and with an ASA physical status of 3 or 4 were randomly assigned to two treatment groups and received IV analgesia with an injection of either 0.2 mg/kg nalbuphine or 2 micrograms/kg fentanyl. Three minutes later, local anesthesia was administered. Respiratory rate, heart rate, arterial blood pressure, and oxyhemoglobin saturation (SpO2) were recorded before and during surgery. After the operation, the patient, surgeon, and anesthesiologist were asked to complete questionnaires regarding drug effects. Analgesia and sedation appeared sufficient and comparable according to the surgeon, anesthesiologists, and patients in the two groups, and there were no significant differences in blood pressure or heart rate. Respiratory rate and SpO2 were lower in patients treated with fentanyl (P < 0.05), and eight patients of this group experienced episodes of oxygen desaturation (SpO2 < 90%) compared with only two patients who received nalbuphine (P < 0.05). Nalbuphine produced less respiratory depression and should be considered a suitable alternative to fentanyl for use in medically compromised patients undergoing oral surgery.
Ceramide regulates oxidant release in adherent human neutrophils (1994)

We investigated the role of sphingolipids in regulating oxidant release in adherent human neutrophils. Stimulation of adherent neutrophils with formyl-Met-Leu-Phe (fMLP) resulted in the accumulation of ceramide at a time when H2O2 release is terminated. H2O2 release in fMLP-stimulated neutrophils was suppressed in a concentration-dependent manner by the exogenous addition of several free sphingoid amines and short chain ceramides. Sphingosine, dihydrosphingosine, phytosphingosine, N-acetylsphingosine, and N-acetylphytosphingosine, but not N-acetyldihydrosphingosine, inhibited formyl peptide-stimulated oxidant release. The half-maximal inhibitory concentrations of N-acetylsphingosine and N-acetylphytosphingosine were 0.51 and 0.38 microM, respectively. Sphingosine, dihydrosphingosine, and phytosphingosine were less potent inhibitors with half-maximal inhibitory concentrations of 1.78, 15.4, and 1.48 microM, respectively. The 4 beta-phorbol 12 beta-myristate 13 alpha-acetate-induced respiratory burst was inhibited by 5 microM of sphingosine but not by 5 microM of N-acetylsphingosine. The effects of N-acetyl-conjugated sphingols (C2 ceramides) on phosphatidylcholine-specific phospholipase D and phosphatidic acid phosphohydrolase were markedly different from the effects of the related sphingoid bases. Both C2 ceramides and sphingoid bases partially inhibited the diradylglycerol formation by the phosphatidylcholine-specific phospholipase D pathway. Under the same conditions, however, N-acetyldihydrosphingosine and dihydrosphingosine failed to suppress H2O2 release in fMLP-stimulated neutrophils. These findings demonstrate that C2 ceramides inhibit H2O2 generation in fMLP-stimulated neutrophils via protein kinase C- or sphingoid base-independent mechanisms. The effect of ceramide in inhibiting the respiratory burst is structurally specific, because either a 4,5-trans double bond or 4-hydroxyl group is required for the inhibition. Therefore, ceramides may regulate oxidant release in adherent neutrophils.
Halten die COX-2-Hemmer was sie versprechen? (2004)

Vor gut zwölf Jahren hat die Entdeckung, dass Cyclooxygenasefunktionen von zwei verschiedenen Enzymen vermittelt werden, die Hoffnung auf wesentlich besser verträgliche Antiphlogistika und Analgetika geweckt. In den letzten Jahren kamen mit Celecoxib und Rofecoxib zwei selektive COX-2-Hemmstoffe auch in Deutschland zur Zulassung. Klinische Studien bestätigen nun, dass die selektiven COX-2-Inhibitoren eine deutlich reduzierte gastrointestinale Toxizität bei vergleichbarer analgestischer Wirkung aufweisen. Andere unerwünschte Wirkungen wie die Ödembildung und eine leichte Erhöhung des systolischen Blutdrucks scheinen dagegen bei den selektiven COX-2-Inhibitoren und klassischen NSAIDs in etwa vergleichbarem Umfang aufzutreten. Ob die bessere gastrointestinale Verträglichkeit auch mit neuen Risiken etwa erhöhter Thrombose und Myokardinfarktraten, verbunden ist, wird gegenwärtig diskutiert.
Integration of Combinatorial Synthesis, Rapid Screening, and Computational Modeling in Biomaterials Development (2004)

Abstract Summary: The advent of high‐throughput combinatorial synthesis techniques in drug discovery has stimulated efforts to apply these techniques to the discovery of biomaterials. To be of practical utility, combinatorial approaches to biomaterials design require (i) the availability of parallel synthesis techniques to generate libraries of polymers, (ii) efficient assays for the rapid characterization of biorelevant material properties, and (iii) computational methods to efficiently model different biological responses in the presence of polymers. Here we report the integration of these methodologies and illustrate the potential of this approach to accelerate the development of new biomaterials. The parallel synthesis of a library of 112 biodegradable polyarylates has been reported previously. This library was used to develop efficient screening techniques to determine biorelevant polymer properties (fibrinogen adsorption, gene expression in macrophages, growth of fetal rat lung fibroblasts (RLFs)). A Surrogate (semiempirical) Model was developed (i) to determine molecular‐scale polymer properties that correlate to various biological responses, and (ii) to predict fibrinogen adsorption and RLF growth on polymeric surfaces. For 38 out of 45 polymers, the model predicted the amount of fibrinogen adsorbed correctly within the error of the experimental measurements. The growth of rat lung fibroblasts was correctly predicted by the model for 41 out of 48 polymers. The correlation factor between the model's predicted values and the experimentally determined data was 0.54 ± 0.09 and 0.69 ± 0.12 for fibrinogen adsorption and RLF growth, respectively. The results presented here demonstrate the utility of combinatorial and computational approaches for the rational design of polymers for biomedical applications. Design of the library of polyarylates, which are copolymers of a diacid and a diphenol. Chemical diversity was created by variations in the structure of the diacid (marked as “Y”) and the pendent chain (marked as “R”). magnified image Design of the library of polyarylates, which are copolymers of a diacid and a diphenol. Chemical diversity was created by variations in the structure of the diacid (marked as “Y”) and the pendent chain (marked as “R”).
Gas phase hydration of organic ions (2008)

In this work, we study the hydration phenomenon on a molecular level in the gas phase where a selected number of water molecules can interact with the organic ion of interest. The stepwise binding energies (DeltaH degrees (n-1,n)) of 1-7 water molecules to the phenyl acetylene cation are determined by equilibrium measurements using an ion mobility drift cell. The stepwise hydration energies DeltaH degrees (n-1,n) are nearly constant at 39.7 +/- 6.3 kJ mol(-1) from n = 1 to 7. The entropy change is larger in the n = 7 step, suggesting cyclic or cage-like water structures. No water addition is observed on the ionized phenyl acetylene trimer consistent with cyclization of the trimer ion to form triphenyl benzene cations C(24)H(18) (+) which are expected to interact weakly with the water molecules due to steric interactions and the delocalization of the charge on the large organic ion. The work demonstrates that hydration studies of organic ions can provide structural information on the organic ions.
Langmuir–Blodgett Thin Films of Diketopyrrolopyrrole-Based Amphiphiles (2018)

We report on two π-conjugated donor-acceptor-donor (D-A-D) molecules of amphiphilic nature, aiming to promote intermolecular ordering and carrier mobility in organic electronic devices. Diketopyrrolopyrrole was selected as the acceptor moiety that was disubstituted with nonpolar and polar functional groups, thereby providing the amphiphilic structures. This structural design resulted in materials with a strong intermolecular order in the solid state, which was confirmed by differential scanning calorimetry and polarized optical microscopy. Langmuir-Blodgett (LB) films of ordered mono- and multilayers were transferred onto glass and silicon substrates, with layer quality, coverage, and intermolecular order controlled by layer compression pressure on the LB trough. Organic field-effect transistors and organic photovoltaics devices with active layers consisting of the amphiphilic conjugated D-A-D-type molecules were constructed to demonstrate that the LB technique is an effective layer-by-layer deposition approach to fabricate self-assembled, ordered thin films.
Synthesis of Amphiphilic Block Copolymers for Use in Biomedical Applications (2010)

The research presented in this thesis focuses on the synthesis of three amphiphilic block copolymer systems containing poly(ethylene oxide) (PEO) blocks. The polymer systems were developed for use in biomedical applications. The first of these is a series of poly(ethylene oxide-b-oxazoline) (PEO-b-POX) diblock copolymers for use in the progress towards novel nonviral gene transfer vectors. Poly(ethylene oxide-b-2-ethyl-2-oxazoline) (PEO-b-PEOX) and poly(ethylene oxide-b-2-methyl-2-oxazoline) (PEO-b-PMOX) were investigated. The PEOX block was hydrolyzed with acid to form linear polyethylenimine (L-PEI). The polycation L-PEI is well known for its DNA binding efficiency but the water solubility of the resulting DNA/polymer complex is limited. Addition of a PEO block is directed towards the formation of a water dispersible DNA/copolymer complex. Dynamic light scattering of the PEO-b-PEOX and PEO-b-PEI block copolymers indicated that both systems existed as single chains in aqueous solution at pH 7. PEO copolymers also play a significant role in the formation of magnetic magnetite nanoparticles, which are dispersible in water at biological pH (pH =7). There is significant interest in the design of magnetic nanoparticle fluids for biomedical applications including magnetic field-directed drug delivery, magnetic cell separations, and blood purification. For use in vivo, the magnetite nanoparticles must be coated with biocompatible materials. Such polymers render the nanoparticles dispersible in water. Harris et al. synthesized PEO based,
Prevalence and Predictors of Prolonged Cognitive and Psychological Symptoms Following COVID-19 in the United States (2021)

Prolonged symptoms occurred in 25% of COVID-19 positive participants, and NeuroQoL cognitive dysfunction scores were significantly worse among COVID-19 positive subjects, even after accounting for demographic and stressor covariates. Fatigue, anxiety, depression, and sleep scores did not differ between COVID-19 positive and negative respondents.
Technical new feature (1978)

Abstract A continuous process for the commercial production of isopropenyl stearate (IPS) from triple pressed stearic acid and a stabilized form of propyne has been developed. Cost estimates, including capital costs, operating costs, and profitability, for commercial scale plant production which show the process to be economically feasible are presented. This potentially profitable process offers the advantages of reliable raw material sources, minimal external thermal requirements, and usable process waste streams. For a plant producing 5 million pounds of IPS per year, the selling price range is 80 to 107 cents/lb IPS, corresponding to a raw material cost range of 27 to 54 cents/lb of IPS. For a 20 million pound per year plant, the selling price range is 58 to 85 cents/lb IPS. The selling prices include a 20% annual return on fixed capital investment. Fixed capital requirement ranges from 2.7 to 10.9 million dollars (3rd quarter, 1975) for plants ranging in size from 5 to 50 million pounds of IPS per year, respectively.
Atrous Residual Interconnected Encoder to Attention Decoder Framework for Vertebrae Segmentation via 3D Volumetric CT Images (2021)

Automatic medical image segmentation based on Computed Tomography (CT) has been widely applied for computer-aided surgery as a prerequisite. With the development of deep learning technologies, deep convolutional neural networks (DCNNs) have shown robust performance in automated semantic segmentation of medical images. However, semantic segmentation algorithms based on DCNNs still meet the challenges of feature loss between encoder and decoder, multi-scale object, restricted field of view of filters, and lack of medical image data. This paper proposes a novel algorithm for automated vertebrae segmentation via 3D volumetric spine CT images. The proposed model is based on the structure of encoder to decoder, using layer normalization to optimize mini-batch training performance. To address the concern of the information loss between encoder and decoder, we designed an Atrous Residual Path to pass more features from encoder to decoder instead of an easy shortcut connection. The proposed model also applied the attention module in the decoder part to extract features from variant scales. The proposed model is evaluated on a publicly available dataset by a variety of metrics. The experimental results show that our model achieves competitive performance compared with other state-of-the-art medical semantic segmentation methods.
Extending lithography with advanced materials (2014)

Material evolution has been a key enabler of lithography nodes in the last 30 years. This paper
explores the evolution of anti-reflective coatings and their transformation from materials that provide only
reflection control to advanced multifunctional layers. It is expected that complementary processes that do
not require a change in wavelength will continue to dominate the development of new devices and
technology nodes. New device architecture, immersion lithography, negative-tone development, multiple
patterning, and directed self-assembly have demonstrated the capabilities of extending lithography nodes
beyond what anyone thought would be possible. New material advancements for future technology nodes
are proposed.
INTRODUCTION: LAP-SHOULDER BELTS: SOME HISTORICAL ASPECTS. IN: SEAT BELTS: THE DEVELOPMENT OF AN ESSENTIAL SAFETY FEATURE (2003)

This paper provides a historical review of the development of lap-shoulder belts. The 1955 patent by R. Griswold and H. DeHaven is often considered the origin of the modern day seat belt. The 1955 belt was based on the inventors' extensive military and aviation crash safety research. Yet as early as 1920s-1930s, belt restraints were considered for aviation and passenger vehicle safety, and some of these designs were patented for motor vehicles with flexible connections to the seat, easy latching and inertia locking or take-up reels. Over the years, refinements have been introduced to the lap-shoulder belts, and today, lap-shoulder belts are commonplace and have a proven safety record. They are the most effective restraint in protecting occupants in severe crashes and the reductions in risk are even higher for serious injury than fatalities.
Lineage restriction of neuroepithelial precursor cells from fetal human spinal cord (1999)

In the presence of epidermal growth factor (EGF) and/or fibroblast growth factor 2 (FGF2), neuroepithelial precursor cells from dissociated fetal human spinal cord are mitotically active and form free-floating spheres of undifferentiated cells. Proliferating cells were obtained in approximately 40% of preparations with each mitogen, were immunoreactive for the intermediate filament nestin, and did not express neuronal- or glial-specific markers. Early passage neuroepithelial precursor cells were pluripotent and differentiated into neurons expressing MAP2a,b, NF-M, and TuJ1, and GFAP-positive astrocytes; however, oligodendrocytes were never seen. As the cells were passaged from P0 to P4, the percentage of differentiating neurons significantly decreased and the prevalence of astrocytes significantly increased. While the majority of cell populations from individual preparations stopped proliferating between 3 and 6 passages, two expanding cell lines have been successfully expanded in EGF and FGF2 for over 25 passages and have been maintained in culture for over one year. These cells express nestin and not other cell-specific lineage markers. When differentiated, these neuroepithelial cell lines differentiate only into astrocytes, showing no expression of any neuronal marker. These data suggest that continued passage under these conditions preferentially selects for spinal cord neural precursors that are restricted to the astrocytic lineage. Despite the lineage restriction of later passage cell populations, these results provide a rationale for future investigation into the lineage potential of these cells in vivo following transplantation into the adult CNS, potentially as a therapeutic approach for traumatic injury and neurodegenerative disease. J. Neurosci. Res. 57:590–602, 1999. © 1999 Wiley-Liss, Inc.
Rapid Flow Surveys via Rotating Rake System and Use in Powered Wind Tunnel Models (2014)

This paper describes a rotating rake system for rapid measurement of total and static pressure distributions in powered airframe models with complex geometries. The local actuation of the rake rotation mechanism allows access to regions of the flow not easily accessible to traditional traverse systems with wall-mounted leadscrew actuators. Local indexing of the rake pivot to the model precisely positions the rake in the presence of model vibration. The total and static rakes and mechanisms are built from commercially available hardware and materials. The rotating rake system was employed to measure total and static pressures in the propulsive streamtubes of a boundary-layer ingesting powered aircraft model in the NASA Langley 14’×22’ wind tunnel. The specific quantity of interest was the total pressure flux into and out of the propulsors, needed to quantify the power-saving benefits of the boundary layer ingestion system. The paper discusses the benefits and drawbacks of the rotating rake system for the demonstrated wind tunnel experiment and for more general flow measurements.
Colloidal Particles from conventional diagnostic to bionanotechnogy applications (2009)

International audience
Long-term in vivo monitoring of mouse and human hematopoietic stem cell engraftment with a human positron emission tomography reporter gene (2013)

Positron emission tomography (PET) reporter genes allow noninvasive whole-body imaging of transplanted cells by detection with radiolabeled probes. We used a human deoxycytidine kinase containing three amino acid substitutions within the active site (hdCK3mut) as a reporter gene in combination with the PET probe [(18)F]-L-FMAU (1-(2-deoxy-2-(18)fluoro-β-L-arabinofuranosyl)-5-methyluracil) to monitor models of mouse and human hematopoietic stem cell (HSC) transplantation. These mutations in hdCK3mut expanded the substrate capacity allowing for reporter-specific detection with a thymidine analog probe. Measurements of long-term engrafted cells (up to 32 wk) demonstrated that hdCK3mut expression is maintained in vivo with no counter selection against reporter-labeled cells. Reporter cells retained equivalent engraftment and differentiation capacity being detected in all major hematopoietic lineages and tissues. This reporter gene and probe should be applicable to noninvasively monitor therapeutic cell transplants in multiple tissues.
Three-Dimensional Ray Tracing in Toroidal Stellarators (1987)

We have applied a fully three-dimensional ray-tracing code to stellarators to examine the propagation of electromagnetic radiation near the electron cyclotron frequency in straight stellarators, toroidal stellarators, and tokamaks. The stellarators are simulated by using numerically computed vacuum magnetic fields and are assumed to have temperatures and densities which are constant on the flux surfaces. A comparison of the topology shows that, even for large aspect ratios, the 1/R B-dependence is the dominant effect on the location of the resonance and cutoff layers in the toroidal devices. Hence, straight stellarator geometry is not appropriate for ray-tracing purposes in this parameter regime.
ChemInform Abstract: A Novel Route to Preussomerins via 2‐Arylacetal Anions. (2000)

Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.