gebhart/patrepeval huggingface dataset:
Binding and activation of plasminogen at the surface of <i>Staphylococcus aureus</i> (1990)

Untreated Staphylococcus aureus cells, strain Cowan I, specifically bound 125I-Glu-plasminogen. The binding was inhibited by both unlabeled Glu-plasminogen and Glu-plasmin. The Lys form of plasminogen, which lacks the 8-kDa amino-terminal activation peptide, was approximately 100-fold more effective than the Glu form in competing with the binding of 125I-labeled Glu-plasminogen. This suggests an increase in binding affinity upon removal of the activation peptide. Fibronectin, fibrinogen and IgG, plasma components known to bind to the staphylococcal surface, did not significantly interfere with the binding. The competing activity in plasma was abolished by specifically absorbing plasminogen from the plasma sample. L-Lysine and a fragment of plasminogen containing three of the first five protein attachment domains present in the molecule (kringle structures) also competed with plasminogen for binding suggesting that the lysine-binding sites of plasminogen were involved in its interaction with staphylococci. Scatchard analysis revealed high- and low-affinity binding sites. Kd and the number of high-affinity binding sites were 1.7 nM and 780 binding sites/bacterial cell, respectively. 125I-Glu-plasminogen bound to staphylococcal surface was converted to plasmin by tissue-type plasminogen activator. The conversion took place also in the presence of plasma. If the conversion was carried out in the absence of low-molecular-mass plasmin inhibitors such as aprotinin, the bound Glu-plasmin was further converted to Lys-plasmin. The surface-bound plasmin was enzymically active, as judged by digestion of the synthetic substrate, S-2251. The plasminogen conversion shown by the present experiments not only leads to the surface-bound plasmin but seems to considerably increase the affinity of plasmin for its binding site. This may represent a physiologically relevant method for a bacterial cell to retain surface-bound active plasmin which is also protected from its soluble plasma inhibitors. This novel mechanism for staphylococci to adopt surface-bound proteolytic activity, without the interference of plasma components, may have some role in the tissue penetration and invasion of microbes during infection.
Lipid signal transduction pathways in angiotensin II type 1 receptor-transfected fibroblasts (1995)

A stable Chinese hamster ovary fibroblast line expressing the rat vascular type 1a angiotensin II (ANG II) receptor was used to study the lipid-derived signal transduction pathways elicited by type 1a ANG II receptor activation. ANG II caused a biphasic and dose-dependent increase in diacylglycerol (DAG) accumulation with an initial peak at 15 s (181 +/- 11% of control, P < 0.02) and a second sustained peak at 5-10 min (214 +/- 10% of control, P < 0.02). The late DAG peak was derived from phosphatidylcholine (PC), and the formation was blocked by ethylene glycol-bis(beta-aminoethyl ether)-N,N,N',N'-tetraacetic acid. ANG II also increased phosphatidic acid (PA) production nearly fourfold by 7.5 min. In the presence of ethanol, ANG II markedly increased phosphatidylethanol (PEt) formation, indicating activation of phospholipase D (PLD). ANG II was shown to increase the mass of three separate PA species, one of which apparently originated from DAG kinase action on PC-phospholipase C (PLC)-produced DAG, providing evidence for PC-PLC activity. ANG II also formed a third PA species, which originated neither from PLD nor from DAG kinase. These results demonstrate that multiple lipid signals propagated via collateral stimulation of PLC and PLD are generated by specific activation of the vascular type 1a ANG II receptor.
Polymerizable Liquid Crystals as Building Blocks for Functional, Nanostructured Materials (1999)

The development of synthetic materials with nanometer-scale architectural sophistication is one of the new frontiers in polymer and materials chemistry. Liquid crystals represent a viable venue for such efforts because they offer excellent control over parameters such as orientation, organization, geometry, and symmetry on the molecular level via molecular design. In addition, this control can be extended to the macroscopic regime through appropriate alignment techniques. New advances in the design of functional, nanostructured organic materials using polymerizable liquid crystals as building blocks are presented herein.
Enhancing speech degrated by additive noise or interfering speakers (1989)

The author examines some of the ways that speech signals, subjected to certain degradations (e.g. additive noise, interfering speakers, bandlimiting, single-channel data), can be processed to increase the likelihood of being correctly understood. He concentrates on applications that involve monaural listening. He treats spectral and time-domain subtraction techniques, methods involving fundamental frequency tracking, and enhancement by resynthesis.< <ETX xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">></ETX>
The Discovery of Asunaprevir (BMS-650032), An Orally Efficacious NS3 Protease Inhibitor for the Treatment of Hepatitis C Virus Infection (2014)

The discovery of asunaprevir (BMS-650032, 24) is described. This tripeptidic acylsulfonamide inhibitor of the NS3/4A enzyme is currently in phase III clinical trials for the treatment of hepatitis C virus infection. The discovery of 24 was enabled by employing an isolated rabbit heart model to screen for the cardiovascular (CV) liabilities (changes to HR and SNRT) that were responsible for the discontinuation of an earlier lead from this chemical series, BMS-605339 (1), from clinical trials. The structure-activity relationships (SARs) developed with respect to CV effects established that small structural changes to the P2* subsite of the molecule had a significant impact on the CV profile of a given compound. The antiviral activity, preclincial PK profile, and toxicology studies in rat and dog supported clinical development of BMS-650032 (24).
Thrombocytopenia and hemorrhages in veal calves infected with bovine viral diarrhea virus (1990)

The relationship between bovine viral diarrhea virus (BVDV) infection and thrombocytopenia was studied in 18 veal calves experimentally infected with BVDV. All calves were free of BVDV, and 13 calves were free of serum neutralizing antibodies to BVDV before virus inoculation. Calves were inoculated at approximately 10 days of age, and platelet counts were monitored over a period of several weeks. Ten additional calves housed in close proximity were kept as uninoculated controls. A profound decrease in platelet counts by 3 to 11 days after inoculation was seen in all calves that had neutralizing antibody titers less than 1:32 before infection. Severe thrombocytopenia (less than 5,000 platelets/microliter) was seen in 12 calves, 11 of which also developed hemorrhages. Necropsy findings in 3 severely thrombocytopenic calves that died included multiple hemorrhages throughout the body. Calves that recovered had increased platelet counts, and in most instances, a corresponding increase in neutralizing antibody titers to BVDV. At 11 days after inoculation, BVDV was detected on platelets by use of immunofluorescence, but evidence of surface-bound immunoglobulin was not found. The results suggest that a nonimmunoglobulin-mediated method of platelet destruction or sequestration develops as a sequela to BVDV infection.
The Coherent X-ray Imaging (CXI) instrument at the Linac Coherent Light Source (LCLS) (2010)

The Linac Coherent Light Source (LCLS) became the first ever operational hard x-ray free-electron laser in 2009. It will operate as a user facility capable of delivering unique research opportunities in multiple fields of science. The LCLS and the LCLS Ultrafast Science Instruments (LUSI) construction projects are developing instruments designed to make full use of the capabilities afforded by the LCLS beam. One such instrument is being designed to utilize the LCLS coherent beam to image with high resolution any sub-micron object. This instrument is called the Coherent X-ray Imaging (CXI) instrument. This instrument will provide a flexible optical system capable of tailoring key beam parameters for the users. A suite of shot-to-shot diagnostics will also be provided to characterize the beam on every pulse. The provided instrumentation will include multi-purpose sample environments, sample delivery and a custom detector capable of collecting two-dimensional (2D) data at 120 Hz. In this paper, the LCLS will be briefly introduced, as well as the technique of coherent x-ray diffractive imaging (CXDI). A few examples of scientific opportunities arising from use of the CXI instrument will be described. Finally, the conceptual layout of the instrument will be presented, together with a description of the key requirements for the overall system and of specific devices required.
Chemical properties of surface waters in the limestone regions of western Japan : Evaluation of chemical conditions for the deposition of tufas. (1998)

In order to understand the chemical conditions for the depositionof tufas, chemical properties of were investigated for the 201 surface waters collected from the limestone regions including newly discovered localities of tufas. The collected waters were categorized, according to the association with tufas, mainly into; category N (waters without tufa deposition), category T (waters depositing tufas), and category S (spring waters of tufa-depositing streams). These three categories clearly differ in Ca contents, equilibrium CO 2 partial pressure (PCO2), and saturation index for calcite (SIC); all of which are the most important chemical properties for the deposition of tufas. The waters of the category N are characterized by small Ca contents (mainly 15～35 ppm) and low PCO2(350～1,000 µatm) which indicate that they are basically flowing on a limestone substrate without an efficient CO2 uptake from soils. Their SIC never exceeds +0.5. The waters depositing tufas (category T) normally exhibitCa contents more than 45 ppm and PCO2 ranging 500～2,000 µatm. The waters of category S show comparable or slightly larger Ca contents than category T, however their PCO2 is considerably higher (than 2,000 µatm). Their raised values of Ca contents and PCO2 are ascribed to efficient CO2 uptake in a soil layer and subsequent dissolution of CaCO3. Furthermore, their SIC around 0.0 indicates that the waters dissolve CaCO3 until they reach the saturation in underground water systems. The large difference in PCO2 between categories T and S results from degassing of CO2 during flowing on the streams. The degassing increases pH and SIC of the waters. The SIC of category T mostly exceeds +0.5, that is probably the most important chemical condition for an efficient deposition of tufas. This study indicates that tufas are not very rare, but also that their distribution tends to be concentrated in a certain area, such as northwestern Okayama Prefecture. Local geological and hydrological conditions can be also important controls for deposition of tufas.
Inhibition of factor I by diisopropylfluorophosphate. Evidence of conformational changes in factor I induced by C3b and additional studies on the specificity of factor I. (1990)

The factor I-mediated cleavage of C3b, using factor H as a cofactor was completely inhibited by diisopropylfluorophosphate (DFP) when factor I and C3b were incubated with DFP before the addition of factor H. Inhibition, although to a lesser degree, was observed when factor H was present during DFP-exposure. No inhibition in factor I activity was seen when factor I and H were incubated with DFP either alone or together. It was also demonstrated that the 38-kDa subunit of factor I bound radiolabeled DFP when factor I and C3b together were exposed to DFP. These observations suggest that factor I interacts with C3b in a manner that exposes its catalytic site to DFP, an interaction that is independent of factor H. The inhibitory effect by DFP on factor I led us to further investigate the factor I cleavage products of iC3b, inasmuch as previous reports were ambiguous as to whether digestion occurs in the presence of DFP. Digestion of C3b bound to activated thiol Sepharose (ATS-C3b) in the presence of factor H at low pH and ionic strength and in serum by complement activation produced C3d,g-like fragments with apparent molecular mass of 41 and 43 kDa. These fragments were shown to have three different N-terminal and two different C-terminal ends. The major fragments had N-terminal sequences starting with Glu933, as shown by sequence determination. Traces of fragments extending beyond this point were also found, shown by Western blot analysis using a panel of mAb previously shown to bind to epitopes exposed within a region of C3 spanning residues 929 to 943, as well as a shorter fragment starting with Glu938. When digestion of C3b is carried out in the presence of DFP, the factor I level necessary for digestion is elevated and may explain how the first two cleavages producing iC3b but not the following giving C3d,g, can occur. The finding of several factor I cleavage sites in the C3d,g region of C3 demonstrates that factor I has a broad specificity, mainly for arginyl bonds. It has also been shown to digest a lysyl bond exposed in ATS-bound C3b.
Ischemic tissue injury. (1975)

The subendocardial to subepicardial gradient in the severity of ischemia following acute coronary occlusion is described. The effects of mild, moderate, and severe ischemia on cell structure and function are compared in summary form, and special attention is given to the effects of severe ischemia on myocardial cells. The characteristics of reversible and irreversible ischemic injury are defined in biologic terms. The failure of cell volume regulation in cells which have entered an irreversible state of ischemic injury is demonstrated by the use of free-hand slices in vitro. Irreversibility is associated with structural defects in the plasma membrane and is reflected in an increased slice inulin-diffusible space, increased slice H2O and Na+ content, and failure of the tissue to maintain the high K+ and Mg2+ levels characteristic of normal left ventricular myocardium. Defective cell membrane function is an early feature of irreversible ischemic injury and may be a primary event in the genesis of the irreversible state.
Toughening PLA with E-MA-GMA (2008)

E-MA-GMA was introduced to toughen PLA and the contents of E-MA-GMA were 5%、10%、15%、20%,respectively.The infrared spectroscopy(IR) and rheometer were used to characterize the reaction occurring in the blend.The melt index and rheological behaviors of blend were investigated.Mechanical properties were also investigated to view the toughening of different contents of E-MA-GMA.With the addition of E-MA-GMA,the failure mode changed from brittle fracture of the neat PLA to ductile fracture of the blend as demonstrated by scanning electron microcopy(SEM).It is found that the epoxy functional group of E-MA-GMA can react with the end group of PLA,which makes PLA partial compatible with E-MA-GMA.Therefore,the impact strength PLA is improved.When adding 20% E-MA-GMA,the Izod impact strength increases by 329.7%.
Effect of a robotic rehabilitation device on upper limb function in a sub-acute cervical spinal cord injury population (2011)

Robotic rehabilitation devices have been suggested as a tool to increase the amount of rehabilitation delivered after a neurological injury. Clinical robotic rehabilitation studies of the upper extremity have generally focused on stroke survivors. We present the results of a multi-center pilot study where an upper-limb robotic rehabilitation device (Armeo Spring®, Hocoma AG) was incorporated into the rehabilitation program of 12 subjects with sub-acute cervical spinal cord injury (motor level C4-C6, AIS A-D). Outcomes were measured using two tests of upper extremity function: ARAT and GRASSP. The change in scores for the arm receiving the Armeo training were not statistically significant when compared to the arm not receiving the Armeo training at discharge from therapy and over follow up assessments (8.7 +/- 2.9 compared to 7.4 +/- 2.5 for ARAT at discharge, p = 0.98, and 13.0 +/- 3.2 compared to 13.3 +/- 3.3 for GRASSP at discharge, p = 0.69). Nevertheless, subjects with some minimal (partial) hand function at baseline had a significantly larger increase in GRASSP scores than subjects with no minimal hand function preserved at baseline (19.3 +/- 2.4 compared to 6.6 +/- 4.7, p = 0.02). This suggests that the initial functional capabilities of patients can influence the benefits measured after robotic rehabilitation training and heterogeneous subject populations should be avoided in early phase studies.
Multiple genes in human 20q13 chromosomal region are involved in an advanced prostate cancer xenograft. (2002)

We analyzed a prostate cancer xenograft derived from a locally advanced tumor using combined cytogenetic, array-based comparative genomic hybridization and expression analyses. This analysis revealed that genes in the 20q13 chromosomal region, CSE1L, ZNF217, MYBL2, and STK15, were significantly overexpressed in this tumor. The expression pattern of these genes was then confirmed in two large human prostate cancer microarray databases. Furthermore, the MYBL2 and STK15 have been significantly overexpressed in prostate metastases, allowing a clear distinction between localized tumors and metastases. Our data suggest these genes to be involved in advanced stages of prostate tumorigenesis and as such, they may serve as markers for tumor progression.
The valve‐in‐valve technique: Transcatheter treatment of aortic bioprothesis malposition (2008)

Percutaneous aortic valve replacement is an emerging alternative to palliative medical therapy for nonsurgical patients with severe aortic valve stenosis. The impossibility of repositioning of the current transcatheter prosthesis in case of suboptimal placement is the main limit of these devices. Here, we report on a case of an 84-year-old woman successfully treated with implantation of two 18-Fr CoreValve prosthesis (CoreValve, Irvine, California), because of the suboptimal deployment of the first one, analyzing the procedural technique and the immediate and short-term clinical and hemodynamic results.
Comparison of fibulin-3 and mesothelin as markers in malignant mesothelioma (2014)

Soluble mesothelin is a superior diagnostic biomarker for MM compared with fibulin-3, whereas fibulin-3 provides superior prognostic information compared with mesothelin.
RMN du Carbone 13 des Alcaloïdes du Type Borrérine-Borrévérine-Isoborrévérine (1985)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTRMN du Carbone 13 des Alcaloïdes du Type Borrérine-Borrévérine-IsoborrévérineF. Tillequin, M. Koch, and A. RabaronCite this: J. Nat. Prod. 1985, 48, 1, 120–123Publication Date (Print):January 1, 1985Publication History Published online1 July 2004Published inissue 1 January 1985https://pubs.acs.org/doi/10.1021/np50037a023https://doi.org/10.1021/np50037a023research-articleACS PublicationsRequest reuse permissionsArticle Views199Altmetric-Citations11LEARN 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
Pharmacokinetics and Urinary Excretion of Clavulanic Acid After Oral Administration of Amoxicillin and Potassium Clavulanate (1984)

Clavulanic acid is a beta-lactamase inhibitor which prevents microbial lactamase inactivation of beta-lactam antibiotics. The pharmacokinetics and urinary excretion of clavulanic acid were studied in eight healthy adult volunteers after oral administration of 500 mg amoxicillin and 125 mg potassium clavulanate. Serum and urine clavulanic acid concentrations were assayed using high-performance liquid chromatography. Pharmacokinetic parameters were: t 1/2 beta = 1.019 +/- 0.090 hour, t 1/2 alpha = 0.276 +/- 0.031 hour, lag time = 0.321 +/- 0.018 hour, tmax = 1.042 +/- 0.80 hour, Cmax = 2.098 +/- 0.441 micrograms/ml, and AUC = 4.897 +/- 0.979 micrograms X hr/ml. Cumulative urinary excretion of clavulanic acid (as percentage of dose administered) was: 14.05 +/- 2.87 within 2 hours, 25.77 +/- 3.98 within 4 hours, and 27.85 +/- 4.27 within 6 hours after administration.
Impact of Layout on 90nm CMOS Process Parameter Fluctuations (2006)

A test chip has been built to study the effects of layout on the delay and leakage of digital circuits in 90nm CMOS. The delay is characterized through the spread of ring oscillator frequencies and the transistor leakage is measured by using an on-chip ADC
Secreted Glypican Binds to the Amyloid Precursor Protein of Alzheimer's Disease (APP) and Inhibits APP-induced Neurite Outgrowth (1996)

The amyloid precursor protein (APP) of Alzheimer's disease has been shown to stimulate neurite outgrowth in vitro. The effect of APP on neurite outgrowth can be enhanced if APP is presented to neurons in substrate-bound form, in the presence of heparan sulfate proteoglycans. To identify specific heparan sulfate proteoglycans that bind to APP, conditioned medium from neonatal mouse brain cells was subjected to affinity chromatography with recombinant APP695 as a ligand. Glypican bound strongly to the APP affinity column. Purified glypican bound to APP with an equilibrium dissociation constant of 2.8 nM and inhibited APP-induced neurite outgrowth from chick sympathetic neurons. The effect of glypican was specific for APP, as glypican did not inhibit laminin-induced neurite outgrowth. Furthermore, treatment of cultures with 4-methylumbelliferyl-beta-D-xyloside, a competitive inhibitor of proteoglycan glycanation, inhibited APP-induced neurite outgrowth but did not inhibit laminin-induced neurite outgrowth. This result suggests that endogenous proteoglycans are required for substrate-bound APP to stimulate neurite outgrowth. Secreted glypican may act to inhibit APP-induced neurite outgrowth in vivo by competing with endogenous proteoglycans for binding to APP.
Bioorganic Investigation of Multicationic Antimicrobials to Combat QAC-Resistant <i>Staphylococcus aureus</i> (2015)

Quaternary ammonium compounds (QACs) have historically served as a first line of defense against pathogenic bacteria. Recent reports have shown that QAC resistance is increasing at an alarming rate, especially among methicillin-resistant Staphylococcus aureus (MRSA), and preliminary work has suggested that the number of cations present in the QAC scaffold inversely correlates with resistance. Given our interest in multiQACs, we initiated a multipronged approach to investigate their biofilm eradication properties, antimicrobial activity, and the propensity of methicillin-susceptible S. aureus (MSSA) to develop resistance toward these compounds. Through these efforts we identified multiQACs with superior profiles against resistant (MRSA) planktonic bacteria and biofilms. Furthermore, we document the ability of MSSA to develop resistance to several commercial monoQAC disinfectants and a novel aryl bisQAC, yet we observe no resistance to multiQACs. This work provides insight into the mechanism and rate of resistance development of MSSA and MRSA toward a range of QAC structures.