gebhart/patrepeval huggingface dataset:
A selective .delta.1 opioid receptor agonist derived from oxymorphone. Evidence for separate recognition sites for .delta.1 opioid receptor agonists and antagonists (1993)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTA selective .delta.1 opioid receptor agonist derived from oxymorphone. Evidence for separate recognition sites for .delta.1 opioid receptor agonists and antagonistsP. S. Portoghese, S. T. Moe, and A. E. TakemoriCite this: J. Med. Chem. 1993, 36, 17, 2572–2574Publication Date (Print):August 1, 1993Publication History Published online1 May 2002Published inissue 1 August 1993https://pubs.acs.org/doi/10.1021/jm00069a017https://doi.org/10.1021/jm00069a017research-articleACS PublicationsRequest reuse permissionsArticle Views216Altmetric-Citations69LEARN ABOUT THESE METRICSArticle Views are the COUNTER-compliant sum of full text article downloads since November 2008 (both PDF and HTML) across all institutions and individuals. These metrics are regularly updated to reflect usage leading up to the last few days.Citations are the number of other articles citing this article, calculated by Crossref and updated daily. Find more information about Crossref citation counts.The Altmetric Attention Score is a quantitative measure of the attention that a research article has received online. Clicking on the donut icon will load a page at altmetric.com with additional details about the score and the social media presence for the given article. Find more information on the Altmetric Attention Score and how the score is calculated. Share Add toView InAdd Full Text with ReferenceAdd Description ExportRISCitationCitation and abstractCitation and referencesMore Options Share onFacebookTwitterWechatLinked InRedditEmail Other access optionsGet e-Alertsclose Get e-Alerts
Switchgrass Winter Yield, Year‐Round Elemental Concentrations, and Associated Soil Nutrients in a Zero Input Environment (2013)

The maximum biomass yield of switchgrass ( Panicum virgatum L.) usually is achieved with one seasonal autumn harvest. However, information is limited on the influences of winter harvesting on annual biomass yield and on quality parameters impacting conversion into bioethanol. Accordingly, the objectives of this study were to assess: (i) yield of standing field cured biomass at monthly intervals through winter, (ii) year‐round elemental composition of biomass, and (iii) associated year‐round soil nutrient status. An unfertilized ‘Kanlow’ switchgrass planting established in 1998 was used for this study conducted from November 2007 to October 2010. The experimental treatment was monthly harvest from November to the following March and year‐round monthly sampling of biomass (except April) and soil for chemical analyses. The 3‐yr mean dry matter yield of winter harvests was 5.94Mg ha −1 , ranging from 3.88 Mg ha −1 in the winter of 2007–2008 to 7.55 Mg ha −1 in 2009–2010. Monthly biomass yield differences were significant in Years 1 and 3 but not in Year 2. Concentrations of biomass elements and soil nutrients changed with various degrees over the 3 yr. Concentrations of ash, cell wall components, and mineral nutrients, except P, K, and S, did not change appreciably across winter months. Early winter harvests resulted in less yield loss compared to late winter harvests. These findings will be valuable in harvest management for switchgrass biomass production.
Near Infrared Spectroscopic Authentication of Seafood (2013)

Near infrared (NIR) spectroscopic investigations of whole fish and fish fillets with a miniaturised, hand-held instrument were performed to demonstrate the feasibility of discriminating high-quality, expensive from lower-quality, less expensive, substitutes and responding to the increasing concerns regarding fraud and deception in seafood marketing. Generally, such problems can occur due to the mislabelling of products in the harvesting and processing system or species substitution at the restaurant level. To test the possibility of distinguishing superior from lower quality fish species, NIR spectra were measured in diffuse reflection from the skin and meat of the investigated fish. Subsequently, the spectra were evaluated by principal component analysis and further classified by soft independent modelling of class analogies. In the present communication, the results obtained with respect to the authentication of two different species of mullet, cod and trout, respectively, will be discussed in some detail.
Electrochemical detection of <i>Pseudomonas</i> in wound exudate samples from patients with chronic wounds (2016)

In clinical practice, point-of-care diagnostic testing has progressed rapidly in the last decade. For the field of wound care, there is a compelling need to develop rapid alternatives for bacterial identification in the clinical setting, where it generally takes over 24 hours to receive a positive identification. Even new molecular and biochemical identification methods require an initial incubation period of several hours to obtain a sufficient number of cells prior to performing the analysis. Here we report the use of an inexpensive, disposable electrochemical sensor to detect pyocyanin, a unique, redox-active quorum sensing molecule released by Pseudomonas aeruginosa, in wound fluid from patients with chronic wounds enrolled in the WE-HEAL Study. By measuring the metabolite excreted by the cells, this electrochemical detection strategy eliminates sample preparation, takes less than a minute to complete, and requires only 7.5 μL of sample to complete the analysis. The electrochemical results were compared against 16S rRNA profiling using 454 pyrosequencing. Blind identification yielded 9 correct matches, 2 false negatives, and 3 false positives giving a sensitivity of 71% and specificity of 57% for detection of Pseudomonas. Ongoing enhancement and development of this approach with a view to develop a rapid point-of-care diagnostic tool is planned.
Discovery of 2-[1-(4,4-Difluorocyclohexyl)piperidin-4-yl]-6-fluoro-3-oxo-2,3-dihydro-1<i>H</i>-isoindole-4-carboxamide (NMS-P118): A Potent, Orally Available, and Highly Selective PARP-1 Inhibitor for Cancer Therapy (2015)

The nuclear protein poly(ADP-ribose) polymerase-1 (PARP-1) has a well-established role in the signaling and repair of DNA and is a prominent target in oncology, as testified by the number of candidates in clinical testing that unselectively target both PARP-1 and its closest isoform PARP-2. The goal of our program was to find a PARP-1 selective inhibitor that would potentially mitigate toxicities arising from cross-inhibition of PARP-2. Thus, an HTS campaign on the proprietary Nerviano Medical Sciences (NMS) chemical collection, followed by SAR optimization, allowed us to discover 2-[1-(4,4-difluorocyclohexyl)piperidin-4-yl]-6-fluoro-3-oxo-2,3-dihydro-1H-isoindole-4-carboxamide (NMS-P118, 20by). NMS-P118 proved to be a potent, orally available, and highly selective PARP-1 inhibitor endowed with excellent ADME and pharmacokinetic profiles and high efficacy in vivo both as a single agent and in combination with Temozolomide in MDA-MB-436 and Capan-1 xenograft models, respectively. Cocrystal structures of 20by with both PARP-1 and PARP-2 catalytic domain proteins allowed rationalization of the observed selectivity.
1/2-inch 7.2MPixel CMOS Image Sensor with 2.25/spl mu/m Pixels Using 4-Shared Pixel Structure for Pixel-Level Summation (2006)

A 1/2-inch 7.2Mpixel CMOS image sensor with 2.25μm pixels employs a 4-shared pixel structure with pixel-level charge summation. It achieves a 57% fill factor, full well capacity of 14ke- with 41dB maximum SNR at full resolution, 8e-random noise, 15ke-/lux-s sensitivity, and a 3dB increment in SNR for pixel-level charge summation and sub-sampling operation. A 0.13μm Cu process is used
Static power reduction in caches using deterministic naps (2014)

We propose a technique that reduces static power consumption in caches with negligible hardware overhead and no performance penalties. Our proposed architecture achieves this by deterministically lowering the power state of cache lines that are guaranteed not to be accessed in the immediate future by exploiting in-flight cache access information. We simulated our architecture using the Simplescalar and Cacti toolsets, and observed up to 92% reduction in static power consumption in SPEC2006 benchmarks with no performance penalties and minimal hardware overhead.
Investigation of a genetic transformation system in onion (1994)

A genetic transformation system via the pollen tube pathway was investigated. Plasmid pD0432 (Ow et al., 1986), containing the cauliflower mosaic virus 35S promoter fused to the firefly(Photinus pyralis Linnaeus) luciferase coding sequence and a nopaline synthase terminator sequence, was used as the vector. Plasmid DNA prepared with each of 4 different methods was applied to the surface of the remaining style of florets decapitated 18 or 24 hours following pollination. There were no significant differences in percentage of fruit set between exogenous DNA application time (18 or 24 hours following pollination), among treatments (plasmid DNA solution, control solution, and no solution applied), or interaction between application time and treatments. According to the observation of the movement of EB-labeled plasmid DNA, plasmid DNA reached the ovules of decapitated florets within 24 hours after its application to the surface of remaining styles at 18 hours after pollination. Plasmid DNA mixed with 1/2 liquid MS medium (Musrashige & Skoog, 1964) containing 4 mg/l NAA and 4 mg/l GA3, plus 0.25% DMSO may have facilitated the entrance of plasmid DNA into onion ovules via the pollen tube pathway. Based on the result of PCR analysis of genomic DNA, 12 to 15% of the plants tested had the 282 bp fragment, the specific portion of the luciferase gene construct. Exogenous DNA should be applied to the decapitated onion florets no later than 18 hour following pollination. Southern blotting of genomic DNA from PCR positive plants indicated that the firefly luciferase gene construct may have been incorporated into the genomic DNA of onion. However, insertion of the foreign DNA in some of the PCR positive plants may have been chimeric since the 282 bp PCR amplified fragment could not be detected at their maturing stages and thereafter (in Allium, cepa cv. DG133), and in some sexually produced progeny (in A fistulosum cv. Heshiko). In addition, expression of the firefly luciferase gene construct was not detected in any of the putative transgenic plants. Some of the PCR positive Heshiko plants, derived from seeds harvested from florets treated with a DNA preparation containing 1/2 liquid MS medium supplied with 4 mg/l NAA, 4 mg/l GA3, still had the 282 bp fragment of the luciferase gene construct in their sexually produced progenies. These results indicated that transformation via the pollen tube pathway has the potential to produce stably transformed onion plants.
Prostaglandin E2 is essential for efficacious skeletal muscle stem-cell function, augmenting regeneration and strength (2017)

Skeletal muscles harbor quiescent muscle-specific stem cells (MuSCs) capable of tissue regeneration throughout life. Muscle injury precipitates a complex inflammatory response in which a multiplicity of cell types, cytokines, and growth factors participate. Here we show that Prostaglandin E2 (PGE2) is an inflammatory cytokine that directly targets MuSCs via the EP4 receptor, leading to MuSC expansion. An acute treatment with PGE2 suffices to robustly augment muscle regeneration by either endogenous or transplanted MuSCs. Loss of PGE2 signaling by specific genetic ablation of the EP4 receptor in MuSCs impairs regeneration, leading to decreased muscle force. Inhibition of PGE2 production through nonsteroidal anti-inflammatory drug (NSAID) administration just after injury similarly hinders regeneration and compromises muscle strength. Mechanistically, the PGE2 EP4 interaction causes MuSC expansion by triggering a cAMP/phosphoCREB pathway that activates the proliferation-inducing transcription factor, <i>Nurr1</i> Our findings reveal that loss of PGE2 signaling to MuSCs during recovery from injury impedes muscle repair and strength. Through such gain- or loss-of-function experiments, we found that PGE2 signaling acts as a rheostat for muscle stem-cell function. Decreased PGE2 signaling due to NSAIDs or increased PGE2 due to exogenous delivery dictates MuSC function, which determines the outcome of regeneration. The markedly enhanced and accelerated repair of damaged muscles following intramuscular delivery of PGE2 suggests a previously unrecognized indication for this therapeutic agent.
A MEMS-Based Fuel Cell for Microscale Energy Conversion (2002)

A novel approach to realize a miniature fuel cell power source by combining thin film solid-oxide or proton exchange membrane electrolyte-electrode materials with MEMS techniques to integrate a fuel cell stack monolithically on a manifolded host structure is described. This architecture enable a scalable, portable fuel cell power source system for a broad range of applications having power requirements in the < 1 W to > 10 W regime. The MEMS approach offers a direct means to integrate the fuel cell stack with required manifolding and fuel delivery system, while providing the means to control the performance of the power source for specific applications. Results describing the fabrication, integration, and testing of MEMS-based fuel cells are presented below.
Regulation of Rad51 promoter (2014)

The DNA double-strand break repair and homologous recombination protein Rad51 is overexpressed in the majority of human cancers. This correlates with therapy resistance and decreased patient survival. We previously showed that constructs containing Rad51 promoter fused to a reporter gene are, on average, 850-fold more active in cancer cells than in normal cells. It is not well understood what factors and sequences regulate the Rad51 promoter and cause its high activity in cancerous cells. Here we characterized regulatory regions and examined genetic requirements for oncogenic stimulation of the Rad51 promoter. We identified specific regions responsible for up- and downregulation of the Rad51 promoter in cancerous cells. Furthermore, we show that Rad51 expression is positively regulated by EGR1 transcription factor. We then modeled the malignant transformation process by expressing a set of oncoproteins in normal human fibroblasts. Expression of different combinations of SV40 large T antigen, oncogenic Ras and SV40 small T antigen resulted in step-wise increase in Rad51 promoter activity, with all the 3 oncoproteins together leading to a 47-fold increase in expression. Cumulatively, these results suggest that Rad51 promoter is regulated by multiple factors, and that its expression is gradually activated as cells progress toward malignancy.
Efficient large size transforms for high-performance video coding (2010)

This paper describes design of transforms for extended block sizes for video coding. The proposed transforms are orthogonal integer transforms, based on a simple recursive factorization structure, and allow very compact and efficient implementations. We discuss techniques used for finding integer and scale factors in these transforms, and describe our final design. We evaluate efficiency of our proposed transforms in VCEG's H.265/JMKTA framework, and show that they achieve nearly identical performance compared to much more complex transforms in the current test model.
Targeting recombinant thrombomodulin fusion protein to red blood cells provides multifaceted thromboprophylaxis (2012)

Thrombin generates fibrin and activates platelets and endothelium, causing thrombosis and inflammation. Endothelial thrombomodulin (TM) changes thrombin's substrate specificity toward cleavage of plasma protein C into activated protein C (APC), which opposes its thrombotic and inflammatory activities. Endogenous TM activity is suppressed in pathologic conditions, and antithrombotic interventions involving soluble TM are limited by rapid blood clearance. To overcome this problem, we fused TM with a single chain fragment (scFv) of an antibody targeted to red blood cells. scFv/TM catalyzes thrombin-mediated generation of activated protein C and binds to circulating RBCs without apparent damage, thereby prolonging its circulation time and bioavailability orders of magnitude compared with soluble TM. In animal models, a single dose of scFv/TM, but not soluble TM, prevents platelet activation and vascular occlusion by clots. Thus, scFv/TM serves as a prodrug and provides thromboprophylaxis at low doses (0.15 mg/kg) via multifaceted mechanisms inhibiting platelets and coagulation.
Artificial Soil With Build-In Plant Nutrients (1995)

Nutrients contained in sandlike material. Artificial soil provides nutrients to plants during several growing seasons without need to add fertilizer or nutrient solution. When watered, artificial soil slowly releases all materials a plant needs to grow. Developed as medium for growing crops in space. Also used to grow plants on Earth under controlled conditions or even to augment natural soil.
Reliability Aspects of Capacitive MEMS Devices (2011)

Capacitive MEMS device forms a key building block for many applications, including sensors, RF applications, user interface technologies, transducers, MEMS displays. In this paper, some important concepts of capacitive MEMS reliability physics will be discussed along with the methodology to evaluate it. Packaging effects will also be covered, as investigated under controlled environment in a dedicated vacuum chamber.
Mid-Infrared Single-Photon Detection with Tungsten Silicide Superconducting Nanowires (2013)

Get PDF Email Share Share with Facebook Tweet This Post on reddit Share with LinkedIn Add to CiteULike Add to Mendeley Add to BibSonomy Get Citation Copy Citation Text F. Marsili, V. B. Verma, M. J. Stevens, J. A. Stern, M. D. Shaw, A. J. Miller, D. Schwarzer, A. Wodtke, R. P. Mirin, and S. W. Nam, "Mid-Infrared Single-Photon Detection with Tungsten Silicide Superconducting Nanowires," in CLEO: 2013, OSA Technical Digest (online) (Optical Society of America, 2013), paper CTu1H.1. Export Citation BibTex Endnote (RIS) HTML Plain Text Citation alert Save article
Towards DNA‐Encoded Micellar Chemistry: DNA‐Micelle Association and Environment Sensitivity of Catalysis (2021)

The development of DNA-compatible reaction methodologies is a central theme to advance DNA-encoded screening library technology. Recently, we were able to show that sulfonic acid-functionalized block copolymer micelles facilitated Brønsted acid-promoted reactions such as the Povarov reaction on DNA-coupled starting materials with minimal DNA degradation. Here, the impact of polymer composition on micelle shape, and reaction conversion was investigated. A dozen sulfonic acid-functionalized block copolymers of different molar mass and composition were prepared by RAFT polymerization and were tested in the Povarov reaction, removal of the Boc protective group, and the Biginelli reaction. The results showed trends in the polymer structure-micellar catalytic activity relationship. For instance, micelles composed of block copolymers with shorter acrylate ester chains formed smaller particles and tended to provide faster reaction kinetics. Moreover, fluorescence quenching experiments as well as circular dichroism spectroscopy showed that DNA-oligomer-conjugates, although highly water-soluble, accumulated very effectively in the micellar compartments, which is a prerequisite for carrying out a DNA-encoded reaction in the presence of polymer micelles.
Synergy of Sodium Nitroprusside and Nitrate in Inhibiting the Activity of Sulfate Reducing Bacteria in Oil-Containing Bioreactors (2018)

Sodium nitroprusside (SNP) disrupts microbial biofilms through the release of nitric oxide (NO). The actions of SNP on bacteria have been mostly limited to the genera <i>Pseudomonas</i>, <i>Clostridium</i>, and <i>Bacillus</i>. There are no reports of its biocidal action on sulfate-reducing bacteria (SRB), which couple the reduction of sulfate to sulfide with the oxidation of organic electron donors. Here, we report the inhibition and kill of SRB by low SNP concentrations [0.05 mM (15 ppm)] depending on biomass concentration. Chemical reaction of SNP with sulfide did not compromise its efficacy. SNP was more effective than five biocides commonly used to control SRB. Souring, the SRB activity in oil reservoirs, is often controlled by injection of nitrate. Control of SRB-mediated souring in oil-containing bioreactors was inhibited by 4 mM (340 ppm) of sodium nitrate, but required only 0.05 mM (15 ppm) of SNP. Interestingly, nitrate and SNP were found to be highly synergistic with 0.003 mM (1 ppm) of SNP and 1 mM (85 ppm) of sodium nitrate being sufficient in inhibiting souring. Hence, using SNP as an additive may greatly increase the efficacy of nitrate injection in oil reservoirs.
One-shot deflectometry for high-speed inline inspection of specular quasi-plane surfaces (2021)

Deflectometry is a non-contact optical technique which uses a simple system setup to measure and inspect specular surfaces. Conventional deflectometry methods usually need very complicated system calibration and time-consuming phase-shifting methods, which are not practical for high-speed measurement. But if the measurement target is a quasi-plane surface where the local slope is directly modulated by phase, the complicated system calibration can be neglected. In this study, to reduce error, we investigated and analyzed error contribution when measuring quasi-plane surfaces. A simple and high speed one-shot phase retrieval method is proposed for quickly measuring surface phase. We used a single high carrier-frequency composite pattern for pattern projection, and derivation of the captured fringe pattern for phase retrieval. A phase-related slope is obtained for slope calculation and the 3D shape is reconstructed by integrating the surface slopes. We verified our proposed method by measuring representative quasi-plane surfaces and comparing results with conventional methods.
Alumina Paste Layer as a Sublimation Suppression Barrier for Yb14MnSb11 (2010)

Sublimation is a major cause of degradation of thermoelectric power generation systems. Most thermoelectric materials tend to have peak values at the temperature where sublimation occurs. A sublimation barrier is needed that is stable at operating temperatures, inert against thermoelectric materials, and able to withstand thermal cycling stress. A porous alumina paste layer is suitable as a sublimation barrier for Yb14MnSb11. It can accommodate stress generated by the thermal expansion discrepancy between the suppression layer and thermoelectric materials. Sublimation suppression is achieved by filling pores naturally with YbO2, a natural byproduct of sublimation. YbO2 generated during the sublimation of Yb14MnSb11 fills the porous structure of the alumina paste, causing sublimation to decrease with time as the pores become filled.
Synthetically Simple, Highly Resilient Hydrogels (2012)

Highly resilient synthetic hydrogels were synthesized by using the efficient thiol-norbornene chemistry to cross-link hydrophilic poly(ethylene glycol) (PEG) and hydrophobic polydimethylsiloxane (PDMS) polymer chains. The swelling and mechanical properties of the hydrogels were controlled by the relative amounts of PEG and PDMS. The fracture toughness (Gc) was increased to 80 J/m2 as the water content of the hydrogel decreased from 95% to 82%. In addition, the mechanical energy storage efficiency (resilience) was more than 97% at strains up to 300%. This is comparable with one of the most resilient materials known: natural resilin, an elastic protein found in many insects, such as in the tendons of fleas and the wings of dragonflies. The high resilience of these hydrogels can be attributed to the well-defined network structure provided by the versatile chemistry, low cross-link density, and lack of secondary structure in the polymer chains.