gebhart/patrepeval huggingface dataset:
Synthesis of saframycins. 3. Preparation of a key tricyclic lactam intermediate to saframycin A (1989)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTSynthesis of saframycins. 3. Preparation of a key tricyclic lactam intermediate to saframycin ANaoki Saito, Reiko Yamauchi, Hiroyasu Nishioka, Satoko Ida, and Akinori KuboCite this: J. Org. Chem. 1989, 54, 22, 5391–5395Publication Date (Print):October 1, 1989Publication History Published online1 May 2002Published inissue 1 October 1989https://pubs.acs.org/doi/10.1021/jo00283a043https://doi.org/10.1021/jo00283a043research-articleACS PublicationsRequest reuse permissionsArticle Views205Altmetric-Citations17LEARN 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
Chimeric Bovine Respiratory Syncytial Virus with Attachment and Fusion Glycoproteins Replaced by Bovine Parainfluenza Virus Type 3 Hemagglutinin-Neuraminidase and Fusion Proteins (2001)

Chimeric bovine respiratory syncytial viruses (BRSV) expressing glycoproteins of bovine parainfluenza virus type 3 (BPIV-3) instead of BRSV glycoproteins were generated from cDNA. In the BRSV antigenome cDNA, the open reading frames of the major BRSV glycoproteins, attachment protein G and fusion protein F, were replaced individually or together by those of the BPIV-3 hemagglutinin-neuraminidase (HN) and/or fusion (F) glycoproteins. Recombinant virus could not be recovered from cDNA when the BRSV F open reading frame was replaced by the BPIV-3 F open reading frame. However, cDNA recovery of the chimeric virus rBRSV-HNF, with both glycoproteins replaced simultaneously, and of the chimeric virus rBRSV-HN, with the BRSV G protein replaced by BPIV-3 HN, was successful. The replication rates of both chimeras were similar to that of standard rBRSV. Moreover, rBRSV-HNF was neutralized by antibodies specific for BPIV-3, but not by antibodies specific to BRSV, demonstrating that the BRSV glycoproteins can be functionally replaced by BPIV-3 glycoproteins. In contrast, rBRSV-HN was neutralized by BRSV-specific antisera, but not by BPIV-3 specific sera, showing that infection of rBRSV-HN is mediated by BRSV F. Hemadsorption of cells infected with rBRSV-HNF and rBRSV-HN proved that BPIV-3 HN protein expressed by rBRSV is functional. Colocalization of the BPIV-3 glycoproteins with BRSV M protein was demonstrated by confocal laser scan microscopy. Moreover, protein analysis revealed that the BPIV-3 glycoproteins were present in chimeric virions. Taken together, these data indicate that the heterologous glycoproteins were not only expressed but were incorporated into the envelope of recombinant BRSV. Thus, the envelope glycoproteins derived from a member of the Respirovirus genus can together functionally replace their homologs in a Pneumovirus background.
Inhibiting the Initiation ofClostridium difficileSpore Germination using Analogs of Chenodeoxycholic Acid, a Bile Acid (2010)

To cause disease, Clostridium difficile spores must germinate in the host gastrointestinal tract. Germination is initiated upon exposure to glycine and certain bile acids, e.g., taurocholate. Chenodeoxycholate, another bile acid, inhibits taurocholate-mediated germination. By applying Michaelis-Menten kinetic analysis to C. difficile spore germination, we found that chenodeoxycholate is a competitive inhibitor of taurocholate-mediated germination and appears to interact with the spores with greater apparent affinity than does taurocholate. We also report that several analogs of chenodeoxycholate are even more effective inhibitors. Some of these compounds resist 7α-dehydroxylation by Clostridium scindens, a core member of the normal human colonic microbiota, suggesting that they are more stable than chenodeoxycholate in the colonic environment.
Berberine sensitizes TRAIL-induced apoptosis through proteasome-mediated downregulation of c-FLIP and Mcl-1 proteins (2010)

Berberine (BBR) is an isoquinoline alkaloid which has a wide spectrum of clinical applications including anti-tumor, anti-microbial and anti-inflammatory activities. In this study, we showed that co-treatment with subtoxic doses of BBR and tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) induced apoptosis in human renal cancer cells, Caki cells, but not in normal tubular kidney cells. Treatment of Caki cells with BBR resulted in downregulation of c-FLIP and Mcl-1 proteins in a dose-dependent manner. The BBR-induced downregulation of c-FLIP and Mcl-1 proteins were involved in proteasome dependent pathways, which was confirmed by the result that pre-treatment with the proteasome inhibitor MG132 inhibited berberine-induced downregulation of the c-FLIP and Mcl-1 proteins. Pretreatment with N-acetyl-L-cysteine (NAC) significantly inhibited the cell death induced by the combined treatment with BBR and TRAIL as well as recovered the expression levels of c-FLIP and Mcl-1 downregulated by treatment with BBR. These results suggested that BBR-stimulated TRAIL-induced apoptosis is dependent on the generation of reactive oxygen species through the downregulation of c-FLIP and Mcl-1 proteins. In conclusion, this study demonstrates that BBR enhances TRAIL-induced apoptosis in human renal cancer cells by ROS-mediated c-FLIP and Mcl-1 down-regulation.
Medical ultrasonic probe using electrostrictive-ceramics/polymer composite (2003)

A medical ultrasonic probe the sensitivity of which is controlled by a DC bias field is developed using an electrostrictive-ceramics-polymer composite as a transducer material. (1-x)Pb(Mg/sub 1/3/Nb/sub 2/3/)O/sub 3/-xPbTiO/sub 3/ electrostrictive-ceramics ((1-x)PMN-xPt) are used because they have a large electromechanical coupling factor for the thickness vibrational mode, k/sub t/, under a practical bias field. 0.91PMN-0.09PT/polyurethane 1-3 composites (thickness 0.22 mm, 7.5 MHz) are fabricated using a dicing and filling technique. The 0.91PMN-0.09PT has no residual k/sub t/ after removing the DC bias field around room temperature. Pulse-echo experimentation shows that the echo amplitude increases with the bias field, as expected from the relationship between k/sub t/ and the bias field.< <ETX xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">&gt;</ETX>
Nanolithography using wet etched silicon nitride phase masks (1998)

A new technique for performing chromeless phase shift optical nanolithography is presented. Phase masks have been wet etched into silicon nitride membranes, using either hot H3PO4 or HF. Contact exposure through these masks results in developed photoresist features as small as 90 nm, even for masks with shallow sidewall slopes. The observed effect is attributed to the presence of an abrupt phase step at some point on the wet etch profile, although this does not need to correspond to a π phase shift in order to obtain good contrast exposures. Simulations have been performed for typical wet-etching profiles, and it is found that good contrast is expected for a very wide range of etch depths. In addition, the width of the null in the near-field intensity profile varies with etch depth, indicating that control of feature size is possible. This technique is simple and inexpensive, making it an attractive candidate for nanopatterning a wide variety of substrates.
A monoclonal antibody raised to lipomodulin recognizes T suppressor factors in two independent hapten-specific suppressor networks. (1989)

Five different Ag-binding suppressor factors from two types of hapten-specific Ts cell hybridomas (TsF1 inducer and TsF3 effector factors) were bound by an anti-lipomodulin mAb (141-B9), that crossreacts with rodent glycosylation inhibition factor (GIF). The Ag-specific suppressor activity in these hybridoma supernatants was bound by anti-lipomodulin columns and could be recovered by elution at acid pH. Additional evidence for the expression of lipomodulin/GIF activity on these TsF molecules was demonstrated by the ability of the eluted fractions to inhibit the glycosylation of IgE-binding peptides during their biosynthesis. The same biologic activity is associated with GIF and lipomodulin. The relationship between TsF and lipomodulin/GIF was confirmed in a serologic assay, which showed that TsF1 and TsF3 molecules, whether purified over Ag, anti-IJ or anti-TsF columns, are recognized by the mAb. 141-B9. The combined results indicate that Ag-binding Ts factors share a common antigenic determinant with phospholipase inhibitory proteins such as lipomodulin and GIF. In addition, the demonstration of glycosylation regulatory activity carried on these TsF molecules suggests a possible mode for their bioactivity.
Stiffness of Central Venous Catheters (1983)

Catheter stiffness has been suggested to be a principal factor in the thrombogenesis encountered after central venous cannulation. However, no data have been published to date about the stiffness of central venous catheters. A method for measuring catheter stiffness has been developed. The force needed to deflect a catheter tip 1.2 mm from a fastening point was measured with the help of a cantilever beam (Grass Model DA-7). Six different sections of each catheter were measured, and the final results expressed as an average of these. Twenty-seven central venous catheters made of silicone elastomer, polyurethane, polyvinylchloride, polyethylene and teflon were tested. The bending stiffness, EI (E = elastic modulus of the material, I = moment of inertia of catheter (a geometrical property)) was below 16 X 10(-6) Nm2 for all catheters made of silicone elastomer, polyvinylchloride and polyurethane. Polyethylene catheters were stiffer, but could be made softer by reduction of their diameters. Teflon catheters were up to 10 times stiffer than the catheters in the soft group. Heparinization and radioopacity of catheters do not significantly alter their bending stiffness. In a concomitant study the results indicate that there is a significantly lower incidence of thrombus formation in catheters with a bending stiffness below 16 X 10(-6) Nm2.
CpG island methylator phenotype in colorectal cancer (1999)

Aberrant methylation of promoter region CpG islands is associated with transcriptional inactivation of tumor-suppressor genes in neoplasia. To understand global patterns of CpG island methylation in colorectal cancer, we have used a recently developed technique called methylated CpG island amplification to examine 30 newly cloned differentially methylated DNA sequences. Of these 30 clones, 19 (63%) were progressively methylated in an age-dependent manner in normal colon, 7 (23%) were methylated in a cancer-specific manner, and 4 (13%) were methylated only in cell lines. Thus, a majority of CpG islands methylated in colon cancer are also methylated in a subset of normal colonic cells during the process of aging. In contrast, methylation of the cancer-specific clones was found exclusively in a subset of colorectal cancers, which appear to display a CpG island methylator phenotype (CIMP). CIMP+ tumors also have a high incidence of p16 and THBS1 methylation, and they include the majority of sporadic colorectal cancers with microsatellite instability related to hMLH1 methylation. We thus define a pathway in colorectal cancer that appears to be responsible for the majority of sporadic tumors with mismatch repair deficiency.
Recurrent convolutional neural networks for object-class segmentation of RGB-D video (2015)

Object-class segmentation is a computer vision task which requires labeling each pixel of an image with the class of the object it belongs to. Deep convolutional neural networks (DNN) are able to learn and exploit local spatial correlations required for this task. They are, however, restricted by their small, fixed-sized filters, which limits their ability to learn long-range dependencies. Recurrent Neural Networks (RNN), on the other hand, do not suffer from this restriction. Their iterative interpretation allows them to model long-range dependencies by propagating activity. This property might be especially useful when labeling video sequences, where both spatial and temporal long-range dependencies occur. In this work, we propose novel RNN architectures for object-class segmentation. We investigate three ways to consider past and future context in the prediction process by comparing networks that process the frames one by one with networks that have access to the whole sequence. We evaluate our models on the challenging NYU Depth v2 dataset for object-class segmentation and obtain competitive results.
Dexmedetomidine Directly Increases Tau Phosphorylation (2015)

Exposure to anesthetic agents has been linked to abnormal tau protein phosphorylation, an antecedent to the development of neurofibrillary tangles. This study evaluates the direct and indirect effects of dexmedetomidine. Primary culture of cortical neurons established from Sprague-Dawley (SD) rat embryos were exposed to dexmedetomidine for 1 or 6 hours, and the degree of tau phosphorylation at the AT8, AT180, and S396 sites was assessed by western blot analysis. To assess and compare their relative in vivo effects, the same agent was administered intravenously to 8 to 10 week old male SD rats and titrated to the loss of the righting reflex for 2 hours. After 1 hour of recovery, the rats were sacrificed and samples taken from the cortex and hippocampus were subjected to western blot and immunohistochemical analysis. The in vitro studies reviewed significant hyperphosphorylation only at the S396 site, and these changes have largely disappeared at 6 hours. With temperature maintenance, dexmedetomidine induced significant changes in hyperphosphorylation at the AT8 site in the cortex and hippocampus and at the AT180 in the hippocampus. The direct effect of anesthetic agents on fully differentiated cortical neurons is epitope-specific and short-lived. The in vivo effects are comparatively more complicated and depend not only on the phosphorylation site but the regions of the brain examined. These findings suggest that dexmedetomidine increases tau phosphorylation both in vitro and in vivo under normothermic conditions, and further studies are warranted to determine the long-term impact of this anesthetic on the tau pathology and even cognitive function.
Histochemical Staining Following LacZ Gene Transfer Underestimates Transfection Efficiency (1997)

Analysis of LacZ gene expression is conventionally inferred from blue staining that results from exposure of the transfected cells or tissue to the substrate 5-bromo-4-chloro-3-indolyl-beta-D-galactopyranoside (X-Gal). Such histochemical staining reports not whether the gene product is present or absent, but where it is active. We investigated the hypothesis that identification of activity, as opposed to presence, of the enzyme underestimates gene expression following LacZ gene transfer. Under conditions optimized for in vitro histochemistry, up to 20% of cells stably transfected with nls-LacZ remained unstained by X-Gal. In contrast, immunostaining with a monoclonal or a polyclonal anti-beta-galactosidase (beta-Gal) antibody positively stained 99% of the cell nuclei. Following in vivo transfection of naked DNA encoding for nls-LacZ, X-Gal staining disclosed 2.7 +/- 1.7 positive nuclei per LacZ-transfected animal, or a transfection efficiency of 0.015%. In contrast, immunohistochemical staining disclosed 118 +/- 32.7 positive nuclei per transfected animal, yielding a transfection efficiency of 0.64% (p < 0.0001 versus X-Gal staining). Thus, 42.9 times more positive cells were detected by antibody than X-Gal staining. Finally, LacZ gene expression following intramuscular gene transfer with an adenoviral vector was observed in 7.6% of skeletal muscle cells assessed with X-Gal; anti-beta-Gal antibody identified 21.8% of cells as being successfully transfected (p < 0.0001). Thus, X-Gal histochemistry following gene transfer of constructs encoding LacZ may underestimate the anatomic extent of gene expression. The superior sensitivity of immunostaining suggests that anti-beta-Gal antibody represents the preferred analytical tool for light microscopic evaluation of LacZ gene transfer.
Calculation of the Maximum Efficiency of the Thermionic Converter (1961)

A theoretical analysis of the efficiency of a thermionic converter is made in terms of the following parameters: Va, the potential difference between the top of the potential barrier in the interelectrode space and the Fermi level of the anode; VL, the potential drop across a load impedance in series with the converter; and Vl, the potential drop in the necessary electrical connection to the cathode. The analysis is carried out by developing an expression for the efficiency of the converter and then maximizing this expression with respect to VL and Vl. This method yields optimum values of load impedance, cathode lead geometry, and cathode work function in terms of Va, cathode temperature, cathode emission constant (usually denoted by A), and effective emissivity of the cathode. A hypothetical example is worked out numerically and the results show that (1) a low value of Va is required for high efficiency, and (2) relatively low values of cathode work function are required for maximum efficiency at ordinary cathode temperatures.
Activation of Erk in the Anterior Cingulate Cortex During the Induction and Expression of Chronic Pain (2008)

The extracellular signal-regulated kinase (Erk) activity contributes to synaptic plasticity, a key mechanism for learning, memory and chronic pain. Although the anterior cingulate cortex (ACC) has been reported as an important cortical region for neuronal mechanisms underlying the induction and expression of chronic pain, it has yet to be investigated whether or not Erk activity in the ACC may be affected by peripheral injury or in chronic pain state. In the present study, we use adult rat animal models of inflammatory and neuropathic pain and demonstrate that Erk signaling pathway in the ACC is potently activated after peripheral tissue or nerve injury. Furthermore, we demonstrate that mechanical allodynia significantly activated Erk activity at synaptic sites at two weeks after the injury. We propose a synaptic model for explaining the roles of Erk activity during different phases of chronic pain. Our findings suggest that cortical activation of Erk may contribute to both induction and expression of chronic pain.
Effective therapy of human lymphoma xenografts with a novel recombinant ribonuclease/anti-CD74 humanized IgG4 antibody immunotoxin (2005)

Ranpirnase (Rap) is a cytotoxic ribonuclease (RNase) isolated from frog oocytes. Here we describe high antitumor activity of a novel immunotoxin, 2L-Rap-hLL1-gamma4P, composed of 2 Rap molecules, each fused to the N terminus of the light chain of hLL1, an internalizing anti-CD74 humanized antibody. To reduce unwanted side effects, the constant region of hLL1 was changed from gamma1 to gamma4 and further to gamma4P by replacing serine228 to proline to prevent the formation of a half immunoglobulin G (IgG) common for IgG4. In vitro, 2L-Rap-hLL1-gamma4P retained RNase activity, specific binding to CD74, and was significantly more potent against CD74+ cell lines (Daudi, Raji, and MC/CAR) than naked hLL1. In vivo, the pharmacokinetic profile of 2L-Rap-hLL1-gamma4P was similar to that of naked hLL1. The maximum tolerated dose of 2L-Rap-hLL1-gamma4P in severe combined immunodeficient mice (SCID) or BALB/c mice was 50 microg per mouse. In Raji and Daudi Burkitt lymphoma xenograft models, treatment with a single 5 to 50 microg dose of 2L-Rap-hLL1-gamma4P, given as early or delayed treatment, resulted in cures of most animals. Treatment with 2L-Rap-hLL1-gamma4P was significantly better than all controls, including saline, naked hLL1, and nonspecific immunotoxin. In conclusion, 2L-Rap-hLL1-gamma4P demonstrated excellent in vitro and in vivo efficacy and thus merits further consideration as a therapeutic for CD74+ tumors.
Graphene-based quantum hall effect infrared photodetectors (2011)

Graphene is a promising material for optoelectronics and photonics. Recent experiments demonstrated graphene photodectectors based on interband transitions working at Mid and Near-IR/Visible regions. Extension of spectral range to longer wavelengths requires alternative photoresponse mechanisms. One of the mechanisms which has been proven to be efficient for THz detection in "classical" semiconductor materials is the optically-induced breakdown of quantum Hall effect. In our work we successfully demonstrated a graphene-based QHE photodetector. Our result demonstrates the potential of graphene as a material for Far-IR photodetectors. Further improvement in device design and use of more efficient radiation coupling solutions should enable graphene photodetectors with broader spectral range, higher sensitivity, and elevated operating temperatures for a variety of applications.
On the synthesis of N-maleoyl amino acids in aqueous media: cautionary tales for the unwary traveller (2010)

The high cost or protracted syntheses associated with N-maleoyl amino acid derivatives coupled with a considerable demand from both the life and physical sciences has spurred the search for facile, low-cost routes to these compounds. Herein, we demonstrate that a recently published method purporting to deliver N-maleoyl amino acids by cyclization of maleamic acids in water, instead results in a hydrolysis product, namely the corresponding hemi-maleate salt.
Importance of the role of calcium in programmed cell death: a review. (1999)

Calcium plays an important role in physiological cell death processes such as terminal differentiation and apoptosis. Cell injury occurs when the intracellular calcium pool is disturbed, which in turn may lead to cell death. Calcium in calcium-dependent enzymes, transglutaminases, various proteases, phosphorylases and kinase, is involved in the process of cell death. Examples of such enzymes involved in cell death, and the role of calcium levels in regulation of these enzymes, are described and discussed.
ChemInform Abstract: SYNTHESIS OF 6‐AMINOBENZOTHIAZOLES FROM P‐BENZOQUINONE IMINE DERIVATIVES (1978)

Abstract Bisacyliertes p‐Phenylendiamin (I) wird mit Bleitetraacetat zu Chinoniminen (II) oxidiert und mit Thioessigsäure bei sukzessiver Behandlung mit Salzsäure und Natronlauge zu 6‐Aminobenzothiazolen (III) umgesetzt.