gebhart/patrepeval huggingface dataset:
Protoporphyrin IX/Cobyrinate Derived Hybrids – Novel Activators of Soluble Guanylyl Cyclase (2013)

A new cobyrinate/protoporphyrin IX molecular hybrids were prepared via CuAAC reaction. The synthesis involved selective preparation of cobyrinate and PpIX derived building blocks possessing respectively terminal alkyne and azide moieties followed by the CuOAc catalyzed cycloaddition reaction. Synthesized molecules activated soluble guanylyl cyclase showing strong linker length/activation dependence.
Total Synthesis of Narbonolide and Biotransformation to Pikromycin (2006)

An improved total synthesis of narbonolide and its biotransformation to pikromycin is reported. This total synthesis utilized an intramolecular Nozaki-Hiyama-Kishi coupling that significantly improved macrocyclization yields (90-96%) and allowed for differentiation of the C3- and C5-oxidation states. A pikAI deletion mutant of Streptomyces venezuelae was used to biotransform synthetic narbonolide to pikromycin by glycosylation and oxidation in vivo. This integration of synthetic chemistry and engineered biotransformations holds great promise for the synthesis of novel macrolide analogues of biological interest.
Hybrid quantum circuits: Superconducting circuits interacting with other quantum systems (2013)

Hybrid quantum circuits combine two or more physical systems, with the goal of harnessing the advantages and strengths of the different systems in order to better explore new phenomena and potentially bring about novel quantum technologies. This article presents a brief overview of the progress achieved so far in the field of hybrid circuits involving atoms, spins, and solid-state devices (including superconducting and nanomechanical systems). How these circuits combine elements from atomic physics, quantum optics, condensed matter physics, and nanoscience is discussed, and different possible approaches for integrating various systems into a single circuit are presented. In particular, hybrid quantum circuits can be fabricated on a chip, facilitating their future scalability, which is crucial for building future quantum technologies, including quantum detectors, simulators, and computers.
CAD-based graphical computer simulation in endoscopic surgery. (1993)

This article presents new techniques for three-dimensional, kinematic realtime simulation of dextrous endoscopic instruments. The integrated simulation package KISMET is used for engineering design verification and evaluation. Geometric and kinematic computer models of the mechanisms and the laparoscopic workspace were created. Using the advanced capabilities of high-performance graphical workstations combined with state-of-the-art simulation software, it is possible to generate displays of the surgical instruments acting realistically on the organs of the digestive system. The organ geometry is modelled in a high degree of detail. Apart from discussing the use of KISMET for the development of MFM-II (Modular Flexible MIS Instrument, Release II), the paper indicates further applications of realtime 3D graphical simulation methods in endoscopic surgery.
<title>Approximate models for resist processing effects</title> (1996)

Process windows are frequently generated from simulated aerial image profiles by use of a threshold model for the resist process, an assumption which is not accurate for many processes. In this paper, we present new computationally efficient methods for incorporating the effects of resist processing into simulated images. The First Order Model of development leads to the simple result that the resist linewidth W is smaller than the threshold linewidth W<SUB>thresh</SUB> by an amount (Delta) W approximately equals 2 [ln(D(gamma) s)-1]/((gamma) s), where D is the resist thickness, (gamma) is the resist process non-linearity and s is the log-slope of the image. A Second Order Model based on a segmented development path is also presented. These models allow the prediction of resist linewidths based on calculated image profiles for any wet developed process: optical, X-ray or e-beam lithography, both positive and negative resists. The predictions of these models show good agreement with full PROLITH/2 resist profile simulations. We have also incorporated a Fickian diffusion of the intensity profile into our model, to account for acid diffusion, stepper vibration, lens aberrations, and other effects which reduce process resolution. Experimental process windows are well matched by such models, and are significantly different than threshold model predictions.
HOPES RIDE ON DRUG CANDIDATES (2005)

RETURN TO ISSUEPREVNewsNEXTHOPES RIDE ON DRUG CANDIDATESResearchers reveal potential new medicines for thrombosis, anxiety, diabetes, and cancerSTU BORMANCite this: Chem. Eng. News 2005, 83, 16, 40–44Publication Date (Print):April 18, 2005Publication History Published online14 November 2010Published inissue 18 April 2005https://pubs.acs.org/doi/10.1021/cen-v083n016.p040https://doi.org/10.1021/cen-v083n016.p040newsACS PublicationsCopyright © 2005 AMERICAN CHEMICAL SOCIETYArticle Views13Altmetric-Citations4LEARN 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 options SUBJECTS:Pharmaceuticals Get e-Alerts
The preparation of thiophene-S,S-dioxides and their role in organic electronics (2012)

In the last decade, Rozen's reagent (HOF·CH3CN) has been shown to be powerful yet selective enough to oxidize thiophene moieties in various environments. The resulting thiophene-S,S-dioxides display attractive properties for electronic devices, in particular a reduced HOMO–LUMO band gap. This highlight illustrates how utilizing this unprecedentedly potent oxidizing agent allows access to an exciting new family of molecules that show great promise for semiconductors.
A QSAR Approach for the Prediction of Stability of Benzoglycolamide Ester Prodrugs (2006)

A method consisting of quantitative structure-activity relationship (QSAR) (MLR) was developed to predict the hydrolytic rate constant of 37 benzoglycolamide ester prodrugs. The regression method was used as a calibration model for calculating the hydrolytic rate constant and investigating their linear characteristics. The QSAR study indicated the importance of the descriptors charge on amide nitrogen (AN), lipophilic parameter (log P) and nucleophilic frontal density (NUFD) in contribution to the ester hydrolysis with the correlation coefficient value of 0.908 for the developed MLR model. The models were validated by leave one out (LOO) technique as well as by the calculation of statistical parameters for the developed MLR models.
Sugar-Dependent Expression of the CHS-A Gene for Chalcone Synthase from Petunia in Transgenic Arabidopsis (1991)

Transgenic Arabidopsis thaliana plants were constructed by introduction of a fusion of the gene for beta-glucuronidase (GUS) to the CHS-A gene, which is one of the two genes for chalcone synthase that are actively expressed in the floral organs of petunia. The expression of the fusion gene CHS-A::GUS was low in transgenic Arabidopsis plantlets, but it was enhanced when plantlets or detached leaves were transferred to a medium that contained 0.3 molar sucrose, glucose, or fructose. No enhancement was observed when plantlets were transferred to a medium that contained 0.3 molar mannitol. Measurements of cellular levels of sugars revealed a tight linkage between the level of expression of the CHS-A::GUS gene and the level of accumulation of exogenously supplied sugars, in particular sucrose. The parallelism between the organ-specific accumulation of sugar and the organ-specific expression of the CHS-A::GUS gene was also observed in petunia and A. thaliana plants grown under normal conditions in soil. The consensus sequences for sugar responses, such as boxes II and III in members of the family of sporamin genes from the sweet potato, were found in the promoter region of the CHS-A gene that was used for fusion to the GUS gene. It is suggested that the expression of the CHS-A gene is regulated by sugars, as is the expression of other sugar-responsive genes, such as the genes for sporamin. A putative common mechanism for the control of expression of "sugar-related" genes, including the CHS-A gene, is discussed.
Tracks on the road-myth: Indo-European religions beyond Georges Dumezil’s moyen d’analyser (1999)

Dumézil regarded the insistence on etymological equations as a blockage in consideration of the Indo-European ideology, whereas the occurrence of a comparative grammar and a common religious nomenclature necessitated the advantage of genetic comparisons over comparisons excluding the notions of organic contiguity. He considered it self-evident that societies sharing a political, juridical, ethical, and religious vocabulary likewise share a coherent system of thought, and that this system may be sought beyond the manifestations of signs. This presupposition led Dumézil to compare sets of ideas, circumscribed by their inherent systematic constancy, yet dissolved in an irreversible cluster of formal variability.
PROOF: An Architecture for Rendering In Object Space (1988)

This paper gives a short introduction into the field of computer image generation in hardware. It discusses the two main approaches, namely partitioning in Image space and In object space. Based on the object space partitioning approach we have defined the PROOF architecture. PROOF is a system that aims at high performance and high quality rendering of raster images. high performance means that up to 30 pictures are generated in one second. The pictures are shaded and anti-allased, giving the images a high degree of realism. The architecture comprises tnree stages which are responsible for hidden surface removal, shading, and filtering respectively. The first of these stages a pipeline of object processors. Each of these processors stores and scan converts one obiect Furthermore, It interpolates the depth and the normal vector across the Object. Each object processor IS able to handle objects of a certain primitive type. The specialization of an object processor to a certain primitive type is encapsulated in a Single block called primitive processor. The Outout of the object processor pipeline is the input to a stage for shading. The illumination model employed takes In~o account both diffuse and specular reflections. The paper reviews Gouraud and Phong shading with regard to their suitability for a hardware implementation. The final stage of the PROOF system is formed by a stage for filtering the colours of those objects that contribute to a pixel. This done by constructing a subpixel mask and filtering across an area of 2x2 pixels. At the end. the paper briefly reports on the current state of the project.
Genome-Wide Association Studies of Anthracnose and Angular Leaf Spot Resistance in Common Bean (Phaseolus vulgaris L.) (2016)

The common bean (Phaseolus vulgaris L.) is the world's most important legume for human consumption. Anthracnose (ANT; Colletotrichum lindemuthianum) and angular leaf spot (ALS; Pseudocercospora griseola) are complex diseases that cause major yield losses in common bean. Depending on the cultivar and environmental conditions, anthracnose and angular leaf spot infections can reduce crop yield drastically. This study aimed to estimate linkage disequilibrium levels and identify quantitative resistance loci (QRL) controlling resistance to both ANT and ALS diseases of 180 accessions of common bean using genomewide association analysis. A randomized complete block design with four replicates was performed for the ANT and ALS experiments, with four plants per genotype in each replicate. Association mapping analyses were performed for ANT and ALS using a mixed linear model approach implemented in TASSEL. A total of 17 and 11 significant statistically associations involving SSRs were detected for ANT and ALS resistance loci, respectively. Using SNPs, 21 and 17 significant statistically associations were obtained for ANT and angular ALS, respectively, providing more associations with this marker. The SSR-IAC167 and PvM95 markers, both located on chromosome Pv03, and the SNP scaffold00021_89379, were associated with both diseases. The other markers were distributed across the entire common bean genome, with chromosomes Pv03 and Pv08 showing the greatest number of loci associated with ANT resistance. The chromosome Pv04 was the most saturated one, with six markers associated with ALS resistance. The telomeric region of this chromosome showed four markers located between approximately 2.5 Mb and 4.4 Mb. Our results demonstrate the great potential of genome-wide association studies to identify QRLs related to
Recent Advances in the Synthesis of C-oligosaccharides (2005)

This paper reviews the recent advances in the synthesis of catabolically stable sugar mimetics, C-oligosaccharides. These compounds are synthetic analogs of the naturally occurring O-oligosaccharides, in which the interglycosidic oxygen has been replaced by a methylene group. This review is organized in terms of chemistry used to assemble C-oligosaccarides under the sub-headings: anionic approaches, cationic methods, reductive glycosyl samarium chemistry, cyclization methodology, and free radical chemistry.
Targeting virulence not viability in the search for future antibacterials (2014)

New antibacterials need new approaches to overcome the problem of rapid antibiotic resistance. Here we review the development of potential new antibacterial drugs that do not kill bacteria or inhibit their growth, but combat disease instead by targeting bacterial virulence.
Hypocholesterolemic activity of synthetic and natural tocotrienols. (1992)

Tocotrienols are farnesylated benzopyran natural products that exhibit hypocholesterolemic activity in vitro and in vivo. The mechanism of their hypolipidemic action involves posttranscriptional suppression of HMG-CoA reductase by a process distinct from other known inhibitors of cholesterol biosynthesis. An efficient synthetic route to tocotrienols and their isolation from palm oil distillate using an improved procedure is presented. gamma-Tocotrienol exhibits a 30-fold greater activity toward cholesterol biosynthesis inhibition compared to alpha-tocotrienol in HepG2 cells in vitro. The synthetic (racemic) and natural (chiral) tocotrienols exhibit nearly identical cholesterol biosynthesis inhibition and HMG-CoA reductase suppression properties as demonstrated in vitro and in vivo.
Somatic Transgene Immunization with DNA Encoding an Immunoglobulin Heavy Chain (1997)

A plasmid DNA containing a chimeric immunoglobulin heavy-chain gene with tissue-specific promoter and enhancer elements was used as a model system to study the events triggered by a single intraspleen DNA inoculation in adult C57Bl/6 mice. A single intraspleen inoculation was followed in a week by secretion of transgene immunoglobulins and production of immunoglobulin M (IgM) anti-immunoglobulins. Their kinetics of serum appearance were almost superimposable. While anti-immunoglobulin antibodies remained detectable for over 6 months, transgene immunoglobulins disappeared after 3-4 weeks. However, transgene mRNA was detected in the spleen for 4 months. A multiplex polymerase chain reaction (PCR) analysis on splenic genomic DNA 17 days after inoculation demonstrated that the transgene was integrated in the host chromosomal DNA. The nucleotide sequence of the rearranged VDJ region from splenic genomic DNA was identical to that of the parental plasmid DNA, hence ruling out that hypermutation had occurred. A booster injection of immunoglobulin encoded by the transgene on day 200 elicited a typical secondary immune response with IgG1 and IgG2b antibodies. These results demonstrate that a single inoculation of an immunoglobulin heavy-chain DNA targeted to spleen lymphocytes leads to spontaneous integration of the transgene into the host DNA, and that this is sufficient to initiate immunity and establish immunologic memory. Our data also show that minute amounts (<100 ng/ml) of an endogenously produced protein secreted in the microenvironment of a lymphoid tissue generate immunity and establish immunologic memory rather than tolerance.
Effects of blocking B7-1 and B7-2 interactions during a type 2 in vivo immune response (1997)

The costimulatory signal provided to T cells through CD28/CTLA-4 interactions is required for in vivo Th cell effector function associated with cytokine production. However, it is uncertain whether the two well-characterized ligands for these molecules, B7-1 and B7-2, differentially influence the consequent development of a type 1 or a type 2 primary response. We have examined the in vivo effects of blocking B7-1 and/or B7-2 ligand interactions on the type 2 mucosal immune response that follows oral infection of mice with the nematode parasite, Heligmosomoides polygyrus. Administration of the combination of anti-B7-1 and anti-B7-2 Abs inhibited H. polygyrus-induced increases in serum IgG1 and IgE levels, the expansion of mesenteric lymph node (MLN) germinal centers, in situ CD4+ T cell expansion, elevated blood eosinophils, and increased intestinal mucosal mast cells. Similarly, both Abs blocked MLN and Peyer's patch cytokine gene expression and elevations in MLN T cell-derived IL-4 protein secretion. However, in the same experiments, administration of either anti-B7-1 or anti-B7-2 Abs alone had little effect on any of these parameters. T cell and B cell activation was also blocked by the combination of anti-B7-2 and a B7-1-specific mutant Y100F CTLA-4Ig construct. These results suggest that to the extent that anti-B7-1 and anti-B7-2 mAbs block B7 interactions, either B7-1 or B7-2 ligand interactions can provide the required costimulatory signals that lead to T cell effector function during a type 2 in vivo immune response.
Intel's 80960: an architecture optimized for embedded control (1988)

Important features and capabilities of the 80960 are briefly examined, and an overview of its architecture is given. A detached discussion is presented of the register model, core instruction set, register operations, memory operations, control operations instruction cache, user-supervisor protection, interrupts, faults, and debug support.< <ETX xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">&gt;</ETX>
Chemokines and Their Receptors: Drug Targets in Immunity and Inflammation (2007)

The chemokine system coordinates leukocyte migration in immunity and inflammation and is implicated in the pathogenesis of many human diseases. Although several successful strategies have been identified to develop drugs targeting chemokines and their receptors, this has not yet resulted in many new therapeutics. This is likely due to a complexity of the chemokine system, which was not initially appreciated, that is characterized by redundancy, pleiotropy, and differences among species. Nevertheless, our understanding of chemokine biology is continuing to grow and several promising drugs are currently being tested in late-stage clinical trials. In this review, we examine the role of chemokines in health and diseases and discuss strategies to target the chemokine system.
A Dual-Catalysis Approach to Enantioselective [2 + 2] Photocycloadditions Using Visible Light (2014)

In contrast to the wealth of catalytic systems that are available to control the stereochemistry of thermally promoted cycloadditions, few similarly effective methods exist for the stereocontrol of photochemical cycloadditions. A major unsolved challenge in the design of enantioselective catalytic photocycloaddition reactions has been the difficulty of controlling racemic background reactions that occur by direct photoexcitation of substrates while unbound to catalyst. Here, we describe a strategy for eliminating the racemic background reaction in asymmetric [2 + 2] photocycloadditions of α,β-unsaturated ketones to the corresponding cyclobutanes by using a dual-catalyst system consisting of a visible light-absorbing transition-metal photocatalyst and a stereocontrolling Lewis acid cocatalyst. The independence of these two catalysts enables broader scope, greater stereochemical flexibility, and better efficiency than previously reported methods for enantioselective photochemical cycloadditions.
Persistent expression of human clotting factor IX from mouse liver after intravenous injection of adeno-associated virus vectors (1997)

We previously found that gene transduction by adeno-associated virus (AAV) vectors in cell culture can be stimulated over 100-fold by treatment of the target cells with agents that affect DNA metabolism, such as irradiation or topoisomerase inhibitors. Here we show that previous gamma-irradiation increased the transduction rate in mouse liver by up to 900-fold, and the topoisomerase inhibitor etoposide increased transduction by about 20-fold. Similar rates of hepatic transduction were obtained by direct injection of the liver or by systemic delivery via tail vein injection. Hepatocytes were much more efficiently transduced than other cells after systemic delivery, and up to 3% of all hepatocytes could be transduced after one vector injection. The presence of wild-type AAV, which contaminates many AAV vector preparations, was required to observe a full response to gamma-irradiation. Injection of mice with AAV vectors encoding human clotting factor IX after gamma-irradiation resulted in synthesis of low levels of human clotting factor IX for the 5-month period of observation. These studies show the potential of targeted gene transduction of the liver by AAV vectors for treatment of various hematological or metabolic diseases.
Interaction of Human Arp2/3 Complex and the Listeria monocytogenes ActA Protein in Actin Filament Nucleation (1998)

Actin filament assembly at the cell surface of the pathogenic bacterium Listeria monocytogenes requires the bacterial ActA surface protein and the host cell Arp2/3 complex. Purified Arp2/3 complex accelerated the nucleation of actin polymerization in vitro, but pure ActA had no effect. However, when combined, the Arp2/3 complex and ActA synergistically stimulated the nucleation of actin filaments. This mechanism of activating the host Arp2/3 complex at the L. monocytogenes surface may be similar to the strategy used by cells to control Arp2/3 complex activity and hence the spatial and temporal distribution of actin polymerization.
Stem cells and lung cancer: future therapeutic targets? (2009)

In both the UK and USA more people die of lung cancer than any other type of cancer. Lung cancer's high mortality rate is also reflected on a global scale, with lung cancer accounting for more than 1 million deaths per year. In tissues with ordered structure such a lung epithelia, it is likely that the cancers have their origins in normal adult stem cells, and then the tumours themselves are maintained by a population of malignant stem cells - so-called cancer stem cells. This review examines both these postulates in animal models and in the clinical setting, noting that stem cell niches appear to foster tumour development, and that drug resistance can often be attributed to malignant cells with stem cell properties.