gebhart/patrepeval huggingface dataset:
Adenosine relaxation of isolated vascular smooth muscle (1976)

Adenosine relaxed hog carotid media strips contracted with norepinephrine (NE) and potassium (K+). Adenosine (3 X 10(-6)M) was more effective in relaxing the NE contractures than those produced by K+. In both cases, adenosine's efficacy decreased with increasing concentrations of the stimulating agent. A high adenosine concentration (1 X 10(-3)M) was necessary to elicit relaxation of completely depolarized (124 mM K+) media strips and equimolar concentrations of aminophylline caused greater relaxation than did adenosine. Adenosine inhibited the Ca2+ dose-response curves of strips stimulated with 20 mM and 30 mM K+ and its effect was dependent on the Ca2+ concentration. Neither 1 X 10(-6)M nor 1 X 10(-4)M adenosine produced any change in the cAMP content of vascular strips. Only at high concentrations did adenosine increase the cAMP content of vascular strips, but the increase was signficantly more than that observed with the same dose of aminophylline. The present results are consistent with the possibility that adenosine relaxes vascular smooth muscle by directly altering Ca2+ permeability and/or membrane potential; they do not support a role for cAMP in the adenosine-induced relaxation of vascular smooth muscle.
Lapatinib can restore capecitabine sensitivity in HER2-positive breast cancer. (2009)

Abstract Abstract #3157 Background: Lapatinib in combination with capecitabine is an effective treatment option in HER2-positive metastatic breast cancer (MBC) that has progressed after trastuzumab-based therapy. However, the efficacy of lapaptinib plus capecitabine in capacitabine resistant MBC patients and mechanism of sensitivity in these patients is unclear.&#x2028; Methods: In the preclinical part of the study, the effect of lapatinib on 5-FU sensitivity was investigated in a HER2 amplified breast cancer cell line (SKBr3). In the clinical part, MBC patients who progressed after treatments with trastuzumab, anthracycline, and taxane were enrolled in an open-label expanded-access study of lapatinib plus capecitabine (GlaxoSmithKline, USA) at Seoul National University Hospital from Mar 2007 to Apr 2008. Patients received lapatinib (1,250mg/day, 1-21) and capecitabine (2,000mg/m2, D1-14) combination treatment every 3weeks. The clinical data were prospectively collected.&#x2028; Results: In SKBr3 cell line, genes related to 5-FU sensitivity [TS, thymidine kinase 1(TK1), dihydrofolate reductase (DHFR), and ribonucleotide reductase M2 (RRM2)] were downregulated after lapatinib treatment. These genes were more significantly reduced after lapatinib-treatment compared with gefitinib or trastuzumab. In addition, TS reporter gene expression was enhanced by EGFR/HER2. Nuclear translocation of EGFR/HER2 induced by EGF and its association with TS promoter was effectively abolished by lapatinib. In the clinical study, a total of 37 female patients with HER2-positive MBC were analyzed. Sixteen (43%) patients had previously been treated with capecitabine. Overall response rate (RR) was 27.0% (95% CI 12.7-41.3), and disease control rate (DCR) was 83.8% (95% CI 71.9-95.7). During the median follow-up duration of 9.1 months, median progression-free survival (PFS) was 5.6 months (95% CI 4.0-7.2), and median overall survival has not been reached yet. There was no significant difference in RR/DCR and PFS according to prior capecitabine use. Prior capecitabine treatment had been discontinued due to disease progression during treatment in 13 patients. Among these patients with resistance to capecitabine, lapatinib and capecitabine resulted in DCR/PFS comparable to that of patients without exposure to capecitabine. Biomarker analysis of tissue specimen is currently underway and will be presented at the meeting.&#x2028; &#x2028; Conclusion: Lapatinib plus capecitabine demonstrated clinical activity in capecitabine pretreated MBC. Our data suggests that lapatinib may resensitize capecitabine resistant tumors to capecitabine by downregulation of nuclear EGFR/HER2 and TS. Citation Information: Cancer Res 2009;69(2 Suppl):Abstract nr 3157.
The Synthesis of Regiospecifically 13C-Labeled a-Tocopheryl Acetate (1981)

S u m a r y : A convenient procedure for the synthesis of reglospeclrlcally 13C-labeled d-tocopheryl acetate of h ~g h enr~chment is described.
Antimalarial Drug Toxicity: A Review (2007)

Antimalarial drug toxicity is viewed differently depending upon whether the clinical indication is for malaria treatment or prophylaxis. In the treatment of Plasmodium falciparum malaria, which has a high mortality if untreated, a greater risk of adverse reactions to antimalarial drugs is inevitable. As chloroquine resistance has become widespread, alternative agents may be used in treatment regimens, however, the toxicity of these antimalarial agents should be considered. Quinine is the mainstay for treating severe malaria due to its rare cardiovascular or CNS toxicity, but its hypoglycemic effect may be problematic. Mefloquine can cause dose-related serious neuropsychiatric toxicity and pyrimethamine-dapsone is associated with agranulocytosis, especially if the recommended dose is exceeded. Pyrimethamine-sulfadoxine and amodiaquine are associated with a relatively high incidence of potentially fatal reactions, and are no longer recommended for prophylaxis. Atovaquone/proguanil is an antimalarial combination with good efficacy and tolerability as prophylaxis and for treatment. The artemisinin derivatives have remarkable efficacy and an excellent safety record. Prescribing in pregnancy is a particular problem for clinicians because the risk-benefit ratio is often very unclear.
Properties of Carbon Nanotube - Polymer Composites (2008)

In the last ten years carbon nanotube composites are in the focus of the researchers of polymer blends. Different composition of carbon nanotubes and polymers were produced by a special mixing unit called Infinitely Variable Dynamic Shear Mixer (IDMX). In the experiments polypropylene and polycarbonate polymers were used as matrix materials. Nanotube masterbatches were used to prepare different compositions. Concentration series were manufactured by the dynamic mixer. The prepared materials were characterised by scanning electron microscopy. Mechanical, electrical and burning properties of the materials were also determined. Thermal properties were examined by DSC.
Structural Rationale for Low-Nanomolar Binding of Transition State Mimics to a Family GH3 β-<scp>d</scp>-Glucan Glucohydrolase from Barley<sup>,</sup> (2005)

The interactions of a transition state mimic anilinomethyl glucoimidazole (AmGlcIm), with a K(i) constant of 0.6 x 10(-)(9) M and a Gibbs free energy value of -53.5 kJ/mol, with a family GH3 beta-d-glucan glucohydrolase from barley have been analyzed crystallographically and by ab initio quantum mechanical modeling. AmGlcIm binds 3 times more tightly to the beta-d-glucan glucohydrolase than a previously investigated phenyl glucoimidazole. In the enzyme-AmGlcIm complex, an additional residue, Tyr253, and a water molecule positioned between subsites -1 and +1 are recruited for binding. Analyses of the two binary complexes reveal the following. (i) An intricate network exists in which hydrogen bonds between the enzyme's catalytic pocket residues Lys206, His207, Tyr253, Asp285, and Glu491 and the glucoimidazoles are shorter by 0.15-0.53 A, compared with distances of hydrogen bonds in the Michaelis complex. (ii) The "glucose" moiety of the glucoimidazoles adopts a (4)E conformation that is vital for the low-nanomolar binding. (iii) The N1 atoms of the glucoimidazoles are positioned nearly optimally for in-line protonation by the Oepsilon1 atom of the catalytic acid/base Glu491. (iv) The enzyme derives binding energies from both glycone and aglycone components of the glucoimidazoles. (iv) The prevalent libration motion of the two domains of the enzyme could play a significant role during induced fit closure in the active site. (v) Modeling based on the structural data predicts that protons could be positioned on the N1 atoms of the glucoimidazoles, and the catalytic acid/base Glu491 could carry an overall negative charge. (vi) The enzyme-AmGlcIm complex reveals the likely structure of an early transition state during hydrolysis. Finally, the high-resolution structures enabled us to define minimal structures of oligosaccharides attached to Asn221, Asn498, and Asn600 N-glycosylation sites.
Explicit (Noniterative) Loran Solution (1967)

the main computational requirement for LORAN navigation systems is the transformation to geographic latitude and longitude of time difference measurements made by the LORAN receiver. It is desirable to maintain a computational accuracy of less than one second of arc to avoid degradation of the inherently attainable LORAN system accuracy. It is therefore necessary to take into account the effect of a non-spherical earth (ellipticity correction) and variable velocity of propagation (secondary phase correction.) Incorporation of these corrections into the analysis results in two non-linear equations in two unknowns. This paper presents a derivation and discussion of an explicit, noniterative, LORAN mechanization of very high accuracy (approximately one second of arc). The advantages of this explicit solution are as follows: 1. No initial guess as to receiver position is required. This provides for a self-sufficient LORAN system. 2. Perfect computational repeatability is achieved. 3. With the explicit solution, it is always possible to select the proper solution of the two possible solutions. 4. The simple explicit equations lead to reduced computational time and memory storage requirements for the computer. This technique has been programmed on the RECOMP III Computer. It was tested for accuracy by comparison with the National Bureau of Standards computations [2] for the East Coast LORAN Net. Representative samples of the results are given.
Modulation of Circadian Rhythm of Blood Pressure by Cortisol in Patients with Hypopituitarism (1994)

We conducted a study to determine the effect of exogenous cortisol on circadian blood pressure changes in patients with hypopituitarism. Under replacement with hydrocortisone of 15 to 25mg either once (8:00) or twice a day (8:00 and 20:00), and with prednisolone of 3.75 to 5mg once a day, the patients underwent non-invasive ambulatory blood pressure monitoring for 24 hours. The average 24-hour blood pressure before hydrocortisone replacement was 92.9 +/- 1.0 (systolic)/53.2 +/- 0.8mmHg (diastolic), while that after hydrocortisone replacement once or twice a day and prednisolone replacement significantly increased to 108.2 +/- 1.4/63.5 +/- 0.9mmHg, 109.1 +/- 1.6/62.3 +/- 1.0mmHg, and 105.4 +/- 1.2/62.3 +/- 0.9mmHg, respectively. Hydrocortisone replacement once a day showed a significant increase in day-night differences of blood pressure, while hydrocortisone replacement twice a day did not. There were no differences in nocturnal decrease in pulse rate between these two replacements. The daytime and nighttime urinary excretions of 17-hydroxycorticosteroids in hydrocortisone replacement once a day were 7.7mg/12hr (daytime) and 1.4mg/12hr (nighttime), respectively, while those in hydrocortisone replacement twice a day were 3.9mg/12hr (daytime) and 3.6mg/12hr (nighttime), respectively. Urinary 17-ketosteroids, epinephrine and norepinephrine did not show any differences between hydrocortisone replacement once and twice a day. These results suggest that hydrocortisone administration is one of the factors which modulate the circadian variation of blood pressure in patients with hypopituitarism, and may also suggest that the circadian change of cortisol secretion participates, at least in part, in the formation of an intrinsic circadian rhythm of blood pressure.
Crystal structure of 2-sulfanilamidopyrimidinesilver(I) (1976)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTCrystal structure of 2-sulfanilamidopyrimidinesilver(I)N. C. Baenziger and Arthur W. StrussCite this: Inorg. Chem. 1976, 15, 8, 1807–1809Publication Date (Print):August 1, 1976Publication History Published online1 May 2002Published inissue 1 August 1976https://pubs.acs.org/doi/10.1021/ic50162a014https://doi.org/10.1021/ic50162a014research-articleACS PublicationsRequest reuse permissionsArticle Views259Altmetric-Citations109LEARN 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-AlertscloseSupporting Info (1)»Supporting Information Supporting Information Get e-Alerts
Bacteriuria and primary biliary cirrhosis. (1984)

Significant bacteriuria was found in 19% of 87 women with primary biliary cirrhosis, whereas in 89 women with other types of chronic liver disease bacteriuria was present in only 7%. In 74 women with rheumatoid arthritis 8% were bacteriuric. Midstream urine specimens obtained from 144 consecutive women with primary biliary cirrhosis attending hospital over a two year period showed that 50 (35%) developed bacteriuria during 12 months of follow up. Bacteriuria was unrelated to age, raised serum bilirubin, drug therapy or urinary pH but was more common in patients with late stage (fibrotic) disease as judged by histological criteria. Fifty seven per cent of bacteriuric primary biliary cirrhosis patients suffered more than one urinary infection. Fifty nine per cent of the 156 bacteriuric episodes were asymptomatic. The types of organism isolated, the antibiotic sensitivity patterns and cure rate were similar to those reported in bacteriuric women without other underlying disease. The reinfection rate (34%), however, was double that reported for bacteriuric episodes in 'problem' women with recurrent bacteriuria, indicating a special susceptibility to urinary infection. The most common isolates were E coli (70%), which did not show abnormal adhesiveness to uroepithelial or buccal cells of normal women, or to those of primary biliary cirrhosis patients. Patients with primary biliary cirrhosis have not been reported to be more susceptible to infection in general. Bacteriuria, however, was common throughout all clinical stages of primary biliary cirrhosis. Thus there may be a unique association between bacteriuria and primary biliary cirrhosis.
Comparative Study of the Effects of 2% Ibopamine, 10% Phenylephrine, and 1% Tropicamide on the Anterior Segment (2003)

The results confirm the potent mydriatic effect of 2% ibopamine, which is greater than that of either 10% phenylephrine or 1% tropicamide, as well as its ability to induce an increase in intraocular pressure when used in patients with glaucoma alone. These data support the hypothesis that the widening of the ACA induced by 2% ibopamine is due to posterior rotation of the iris plane and ciliary processes. These changes are quantitatively greater than those induced by 10% phenylephrine and 1% tropicamide and are related to the greater mydriatic effect of the drug.
Cationic polymerization of α‐methylstyrene from polydienes. I. Synthesis and characterization of poly(butadiene‐<i>g</i>‐α‐methylstyrene) copolymers (1979)

Abstract The preparation of poly(butadiene‐ g ‐α‐methylstyrene) copolymers was investigated with three different alkylaluminum coinitiators. The alkylaluminum compounds in conjunction with polybutadiene which contained a low concentration of labile chlorine atoms initiated the polymerization of α‐methylstyrene to produce graft copolymers. Trimethylaluminum gave higher grafting efficiencies than diethylaluminum chloride at comparable monomer conversions. Triethylaluminum produced only very low monomer conversions (<5%), even at long reaction times, and for this reason was not studied extensively. The number of grafts per polybutadiene backbone was determined for a number of copolymers and found to increase slightly as the allylic chlorine concentration in the polybutadiene backbone was increased. In all cases, however, only a low percentage of the available labile chlorine sites along the polybutadiene backbone resulted in grafted α‐methylstyrene side chains. The addition of small quantities of water to the polymerization solvent greatly enhanced the grafting rate and ultimate monomer conversion during the synthesis of these poly(butadiene‐ g ‐α‐methylstyrene) copolymers. The mechanistic role of water during these grafting reactions is unknown at the present time.
Bone metabolism and clinical study of 44 patients with bisphosphonate-related osteonecrosis of the jaws (2012)

According to our results, osteonecrosis of the jaws affects elderly patients. We found a direct relationship between the duration of exposure and the accumulated dose. Other relevant factors are: Poor oral and dental health, corticoids, diabetes and teeth extractions. In essence, it is a clinical diagnosis. Prevention is the best strategy to handle this clinical entity.
Effects of deglycosylation of human thyroperoxidase on its enzymatic activity and immunoreactivity (1992)

ABSTRACT Thyroid peroxidase (TPO) is a glycoprotein enzyme which catalyses the iodination of thyroglobulin and the coupling of iodinated tyrosines. Human TPO (hTPO) is the microsomal antigen recognized by the autoantibodies in the serum of patients with autoimmune thyroid disease. An active detergent-solubilized immunoaffinitypurified hTPO was deglycosylated, either by peptide N-glycosidase F (PNGase F) or by endo-β-N-acetylglucosaminidase H (endo H), and the enzymatic activity and immunoreactivity of the native and degylcosylated forms were compared. Electrophoretic controls and affinoblotting with concanavalin A showed that deglycosylation was not total and that it was more pronounced with endo H than with PNGase F. The enzymatic activity of hTPO was inhibited by endo H deglycosylation, but not by PNGase F deglycosylation; this inhibition was not due to aggregation and/or insolubilization of the molecule subsequent to deglycosylation. Immunoreactivity was monitored by enzyme-linked immunosorbant assay (ELISA) with 13 mouse monoclonal antibodies, rabbit polyclonal antibodies and antibodies from serum of patients with Hashimoto's thyroiditis. In contrast with enzymatic activity, immunoreactivity was not modified or was slightly enhanced (with four monoclonal antibodies) by deglycosylation. The results indicate that strong, if not total, deglycosylation induces a modification of the tertiary structure of hTPO, which affects the enzymatic site but does not modify markedly the epitopes implicated in the recognition of the molecule by the antibodies tested. Journal of Endocrinology (1992) 132, 317-323
Design and implementation of DV stream over Internet (2003)

An Internet Protocol (IP) based high-quality real-time audio-visual (AV) communication tool has been developed. A digital video (DV) camcorder and VCR, being consumer market products, are adopted as the AV codec. The AV devices, which have an IEEE-1394 (Firewire) interface, are connected to the IP host with its interface. The original packet format is adopted by simply encapsulating the isochronous stream packet of the DV with UDP/IP. In the highest quality of communication, the system consumes over 35 Mbps of network bandwidth. The system can also change the bandwidth adaptively for end-to-end network conditions. The DV communication effort was performed using the APAN TransPAC link between the USA and Asia (Japan and Korea).
Limits on the Corrosion Rate of Si Surfaces in Contact with CH3OH-Ferrocene+/0 and CH3OH-1,1'-Dimethylferrocene+/0 Solutions (1995)

Although Si/CH^3OH contacts have been extensively investigated and reported to provide highly efficient photoelectrochemical energy conversion devices, a recent study using the scanning electrochemical microscope (SECM) has claimed that, in CH_3OH solutions, Si surfaces in contact with 4.57 mM ferrocenium (Fc^+) were etched in the dark at a mass-transport-limited rate. The reported etching rate constant of > 0.37 cm s^-1) at 4.57 mM ferrocenium corresponds to an equivalent corrosion current density of > 240 mA cm^(-2) and to a Si etch rate of > 75 nm s^(-1). The presence of such severe corrosion was inferred from an unexpectedly large feedback current in an SECM experiment. The present work describes a search for corrosion of Si in contact with CH_3OH-ferrocene^+/0) and CH_3OH-dimethylferrocene(Me2Fc)^(+/0) solutions through the use of very sensitive electrochemical, chemical, and physical methods. For CH_3OH - 1.0 M LiClO_4 - 100 mM Me_2Fc- 80 mM Me_2Fc^+ solutions, an upper limit on the etch rate of 6.6 x10^(-6) nm s^-1) has been established through direct experimental measurements; thus, a 400 pm thick Si photoelectrode in contact with the CH_3OH-Me_2-Fc^(+/0) electrolyte would require over 1500 years to corrode completely at room temperature. An alternative explanation for the SECM data, based on the documented existence of an inversion layer at the Si/liquid contact, is presented and shown to be consistent with the available data.
Primitives for programming multi-user interfaces (1991)

We have designed a set of primitives for programming multi-user interfaces by extending a set of existing high- level primitives for programming single-user interfaces.
Regulation of phospholipid synthesis in Escherichia coli. Composition of the acyl-acyl carrier protein pool in vivo. (1982)

The regulation of membrane lipid biogenesis was investigated by measuring the levels of the acyl-acyl carrier protein (acyl-ACP) intermediates in the biosynthetic pathway. In particular, the role of the sn-glycerol-3-phosphate acyltransferase was assessed by focusing on the size and composition of the long chain acyl-ACP pool. The ACP( pool was specifically labeled in vivo with beta-[3-3H]alanine and the ACP subspecies analyzed by reversed phase liquid chromatography and conformationally sensitive gel electrophoresis. The acyl-ACP pool was found to be a small fraction of the total ACP in normally growing cells and was particularly devoid of chain lengths that could serve as acyltransferase substrates. Inhibition of phospholipid synthesis at the acyltransferase step resulted in a rapid increase in the content of acyl-ACP, and analysis showed the presence of chain lengths that are acyltransferase substrates. Acyl-CoAs were not detected during interruption of acyl transfer activity. These results show that 1) acyl-ACPs are the acyl donors for phospholipid synthesis in vivo, 2) the acyltransferase does not play a role in the regulation of the lipid biosynthetic rate or the composition of phospholipid acyl moieties, 3) the primary regulatory site in phospholipid biosynthesis is at an early step in fatty acid biosynthesis, 4) feedback regulation by long chain acyl-ACP's is not a controlling mechanism for fatty acid synthesis under normal physiological circumstances, and 5) enzymes that utilize acyl-ACPs are involved in kinetic competition for the scarce acyl-ACP substrates.