gebhart/patrepeval huggingface dataset:
Effect of bridge region variation on antifolate and antitumor activity of classical 5-substituted 2,4-diaminofuro[2,3-d]pyrimidines (1995)

Variation of the bridge linking the heterocyclic ring and p-aminobenzoyl-L-glutamate portions of our previously described classical 2,4-diaminofuro[2,3-d]pyrimidines 1 and 2 are reported as inhibitors of dihydrofolate reductase (DHFR) and thymidylate synthase (TS) and as antitumor agents. Specifically -CH2CH2- and -CH2NHCH2- bridged analogues, N-[4-[2-(2,4-diaminofuro[2,3-d]pyrimidin-5-yl) ethyl]benzoyl]-L-glutamic acid (3) and N-[4-[[N-[(2,4-diaminofuro[2,3-d]pyrimidin-5-yl) methyl]amino]methyl]benzoyl]-L-glutamic acid (4), respectively, were synthesized. Compound 3 was obtained via a Wittig reaction of the tributylphosphonium salt of 2,4-diamino-5-(chloromethyl)furo[2,3-d]pyrimidine (5) and methyl 4-formylbenzoate (6) followed by reduction and coupling with the diethyl ester of L-glutamic acid. Compound 4 was synthesized by the nucleophilic displacement of 5 with diethyl N-[4-(aminomethyl)benzoyl]-L-glutamate (15) and saponification. Both analogues were evaluated in vitro as inhibitors of DHFRs from (recombinant) human, human CCRF-CEM cells, and Lactobacillus casei. Compound 3 showed moderate activity (IC50 10(-6)-10(-7) M). Compound 4 was essentially inactive (IC50 10(-5) M, CCRF-CEM). The compounds were also evaluated against TS from (recombinant) human and L. casei and were of low activity (IC50 10(-5) M). The three-atom-bridged analogue 4 was somewhat more inhibitory to human TS than methotrexate (MTX). Compound 3 inhibited the growth of tumor cells in culture (IC50 10(-7) M) while 4 showed a low level of growth inhibitory activity. The inhibition of the growth of leukemia CCRF-CEM cells by both compounds parallels their inhibition of CCRF-CEM DHFR. Analogue 3 was a good substrate for human folylpolyglutamate synthetase (FPGS) derived from CCRF-CEM cells (Km 8.5 microM). Further evaluation of the growth inhibitory activity of 3 against the MTX-resistant subline of CCRF-CEM cells (R30dm) with decreased FPGS indicated that poly-gamma-glutamylation was important for its action. Protection studies with 3 in the FaDu squamous cell carcinoma cell line indicated that inhibition was completely reversed by leucovorin [(6R,S-5-formyltetrahydrofolate] or by a combination of thymidine and hypoxanthine, suggesting an antifolate effect directed at DHFR.
10.5 W Time-Averaged Power Mid-IR Supercontinuum Generation Extending Beyond 4 <formula formulatype="inline"> <tex Notation="TeX">$\mu$</tex> </formula>m With Direct Pulse Pattern Modulation (2009)

A novel, all-fiber-integrated supercontinuum (SC) laser is demonstrated and provides up to 10.5 W time-averaged power with a continuous spectrum from ~0.8 to 4 mum. The SC is generated in a combination of standard single-mode fibers and ZrF <sub xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">4</sub> -BaF <sub xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">2</sub> -LaF <sub xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">3</sub> -AlF <sub xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">3</sub> -NaF (ZBLAN) fluoride fibers pumped by a laser-diode-based cladding-pumped fiber amplifier system. The output SC pulse pattern can be modulated by directly modulating the seed laser diode. Near-diffraction-limited beam qualities are maintained over the entire SC spectrum. The SC average power is also linearly scalable by varying the input pump power and pulse repetition rate. We further investigate the theoretical limitations on the achievable average power handling and spectral width for the SC generation in ZBLAN fibers. Based on the thermal modeling, the standard ZBLAN fiber can handle a time-averaged power up to ~15 W, which can be further scaled up to ~40 W with a proper thermal coating applied onto the ZBLAN fiber. The SC long-wavelength edge is limited by the nonlinear wavelength generation processes, fiber bend-induced loss, and glass material loss. By using a ZBLAN fiber with a 0.3 numerical aperture, the SC spectrum could extend out to ~4.5 mum, which is then limited by the material loss.
Amyloid β‐peptide induces nitric oxide production in rat hippocampus: association with cholinergic dysfunction and amelioration by inducible nitric oxide synthase inhibitors (2001)

ABSTRACT Amyloid β‐peptide (Aβ) plays a critical role in the development of Alzheimer's disease. However, the molecular mechanisms of Aβ‐induced brain damage in vivo remain to be elucidated. Here, we investigated whether overproduction of nitric oxide (NO) catalyzed by inducible NO synthase (iNOS) is involved in Aβ‐induced brain dysfunction. Chronic intracerebroventricular infusion of Aβ1‐40 induced iNOS mRNA expression in the hippocampus on days 3 and 5 after the infusion. An accumulation of NO metabolites was observed, and the peak correlated with expression of iNOS mRNA. Measurement of NOS activities revealed an increase in Ca 2+ ‐independent, but not Ca 2+ ‐dependent, activity. Immunohistochemistry identified numerous iNOS‐immunoreactive microglia and astrocytes in the dentate gyrus and to a lesser extent in the CA1 subfield of the hippocampus. Daily treatment with the iNOS inhibitor aminoguanidine (AG, 100 mg/kg/day, i.p.) or S ‐methylisothiourea (10 mg/kg/day, i.p.) during Aβ infusion prevented an impairment of nicotine‐evoked acetylcholine release induced by Aβ, whereas the neuronal NOS inhibitor 7‐nitroindazole (30 mg/kg/day, i.p.) had no effect. Daily treatment with AG also ameliorated the impairment of spatial learning of Aβ‐infused rats in a radial arm maze. Our findings suggest that overproduction of NO catalyzed by iNOS is responsible for Aβ‐induced brain dysfunction.
Antibiotic effect of lysostaphin on granulation wound (2006)

Objective To investigate the effect of lysostaphin on golden staphylococcal bacteria in vitro and on acestoma tissue.Methods Effects of lysostaphin on golden staphylococcal bacteria,Candida albicans and P.aeruginosa were detected by drug sensitivity test.Quantitative analysis of bacteria was used to detect the effect of lysostaphin on golden staphylococcal bacteria in 29 cases of 10%-30% TBSA.Results Most golden staphylococcal bacteria,as well as Candida albicans could be killed by lysostaphin.Lysostaphin had little effect on P.aeruginosa.Eighty-nine percent bacteria could be killed by lysostaphin after gauze with lysostaphin had been used for over 3 d,indicating lysostaphin may control bacteria quantity and improve survival rate of skin graft on granulation tissue.Gauze with lysostaphin contained biological enzymes and it had no systemic side effects.Conclusion Gauze with lysostaphin may be available on controlling golden staphylococcal bacteria as well as Candida albicans in burnt patients.Lysostaphin is effective in controlling residual trauma infected by golden staphylococcal bacteria.
Roughness spectrum and surface plasmons for surfaces of silver, copper, gold, and magnesium deposits (1983)

The roughness spectrum $g(\stackrel{\ensuremath{\rightarrow}}{\mathrm{k}})$ (or spectral density function) for surfaces of silver, copper, gold, and magnesium deposits is deduced from surface profiles determined by using microdensitometer analysis of micrographs of shadowed-surface carbon replicas. A process based on computation of autocovariance function via the fast-Fourier-transform algorithm is used. It is shown that the $g(\stackrel{\ensuremath{\rightarrow}}{\mathrm{k}})$ function is not a perfect Gaussian function as is usually assumed. An analytical model is given that provides a rather suitable fit to the computed $g(\stackrel{\ensuremath{\rightarrow}}{\mathrm{k}})$ functions. Results are compared with those obtained from optical experiments (mainly the attenuated-total-reflection method). Discrepancies between the values of $\ensuremath{\delta}$ (rms roughness) and $\ensuremath{\sigma}$ (autocorrelation length) determined by the use of our procedure and corresponding values deduced from optical experiments are elucidated.
Drug Delivery Systems (2005)

Drugs, in the majority of cases, are toxic at high doses however, they must be present in the circulation for a time sufficient to reach therapeutically useful results. This is commonly achieved by repeated drug administrations, which give rise to peak and valley drug concentration. Such a method of administration has two disadvantages: on the one hand the low compliance by the patient and, on the other, the risk of reaching toxic levels. This chance is very severe in particular for new biotechnological drugs such as peptides, proteins, or oligonucleotides that usually are very active and often have a very narrow therapeutic window. A solution to these problems comes now from the drug controlled release technology, meaning with this word also programmable or pulse release from insoluble matrices. The chemical modification of the drug by soluble polymers to increase the residence time in blood, as well as to convey more favorable properties such as the reduction of antigenicity or increased stability toward enzymes, is also considered part of the technology. In any of these cases not only desirable and constant drug levels are reached, but also a release that may last for a long time, up to one year. To reach this goal the drug is usually entrapped when the matrix is produced or shaped, and only in rare cases is it absorbed into the matrix from a concentrated drug solution. The technology described above does not apply only to systemic drug treatment, i.e., distribution through the whole body via the blood, but also sometimes to localization in a particular area, as occurs, for instance, in wound treatment and in medication of inflamed epidermis as well as of eyes,
Surface-Enhanced Emission from Single Semiconductor Nanocrystals (2002)

The fluorescence behavior of single CdSe(ZnS) core-shell nanocrystal (NC) quantum dots is dramatically affected by electromagnetic interactions with a rough metal film. Observed changes include a fivefold increase in the observed fluorescence intensity of single NCs, a striking reduction in their fluorescence blinking behavior, complete conversion of the emission polarization to linear, and single NC exciton lifetimes that are >10(3) times faster. The enhanced excited state decay process for NCs coupled to rough metal substrates effectively competes with the Auger relaxation process, allowing us to observe both charged and neutral exciton emission from these NC quantum dots.
Efficient fermentation of Pinus sp. acid hydrolysates by an ethanologenic strain of Escherichia coli (1992)

Process conditions for the acid hydrolysis of pine hemicellulose and cellulose have been described which provide a biocompatible sugar solution. By using an improved strain of recombinant Escherichia coli, strain KO11, hydrolysates supplemented with yeast extract and tryptone nutrients were converted to ethanol with an efficiency of 85% to over 100% on the basis of monomer sugar content (approximately 72 g/liter) and with the production of 35 g of ethanol per liter in 48 h. In the process described, approximately 347 liters of ethanol could be produced per dry metric ton of lignocellulose.
Efficient AC and noise analysis of two-tone RF circuits (1996)

Article Efficient AC and noise analysis of two-tone RF circuits Share on Authors: Ricardo Telichevesky Cadence Design Systems, San Jose California Cadence Design Systems, San Jose CaliforniaView Profile , Ken Kundert Cadence Design Systems, San Jose California Cadence Design Systems, San Jose CaliforniaView Profile , Jacob White Massachusetts Institute of Technology, Cambridge, Massachusetts Massachusetts Institute of Technology, Cambridge, MassachusettsView Profile Authors Info & Claims DAC '96: Proceedings of the 33rd annual Design Automation ConferenceJune 1996 Pages 292–297https://doi.org/10.1145/240518.240572Online:01 June 1996Publication History 68citation415DownloadsMetricsTotal Citations68Total Downloads415Last 12 Months12Last 6 weeks4 Get Citation AlertsNew Citation Alert added!This alert has been successfully added and will be sent to:You will be notified whenever a record that you have chosen has been cited.To manage your alert preferences, click on the button below.Manage my AlertsNew Citation Alert!Please log in to your account Save to BinderSave to BinderCreate a New BinderNameCancelCreateExport CitationPublisher SiteGet Access
Passive or Active Inspired Gas Humidification Increases Thermal Steady-State Temperatures in Anesthetized Infants (1989)

We tested the hypothesis that active and passive airway humidification minimize hypothermia in infants, but that maintaining normothermia does not decrease the duration of postoperative recovery. A circle system was used to ventilate the lungs of anesthetized, intubated infants who were randomly assigned to active airway humidification and warming with use of an MR450 Servo airway heater and humidifier set at 37 degrees C (n = 10), passive airway humidification with use of the Humid-Vent Mini heat and moisture exchanger placed between the Y-piece of the circle and the endotracheal tube (n = 10), or no airway humidification and heating (control, n = 10). Anesthesia was induced with thiopental and maintained with isoflurane and nitrous oxide in oxygen. The relative humidity of inspired respiratory gases was approximately 35% in the control group and approximately 90% in the group undergoing active airway humidification. Initial inspired humidity in the passive humidification group (45%) increased to approximately 80% after 1 h of anesthesia. Humidity differed significantly across groups at all times (P less than or equal to 0.05). Steady-state rectal temperatures (100-120 min after induction) were 36.2 +/- 0.7 degrees C in patients given active humidification and heating, 35.7 +/- 0.9 degrees C in the passively humidified group, and 35.2 +/- 0.4 degrees C in the control group (P less than or equal to 0.05 between each group). Recovery from general anesthesia was rapid in all patients and did not correlate with central temperature changes or type of humidification (P = NS).(ABSTRACT TRUNCATED AT 250 WORDS)
A Model for Optimizing Retail Space Allocations (1981)

The allocation of scarce shelf space among competing products is a central problem in retailing. Space allocation affects store profitability through both the demand function, where both main and cross space elasticities have to be considered, and through the cost function (procurement, carrying and out-of-stock costs). A model is developed which uniquely incorporates both effects. A case study is used to estimate the parameters and the problem is solved within a geometrical programming framework. An extensive comparison with alternative procedures suggests this general model leads to significantly different allocation rules and superior profit performance.
Transcriptional regulation of the human CRLR in microvascular endothelial cells (2002)

Conference Abstract| June 01 2002 Transcriptional regulation of the human CRLR in microvascular endothelial cells L. L. Nikitenko; L. L. Nikitenko 1Nuffield Department of Obstetrics and Gynaecology, University of Oxford, John Radcliffe Hospital, Oxford, OX3 9DU, UK2Molecular Angiogenesis Laboratory, Imperial Cancer Research Fund, Institute of Molecular Medicine, University of Oxford, John Radcliffe Hospital, Oxford, OX3 9DU, UK Search for other works by this author on: This Site PubMed Google Scholar C. M. P. Rees; C. M. P. Rees 1Nuffield Department of Obstetrics and Gynaecology, University of Oxford, John Radcliffe Hospital, Oxford, OX3 9DU, UK Search for other works by this author on: This Site PubMed Google Scholar R. Bicknell R. Bicknell 1Nuffield Department of Obstetrics and Gynaecology, University of Oxford, John Radcliffe Hospital, Oxford, OX3 9DU, UK Search for other works by this author on: This Site PubMed Google Scholar Biochem Soc Trans (2002) 30 (3): A59. https://doi.org/10.1042/bst030a059b Views Icon Views Article contents Figures & tables Video Audio Supplementary Data Share Icon Share Twitter LinkedIn Cite Icon Cite Get Permissions Citation L. L. Nikitenko, C. M. P. Rees, R. Bicknell; Transcriptional regulation of the human CRLR in microvascular endothelial cells. Biochem Soc Trans 1 June 2002; 30 (3): A59. doi: https://doi.org/10.1042/bst030a059b Download citation file: Ris (Zotero) Reference Manager EasyBib Bookends Mendeley Papers EndNote RefWorks BibTex toolbar search Search nav search search input Search input auto suggest search filter All ContentAll JournalsBiochemical Society Transactions Search Advanced Search This content is only available as a PDF. © 2002 Biochemical Society2002 Article PDF first page preview Close Modal You do not currently have access to this content.
Characterization of antibody responses to combinations of a dengue-2 DNA and dengue-2 recombinant subunit vaccine. (2001)

A dengue-2 (DEN-2) DNA vaccine coding for the premembrane and envelope (E) proteins and a recombinant fusion protein containing the B domain of the DEN-2 E protein fused to the maltose-binding protein (MBP) of Escherichia coli both elicited neutralizing antibody in mice. In order to achieve more rapid protective immunity as well as to increase the persistence of neutralizing antibody, we primed mice with the DNA vaccine (D), the recombinant MBP protein (R), or both (RD) given simultaneously, and then boosted twice with either the R (R/R/R or D/R/R) or D (D/D/D or R/D/D) constructs alone or the RD (RD/RD/RD) combination. All of the recombinant protein vaccines were given with alum as an adjuvant. The serum antibody response measured by enzyme-linked immunosorbent assay was highest in D/D/D mice and RD/RD/RD mice. The D/R/R mice showed an intermediate response, and the R/D/D and R/R/R showed the lowest response. The geometric mean (GM) 50% neutralizationtiter (50% plaque reduction neutralization, or PRNT50) was marginally higher for RD/RD/RD mice (891) at 9 months after priming than that for R/R/R mice (724). T he lowest GM PRNT50 titers were seen in the D/D/D mice (33) and R/D/D mice (40), and the D/R/R group had a slightly higher titer (156) than these 2 groups. The predominant antibody subclass for the D/D/D mice was immunoglobulin (Ig) G2a, similar to mice infected with live virus. The R/R/R mice showed an exclusive IgGI antibody response, and the RD/RD/RD response also was predominantly IgGI. The antibody subclass pattern of the R/D/D and D/R/R mice showed a more balanced distribution of both IgG1 and IgG2a. Investigating the neutralizing capacity of antibody subclasses suggested that both IgG1 and IgG2a could neutralize DEN-2 virus. Our observations indicate that the combination RD prime-boost regimen warrants further investigation as a vaccine strategy to prevent dengue infection.
Scattering of ultrasound by emulsions (1989)

Ultrasonic scattering theory is used to relate the ultrasonic velocity and attenuation of emulsions to their physical properties (e.g. droplet size and volume fraction). This theory includes visco-inertial and thermal scattering mechanisms and corrections due to multiple scattering. The physical significance of the scattering mechanisms is discussed so as to highlight the factors which influence ultrasonic measurements in these systems. Theoretical predictions were compared with experimental measurements of velocity and attenuation in sunflower oil in water emulsions with varying droplet radii (0.14-0.74 mu m), mass fraction (0-0.5) and frequency (1.25-10.0 MHz) at 293.1 K. Appreciable excess attenuation and velocity dispersion were observed which could be attributed to thermal scattering. The relationship between the measurable ultrasonic parameters and the physical properties of emulsions means ultrasonic scattering should prove a useful means of investigating these systems.
The thioredoxin reductase/thioredoxin system: Novel redox targets for cancer therapy (2005)

Thioredoxin reductase (TRX) is a selenoprotein that reduces oxidized protein substrates in an NADPH-dependent process (cf. Fig. 1). The thioredoxins (TX) are a family of small redox active proteins that undergo reversible oxidation/reduction and help to maintain the redox state of cells. TX serves as a cofactor in many TRX-catalyzed reductions in a manner similar to glutathione (GSH) in thioltransferase reactions. For example, TX is a cofactor in protein disulfide reduction and DNA synthesis, but independently, it inhibits apoptosis, stimulates cell proliferation and angiogenesis, and increases transcription factor activity. The role of the TRX/TX system is limited by its reducing capacity as well as the additional supply of electrons in the form of NADPH provided by hexose monophosphate shunt (HMPS). TX is limited by the reduction capacity of its vicinal sulfhydryls and needs a source of electrons from the HMPS and TRX- coupled system to reduce disulfides. Oxidized TX is reduced by TRX and NADPH. Several lines of evidence suggest that the coupled HMPS/TRX/TX system represents an important target for cancer therapy. TX overexpression has been reported in several malignancies and may be associated with aggressive tumor growth and poor survival. In some cells, TX is an important factor in conferring resistance to chemotherapy and in stimulating production of hypoxia-inducible factor (HIF-1). Several inhibitors of the TRX/TX system have been evaluated in experimental cancer models: these include HMPS inhibitors, carbohydrate analogues, NADP synthesis blockers, vicinal thiol reactants, cisplatin, and TRX inhibitors. More recently, the targeted anti-cancer agent motexafin gadolinium has been identified. Motexafin gadolinium is a redox mediator that selectively localizes to cancer cells, and reacts with reducing metabolites and vicinal thiols to generate reactive oxygen species that ultimately block the TRX enzyme as well as the analogous glutaredoxin activity. In cell and animal models, motexafin gadolinium is directly cytotoxic to various tumor cells and enhances the activity of radiation therapy and chemotherapy. This drug is now in a broad range of clinical trials investigating its therapeutic potential when used as a single agent or in combination with either chemotherapy or radiation therapy. Promising clinical activity has been reported in a clinical trial with motexafin gadolinium and whole brain radiation therapy for treatment of brain metastases from solid tumors. These findings suggest that the TRX/TX system may represent an attractive target for development of new cancer therapeutics.
Changes in Energy Expenditure Resulting from Altered Body Weight (1995)

Maintenance of a reduced or elevated body weight is associated with compensatory changes in energy expenditure, which oppose the maintenance of a body weight that is different from the usual weight. These compensatory changes may account for the poor long-term efficacy of treatments for obesity.
Erhebliche Zweifel an der naturschutzfachlichen Invasivitätsbewertung einiger forstlich relevanter Baumarten [1] (2014)

Invasive Pflanzen- und Tierarten konnen die biologische Vielfalt negativ beeinflussen. Eine vom Bundesamt fur Naturschutz (BfN) beauftragte Autorengruppe hat erstmalig eine bundesweite naturschutzfachliche Bewertung von in Deutschland lebenden gebietsfremden Gefaspflanzen vorgelegt (BfN-Skripte 340, 352). Nach ihren Ergebnissen sind einige - darunter die forstlich kultivierten Baumarten Douglasie, Roteiche, Weymouthkiefer, Robinie und Hybridpappel - als invasive anzusehen, die nachweislich heimische Arten gefahrden sollen. Sie werden einer schwarzen Liste zugeordnet, fur die ein spezielles, bundesweites Management zur Kontrolle und Ausbreitungsbegrenzung vorgesehen ist. Die Forstwirtschaft wird neben dem Gartenbau als Einfuhrvektor fur die Ausbreitung von invasiven Geholzarten genannt und dafur verantwortlich gemacht.