gebhart/patrepeval huggingface dataset:
Cloning and Disruption of <i>Ustilago maydis</i> Genes (1989)

We have demonstrated that genes from Ustilago maydis can be cloned by direct complementation of mutants through the use of genomic libraries made in a high-frequency transformation vector. We isolated a gene involved in amino acid biosynthesis as an illustrative example and showed that integrative and one-step disruption methods can be used to create null mutations in the chromosomal copy of the gene by homologous recombination. The results of this investigation make it clear that one-step gene disruption will be of general utility in investigations of U. maydis, since simple, precise replacement of the sequence under study was readily achieved.
Plasma adenosine levels and P-selectin expression on platelets in preeclampsia (2001)

To measure the correlation of plasma adenosine levels with platelet activation in women with preeclampsia.Plasma adenosine concentration and expression of P-selectin, a marker for platelet activation, were measured in 18 normal pregnant women and 18 preeclamptic women. The effect of 8-sulfophenyltheophylline, an adenosine receptor blocker, on expression of P-selectin on platelets also was measured.Plasma adenosine level averaged 0.77 +/- 0.11 microM (standard error of the mean [SEM]) in women with preeclampsia, significantly higher than the mean level of 0.47 +/- 0.08 microM in women with normal pregnancies (P <.05). Expression of P-selectin on platelets averaged 7.8 +/- 1.2% in women with preeclampsia, also significantly higher than the mean level of 4.7 +/- 0.7% in normal pregnancy (P <.05). Adenosine receptor blockade significantly increased expression of P-selectin on platelets in women with preeclampsia by 26% (P <.05), which was significantly higher than the 13% increase of activation in those with normal pregnancies (P <.05).Adenosine is an established platelet activation suppressor. Increased plasma levels of adenosine in preeclampsia might partially compensate and tend to prevent further excessive platelet activation in women with preeclampsia.
Rigorous three-dimensional photoresist exposure and development simulation over nonplanar topography (1997)

A rigorous three-dimensional (3-D) simulation method for photoresist exposure and development is presented in which light scattering due to a nonplanar topography is calculated using the Maxwell equations. The method relies on a Fourier expansion of the electromagnetic field and extends the two-dimensional (2-D) differential method to the third dimension. The model accounts for partial coherent illumination and considers the nonlinear bleaching reaction of the photoresist. For the development process, the cellular-based topography simulator has been extended. A detailed description of the theory behind the simulation method is presented, the computational efficiency is discussed, and simulation results are given.
Pharmacokinetics of Intravitreal Anti-VEGF Drugs in Age-Related Macular Degeneration (2019)

Intravitreal administration of anti-vascular endothelial growth factor (VEGF) antibodies has become the standard treatment for Age-Related Macular Degeneration; however, the knowledge of their pharmacokinetics is limited. A comprehensive review of the preclinical and clinical pharmacokinetic data that were obtained in different studies with intravitreal bevacizumab, ranibizumab, and aflibercept has been conducted. Moreover, the factors that can influence the vitreous pharmacokinetics of these drugs, as well as the methods that were used in the studies for analytical determination, have been exposed. These anti-VEGF drugs present different charge and molecular weights, which play an important role in vitreous distribution and elimination. The pharmacokinetic parameters that were collected differ depending on the species that were involved in the studies and on physiological and pathological conditions, such as vitrectomy and lensectomy. Knowledge of the intravitreal pharmacokinetics of the anti-VEGF drugs that were used in clinical practice is of vital importance.
In Vitro Activity of Tomopenem (CS-023/RO4908463) against Anaerobic Bacteria (2008)

The antianaerobic activity of tomopenem, a new longer-half-life parenteral carbapenem, was compared with other carbapenems. Tomopenem showed broad activity against 63 reference species. The activity of tomopenem against 293 clinical isolates was potent (MIC(90), 0.06 to 4 microg/ml) and comparable to those of meropenem and doripenem and more potent than that of panipenem.
Evaluation of virucidal activity of a few physicochemical agents against goat-pox virus (1998)

Physico-chemical agents. viz. formalin (4%), sodium hypochlorite (0.4%), sodium hydroxide (4%), hydrochloric acid (0.4%), phenol (2%) sunlight and environmental temperatures (summer and winter), were examined against goat-pox virus for virucidal activity. Formalin and phenol completely inactivated the virus in 10 min, whereas hydrochloric acid did so in 30 min. Sodium hypochlorite failed to inactivate the virus in 30 min as there was only one log fall in residual titre. Sunlight inactivated the virus in 60 min. The rate of inactivation was faster at 45°C (summer temperature) as compared to the winter temperature (25°C-27°C) though the residual virus was recovered at the both temperatures after 180 min exposure. On the basis of the results obtained, phenol in 2% concentration can be recommended for disinfecting goat premises during goat-pox infection. Phenol is cheap, easily available and less irritant to tissues as compared to formalin.
INTERACTION-ORIENTED SOFTWARE DEVELOPMENT (2001)

This paper describes a new approach to the production of robust software. We first motivate the approach by explaining why the two major goals of software engineering — correct software and reusable software — are not being addressed by the current state of software practice. We then describe a methodology based on active, cooperative, and persistent software components, i.e., agents, and show how the methodology produces robust and reusable software. We derive requirements for the structure and behavior of the agents, and report on preliminary experiments on applications based on the methodology. We conclude with a roadmap for development of the methodology and ruminations about uses for the new computational paradigm.
Clinical and hematologic aspects of hemoglobin E β-thalassemia (2000)

Hemoglobin E beta-thalassemia is an important cause of childhood chronic disease in Southeast Asia. It is characterized by the presence of hemoglobin E and F, and the amount of hemoglobin E ranges from 35% to 75%. The patients are generally classified as having thalassemia intermedia because they have inherited a beta-thalassemia allele and hemoglobin E, which acts as a mild beta+-thalassemia. However, a remarkable variability in the clinical expression, ranging from a mild form of thalassemia intermedia to transfusion-dependent conditions, is observed. Severe hemoglobin E beta-thalassemia may have clinical features of thalassemia major. Phenotypes of thalassemia major can be predicted from the early onset of clinical symptoms and the requirement of regular blood transfusion from infancy for survival. Coinheritance of alpha-thalassemia alleviated the severity of beta-thalassemia disease in patients with at least one allele of mild beta-thalassemia genotype.
Effects of Apramycin, a Novel Aminoglycoside Antibiotic on Bacterial Protein Synthesis (1979)

1. The novel aminoglycoside antibiotic apramycin is shown to be a potent inhibitor of protein synthesis in bacteria both in vivo and in vitro. 2. In cell-free systems from Escherichia coli programmed with poly(U), apramycin induces translation errors, as assayed by incorporation of leucine, isoleucine and serine, although this effect occurs only to a limited extent. 3. Apramycin inhibits the translocation step of protein synthesis both in vivo, in protoplasts of Bacillus megaterium, and in vitro, in cell-free systems from E. coli. It is proposed that this is the primary inhibitory effect of the drug.
Radical Homopolymerization of Vinylidene Fluoride Initiated by <i>tert</i>-Butyl Peroxypivalate. Investigation of the Microstructure by <sup>19</sup>F and <sup>1</sup>H NMR Spectroscopies and Mechanisms (2002)

The radical polymerization in solution of vinylidene fluoride (VDF) initiated by different peroxides (tert-butyl peroxide and tert-butyl peroxypivalate) and by azo-tert-butane is presented. Various reaction temperatures and times and solvents were chosen to monitor the polymerization in terms of initiating radical generated from these initiators and transferring agents. Homopolymers thus obtained were characterized by 19F and 1H NMR spectroscopies. Different VDF telomers were synthesized (e.g., C4F9(CH2CF2)3H, C6F13CH2CF2CH2CH3, and CH3CF2(CH2CH2)2I) as models to explain the microstructure of these PVDFs. They enable one to identify without any ambiguity most different signals observed in 1H and 19F NMR spectra of PVDFs. From those assignments, an overall reactional mechanism was proposed that allows one to explain each step of polymerization of VDF. In particular, an interpretation of the polymer microstructures and of end groups arising from the radical initiator and from eventual transfers is suggested.
Abstract 4478: Discovery of AZD5363, an orally bioavailable, potent ATP-competitive inhibitor of AKT kinases (2011)

Abstract AKT is a key node in the most frequently de-regulated signaling pathway in human cancer and has been shown to mediate resistance to a range of cytotoxic, anti-hormonal and targeted therapies. We decided to explore inhibitors of AKT as potential new anti-cancer therapeutics. Here we disclose for the first time the discovery and structure of AZD5363, an orally bioavailable, potent ATP-competitive inhibitor of AKT. We evaluated a range of chemical starting points arising from our previous collaboration with the Institute of Cancer Research and Astex Therapeutics Ltd. Ultimately AZD5363 was discovered following a long journey that started from a pyrrolopyrimidine series of compounds. Our first challenge was to improve potency and a second challenge was to improve ROCK selectivity. ROCK is an AGC kinase like AKT but is involved in regulation of vascular tone and thus blood pressure. Extensive SAR studies exploring the series revealed that achieving selectivity over ROCK while retaining AKT potency was quite challenging. Eventually we discovered ways which could improve both selectivity and potency. However, these compounds had significant activity against the hERG ion channel which is implicated in the development of Torsades de Pointes and cardiac death. The next phase of work therefore had to focus on reducing hERG activity, while at the same time not adversely impacting either AKT potency or ROCK selectivity. Finally we discovered that introduction of a key substituent group provided a compound that achieved reduced hERG potency and, surprisingly, also achieved a further small improvement in both AKT potency and ROCK selectivity. This compound was AZD5363. A crystal structure of AZD5363 bound to AKT has revealed some of the key interactions that may contribute to its potency. For example, the pyrrolopyrimidine appears to form hydrogen bonds to the hinge region of the kinase. AZD5363 inhibits all known AKT isoforms with a potency of &amp;lt;10 nM and inhibits phosphorylation of the AKT substrate, PRAS40 in BT474c cells with a potency of 0.31 μM. Activity in in vivo pharmacodynamic and xenograft models has also been demonstrated. A synthetic route suitable for scale-up has been developed. In conclusion, AZD5363 is a potent inhibitor of AKT in vitro and in cells. It has good hERG and ROCK selectivity. It has pharmacodynamic and xenograft activity in vivo. AZD5363 has potential in cancer therapy and is currently in phase 1 clinical trials. Citation Format: {Authors}. {Abstract title} [abstract]. In: Proceedings of the 102nd Annual Meeting of the American Association for Cancer Research; 2011 Apr 2-6; Orlando, FL. Philadelphia (PA): AACR; Cancer Res 2011;71(8 Suppl):Abstract nr 4478. doi:10.1158/1538-7445.AM2011-4478
ChemInform Abstract: INTERACTION OF THIOCARBAMIDES WITH ALPHA‐BROMOKETONES, FORMATION OF SUBSTITUTED 2‐AMINOTHIAZOLES (1973)

Abstract Durch Reaktion entsprechender Thioharnstoffe (I) und Phenacylbdmide (II) in trockenem Aceton werden die Titelverbindungen (III) als Hydrobromid‐ Monohydrate erhalten (Freisetzung der Basen durch thermische Entwässerung und Basifizierung).
Kinetic evaluation of the reactivity of flavonoids as radical scavengers (2002)

The reactivity of flavonoids as radical scavengers was investigated under kinetic considerations using radical polymerization of methyl methacrylates initiated by benzoyl peroxide. The number of radicals which are trapped by each molecule of phenol (the stoichiometric factors, n values) decreased in the order of epigallocatechin-3-O-gallate (ECG) (5.5) > catechin (3.5) > resveratrol (2.4) > quercetin (1.9) > n-propylgallate (1.5) > hesperetin (1.0). The inhibition rate constants (k(inh)) (1-3 x 10(3) 1/(mol s)) for the flavonoids were not different from each other, and, therefore, the radical scavenging activity depend on n values. The n values of the fully oxidized flavonoids were estimated from the frontier orbital theory, using PM3 semiempirical molecular orbital calculation. The experimental n values were consistent with the calculated values.
Carbohydrate determinant NeuAc-Galbeta(1-4) of N-linked glycans modulates the antigenic activity of human immunodeficiency virus type 1 glycoprotein gp120 (1992)

In the present study we investigated to what extent the peripheral carbohydrate structure of N-linked glycans influences the antigenic properties of human immunodeficiency virus type 1 glycoprotein 120 (gp120). Recombinant gp120 was purified from GMK cells infected with a recombinant vaccinia virus expressing gp120. Purified gp120 was then coated onto 96-well ELISA microplates and subjected to sequential removal of peripheral monosaccharide units. Modified or unmodified gp120 was then incubated with monoclonal antibodies recognizing specific epitopes of gp120 and with a reporter lectin to determine the extent of carbohydrate elimination. Antibody and lectin binding was quantified in an enzyme-linked system. We found that the carbohydrate structure NeuAc-Gal beta (1-4) of N-linked glycans, defined both by lectin reactivity and by specific glycosidases, is involved in modulating the binding of antibody to a number of epitopes of peptide nature. The binding of antibody to one class of epitopes, situated in a region between amino acids 200 and 230, was strongly increased by removal of NeuAc-Gal beta (1-4), whereas the binding to epitopes in the V3 region was decreased and the binding to epitopes in the far N-terminal region was not altered by the treatment. These results suggested that peripheral structures of N-glycans are involved in modulating the overall conformation of gp120.
The replace operator (1995)

This paper introduces to the calculus of regular expressions a replace operator and defines a set of replacement expressions that concisely encode alternate variations of the operation. Replace expressions denote regular relations, defined in terms of other regular expression operators. The basic case is unconditional obligatory replacement. We develop several versions of conditional replacement that allow the operation to be constrained by context.
Segment-based etch algorithm and modeling (1991)

A novel approach to modeling the etch process is presented. A structure is represented as a string of nodes connected by line segments. By focusing on the segments one can deduce the behavior of the nodes and derive accurate etch models. These etch models handle naturally the rounding of a corner, handle precisely discontinuities due to material boundaries or shadow edges, and handle fully the complexities of angle-dependent etching. An efficient and accurate node movement algorithm has been developed. Nodes are allocated solely on the basis of curvature and adjust automatically as the structure evolves. The normal tradeoff between time step and accuracy is avoided by moving each node independently in time. This also allows nodes to be stopped at collisions, eliminating the need to detect and deal with loops.< <ETX xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">&gt;</ETX>
Carbamimidothioic acid phenylmethyl ester salts and their N,N'-tetramethyl derivatives as possible antimicrobial agents. (1990)

A series of carbamimidothioic acid phenylmethyl ester salts and their N,N'-tetramethyl derivatives were synthesized, many of which exert an interesting inhibiting action on Gram-positive and Gram-negative bacteria and also on fungi. This activity is noteworthy in view of the large number of strains antagonized; the (3,4,5-trichlorophenyl) methyl ester chloride of carbamimidothioic acid appeared to be the best term of the series. The possible influence on this activity of decomposition kinetics to the corresponding mercapto-derivatives was investigated and compared with that of a series of N,N'-tetramethyl derivatives of previously studied carbamimidothioic acid phenyl ester salts.
<sup>18</sup>F-Fluorobenzyl Triphenyl Phosphonium: A Noninvasive Sensor of Brown Adipose Tissue Thermogenesis (2011)

The intense uptake of (18)F-FBnTP into BAT at room temperature and the response to cold stimulation suggest the unique potential advantage of (18)F-FBnTP not only in detecting unstimulated BAT at high contrast but also in quantifying the mitochondrial thermogenic activity. (18)F-FBnTP PET may serve as a useful technique to assess BAT volume and function.
[The effectiveness of prenatal steroid and ambroxol therapy for the prevention of respiratory distress syndrome in newborns of diabetic mothers]. (2000)

The aim of the study was to determine the effectiveness of antenatal steroids and ambroxol in reduction of respiratory distress syndrome (RDS) in newborns of diabetic mothers. A retrospective chart review was done on 101 diabetic gravidas who were hospitalised at 1st Department of Obstetrics and Gynaecology Medical University in Warsaw between January 1989 and December 1999. We studied the neonatal outcomes for women with diabetes mellitus who delivered before 37 gestational weeks depend on exposition to antenatal steroids or ambroxol. Both groups were compared with unexposed neonates for respiratory distress syndrome. Frequency of occurrence and severity of RDS were similar in all study subgroups. We did not found reduction of respiratory distress syndrome in newborns of diabetic mothers exposed to antenatal steroids or ambroxol.
Preparation of some sulfonamide and diaminodiphenyl sulfone analogs of 1,4-naphthoquinone (1969)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTPreparation of some sulfonamide and diaminodiphenyl sulfone analogs of 1,4-naphthoquinoneF. Ivy Carroll, Kenneth H. Dudley, and H. Wayne MillerCite this: J. Med. Chem. 1969, 12, 1, 187–189Publication Date (Print):January 1, 1969Publication History Published online1 May 2002Published inissue 1 January 1969https://pubs.acs.org/doi/10.1021/jm00301a057https://doi.org/10.1021/jm00301a057research-articleACS PublicationsRequest reuse permissionsArticle Views193Altmetric-Citations5LEARN 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
Observing the brachial artery through a pressure cuff (1993)

A technique is described which enables ultrasonic imaging of the brachial artery whilst pressure is applied via a pressure cuff. This involves a new instrument--a sphygmomanometer, which uses water as opposed to air as the pressure medium, in order to permit ultrasonic imaging through the cuff. The technique was found to be acceptable in the clinical setting, and gave a measurement of the systolic blood pressure which correlated with the conventional cuff measurement in eleven elderly subjects (r = 0.89, p < 0.001). The technique should have an important role to play in studying the origin of differences which occur between direct and indirect blood pressure measurements.
Stable three-stranded DNA made by RecA protein. (1991)

When RecA protein, in the form of a nucleoprotein filament containing circular single-stranded DNA (plus strand only), reacts with homologous linear duplex DNA, a directional transfer ensues of a strand from the duplex DNA to the nucleoprotein filament, resulting in the displacement of the linear plus strand in the 5' to 3' direction. The initial homologous synapsis, however, can occur at either end of the duplex DNA, or anywhere in between, and when homology is restricted to different regions of the duplex DNA, the joint molecules that form in each region show striking differences in stability upon deproteinization: distal joints greater than proximal joints much greater than medial joints. In the deproteinized distal joints, which are thermostable, 2000 nucleotide residues of the circular plus strand are resistant to P1 nuclease; both strands of the original duplex DNA remain resistant to P1 nuclease, and the potentially displaceable linear plus strand, which has a 3' homologous end, remains resistant to Escherichia coli exonuclease I. These observations suggest that RecA protein promotes homologous pairing and strand exchange via long three-stranded DNA intermediates and, moreover, that, once formed, such triplex structures in natural DNA are stable even when RecA protein has been removed.
The Network (1990)

The directorate and management of all businesses have responsibilities towards shareholders, employees, customers and society at large. In meeting the needs of customers and fulfilling obligations towards society, they provide a public service. In the case of the Independent Television companies the public service element was reinforced by contracts with the Independent Television Authority, later the Independent Broadcasting Authority, a statutory body charged by parliament to regulate the system in the public interest.KeywordsChief ExecutiveProgramme StaffMajor CompanyRegional CompanyProgramme ControllerThese keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.
Localization of Two Metabotropic Glutamate Receptor Genes,GRM3andGRM8, to Human Chromosome 7q (1996)

Metabotropic glutamate receptors (GRMs) are neurotransmitter receptors that respond to glutamate stimulations by activating GTP-binding proteins and modulating second-messenger cascades. Eight related GRMs have been identified to date. In this study, we have mapped GRM3 and GRM8 to human chromosome 7q21.1-q21.2 and 7q31.3-q32.1, respectively, using somatic cell hybrid and fluorescence in situ hybridization analysis. A yeast artificial chromosome contig was constructed surrounding the genes, allowing their location to be integrated into the genetic and physical map of chromosome 7.