gebhart/patrepeval huggingface dataset:
<i>C</i><i><sub>2</sub></i>-Symmetric Copper(II) Complexes as Chiral Lewis Acids. Catalytic Enantioselective Carbonyl−Ene Reactions with Glyoxylate and Pyruvate Esters (2000)

The C2-symmetric complexes [Cu(S,S)-tert-butylbis(oxazolinyl)](SbF6)2 (2a), its bis(aquo) counterpart [Cu(S,S)-tert-butylbis(oxazolinyl)(H2O)2](SbF6)2 (4), and [Cu(S,S)-phenylbis(oxazolinyl)](OTf)2 (1c) have been shown to catalyze the enantioselective ene reaction between glyoxylate esters and various olefins. Monosubstituted, disubstituted, and trisubstituted olefins each react with ethyl glyoxylate in the presence of 0.2−10 mol % of catalysts 1, 2, and 4 to afford the ene products in good yield and enantioselectivity. Complex 2a has also been shown to catalyze the addition of 1,1-disubstituted olefins to methyl pyruvate in good yields (76−95%) and excellent enantioselectivies (≥98% ee). The synthetic utility of the glyoxylate−ene reaction was demonstrated by conversion of the resulting α-hydroxy ester into the corresponding methyl ester, free acid, Weinreb amide, and α-azido ester, all with no detectable racemization.
Thermodynamic studies of the reversible association of Escherichia coli ribosomal subunits (1977)

The kinetics of association of Escherichia coli 30S and 50S ribosomal subunits have been carried out as a function of temperature after a magnesium jump from 1.5 to 3 mM. Turbidimetric recordings combined with a stopped-flow apparatus were used to follow the kinetics. The data show that the rates of formation and dissociation of the 70S particles at 3 mM Mg2+ and +25 degrees C were, respectively: k2 = 10(5) M-1 s-1, k1 = 4,5 X 10(-3) s-1; lowering the temperature decreases the rate constants with activation energies equal to E2 = 7.5 kcal/mol, E1 = 26.5 kcal/mol and enhances the association equilibrium towards the 70S species with an enthalpy change (delta H degrees assoc = -19.9 kcal/mol) dominant over the entropy change (delta S degrees assoc = -33 cal/(deg mol)). These thermodynamic parameters were compared to those obtained from studies on the interactions of codon-anticodon in yeast phenylalanine transfer RNA as well as of ribooligonucleotides. The kinetic and thermodynamic data are shown to be consistent with 16S-23S RNA interaction.
Mitigating error propagation of MMSE-DFE by joint parameter optimization (2009)

A joint optimization of the decision feedback equalizer (DFE) filter weights and an erasure slicer is proposed in this letter. The feedback weights of the DFE are constrained with an accurate mean square error (MSE) model as the criterion. An erasure slicer is adopted to further decrease error propagation. Two consecutive 1-D optimizations are shown as good as that of a single 2-D optimization. Simulation results verify the performance improvements of the proposed scheme.
Adjuvant therapy for colorectal cancer: yesterday, today, and tomorrow. (2006)

During the 1980s, the only drug routinely used to treat colorectal carcinoma was single-agent fluorouracil (5-FU), a drug that had shown no proven benefit in the adjuvant setting. Since then, significant improvements in the overall management of colorectal cancer have been made. This review will compare today's standard of care for adjuvant colorectal carcinoma to that practiced 20 years ago. The authors examine key questions asked about adjuvant therapy and the answers that ultimately changed clinical practice standards and improved overall survival for patients diagnosed with this disease. In addition, this review explores whether 5-FU should be given as part of a multidrug regimen and which route of administration is best when this drug is given. Further, the authors delve into both the use of locally directed therapies to the liver or peritoneum to improve outcomes and the selection of patients to receive adjuvant chemotherapy. Finally, a look to the future shows monoclonal antibodies to be an avenue of great promise infighting colorectal cancer.
COLD HARDINESS IN THE TWO‐SPOTTED SPIDER MITE (<i>TETRANYCHUS URTICAE</i> KOCH) (1965)

The effect of temperatures below 0° C on different stages of the two‐spotted spider mite, and in particular on active adult females, has been investigated. Survival of active females at —5° was higher at approximately 100% relative humidity than at a lower degree of humidity. Higher rates of survival were also caused by acclimation of active females and larvae for one day at +5° before storage at —15°. No differences in cold‐hardiness were found in active females from an organophosphorous resistant strain and a susceptible strain, and the ability to survive depended on the time‐temperature exposures (see Fig. 3). Eggs were killed very rapidly at —15° C, while larvae survived longer exposures than active females. Compared at the LT 30 level females in diapause survived three times the exposure endured by acclimated active females. Supercooling points measured at a rate of cooling of 2° C per minute were highest in diapausing females and lowest in eggs. Acclimation had no effect on the supercooling points of active females. All stages were killed by freezing. It seems likely that the difference in survival between acclimated and not acclimated active females at —15° is caused by different ability to live in a supercooled state. ZUSAMMENFASSUNG KÄLTERESISTENZ BEI DER BOHNENSPINNMILBE (TETRANYCHUS URTICAE KOCH ) Es wurde die Wirkung von Temperaturen unter 0° auf verschiedene Stadien der Bohnenspinnmilbe, insbesondere auf aktive erwachsene Weibchen untersucht. Die Überlebensrate aktiver Weibchen war bei nahezu hundertprozentiger relativer Luftfeuchtigkeit höher als bei niederer Feuchtigkeit. Höhere Überlebensraten wurden auch durch Akklimatisation aktiver Weibchen und Larven für einen Tag bei 5° vor der Behandlung mit —15° erreicht. Es wurden keine Unterschiede in der Kältewiderstandfähigkeit aktiver Weibchen eines phosphorsäureesterresistenten und eines anfälligen Stammes gefunden. Die Überlebensfähigkeit hängt von Dauer und Temperatur der Einwirkung ab. Eier wurden von —15° sehr schnell abgetötet, während Larven längere Einwirkungszeiten überlebten als aktive Weibchen. Bei einem Vergleich der LT 50 überlebten diapausierende Weibchen dreimal längere Einwirkungszeiten, als sie von akklimatisierten aktiven Weibchen ertragen wurden. Unterkühlungspunkte — gemessen bei einer Abkühlungsrate von 2° pro Minute — lagen bei diapausierenden Weibchen am höchsten und bei Eiern am niedrigsten. Akklimatisierung hatte keinen Einfluß auf die Unterkühlungspunkte aktiver Weibchen. Durch Gefrieren wurden alle Stadien getötet. Es erscheint möglich, daß der Unterschied im Überleben akklimatisierter und nichtakklimatisierter Weibchen bei —15° durch die verschiedene Fähigkeit bedingt ist, in einem unterkühlten Zustande zu leben.
Formation of α-chiral centers by asymmetric β-C(sp <sup>3</sup> )–H arylation, alkenylation, and alkynylation (2017)

The enzymatic β-C-H hydroxylation of the feedstock chemical isobutyric acid has enabled the asymmetric synthesis of a wide variety of polyketides. The analogous transition metal-catalyzed enantioselective β-C-H functionalization of isobutyric acid-derived substrates should provide a versatile method for constructing useful building blocks with enantioenriched α-chiral centers from this abundant C-4 skeleton. However, the desymmetrization of ubiquitous isopropyl moieties by organometallic catalysts has remained an unanswered challenge. Herein, we report the design of chiral mono-protected aminomethyl oxazoline ligands that enable desymmetrization of isopropyl groups via palladium insertion into the C(sp<sup>3</sup>)-H bonds of one of the prochiral methyl groups. We detail the enantioselective β-arylation, -alkenylation, and -alkynylation of isobutyric acid/2-aminoisobutyric acid derivatives, which may serve as a platform for the construction of α-chiral centers.
Kidney Side Population Reveals Multilineage Potential and Renal Functional Capacity but also Cellular Heterogeneity (2006)

Side population (SP) cells in the adult kidney are proposed to represent a progenitor population. However, the size, origin, phenotype, and potential of the kidney SP has been controversial. In this study, the SP fraction of embryonic and adult kidneys represented 0.1 to 0.2% of the total viable cell population. The immunophenotype and the expression profile of kidney SP cells was distinct from that of bone marrow SP cells, suggesting that they are a resident nonhematopoietic cell population. Affymetrix expression profiling implicated a role for Notch signaling in kidney SP cells and was used to identify markers of kidney SP. Localization by in situ hybridization confirmed a primarily proximal tubule location, supporting the existence of a tubular "niche," but also revealed considerable heterogeneity, including the presence of renal macrophages. Adult kidney SP cells demonstrated multilineage differentiation in vitro, whereas microinjection into mouse metanephroi showed that SP cells had a 3.5- to 13-fold greater potential to contribute to developing kidney than non-SP main population cells. However, although reintroduction of SP cells into an Adriamycin-nephropathy model reduced albuminuria:creatinine ratios, this was without significant tubular integration, suggesting a humoral role for SP cells in renal repair. The heterogeneity of the renal SP highlights the need for further fractionation to distinguish the cellular subpopulations that are responsible for the observed multilineage capacity and transdifferentiative and humoral activities.
Contributions of cochlea-scaled entropy and consonant-vowel boundaries to prediction of speech intelligibility in noise (2012)

Recent evidence suggests that spectral change, as measured by cochlea-scaled entropy (CSE), predicts speech intelligibility better than the information carried by vowels or consonants in sentences. Motivated by this finding, the present study investigates whether intelligibility indices implemented to include segments marked with significant spectral change better predict speech intelligibility in noise than measures that include all phonetic segments paying no attention to vowels/consonants or spectral change. The prediction of two intelligibility measures [normalized covariance measure (NCM), coherence-based speech intelligibility index (CSII)] is investigated using three sentence-segmentation methods: relative root-mean-square (RMS) levels, CSE, and traditional phonetic segmentation of obstruents and sonorants. While the CSE method makes no distinction between spectral changes occurring within vowels/consonants, the RMS-level segmentation method places more emphasis on the vowel-consonant boundaries wherein the spectral change is often most prominent, and perhaps most robust, in the presence of noise. Higher correlation with intelligibility scores was obtained when including sentence segments containing a large number of consonant-vowel boundaries than when including segments with highest entropy or segments based on obstruent/sonorant classification. These data suggest that in the context of intelligibility measures the type of spectral change captured by the measure is important.
Synthesis and Biological Evaluation of Biotinyl Hydrazone Derivatives of Muramyl Peptides (2011)

Muramyl peptides derived from bacterial peptidoglycan have long been known for their ability to trigger host innate immune responses, including inflammation and antimicrobial defense. Muramyl peptides have also been widely studied for their role as immune adjuvants. In mammals, the nucleotide-binding oligomerization domain (Nod) proteins Nod1 and Nod2 detect distinct muramyl peptide structures and mediate their biological activity. Because of the poor immunogenicity of these small peptidoglycan derivatives, research in this field is currently limited by the lack of reagents to track or immobilize specific muramyl peptides. We present here the generation and initial biological characterization of synthetic muramyl peptides covalently coupled to dansyl or biotinyl derivatives and demonstrate that biotinyl coupling on the muramyl moiety results in derivatives that can be tracked by immunofluorescence and maintain full biological activity, as observed by their capacity to trigger Nod signaling. Moreover, using digitonin-mediated permeabilization techniques on live cells, we also demonstrate that biotinylated muramyl peptides efficiently reach the host cytosol, where they activate Nod signaling. Therefore, these derivatives represent useful probes to study the cell biology and the biochemistry of host responses to muramyl peptides.
Mouse Protocadherin-1 Gene Expression Is Regulated by Cigarette Smoke Exposure In Vivo (2014)

Protocadherin-1 (PCDH1) is a novel susceptibility gene for airway hyperresponsiveness, first identified in families exposed to cigarette smoke and is expressed in bronchial epithelial cells. Here, we asked how mouse Pcdh1 expression is regulated in lung structural cells in vivo under physiological conditions, and in both short-term cigarette smoke exposure models characterized by airway inflammation and hyperresponsiveness and chronic cigarette smoke exposure models. Pcdh1 gene-structure was investigated by Rapid Amplification of cDNA Ends. Pcdh1 mRNA and protein expression was investigated by qRT-PCR, western blotting using isoform-specific antibodies. We observed 87% conservation of the Pcdh1 nucleotide sequence, and 96% conservation of the Pcdh1 protein sequence between men and mice. We identified a novel Pcdh1 isoform encoding only the intracellular signalling motifs. Cigarette smoke exposure for 4 consecutive days markedly reduced Pcdh1 mRNA expression in lung tissue (3 to 4-fold), while neutrophilia and airway hyperresponsiveness was induced. Moreover, Pcdh1 mRNA expression in lung tissue was reduced already 6 hours after an acute cigarette-smoke exposure in mice. Chronic exposure to cigarette smoke induced loss of Pcdh1 protein in lung tissue after 2 months, while Pcdh1 protein levels were no longer reduced after 9 months of cigarette smoke exposure. We conclude that Pcdh1 is highly homologous to human PCDH1, encodes two transmembrane proteins and one intracellular protein, and is regulated by cigarette smoke exposure in vivo.
A framework and methodology for development of content-based Web sites (2003)

A Web site is a new broadly used information medium and application platform. One of the features of a Web site is that it is in an endless development cycle. Maintenance and updating happen during a site's life cycle. The structure and content of a Web site are always being extended and modified. Some tools are designed to support maintenance work for the development of a Web site. We believe that the maintenance of a Web site should be considered in the design phase. In this paper, we discuss a component-based approach to design and maintenance of a Web site. Using this approach, the workload of future maintenance can be reduced.
Neutrophil Elastase Potentiates Cathepsin G-lnduced Platelet Activation (1992)

Summary We have previously demonstrated that human neutrophil cathepsin G is a strong platelet agonist that binds to a specific receptor. This work describes the effect of neutrophil elastase on cathepsin G-induced platelet responses. While platelets were not activated by high concentrations of neutrophil elastase by itself, elastase enhanced aggregation, secretion and calcium mobilization induced by low concentrations of cathepsin G. Platelet aggregation and secretion were potentiated in a concentration-dependent manner by neutrophil elastase with maximal responses observable at 200 nM. Enhancement was observed when elastase was preincubated with platelets for time intervals of 10–60 s prior to addition of a low concentration of cathepsin G and required catalytically-active elastase since phenylmethanesulphonyl fluoride-inhibited enzyme failed to potentiate cell activation. Neutrophil elastase potentiation of platelet responses induced by low concentrations of cathepsin G was markedly inhibited by creatine phosphate/creatine phosphokinase and/or indomethacin, indicating that the synergism between elastase and cathepsin G required the participation of ADP and thromboxane A2. On the other hand, platelet responses were not attenuated by the PAF antagonist BN 52021, signifying that PAF-acether did not play a role in elastase potentiation. At higher concentrations porcine pancreatic elastase exhibits similar effects to neutrophil elastase, demonstrating that the effect of elastase was not unique to the neutrophil protease. While neutrophil elastase failed to alter the ability of cathepsin G to hydrolyze a synthetic chromogenic substrate, preincubation of platelets with elastase increased the apparent affinity of cathepsin G binding to platelets. In contrast to their effect on cathepsin G-induced platelet responses, neither neutrophil nor pancreatic elasatse potentiated aggregation or dense granule release initiated by ADP, PAF-acether, arachidonic acid or U46619, a thromboxane A2 mimetic. Moreover, unlike its effect on cathepsin G, neutrophil elastase inhibited thrombin-induced responses. The current observations demonstrate that elastase can potentiate platelet responses mediated by low concentrations of cathepsin G, suggesting that both enzymes may function synergistically to activate platelets under conditions where neutrophil degranulation occurs.
A New Acid-Base Nomogram an Improved Method for the Calculation of the Relevant Blood Acid-Base Data (1960)

(1960). A New Acid-Base Nomogram an Improved Method for the Calculation of the Relevant Blood Acid-Base Data. Scandinavian Journal of Clinical and Laboratory Investigation: Vol. 12, No. 2, pp. 177-186.
Relation of cerebral infarctions to dementia and cognitive function in older persons (2003)

Cerebral infarctions are associated with a twofold increase in odds of dementia. Odds are higher in persons with multiple, large, or clinically evident infarctions. In addition, cerebral infarctions do not affect all cognitive systems equally, showing the strongest association with perceptual speed and the weakest with episodic memory.
Rapid Androgen Actions on Calcium Signaling in Rat Sertoli Cells and Two Human Prostatic Cell Lines: Similar Biphasic Responses Between 1 Picomolar and 100 Nanomolar Concentrations1 (2000)

Androgen-induced calcium fluxes and gap junctional intercellular communication (GJIC) were studied in three different cell types. A transient (2-3 min duration) increase in intracellular calcium levels was observed within 20-30 sec of androgen addition, which was followed by a plateau phase with steroid concentrations higher than 1 nM. The kinetics of the calcium responses were similar in immature rat Sertoli cells, which contain normal nuclear receptors; the human prostatic tumor cell line, LNCaP, which contains a mutated nuclear receptor; and the human prostatic cell line, PC3, which does not contain a nuclear receptor. The human A431 tumor cell line did not respond to androgens. Concentrations of testosterone and the synthetic androgen, R1881, between 1-1000 pM induced transient calcium increases with ED(50) values near 1 pM and 1 nM, whereas dihydrotestosterone (DHT) was not active at these concentrations. At concentrations higher than 1 nM, testosterone, R1881, and DHT were equipotent in stimulating an increase in calcium that lasted for more than 10 min, with ED(50) values between 5 and 20 nM. Testosterone covalently bound to albumin was also active, whereas 11 related androstane compounds as well as progesterone and estradiol-17beta were inactive at 1000 nM. The calcium response induced by the three androgens (10 nM) was abolished in all cell types by hydroxyflutamide (1000 nM) and finasteride (1000 nM), but not by cyproterone acetate (1000 nM). The calcium response was also abolished in the absence of extracellular calcium and strongly inhibited by the presence of verapamil. Exposure of the responsive cells to brief (150-sec) pulses of androgens generated calcium responses that were similar to those after continuous exposure. After exposure of Sertoli cells for only 30 sec to 100 nM testosterone, the calcium response lasted for at least 50 min. Although nuclear binding of androgens could be demonstrated, there was no evidence for tight binding to the plasma membrane under similar conditions. When protein synthesis was inhibited, an enhancement of GJIC between rat Sertoli cells, but not between LNCaP cells or PC3 cells, was observed within 15 min of the addition of 10 nM testosterone. Because nuclear androgens are not present in PC3 cells and many functional properties of the responsive system are different from the nuclear receptor in all three cell types, we postulate the existence of an alternative cell surface receptor system with biphasic response characteristics (high and low affinity). The calcium signals are probably coupled to the regulation of gap junctional efficiency between Sertoli cells. The low-affinity receptors may convey complementary androgen signals at elevated local levels such as in the testis, when nuclear receptors are (over)saturated.
Dynamic bandwidth management and adaptive applications for a variable bandwidth wireless environment (2001)

This article describes an approach for providing dynamic quality of service (QoS) support in a variable bandwidth network, which may include wireless links and mobile nodes. The dynamic QoS approach centers on the notion of providing QoS support at some point within a range requested by applications. To utilize dynamic QoS, applications must be capable of adapting to the level of QoS provided by the network, which may vary during the course of a connection. To demonstrate and evaluate the dynamic QoS concept, we have implemented a new protocol called dynamic resource reservation protocol (dRSVP) and a new QoS application program interface (API). The paper describes this new protocol and API and also discusses our experience with adaptive streaming video and audio applications that work with the new protocol in a testbed network, including wireless local area network connectivity and wireless link connectivity emulated over the wired Ethernet. Qualitative and quantitative assessments of the dynamic RSVP protocol are provided.
Atypical antipsychotics in the treatment of schizophrenia (2003)

Over the last few years atypical antipsychotics have been used increasingly in the pharmacological treatment of schizophrenia. This review provides an overview of the pharmacological and clinical characteristics of atypical antipsychotics. In particular we discuss their efficacy in treating psychotic and negative symptoms as well as treatment-refractory patients. The most important side effects as well as their possible interactions are reviewed in detail. Recommendations for the clinical use are given.