gebhart/patrepeval huggingface dataset:
Enhanced In Vitro Selective Toxicity of Chemotherapeutic Agents for Human Cancer Cells Based on a Metabolic Defect2 (1986)

A metabolic defect that is prevalent in human cancer cell lines was exploited to selectively kill these cells without killing cocultured normal human fibroblasts. Methionine dependence, a metabolic defect seen only in cancer cells or immortalized cell lines in vitro, precludes the cells from growing in media in which methionine is replaced by its immediate precursor, homocysteine, a condition that allows the growth of all normal cell strains tested. The methionine-dependent cells become reversibly blocked in late S-G2 (i.e., late-S and G2 phases) under the above condition, a block that was exploited for selective chemotherapy against these cells. In cultures that were initiated with equal amounts of cancer cells and human diploid fibroblasts, substitution of homocysteine and doxorubicin for methionine in the culture medium followed by methionine repletion with vincristine was totally effective at selectively eliminating a methionine-dependent human sarcoma and 3 methionine-dependent human carcinomas. The above protocol was nearly totally effective against a partially methionine-independent revertant of the sarcoma. The chemotherapeutic procedure used was not lethal to normal cells growing alongside the tumor cells and was ineffective when conducted totally in methionine-containing medium. The optimal procedure was 10(-10) M doxorubicin in methionine-free, homocysteine-containing medium for 10 days followed by 2 x 10(-7) M vincristine in methionine-containing, homocysteine-free medium for 1 day, in turn followed by drug-free methionine-containing, homocysteine-free medium. These results demonstrate the potential for treatment of solid tumors with chemotherapy based on metabolic differences between normal and tumor cells.
Novel Selective and Partial Agonists of 5-HT<sub>3</sub>Receptors. Part 1. Synthesis and Biological Evaluation of Piperazinopyrrolothienopyrazines (1996)

A series of piperazinopyrrolo[1,2-a]thieno[3,2-e]- and -[2,3-e]pyrazine derivatives were prepared and evaluated in order to determine the necessary requirements for high affinity on the 5-HT3 receptors and high selectivity versus other 5-HT receptor subtypes. Various substitutions on the piperazine and the thiophene ring of the pyrrolothienopyrazine moieties were systematically explored as well as replacement of the piperazine by other cyclic amines. The best compounds are in the nanomolar range of affinity of 5-HT3 receptors with high to very high selectivity (up to 10,000 for 14b). These high-affinity compounds have in common a benzyl- or allylpiperazine substituent with no substitutions on the thiophene ring. Five of these compounds (1a, 4b, 13a,b, and 14b) have been evaluated on the Von Bezold-Jarisch reflex and were characterized as partial agonists. One of them, 13a, has shown in vivo at very low dose a potent anxiolytic-like activity in the light/dark test.
Earl Sutherland (1915-1975) and the Discovery of Cyclic AMP (2012)

In 1945, Earl Sutherland (1915-1974) [corrected] and associates began studies of the mechanism of hormone-induced glycogen breakdown in the liver. In 1956, their efforts culminated in the identification of cyclic AMP, an ancient molecule generated in many cell types in response to hormonal and other extracellular signals. Cyclic AMP, the original "second messenger," transmits such signals through pathways that regulate a diversity of cellular functions and capabilities: metabolic processes such as lipolysis and glycogenolysis; hormone secretion; the permeability of ion channels; gene expression; cell proliferation and survival. Indeed, it can be argued that the discovery of cyclic AMP initiated the study of intracellular signaling pathways, a major focus of contemporary biomedical inquiry. This review presents relevant details of Sutherland's career; summarizes key contributions of his mentors, Carl and Gerti Cori, to the knowledge of glycogen metabolism (contributions that were the foundation for his own research); describes the experiments that led to his identification, isolation, and characterization of cyclic AMP; assesses the significance of his work; and considers some aspects of the impact of cyclic nucleotide research on clinical medicine.
Vehicle Maneuver Detection with Accelerometer-Based Classification (2016)

In the mobile computing era, smartphones have become instrumental tools to develop innovative mobile context-aware systems. In that sense, their usage in the vehicular domain eases the development of novel and personal transportation solutions. In this frame, the present work introduces an innovative mechanism to perceive the current kinematic state of a vehicle on the basis of the accelerometer data from a smartphone mounted in the vehicle. Unlike previous proposals, the introduced architecture targets the computational limitations of such devices to carry out the detection process following an incremental approach. For its realization, we have evaluated different classification algorithms to act as agents within the architecture. Finally, our approach has been tested with a real-world dataset collected by means of the ad hoc mobile application developed.
Selective catalytic oxidations of lactose and related carbohydrates (1991)

The progressing exhaustion of oil reseJVes, bas intensified the discussion coneeTDing the need for alternative raw materials for the chemical industries.Carbohydrates are, owing to their relative low heat of combustion, no realistic alternative as a fuel, however they can be an interesting alternative as cheap raw materials for the chemical industries, especially in fine chemistry.This thesis deals with the development of selective catalytic oxidation processes for lactose and related carbohydrates into the corresponding aldobionic acids, with molecular oxygen as the oxidanl Lactose or milksugar, produced from whey, a byproduct from the cheese production, can be converted readily by simple oxidation chemistry into lactose derived aldobionates, which can react by means of an intramolecular esterification into aldobiono-Iactones.These lactose derived aldobiono-lactones can be used as an intennediate in the synthesis of a great variety of interesting products, e.g.biodegradable surfactants, liquid crystals, watersoluble polymers, etc., as described in chapter 1. Chapter 2 describes the development of analytical procedures to follow the oxidation processes in aqueous media qualitatively and quantitatively, necessary to study the kinetics of the reactions investigated.A HPLC analysis and a reversed-phase chromatographic analysis have been developed for the analysis of the sugar components present in the reaction samples, without interference of the produced meidation products.Also a HPLC analysis bas been developed for the analysis of the oxidation products, without interference of the sugar components.In chapter 3 a general literature suJVey is presented, concerning the behaviour of reducing carbohydrates in alkaline media under oxidative and non-oxidative conditions.It can be regarded as an introduetion to the investigations on the homogeneously alkalicatalyzed oxidative degradation of lactose to ~-0-D-galactopyranosyl-(1-+3)-D arabinonate and formate.Chapter 4 deals with the alkali-catalyzed oxidative degradation of lactose and related carbohydrates.The oxidative degradation reaction of lactose proc~eds at standard reaction conditions, i.e. low reaction temperature, 293 K. high oxygen partial pressure, Po 2 1 bar, and a high stirring speed, rpm 1300, with ca.75 mol% selectivity, which decreases dramatically at higher reaction temperatures.Simultaneous addition of both catalytic amounts of antraquinone-2-sulfonic acid (AMS) and hydragen peroxide to the standard process, leads to an increase of the selectivity up to ca. 90 mol%.This increased selectivity is maintained at reaction temperatures up to 323 K. allowing a reduction of the batch time necessary for almast complete conversion from 50 to 1.5 hour.The global activation energy of the process bas been determined for lactose, Dglucose and D-galactose.
A New Method for the Determination of Critical Micelle Concentrations of Un-ionized Associations Colloids in Aqueous or in Non-aqueous Solution (1959)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTA New Method for the Determination of Critical Micelle Concentrations of Un-ionized Associations Colloids in Aqueous or in Non-aqueous SolutionSydney Ross and J. P. OlivierCite this: J. Phys. Chem. 1959, 63, 10, 1671–1674Publication Date (Print):October 1, 1959Publication History Published online1 May 2002Published inissue 1 October 1959https://pubs.acs.org/doi/10.1021/j150580a025https://doi.org/10.1021/j150580a025research-articleACS PublicationsRequest reuse permissionsArticle Views972Altmetric-Citations143LEARN 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 options Get e-Alerts
Amino Acid Sequence Homology of Coat Proteins as a Basis for Identification and Classification of the Potyvirus Group (1988)

Summary Analysis of the 136 possible pairings of the coat protein amino acid sequences from 17 strains of eight distinct potyviruses revealed a bimodal distribution of sequence homology. Distinct members of the group exhibited sequence homologies ranging from 38 to 71% (average 54%) with major differences in the length and sequence of their N termini and high sequence homology in the C-terminal half of the coat proteins. In contrast strains of individual viruses exhibited sequence homologies of 90 to 99% (average 95%) and had very similar N-terminal sequences. These findings cast doubt on the currently held ‘continuum’ hypothesis proposed to explain the unsatisfactory taxonomy of the potyvirus group. The coat protein sequence data, in combination with information on the nature of the potyvirus particle assembly, can be used to develop rationally designed, simple serological techniques that appear to be more useful and more easily applied than those properties previously used for potyvirus identification and classification.
Design of Nx40Gbit/s multi-terabit/s transmission systems assisted by simple analytical tools (2003)

We provide two analytical rules to optimally manage dispersion in Nx40Gbit/s systems, and thus contain nonlinearities. These rules proved helpful for extending the distance of a recent 5Tbit/s experiment from 1200 km to 1500 km.
A Mild Protocol To Generate Uranium(IV) Mixed-Ligand Metallocene Complexes using Copper(I) Iodide (2008)

Reaction of the trivalent uranium complexes (C5Me5)2UI(THF) (1), (C5Me5)2U[N(SiMe3)2] (3), (C5Me5)2U(NPh2)(THF) (4), and (C5Me5)2U(O-2,6-iPr2-C6H3)(THF) (5) with copper(I) iodide affords the corresponding tetravalent uranium diiodide, amide iodide, and aryloxide iodide complexes (C5Me5)2UI2 (2), (C5Me5)2U[N(SiMe3)2](I) (6), (C5Me5)2U(NPh2)(I) (7) and (C5Me5)2U(O-2,6-iPr2-C6H3)(I) (8), respectively. This protocol was also extended to the synthesis of the alkyl iodide complex (C5Me5)2U(CHPh2)(I) (10). The isolation of complex 10 from the in situ generated trivalent uranium alkyl complex (C5Me5)2U(CHPh2)(THF) (9) illustrates the synthetic value of this oxidation procedure in those situations where the uranium(III) metallocene complex cannot be isolated or is unstable. Overoxidation and ligand redistribution are not observed with this Cu-based UIII → UIV oxidation procedure. Attempted functionalization of the UIV amide iodide complex (C5Me5)2U[N(SiMe3)2](I) (6) with Me2Mg afforded the novel azametallacycle (C5Me5)2U[η2(N,C)-CH2SiMe2N(SiMe3)] (12) by intramolecular C−H activation and liberation of methane. Reaction between (C5Me5)2U(NPh2)(I) (7) and Me2Mg afforded a mixture of the products (C5Me5)2U(NPh2)(Me) (13), (C5Me5)2UMe2 (14), and (C5Me5)2U(NPh2)2 (15) at room temperature; heating the mixture smoothly furnished the azametallacycle (C5Me5)2U[η2(N,C)-(o-C6H4)NPh] (16). Similarly, reaction between 14 and HNPh2 at 100 °C produced the azametallacycle 16 by aminolysis and subsequent intramolecular C−H activation.
Improving Efficient Neural Ranking Models with Cross-Architecture Knowledge Distillation (2020)

Teacher train files (ids only), based on the MSMARCO-Passage collection, for the paper: <em>Improving Efficient Neural Ranking Models with Cross-Architecture Knowledge Distillation</em> Sebastian Hofstätter, Sophia Althammer, Michael Schröder, Mete Sertkan and Allan Hanbury (https://arxiv.org/abs/2010.02666) for the documentation please see: https://github.com/sebastian-hofstaetter/neural-ranking-kd
Versatile Platform for Controlling Properties of Plant Oil-Based Latex Polymer Networks (2018)

A series of latexes from acrylic monomers (made from olive, soybean, linseed, and hydrogenated soybean oils), significantly different in terms of fatty acid unsaturation, were synthesized using miniemulsion copolymerization with styrene. The number-average molecular weight and the glass transition temperature of the resulting copolymers with high levels of biobased content (up to approximately 60 wt %) depend essentially on the amount of unsaturation (the number of double bonds in triglyceride fatty acid fragments of plant oil-based monomers) in the reaction feed. When plant oil-based latex films are oxidatively cured, the linear dependence of the cross-link density on reaction feed unsaturation is observed. Dynamic mechanical and pendulum hardness measurements indicate that the properties of the resulting plant oil-based polymer network are mainly determined by cross-link density. On the basis of the linear dependence of the cross-link density on monomer feed unsaturation, it can be concluded that the latex network formation and thermomechanical properties can be adjusted by simply combining various plant oil-based monomers at certain ratios (“given” unsaturations) in the reaction feed. Assuming a broad variety of plant/vegetable oils available for new monomers synthesis, this can be considered as a promising platform for controlling properties of plant oil-based latex polymer networks.
NaCl 수용액내의 양성자와 디이소부틸니트로소아민의 치환흡착과 열역학적 특성 (1983)

Electrochemical adsorption always was accompanied with solvent displacement and relative size factor(χ) of adsorbate and solvent and hydrogen coverage(θ) on the lead anodic film electrode formed in phosphoric acid in NaCl solution and the sea water at 15-35℃ were studied by means of constant current-potential method and potentiodynamic cathodic polarization method. In this experiment, various constants and thermodynamic quantities calculated from the hydrogen coverage ware also described to explain the reactivities of di-iso-butylnitrosoamine(DBNA) and proton(H^+) according to the changes of interactions between solute and solvent in the bulk phase and interphase. It was investigated that the average values of relative size factor and the coverage of hydrogen atoms studied with the electrode of lead anodic film formed in phosphoric acid solution in 60mM DBNA+0.5M NaCl and in 60mM DBNA+6‰ sea water were about 11.0 and 0.2 respectively. Hydrogen evolution was electrochemical mechanism because of substitutional adsorption of aromatic substance with their delocalization of electrons, but in the case of non-charge transfer adsorption of aliphatic substance(DBNA) interacting relatively little with the electrode, it was combination mechanism.
Crystal Structure of a Class XIB Phospholipase A2 (PLA2) (2009)

Phospholipase A(2) catalyzes the specific hydrolysis of the sn-2 acyl bond of various glycerophospholipids, producing fatty acids and lysophospholipids. Phospholipase A(2)s (PLA(2)s) constitute a large superfamily of enzymes whose products are important for a multitude of signal transduction processes, lipid mediator release, lipid metabolism, development, plant stress responses, and host defense. The crystal structure of rice (Oryza sativa) isoform 2 phospholipase A(2) has been determined to 2.0 A resolution using sulfur SAD phasing, and shows that the class XIb phospholipases have a unique structure compared with other secreted PLA(2)s. The N-terminal half of the chain contains mainly loop structure, including the conserved Ca(2+)-binding loop, but starts with a short 3(10)-helix and also includes two short anti-parallel beta-strands. The C-terminal half is folded into three anti-parallel alpha-helices, of which the two first are also present in other secreted PLA(2)s and contain the conserved catalytic histidine and calcium liganding aspartate residues. The structure is stabilized by six disulfide bonds. The water structure around the calcium ion binding site suggests the involvement of a second water molecule in the mechanism for hydrolysis, the water-assisted calcium-coordinate oxyanion mechanism. The octanoate molecule in the complex structure is bound in a hydrophobic pocket, which extends to the likely membrane interface and is proposed to model the binding of the product fatty acid. Due to the differences in structure, the suggested surface for binding to the membrane has a different morphology in the rice PLA(2) compared with other phospholipases.
Noncariogenicity of Erythritol as a Substrate (1992)

Erythritol is a sugar alcohol produced by Aureobasidium sp. from glucose. It is 75-80% as sweet as sucrose and is also nonhygroscopic. The aim of this study was to evaluate this sugar substitute from a cariological point of view. Erythritol was neither utilized as a substrate for the lactic acid production nor for plaque formation of mutans streptococci (serotypes a-h) and certain oral microorganisms. It was not utilized for water-insoluble glucan synthesis or cellular adherence by glucosyltransferase from Streptococcus mutans PS-14 (c) and Streptococcus sobrinus 6715 (g). Finally, a significantly lower caries score (3.1 +/- 0.5; mean +/- SEM) was observed in specific pathogen-free rats infected with S. sobrinus 6715 and fed with a diet containing 26% erythritol, as compared to control rats fed with a diet containing 26% sucrose (60.5 +/- 2.0). Also, rats provided a diet containing 56% erythritol chocolate (23.8% erythritol) and challenged with S. mutans PS-14 exhibited a significantly lower caries score (6.7 +/- 0.8) compared to the sucrose chocolate group (82.8 +/- 2.8). The main conclusion from this study is therefore that erythritol is a promising sugar substitute from a cariological point of view.
Potentiation Effects of Amikacin and Fosfomycin against Selected Amikacin-Nonsusceptible Gram-Negative Respiratory Tract Pathogens (2014)

The amikacin-fosfomycin inhalation system (AFIS) is a combination of 2 antibiotics and an in-line nebulizer delivery system that is being developed for adjunctive treatment of pneumonia caused by Gram-negative organisms in patients on mechanical ventilation. AFIS consists of a combination of amikacin and fosfomycin solutions at a 5:2 ratio (amikacin, 3 ml at 100 mg/ml; fosfomycin, 3 ml at 40 mg/ml) and the PARI Investigational eFlow Inline System. In this antibiotic potentiation study, the antimicrobial activities of amikacin and fosfomycin, alone and in a 5:2 combination, were assessed against 62 Gram-negative pathogens from a worldwide antimicrobial surveillance collection (SENTRY). The amikacin MICs for 62 isolates of Acinetobacter baumannii, Pseudomonas aeruginosa, and Klebsiella pneumoniae were ≥32 μg/ml (intermediate or resistant according to the Clinical and Laboratory Standards Institute [CLSI]; resistant according to the European Committee on Antimicrobial Susceptibility Testing [EUCAST]). Each isolate was tested against amikacin (0.25 to 1,024 μg/ml), fosfomycin (0.1 to 409.6 μg/ml), and amikacin-fosfomycin (at a 5:2 ratio) using CLSI reference agar dilution methods. The median MIC values for amikacin and fosfomycin against the 62 isolates each decreased 2-fold with the amikacin-fosfomycin (5:2) combination from that with either antibiotic alone. Interactions between amikacin and fosfomycin differed by isolate and ranged from no detectable interaction to high potentiation. The amikacin-fosfomycin (5:2) combination reduced the amikacin concentration required to inhibit all 62 isolates from >1,024 to ≤ 256 μg/ml and reduced the required fosfomycin concentration from 204.8 to 102.4 μg/ml. These results support continued development of the amikacin-fosfomycin combination for aerosolized administration, where high drug levels can be achieved.
5‐FLUOROURACIL: A PHARMACOLOGICAL PARADIGM IN THE USE OF CYTOTOXICS (1998)

1. Painstaking progress in drug development is well illustrated by 5-fluorouracil (5FU), originally designed 40 years ago as a fluorinated analogue of the naturally occurring base uracil. Innovative pharmacokinetic and pharmacodynamic strategies have seen significant clinical improvements for cancer patients over the past decade. 2. 5-Fluorouracil acts by three main mechanisms. Principally, the intermediate metabolite fluorodeoxyuridine monophosphate inhibits a key enzyme in pyrimidine biosynthesis, namely thymidylate synthase (TS). Additionally, 5FU is metabolized to ribo- and deoxy-ribonucleotides, which act as false bases for incorporation into RNA and DNA. 3. Biomodulation of 5FU has been attempted with methotrexate (MTX), folinic acid, interferons, cisplatin and radiotherapy. Methotrexate augments the actions of 5FU by inhibiting dihydrofolate reductase and decreasing the folate pool required for pyrimidine biosynthesis, inhibiting TS via MTX-polyglutamate and directly inhibiting purine biosynthesis. Interferons increase steady state concentrations of 5FU. 5-Fluorouracil enhances the cytotoxicity of cisplatin and radiotherapy by inhibiting DNA repair. Folinic acid enhances TS inhibition by increasing the intracellular pool of folates that stabilize the 5FU-TS complex. 4. 5-Fluorouracil has a short plasma half-life. Thymidylate synthase inhibition is limited to the S-phase of the cell cycle and only a small fraction of most cancer cells are in S-phase at any one time. Increased response rates seen with infusional protocols may reflect the effective recruitment of additional mechanisms of cytotoxicity, not dependent on cell cycle, including effects on RNA synthesis. 5. Patients with localized metastatic disease may benefit from locoregional treatments. These include hepatic intra-arterial therapy with related compounds, such as floxuridine, which reach high concentrations at sites of tumour, while systemic toxicities are minimized by efficient hepatic clearance. 6. Recent developments include orally bioavailable formulations, such as ftorafur, capecitabine and the combination of 5FU with the dihydropyrimidine phosphate dehydrogenase inhibitor ethynyluracil. Recognition of diurnal variation in the activity of such key enzymes as DPD has led to the administration of 5FU at regulated, variable infusion rates (chronomodulation). These promising pharmacological approaches may further improve clinical outcomes in common cancers.