gebhart/patrepeval huggingface dataset:
Total Synthesis of Olivomycin A <i>J. Am. Chem. Soc.</i> <b>1999</b>, <i>121</i>, 1990−1991 (1999)

ADVERTISEMENT RETURN TO ISSUEPREVAddition/CorrectionNEXTORIGINAL ARTICLEThis notice is a correctionTotal Synthesis of Olivomycin A J. Am. Chem. Soc.1999, 121, 1990−1991William R. Roush, Richard A. Hartz, and Darin J. GustinCite this: J. Am. Chem. Soc. 1999, 121, 16, 4092Publication Date (Web):April 7, 1999Publication History Published online7 April 1999Published inissue 1 April 1999https://pubs.acs.org/doi/10.1021/ja9955060https://doi.org/10.1021/ja9955060correctionACS PublicationsCopyright © 1999 American Chemical Society. This publication is available under these Terms of Use. Request reuse permissions This publication is free to access through this site. Learn MoreArticle Views609Altmetric-Citations-LEARN 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 PDF (13 KB) Get e-Alertsclose Get e-Alerts
An asymmetric synthesis of (R)-5-(methylamino)-5,6-dihydro-4H-imidazo-[4,5,1-ij]quinolin-2(1H)-one (1) and its [2-14C]- and [6,7-3H2]-labeled forms (1996)

(R)-5-(Methylamino)-5,6-dihydro-4H-imidazo[4,5,1-ij]quinolin-2(1H)-one (1) is a dopamine agonist which shows selectivity for the D2 receptor subtype, and is of interest as a potential drug for the treatment of Parkinson's disease. An asymmetric epoxidation approach has been used to prepare 1 in eleven steps (15% overall yield) from 8-nitroquinoline. An advanced intermediate in this synthesis, tert-butyl (R)-methyl(8-amino-1,2,3,4-tetrahydro-3-quinolinyl)carbamate (10), has been reacted with [14C]phosgene to provide a two-step synthesis of 1 labeled with carbon-14 at the C-2 position (236 μCi/mg). Bromination of 1 gave the dibromo analogue 12b which was reduced in the presence of tritium gas to give 1 labeled with tritium at the C-6 and C-7 positions (28.5 Ci/mmol). In addition to providing syntheses for labeled forms of the drug which are useful in drug disposition and receptor binding studies, this approach also provides a convenient synthesis for the unlabeled form of drug.
State-based join-points: Motivation and requirements (2005)

In developing a real-world complex application, we experience the major problem that complex concerns do not easily map onto low-level aspects with join-points based on fixed points in the program code. It is our observation that modularizing concerns and quantification are to be tackled at design-time, using suitable abstractions, with a translation to dynamic weaving at run-time. In particular, we argue that ‘abstract states’ of software entities (a concern consists of software entities) are a promising instrument for defining higher-level join-points for concerns. The specification and quantification of concerns in terms of abstract states typically result in dynamic weaving, i.e. depending on run-time states of the software entities. Based on experience, we provide requirements for supporting concern modelling and quantification at design-time, as well as an initial sketch of an approach that we investigate in this perspective. The approach is based on a new type of higher-level join-points, called state-based join-points and serves as an example of the necessity for advanced dynamic (state-based) aspect weaving. The approach is motivated and illustrated through a scenario in a real-world application, namely decentralized control software for several automatic guided vehicles in an industrial transportation system.
ANTI-INFLAMMATORY ACTIVITY AND CONCENTRATIONS OF POLYPHENOLS, FLAVONOIDS ETHANOL EXTRACT OF Dodonaea viscosa (SAPINDACEAE) (2012)

Both antiinflamatory activity of ethanolic extract of D. viscosa in induction model of granulomatous tissue and the total polyphenols and flavonoids content were evaluated in this study. The animals treated with the sample showed 54.46 3.99% inhibition of the formation of granulomatous tissue while the control group treated with nimesulide, showed 58.55 1.82% confirmed significant antiinflammatory activity. The measurements of total polyphenols and flavonoids in the extract were significant when compared to the standards, which confirms the popular use of this medicinal plant.
Enhancing our understanding of the molecular responses to hypoxia in mammals using<i>Drosophila melanogaster</i> (2000)

Drosophila melanogaster has been used as a genetic model, especially in the past decade, to examine normative biological processes and disease conditions very effectively. These span a wide range of major issues such as aging, cancer, embryogenesis, neural development, apoptosis, and alcohol intoxication. Here, we detail how the Drosophila melanogaster can be used as a genetic model to study the molecular and genetic underpinnings of the response to hypoxia. In our study of the basis of anoxia tolerance, one of the potent approaches that we use is a mutagenesis screen to identify loss-of-function mutants that are anoxia sensitive. The major advantage of this approach is that it is not biased for any particular gene or gene product. Although our screen is in progress, we already have evidence that this approach is useful.
Metabolism and disposition of the αv‐integrin ß3/ß5 receptor antagonist cilengitide, a cyclic polypeptide, in humans (2015)

Cilengitide (EMD 121974, manufactured by Merck KGaA, Darmstadt, Germany) is an αv-integrin receptor antagonist showing high affinity for αvβ3 and αvβ5.This study determined the mass balance of cilengitide in healthy volunteers receiving a single intravenous infusion of 2.1 MBq (14) C-cilengitide spiked into 250 mL of 2000 mg of cilengitide. Blood, urine, and feces were collected up to day 15 or until excretion of radioactivity was below 1% of the administered dose. Total radioactivity derived from the administration of (14) C-cilengitide and unlabeled cilengitide levels were determined and used for calculation of pharmacokinetic parameters.(14) C-cilengitide-related radioactivity was completely recovered (94.5%; 87.4%-100.6%) and was mainly excreted into urine (mean, 79.0%; range, 70.3%-88.2%) and to a lesser extent into feces (mean, 15.5%; range, 9.3%-20.3%). Of the administered dose, 77.5% was recovered as unchanged cilengitide in urine. The concentration profiles of cilengitide and total radioactivity in plasma were comparable. No circulating metabolites were identified in plasma and urine. Two metabolites,M606-1 and M606-2, were identified in feces considered to be formed by intestinal peptidases or by peptidases from fecal bacteria. In conclusion, the data show that following intravenous administration, (14) C-cilengitide was completely recovered, was excreted mainly via renal elimination, and was not metabolized systemically.
A simple and rapid colorimetric method for phytate determination (1980)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTA simple and rapid colorimetric method for phytate determinationM. Latta and M. EskinCite this: J. Agric. Food Chem. 1980, 28, 6, 1313–1315Publication Date (Print):November 1, 1980Publication History Published online1 May 2002Published inissue 1 November 1980https://pubs.acs.org/doi/10.1021/jf60232a049https://doi.org/10.1021/jf60232a049research-articleACS PublicationsRequest reuse permissionsArticle Views3905Altmetric-Citations574LEARN 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
Targeting the folate receptor for the treatment of ovarian cancer (2015)

While conventional therapies have improved the outcome for patients with ovarian cancer, the disease still accounts for the most gynecological cancer-related deaths. The development of new treatment options is needed and efforts have focused on targeted therapies which aim to improve patient outcome by increasing anti-tumor activity while minimizing toxicity. The frequent overexpression of folate receptor α (FRα) in ovarian cancer has provided the rationale for new promising therapeutic approaches that target this surface protein. Clinical evaluations of compounds that utilize two basic approaches to FR targeting have been conducted or are ongoing. One approach is based on conjugates of folate analogs, such as vintafolide, where payloads are delivered by targeting the high affinity folate binding site of the receptor. A second approach is to use antibodies or antibody-like binders that target the FRα protein. Both naked antibodies (farletuzumab) and antibody conjugates (IMGN853) are being evaluated. This review summarizes the rationale for targeting FRα in ovarian cancer and provides an overview of the promising FRα-targeting compounds being developed.
Total and lipid-bound serum sialic acid in benign and malignant breast disease. (1997)

Elevation in the total sialic acid (TSA), TSA/total protein (TSA/TP) and lipid-bound sialic acid (LASA) concentration in serum occurs in breast cancer and we have studied the applicability of the assays in classification of undefined breast tumors. Sialic acid was determined by HPLC and the statistical evaluation included the receiver operating characteristic (ROC) and Youden's index analyses. In cancer patients, the serum LASA and TSA concentration was significantly higher (p < 0.05) than in patients with benign breast disease and all the markers were significantly higher (p < 0.0001) than in normal controls. All the markers had a low accuracy (AUCs < 0.75) in differentiating between breast cancer and benign breast disease and at the specificity level of 0.95 the corresponding sensitivities were 0.32 (TSA), 0.14 (TSA/TP) and 0.23 (LASA). The results indicate that both breast cancer and benign breast disease cause elevation of TSA, TSA/TP and LASA values in serum and do not provide reliable classification of undefined breast tumors.
Optimisation of a Graph Visualization Tool: Vizz3D (2006)

Vizz3D is a graph visualization tool developed at Växjö University. It is used to visualize different aspects of software systems in 3D, based on the static analysis of source code. It can optionally use Java3D or OpenGL as a graphics library. In order to visualize huge 3D structures performance is very important. This comes from the fact that the structures must be redrawn with no delay when a user interacts with the system. If there were a delay the user would loose the cognitive orientation because his interaction and the feedback would not fit. Vizz3D was not capable to run huge visualizations fast enough, and therefore careful optimisation was essential. Additionally, the Vizz3D tool is just at the beginning of its software life cycle. For optimisation, JOGL (Java Bindings for OpenGL) was chosen. The extension with a JOGL version was necessary since the GL4Java (OpenGL for Java) wrapper used for the implementation of Vizz3D is no longer supported. JOGL was therefore needed for assuring future maintainability. The JOGL version of Vizz3D was optimised to be able to visualize huge graphs with acceptable performance. To determine what areas of Vizz3D that consumed most of its resources, the process of profiling were used. The system performance was improved according to several aspects: Computational performance, Scalability, Perceived performance, RAM footprint and Start-up time. The results were then evaluated by using benchmarking techniques. After optimisation, the performance of Vizz3D was improved a lot which led to that huge graphs now could be visualized with acceptable performance.
Fourier-transformation, phase-iteration, and least-square-fit image processing for Young's fringe pattern (1996)

The fast Fourier transform, phase iteration, and the least-square fit are combined into an automated processing technique for the analysis of Young's fringe patterns. A Young's fringe pattern is first fast-Fourier-transform filtered to get an initial phase, phase iteration is carried out to improve the phase if necessary, and then the phase is least-square fitted to a phase plane. The magnitude and the direction of the displacement associated with the Young's pattern are determined from the phase plane.
Bimodal brain-machine interface for motor control of robotic prosthetic (2004)

We are working on mapping multi-channel neural spike data, recorded from multiple cortical areas of an owl monkey, to corresponding 3D monkey arm positions. In earlier work on this mapping task, we observed that continuous function approximators (such as artificial neural networks) have difficulty in jointly estimating 3D arm positions for two distinct cases-namely, when the monkey's arm is stationary and when it is moving. Therefore, we propose a multiple-model approach that first classifies neural spike data into two classes, corresponding to two states of the monkey's arm: (1) stationary and (2) moving. Then, the output of this classifier is used as a gating mechanism for subsequent continuous models, with one model per class. In this paper, we first motivate and discuss our approach. Next, we present encouraging results for the classifier stage, based on hidden Markov models (HMMs), and also for the entire bimodal mapping system. Finally, we conclude with a discussion of the results and suggest future avenues of research.
Chitin production by <i>Lactobacillus</i> fermentation of shrimp biowaste in a drum reactor and its chemical conversion to chitosan (2005)

Abstract Chitin was produced by fermenting shrimp heads and shells with Lactobacillus plantarum 541 in a drum reactor with an internal volume of 3 dm. The crude chitin yield from heads and shells was 4.5 and 13% respectively, comparable to the values obtained by the chemical method. For shrimp heads 83% deproteination and 88% demineralisation and for shrimp shells 66% deproteination and 63% demineralisation were achieved. The liquor obtained in both cases was of good sensory quality with a high content of essential amino acids and therefore with potential to produce protein powder for human consumption. The crude chitin was refined and converted to chitosan using 12.5 M NaOH. The chitosan obtained had a residual ash and protein content below 1%, a solubility of more than 98%, a viscosity in the range 50–400 cP and a degree of deacetylation of 81–84%. The molecular weight was in the range (0.8–1.4) × 10 6 Da. IR analysis indicated that the chitosan obtained through fermentation was similar to that obtained by the chemical method. Copyright © 2005 Society of Chemical Industry
Le patrimoine, architectures et espaces, pratiques et comportements : les souks et les khans d'Alep (1994)

David Jean-Claude. Le patrimoine, architectures et espaces, pratiques et comportements : les souks et les khans d'Alep. In: Revue du monde musulman et de la Méditerranée, n°73-74, 1994. Figures de l'orientalisme en architecture, sous la direction de C. Bruant, S. Leprun et M. Volait . pp. 189-205.
Harnessing the Versatility of Bacterial Collagen to Improve the Chondrogenic Potential of Porous Collagen Scaffolds (2016)

Collagen I foams are used in the clinic as scaffolds to promote articular cartilage repair as they provide a bioactive environment for cells with chondrogenic potential. However, collagen I as a base material does not allow for precise control over bioactivity. Alternatively, recombinant bacterial collagens can be used as "blank slate" collagen molecules to offer a versatile platform for incorporation of selected bioactive sequences and fabrication into 3D scaffolds. Here, we show the potential of Streptococcal collagen-like 2 (Scl2) protein foams modified with peptides designed to specifically and noncovalently bind hyaluronic acid and chondroitin sulfate to improve chondrogenesis of human mesenchymal stem cells (hMSCs) compared to collagen I foams. Specific compositions of functionalized Scl2 foams lead to improved chondrogenesis compared to both nonfunctionalized Scl2 and collagen I foams, as indicated by gene expression, extracellular matrix accumulation, and compression moduli. hMSCs cultured in functionalized Scl2 foams exhibit decreased collagens I and X gene and protein expression, suggesting an advantage over collagen I foams in promoting a chondrocytic phenotype. These highly modular foams can be further modified to improve specific aspects chondrogenesis. As such, these scaffolds also have the potential to be tailored for other regenerative medicine applications.
Circadian Time‐Dependent Differences in Murine Tolerance to the Antihistaminic Agent Loratadine (2005)

Loratadine is a second-generation histamine H(1)-receptor antagonist used in the treatment of allergic diseases. The aim of the study was to assess whether lethal toxicity and motor incoordination (neurotoxicity) of loratadine is circadian rhythm-dependent. A total of 210 male Swiss mice, aged 10 wk, were synchronized for 3 wk to 12 h light (rest span)/12 h dark (activity span). The drug was administered per os. The choice of the sublethal (TD(50) = 82 mg/kg body weight) and the lethal (LD(50) = 4 g/kg body weight) dosage was based on preliminary studies. Each of these two doses was administered to comparable groups of animals at six different circadian time points (1, 5, 9, 13, 17, and 21 Hours After Light Onset [HALO]). The survival duration was dosing time-dependent (chi(2) = 16.96; p < 0.001). Drug dosing at 17 HALO resulted in best (67%) survival rate; whereas, dosing at 9 HALO resulted in poorest (21%) survival rate. Cosinor analyses (with a trial period tau = 24 h) validated a statistically significant circadian rhythm in survival rate (p < 0.04) with an acrophase (peak time Ø of best tolerance to loratadine) being at 17.5 HALO +/- 4.65 h. Troughs of motor incoordination were located at the administration times of 5 and 17 HALO (60% and 32% of animals affected, respectively), whereas peaks were located at 9 and 21 HALO (87% and 68% of animals affected, respectively). The 24 h mean of the motor incoordination was 61%, the mean proportion of animals affected by the treatment for the six different circadian times studies. The extent of this neurotoxic effect varied as a function of loratadine dosing time (p < 0.001). A statistically significant ultradian component rhythm (p < 0.01) with a trial period tau = 12 h was also validated. The obtained results show that the dosing time of loratadine at the mid-activity (dark) span seems to be optimal, since it corresponds to the longest (21 vs. 12 days) survival span and to least neurotoxicity.
Regional Frequency Analysis of Wabash River Flood Data by L-Moments (1997)

Regional frequency analysis is used to estimate flood quantiles in a region. It is also used to identify parent distributions by analyzing the data from a number of stations within a region. The basic idea behind regional frequency analysis is to make use of similarities in the characteristics of floods at different sites in a region. Consequently, regional homogeneity is essential for such an analysis. L-moments are used in this study to investigate the feasibility of regional frequency analysis in the Wabash River basin. The Wabash River basin is shown to be hydrologically heterogeneous. It is divided into smaller subregions by using L-moment ratio diagrams. The generalized extreme value distribution is recommended to be the regional parent distribution. Both the Pearson-III and the three-parameter lognormal distributions are acceptable at the at-site level. The goodness of fit at both the at-site and regional levels is compared for a homogeneous and for a heterogeneous region.
Involvement of Bcl-2 and IL-2R in HIV-positive patients whose CD4 cell counts fail to increase rapidly with highly active antiretroviral therapy (2002)

Our study characterizes the defective maintenance of peripheral CD4 T lymphocytes in CD4-LR patients, probably resulting from Bcl-2 underexpression and dysregulation of the IL-2R system.
Surface analysis of electrochromic displays of iron hexacyanoferrate films by x-ray photoelectron spectroscopy (1987)

Electrochromic displays made from thin films of iron hexacyanoferrate (Prussian blue) deposited on tin oxide/glass substrates by electroreduction from solution are studied by x-ray photoelectron spectroscopy (XPS). It was determined by XPS that the concentration of potassium ions in the film increased as the number of electrochromic switches the film had undergone increased. This was accompanied by a decrease in the electrochromic performance of the film. The incorporation of potassium ions into the Prussian blue lattice causes a structural reorganization of the lattice with the expulsion of ferric ions from the lattice. The expulsion of ferric ions results in a degradation of the film’s electrochromic properties. This agrees qualitatively with data collected by in situ optical spectroscopy, XPS, atomic absorption spectrometry, optical microscopy, and x-ray diffraction. The rate of degradation can be reduced substantially by inclusion of an Fe(II)/Fe(III) containing solution in switching electrolyte. The role of ionic transport in the degradation mechanism is discussed.
CD8+ but not CD4+ T cells require cognate interactions with target tissues to mediate GVHD across only minor H antigens, whereas both CD4+ and CD8+ T cells require direct leukemic contact to mediate GVL (2008)

Whether T-cell antigen receptors (TCR) on donor T cells require direct interactions with major histocompatibility complex class I or class II (MHCI/MHCII) molecules on target cells to mediate graft-versus-host disease (GVHD) and graft-versus-leukemia (GVL) is a fundamental question in allogeneic stem-cell transplantation (alloSCT). In MHC-mismatched mouse models, these contacts were not required for GVHD. However, this conclusion may not apply to MHC-matched, multiple minor histocompatibility antigen-mismatched alloSCT, the most common type performed clinically. To address this, we used wild-type (wt)-->MHCI-/- or wt-->MHCII-/- bone marrow chimeras as recipients in GVHD experiments. For GVL experiments, we used MHCI-/- or MHCII-/- chronic-phase CML cells created by expressing the BCR-ABL cDNA in bone marrow from MHCI-/- or MHCII-/- mice. TCR/MHCI contact was obligatory for both CD8-mediated GVHD and GVL. In contrast, CD4 cells induced GVHD in wt-->MHCII-/- chimeras, whereas MHCII-/- mCP-CML was GVL-resistant. Donor CD4 cells infiltrated affected skin and bowel in wt-->MHCII-/- recipients, indicating that they mediated GVHD by acting locally. Thus, CD4 cells use distinct effector mechanisms in GVHD and GVL: direct cytolytic action is required for GVL but not for GVHD. If these noncytolytic pathways can be inhibited, then GVHD might be ameliorated while preserving GVL.