gebhart/patrepeval huggingface dataset:
Neue Veresterungsmethoden in der Peptidchemie, IV. Darstellung von tert.‐Butylestern N‐acylierter Aminosäuren mit Hilfe von tert.‐Butylacetat (1961)

Abstract N ‐Acylierte Aminosäuren wurden mit Hilfe von tert.‐Butylacetat in Anwesenheit saurer Katalysatoren in die tert.‐Butylester verwandelt. Die tert.‐Butylester von N ‐Phthalyl‐aminosäuren können durch selektive Hydrazinolyse vom Phthalylrest befreit werden. Der Veresterungsmechanismus wird besprochen.
A New Method for the HPLC Analysis of Pt(II) in Urine (1979)

Abstract An analytical method has been developed to measure Pt(II) in urine via derivatization and UV or HPLC analysis. A measured quantity of urine is heated briefly with diethyl ammonium diethyl-dithiocarbamate, and the resulting Pt(Et2NCS2)2 is extracted into a measured volume of chloroform. Concentrations of Pt(II) are determined by UV absorption at 346 nm or by reverse phase HPLC analysis. The detection limit for Pt(II) as its dithiocarbamate is ∼ 1 ng by HPLC; the concentration limit for HPLC analysis by direct extraction was ∼ 25 ng/ml. Chromatographic response was linearly related to Pt(II) concentration over the range 100-4, 000 ng/ml; dilution of more concentrated samples has extended this range to at least 30, 000 ng/ml. This method has been applied to the analysis of Pt(II) in the urine of patients who have received cis-dichlorodiamniineplatinum(II) (CDDP) chemotherapy.
Cytoplasmic RNA Sensor Pathways and Nitazoxanide Broadly Inhibit Intracellular Mycobacterium tuberculosis Growth (2019)

To establish stable infection, Mycobacterium tuberculosis (MTb) must overcome host innate immune mechanisms, including those that sense pathogen-derived nucleic acids. Here, we show that the host cytosolic RNA sensing molecules RIG-I-like receptor (RLR) signaling proteins RIG-I and MDA5, their common adaptor protein MAVS, and the RNA-dependent kinase PKR each independently inhibit MTb growth in human cells. Furthermore, we show that MTb broadly stimulates RIG-I, MDA5, MAVS, and PKR gene expression and their biological activities. We also show that the oral FDA-approved drug nitazoxanide (NTZ) significantly inhibits intracellular MTb growth and amplifies MTb-stimulated RNA sensor gene expression and activity. This study establishes prototypic cytoplasmic RNA sensors as innate restriction factors for MTb growth in human cells and it shows that targeting this pathway is a potential host-directed approach to treat tuberculosis disease.
Micellar effects on the aggregation of tetraanionic porphyrins. Spectroscopic characterization of free-base meso-tetrakis(4-sulfonatophenyl)porphyrin, (TPPS)H2, and (TPPS)M (M = zinc(II), copper(II), and vanadyl) in aqueous micellar media (1989)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTMicellar effects on the aggregation of tetraanionic porphyrins. Spectroscopic characterization of free-base meso-tetrakis(4-sulfonatophenyl)porphyrin, (TPPS)H2, and (TPPS)M (M = zinc(II), copper(II), and vanadyl) in aqueous micellar mediaKarl M. Kadish, G. B. Maiya, C. Araullo, and R. GuilardCite this: Inorg. Chem. 1989, 28, 14, 2725–2731Publication Date (Print):July 1, 1989Publication History Published online1 May 2002Published inissue 1 July 1989https://pubs.acs.org/doi/10.1021/ic00313a008https://doi.org/10.1021/ic00313a008research-articleACS PublicationsRequest reuse permissionsArticle Views956Altmetric-Citations89LEARN 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
Molecular Characterization and Expression of Pyruvate Formate-Lyase-Activating Enzyme in a Ruminal Bacterium, Streptococcus bovis (2002)

To clarify the significance of the activation of pyruvate formate-lyase (PFL) by PFL-activating enzyme (PFL-AE) in Streptococcus bovis, the molecular properties and gene expression of PFL-AE were investigated. S. bovis PFL-AE was deduced to consist of 261 amino acids with a molecular mass of 29.9 kDa and appeared to be a monomer protein. Similar to Escherichia coli PFL-AE, S. bovis PFL-AE required Fe(2+) for activity. The gene encoding PFL-AE (act) was found to be polycistronic, and the PFL gene (pfl) was not included. However, the act mRNA level changed in parallel with the pfl mRNA level, responding to growth conditions, and the change was contrary to the change in the lactate dehydrogenase (LDH) mRNA level. PFL-AE synthesis appeared to change in parallel with PFL synthesis. Introduction of a recombinant plasmid containing S. bovis pfl and the pfl promoter into S. bovis did not affect formate and lactate production, which suggests that the activity of the pfl promoter is low. When the pfl promoter was replaced by the S. bovis ldh promoter, PFL was overexpressed, which caused an increase in the formate-to-lactate ratio. However, when PFL-AE was overexpressed, the formate-to-lactate ratio did not change, suggesting that PFL-AE was present at a level that was high enough to activate PFL. When both PFL-AE and PFL were overexpressed, the formate-to-lactate ratio further increased. It is conceivable that LDH activity is much higher than PFL activity, which may explain why the formate-to-lactate ratio is usually low.
Estimating Optimal Feature Subsets Using Efficient Estimation of High-Dimensional Mutual Information (2005)

A novel feature selection method using the concept of mutual information (MI) is proposed in this paper. In all MI based feature selection methods, effective and efficient estimation of high-dimensional MI is crucial. In this paper, a pruned Parzen window estimator and the quadratic mutual information (QMI) are combined to address this problem. The results show that the proposed approach can estimate the MI in an effective and efficient way. With this contribution, a novel feature selection method is developed to identify the salient features one by one. Also, the appropriate feature subsets for classification can be reliably estimated. The proposed methodology is thoroughly tested in four different classification applications in which the number of features ranged from less than 10 to over 15,000. The presented results are very promising and corroborate the contribution of the proposed feature selection methodology.
Synthesis and biological activity of several aminonucleoside-platinum(II) complexes (1986)

Several platinum(II) complexes of 3',5'-diamino-3',5'-dideoxythymidine (compound 1), 5'-amino-5'-deoxythymidine (compound 2), and 3'-amino-3'-deoxythymidine (compound 3) and the respective 2'-deoxyuridine amino nucleoside complexes, 4-6, have been synthesized. Whereas compounds 1, 2, and 4-6 had no inhibitory effect on the replication of murine L1210 cells in cell culture, compound 3 [(3'-AdThd)2PtCl2] inhibited these cells with an ED50 of 0.8 microM. Incubation of L1210 cells with 10-20 microM compound 3 for 2 h produced less than 18% inhibition of RNA, DNA, or protein synthesis, which is of questionable significance. However a 16-h incubation resulted in an increased uptake of labeled thymidine into DNA (77%), labeled uridine into RNA (17%), and labeled amino acids into protein (100%). These unexpected results indicate that inhibition of macromolecules may not be involved in the inhibition of the replication of L1210 cells. The increased incorporation of labeled metabolites into macromolecules may be related to the increase in cell volume after a 2-h incubation of L1210 cells with compound 3 plus a marked increase after 2 h in the proportion of cells in their S phase. Compound 3 appears to delay the progression of cells through their cell cycle. A marked inhibitory effect on the transport of methionine or aminoisobutyric acid into L1210 cells was found with compound 3, which was slightly greater than that produced with cisplatin. Compound 3 had a dose-dependent effect on the survival of mice bearing the L1210 ascites neoplasm, with a T/C X 100 of 175 at a dose of 320 mg/kg. Investigation of the kinetics of decomposition in aqueous systems demonstrated that the primary UV-absorbing decomposition product is 3'-amino-3'-deoxythymidine and that only a limited amount of the compound is formed (less than 8%). Although 3'-amino-3'-deoxythymidine could account for a part of the inhibition of the replication of L1210 cells in culture, it cannot account for the inhibition of amino acid transport by compound 3, the platinum complex of 3'-amino-3'-deoxythymidine. Compound 3 has been shown to limit part of the amino acid uptake into L1210 cells in a similar manner to cisplatin.
Topological routing in SURF (1991)

4 multi-layer topological router for generating rubberband sketches is described. The router uses hierarchical top-down partitioning to perform global routing for all nets simultaneously. It combines this with successive refinement to help correct mistakes made before more detailed local info rmation is discovered. Layer assignment is performed during the partitioning process to generate routing that has fewer vias and is not restricted to one-layer one-direction. The local router uses a region connectivity graph to generate shortest-path rubber-band routing.
Transparency for computer synthesized images (1979)

Simple transparency algorithms which assume a linear transparency over an entire surface are the type most often employed to produce computer synthesized images of transparent objects with curved surfaces. Although most of the images created with these algorithms do give the impression of transparency, they usually do not look realistic. One of the most serious problems is that the intensity of the light that is transmitted through the objects is generally not proportional to the amount of material through which it must pass. Another problem is that the image seen behind the objects is not distorted as would naturally occur when the light is refracted as it passes through a material of different density. Use of a non-linear transparency algorithm can provide a great improvement in the realism of an image at a small additional cost. Making the transparency proportional to the normal to the surface causes it to decrease towards the edges of the surface where the path of the light through the object is longer. The exact simulation of refraction, however, requires that each sight ray be individually traced from the observer, through the picture plane and through each transparent object until an opaque surface is intersected. Since the direction of the ray would change as each material of differing optical density was entered, the hidden surface calculations required would be very time consuming. However, if a few assumptions are made about the geometry of each object and about the conditions under which they are viewed, a much simplier algorithm can be used to approximate the refractive effect. This method proceeds in a back to front order, mapping the current background image onto the next surface, until all surfaces have been considered.
Electricity Consumption Prediction Based on Improved WMC-GA-CV-SVR (2013)

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Inferring document relevance via average precision (2006)

We consider the problem of evaluating retrieval systems using a limited number of relevance judgments. Recent work has demonstrated that one can accurately estimate average precision via a judged pool corresponding to a relatively small random sample of documents. In this work, we demonstrate that given values or estimates of average precision, one can accurately infer the relevances of unjudged documents. Combined, we thus show how one can efficiently and accurately infer a large judged pool from a relatively small number of judged documents, thus permitting accurate and efficient retrieval evaluation on a large scale.
Finite Element Analysis of Tire Curing Process (2003)

Curing is one of the most important steps in the tire manufacturing process. During this process, a green tire is formed to the desired shape and the compound is converted to a strong, elastic material to meet tire performance needs. The process of curing is usually accomplished under pressure and an elevated temperature provided by the mold. The curing process is energy consuming and has a strong effect on material properties. To attain an optimal state of cure for different compounds of various dimensions at minimal capital and energy costs requires proper evaluation of the state of cure in a tire. Various numerical models have been proposed to determine the state of cure of rubber compounds in molds. Their applications are limited to simple geometry and boundary conditions. For a tire, which has complex shape and variable boundary conditions and is built from layers of rubber compounds and fiber/rubber composites, the finite element method appears to be an ideal candidate because of its versatility. In this paper, a simulator for the tire curing processes was developed based on the finite element method of an axisymmetric heat transfer problem for composite materials. The anisotropy of heat transfer properties of composite materials, the dependence of properties of rubber compounds on the temperature and/or the extent of cure, the time-varying boundary conditions which include the cooldown of the tire out of the press and the rigorous cure kinetic models are taken into account. The numerical simulation results of a truck tire curing process show that the simulator successfully describes the variation trends in temperature and in state of cure with the tire curing process. It also serves as the core module of an optimization algorithm, which is being developed for the tire curing and rubber formulation designs.
Antifungal activity of fermentates and their potential to replace propionate in bread (2016)

The major objective of this study was to assess the potential of commercially available ‘clean label’ fermentates to replace the preservative function of propionate in bread. This study was performed in two parts. In the first part of the study the inhibitory activities of selected fermentates, FA (cultured corn syrup and citric acid), FB (cultured wheat solids), FC (cultured dextrose) and FD (cultured dextrose), towards Penicillium chrysogenum and Penicillium paneum were assessed as a function of pH (4.5–6.5) on malt extract agar (MEA). In the second part of the study, challenge, shelf-life and sensorial tests were used to determine the suitability of these fermentates to replace calcium propionate in bread. All the fermentates evaluated in this study had appreciable inhibitory activities towards P. chrysogenum and P. paneum. As expected the antifungal activity of the fermentates was greater the lower the pH of the growth medium. Additionally, P. paneum was generally more tolerant to the fermentates than P. chrysogenum. The challenge and sensorial tests showed that bread prepared with FA (1.3%), FB (2%) and FC (1.3 and 2%) were as microbiologically stable and sensorially acceptable as the reference. Therefore, fermentates can be used as ‘label friendly’ preservatives in bread products.
Luminal CCK-releasing factors in the isolated vascularly perfused rat duodenojejunum (1990)

The factors operating at the apical side of the endocrine cell releasing cholecystokinin (CCK) were investigated using the isolated vascularly perfused rat duodenojejunum. In the protease-free intestinal segment, a 30-min infusion of glucose (280 mM), oleic acid (100 mM), or triglycerides containing short- or long-chain fatty acids did not alter significantly the basal level of portal CCK-like immunoreactivity (CCK-LI), while octanoic acid (100 mM) produced a transient rise of plasma CCK-LI to approximately 250% of basal. Infusion of proteins (5% solutions of ovalbumin or casein) or of a mixture of all amino acids brought about a modest CCK secretion. In contrast, isocaloric amounts of an ovalbumin hydrolysate produced a sharp rise of portal CCK-LI to 530% of basal followed by a well-sustained plateau secretion (420% of basal) until the end of the infusion. An acid casein hydrolysate induced a slightly less pronounced CCK-LI release and was followed in decreasing order by meat, casein, and soybean peptones. Simultaneous infusion of trypsin with ovalbumin or casein hydrolysate reduced by approximately 60% the CCK release induced by peptone alone. This effect was reversed by coinfusion of soybean trypsin inhibitor (SBTI) with the trypsin-peptone mixture. Arterial infusion of tetrodotoxin (10(-6) M) or atropine (10(-5) M) had no significant effect on the trypsin-induced inhibition of peptone-mediated CCK-LI release. Administration of SBTI or camostate alone or in combination with trypsin did not alter basal CCK. Monitor peptide produced a dose-dependent transient rise of portal CCK-LI over the range from 2 to 12 micrograms.(ABSTRACT TRUNCATED AT 250 WORDS)
SYNTHESIS OF THIAZOLES CONTAINING PHENOL AND CATECHOL GROUPS. II (1930)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTSYNTHESIS OF THIAZOLES CONTAINING PHENOL AND CATECHOL GROUPS. IIC. M. Suter and Treat B. JohnsonCite this: J. Am. Chem. Soc. 1930, 52, 4, 1585–1587Publication Date (Print):April 1, 1930Publication History Published online1 May 2002Published inissue 1 April 1930https://pubs.acs.org/doi/10.1021/ja01367a046https://doi.org/10.1021/ja01367a046research-articleACS PublicationsRequest reuse permissionsArticle Views233Altmetric-Citations7LEARN 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
ICAM-1 deficiency results in enhanced maintenance of effector CD8 T cells following infection (39.3) (2010)

Abstract CD8 T cell responses are critical for the control of intracellular pathogens, and one hallmark of an effective T cell response is the development of a memory T cell pool which can rapidly respond to reinfection. It is known that the presence of polyfunctional pathogen-specific T cells correlates with more effective protection from persistent infections as well as rechallenge; however the factors that lead to the development of these cells are still poorly understood. Interactions mediated by intercellular adhesion molecule 1 (ICAM-1) have been demonstrated to impact the quality of the T cell response, by enhancing both antigenic and cytokine signals. Utilizing mice deficient for ICAM-1, we investigated the effect of this molecule on T cell priming and the response to acute infections. No pronounced differences were observed in the effector T cell response to acute lymphocytic choriomeningitis virus (LCMV)-Armstrong infection in ICAM-1 deficient animals, however greater numbers of virus-specific cells displaying an effector phenotype (KLRG-1hi CD127lo IFNγ+ IL-2-) were maintained in ICAM-1 deficient mice at memory time points. These ICAM-1 deficient mice exhibited reduced expansion of virus-specific CD8 T cells following secondary challenge when compared to wild type mice, potentially due to already elevated numbers in ICAM-1 null mice. These data indicate a critical role for ICAM-1 in the development of immunological responses to viral pathogens.
Rational thermostabilisation of four-helix bundle dimeric de novo proteins (2021)

The stability of proteins is an important factor for industrial and medical applications. Improving protein stability is one of the main subjects in protein engineering. In a previous study, we improved the stability of a four-helix bundle dimeric de novo protein (WA20) by five mutations. The stabilised mutant (H26L/G28S/N34L/V71L/E78L, SUWA) showed an extremely high denaturation midpoint temperature (T<sub>m</sub>). Although SUWA is a remarkably hyperstable protein, in protein design and engineering, it is an attractive challenge to rationally explore more stable mutants. In this study, we predicted stabilising mutations of WA20 by in silico saturation mutagenesis and molecular dynamics simulation, and experimentally confirmed three stabilising mutations of WA20 (N22A, N22E, and H86K). The stability of a double mutant (N22A/H86K, rationally optimised WA20, ROWA) was greatly improved compared with WA20 (ΔT<sub>m</sub> = 10.6 °C). The model structures suggested that N22A enhances the stability of the α-helices and N22E and H86K contribute to salt-bridge formation for protein stabilisation. These mutations were also added to SUWA and improved its T<sub>m</sub>. Remarkably, the most stable mutant of SUWA (N22E/H86K, rationally optimised SUWA, ROSA) showed the highest T<sub>m</sub> (129.0 °C). These new thermostable mutants will be useful as a component of protein nanobuilding blocks to construct supramolecular protein complexes.
Targets and Intracellular Signaling Mechanisms for Deoxynivalenol-Induced Ribosomal RNA Cleavage (2012)

The trichothecene mycotoxin deoxynivalenol (DON), a known translational inhibitor, induces ribosomal RNA (rRNA) cleavage. Here, we characterized this process relative to (1) specific 18S and 28S ribosomal RNA cleavage sites and (2) identity of specific upstream signaling elements in this pathway. Capillary electrophoresis indicated that DON at concentrations as low as 200 ng/ml evoked selective rRNA cleavage after 6 h and that 1000 ng/ml caused cleavage within 2 h. Northern blot analysis revealed that DON exposure induced six rRNA cleavage fragments from 28S rRNA and five fragments from 18S rRNA. When selective kinase inhibitors were used to identify potential upstream signals, RNA-activated protein kinase (PKR), hematopoietic cell kinase (Hck), and p38 were found to be required for rRNA cleavage, whereas c-Jun N-terminal kinase and extracellular signal-regulated kinase were not. Furthermore, rRNA fragmentation was suppressed by the p53 inhibitors pifithrin-α and pifithrin-μ as well as the pan caspase inhibitor Z-VAD-FMK. Concurrent apoptosis was confirmed by acridine orange/ethidium bromide staining and flow cytometry. DON activated caspases 3, 8, and 9, thus suggesting the possible coinvolvement of both extrinsic and intrinsic apoptotic pathways in rRNA cleavage. Satratoxin G (SG), anisomycin, and ricin also induced specific rRNA cleavage profiles identical to those of DON, suggesting that ribotoxins might share a conserved rRNA cleavage mechanism. Taken together, DON-induced rRNA cleavage is likely to be closely linked to apoptosis activation and appears to involve the sequential activation of PKR/Hck →p38→p53→caspase 8/9→caspase 3.