gebhart/patrepeval huggingface dataset:
Substituent Effects on Oxidation‐Induced Formation of Quinone Methides from Arylboronic Ester Precursors (2013)

A series of arylboronic esters containing different aromatic substituents and various benzylic leaving groups (Br or N(+)Me3Br(-)) have been synthesized. The substituent effects on their reactivity with H2O2 and formation of quinone methide (QM) have been investigated. NMR spectroscopy and ethyl vinyl ether (EVE) trapping experiments were used to determine the reaction mechanism and QM formation, respectively. QMs were not generated during oxidative cleavage of the boronic esters but by subsequent transformation of the phenol products under physiological conditions. The oxidative deboronation is facilitated by electron-withdrawing substituents, such as aromatic F, NO2, or benzylic N(+)Me3Br(-), whereas electron-donating substituents or a better leaving group favor QM generation. Compounds containing an aromatic CH3 or OMe group, or a good leaving group (Br), efficiently generate QMs under physiological conditions. Finally, a quantitative relationship between the structure and activity has been established for the arylboronic esters by using a Hammett plot. The reactivity of the arylboronic acids/esters and the inhibition or facilitation of QM formation can now be predictably adjusted. This adjustment is important as some applications may benefit and others may be limited by QM generation.
Structural Gender Dimorphism and the Biomechanics of the Gluteal Subcutaneous Tissue: Implications for the Pathophysiology of Cellulite (2019)

The interplay of dermal support, septal morphology, and underlying fat architecture contributes to the biomechanical properties of the subdermal junction. This is influenced by sex, age, and body mass index. Cellulite can be understood as an imbalance between containment and extrusion forces at the subdermal junction; aged women with high body mass index have the greatest risk of developing (or worsening of) cellulite.
Seer: Leveraging Big Data to Navigate the Increasing Complexity of Cloud Debugging (2018)

Performance unpredictability in cloud services leads to poor user experience, degraded availability, and has revenue ramifications. Detecting performance degradation a posteriori helps the system take corrective action, but does not avoid the QoS violations. Detecting QoS violations after the fact is even more detrimental when a service consists of hundreds of thousands of loosely-coupled microservices, since performance hiccups can quickly propagate across the dependency graph of microservices. In this work we focus on anticipating QoS violations in cloud settings to mitigate performance unpredictability to begin with. We propose Seer, a cloud runtime that leverages the massive amount of tracing data cloud systems collect over time and a set of practical learning techniques to signal upcoming QoS violations, as well as identify the microservice(s) causing them. Once an imminent QoS violation is detected Seer uses machine-level hardware events to determine the cause of the QoS violation, and adjusts the resource allocations to prevent it. In local clusters with 10 40-core servers and 200-instance clusters on GCE running diverse cloud microservices, we show that Seer correctly anticipates QoS violations 91% of the time, and attributes the violation to the correct microservice in 89% of cases. Finally, Seer detects QoS violations early enough for a corrective action to almost always be applied successfully.
Pyrazolo[4,3‐e]1,2,4‐triazolo[1,5‐c]pyrimidine derivatives: A new pharmacological tool for the characterization of the human A<sub>3</sub> adenosine receptor (2001)

Abstract Adenosine regulates many physiological functions by interaction with four different G‐protein‐coupled receptors classified as A 1 , A 2A , A 2B , and A 3 . While adenosine A 1 and A 2A receptor subtypes have been pharmacologically characterized through the use of selective ligands, the A 2B and A 3 adenosine receptor subtypes are presently under study in order to better understand their physio‐pathological functions. In particular, activation of adenosine A 3 receptors has been shown to stimulate phospholipase C and D and to inhibit adenylate cyclase. Activation of A 3 adenosine receptors also causes the release of inflammatory mediators such as histamine from mast cells, which are responsible for processes such as inflammation and hypotension. For these reasons, it has been suggested that A 3 adenosine receptor antagonists can be considered potential drugs for the treatment of asthma and inflammation. In the last few years different classes of heterocyclic compounds have been identified as A 3 adenosine antagonists, but none of the tested compounds showed significant selectivity for A 3 adenosine receptor subtype. Herein, we report our recent results on a class of pyrazolo[4,3‐e]1,2,4‐triazolo[1,5‐c]pyrimidine derivatives as a new class of potent and selective human A 3 adenosine receptor antagonists. The full characterization of the first high‐affinity radioligand antagonist for this receptor subtype, designated [ 3 H] MRE3008F20, is briefly summarized. Drug Dev. Res. 52:406–415, 2001. © 2001 Wiley‐Liss, Inc.
Channel Estimation Algorithm Based on IEEE802.11a Standard for MIMO-OFDM Systems (2008)

For the channel estimation of MIMO-OFDM(multiple-input multiple-output-orthogonal frequency division multiplexing) systems based on IEEE 802.11a standard,a least square(LS) channel estimation scheme is proposed in time domain.The idea of this scheme is mainly to estimate the time-domain channel responses between transmitting and receiving antennas in accordance to the time-domain signals between transmitting and receiving ends.To make sure that the mean square error(MSE) is minimum in the LS channel estimation,an optimal scheme of pilot sequence is put forward,which requires less training symbols than conventional schemes and the number of those symbols will not increase with the increasing number of antennas.Moreover,the number of transmitting antennas is unlimited.In the scheme proposed all the pilot tones are required to be equipowered and the phase shift should be mutually orthogonal among the pilot sequences of different transmitting antennas.Simulation results show the effectiveness of the scheme proposed.
Recognition of the Lck tyrosine kinase as a tumor antigen by cytotoxic T lymphocytes of cancer patients with distant metastases (2001)

The Lck protein (p56(lck)), a src family tyrosine kinase that is essential for T cell development and function, is aberrantly expressed in metastatic colon cancers. p56(lck) seems to facilitate the malignant transformation of epithelial cells through initiation of anchorage-independent proliferation. We demonstrate that the lck gene encodes antigenic epitopes recognized by the HLA class I-restricted and tumor-specific CTL of metastatic cancer patients. Lck peptides augmented CTL activity in peripheral blood mononuclear cells (PBMC) of colon and other epithelial cancer patients with distant metastases, but not those without distant metastases. CTL precursors recognizing the Lck peptide were identified in freshly prepared PBMC of patients with distant metastases, and their frequency was significantly augmented by stimulation with the peptide. Thus, Lck peptides could be useful in developing a specific immunotherapy for cancer patients with distant metastases.
Selective 5‐<i>exo‐dig</i> Cyclization of <i>in Situ</i> Synthesized <i>N</i>‐Boc‐2‐aminophenyl Ethoxyethynyl Carbenols: Synthesis of Multifunctional Indoles and Their Derivatives (2014)

Abstract A method to prepare 3‐substituted‐2‐formylindole derivatives from N ‐Boc‐ ortho ‐aminoaryl ketones and ethoxyacetylene through a cascade of reactions in a single operation that included a nucleophile‐triggered 5‐ exo‐dig cyclization and an acid‐mediated 1,3‐allyl alcohol isomerization (1,3‐AAI) is described. A variety of aryl, vinyl and alkynyl groups can be introduced at C‐3 of indole‐2‐carboxaldehyde while having a high functional group compatibility. The 3‐alkynyl adducts, which are highly valuable substrates for diversity‐oriented synthesis, can be further transformed to useful carboline and carbazole derivatives through novel pathways. magnified image
Animal models in tuberculosis research – where is the beef? (2015)

Animal models are needed for TB research and provide valuable information on the mechanisms of the disease and on ways of preventing it. However, the data obtained in animal studies need to be carefully interpreted and evaluated before making assumptions concerning humans. With an increasing understanding of disease mechanisms, animal models can be further improved to best serve research goals.
Nuclear lamins: key regulators of nuclear structure and activities (2009)

The nuclear lamina is a proteinaceous structure located underneath the inner nuclear membrane (INM), where it associates with the peripheral chromatin. It contains lamins and lamin-associated proteins, including many integral proteins of the INM, chromatin modifying proteins, transcriptional repressors and structural proteins. A fraction of lamins is also present in the nucleoplasm, where it forms stable complexes and is associated with specific nucleoplasmic proteins. The lamins and their associated proteins are required for most nuclear activities, mitosis and for linking the nucleoplasm to all major cytoskeletal networks in the cytoplasm. Mutations in nuclear lamins and their associated proteins cause about 20 different diseases that are collectively called laminopathies'. This review concentrates mainly on lamins, their structure and their roles in DNA replication, chromatin organization, adult stem cell differentiation, aging, tumorogenesis and the lamin mutations leading to laminopathic diseases.
OneBusAway (2010)

Public transit systems play an important role in combating traffic congestion, reducing carbon emissions, and promoting compact, sustainable urban communities. The usability of public transit can be significantly enhanced by providing good traveler information systems. We describe OneBusAway, a set of transit tools focused on providing real-time arrival information for Seattle-area bus riders. We then present results from a survey of OneBusAway users that show a set of important positive outcomes: strongly increased overall satisfaction with public transit, decreased waiting time, increased transit trips per week, increased feelings of safety, and even a health benefit in terms of increased distance walked when using transit. Finally, we discuss the design and policy implications of these results and plans for future research in this area.
Study on Home-made New Tight-lock Coupler for the City Truck Traffic (2003)

This paper introduced the type,structure,function,and theory of the new tight-lock coupler applying to city track traffic.And it also discussed the key technology and test,such as intensity,kinematics analysis,and manufacture technics.
Dendrimers as non-viral vectors for siRNA delivery (2011)

There is a tremendous interest in moving siRNA therapeutics into a clinical setting for the treatment of various diseases. This in itself however depends largely on the availability of safe and efficient siRNA delivery systems. In this context, dendrimers have attracted considerable attention as siRNA vectors due to their well-defined structures and multivalent features. The present review offers a brief overview of the current status of dendrimers as siRNA delivery vectors, focusing on the different dendrimers investigated for their siRNA delivery ability and the related structural alterations employed to improve their safety and efficiency for this purpose.
Amphetamine-Induced Place Preference and Conditioned Motor Sensitization Requires Activation of Tyrosine Kinase Receptors in the Hippocampus (2006)

The environmental context in which abused drugs are taken contribute to the drug experience and is a powerful and persistent stimulus to elicit memories of that experience even in the abstinent addict. Using amphetamine (AMPH) as the unconditioned stimulus, the present study compared two popular context-dependent paradigms in rats, conditioned motor sensitization (CMS) and conditioned place preference (CPP), to ascertain whether particular brain regions were differentially involved. The neuronal substrates underlying these context-dependent behaviors are poorly understood, but regulators of the neuronal plasticity that accompany learning, such as neurotrophic factors and their cognate tyrosine kinase receptors (e.g., TrkB), are credible candidates. We found a significant elevation of TrkB-like immunoreactivity specifically in CA3/dentate gyrus (DG) subregions of the hippocampus after AMPH (0.3 mg/kg)-induced CPP, but not in the delayed-paired (control) AMPH condition. A higher AMPH dose (1.0 mg/kg) induced both CPP and CMS and elevated TrkB in the CA3/DG as well as in the nucleus accumbens shell. The development of both conditioned behaviors was blocked by intra-CA3/DG infusion of the Trk inhibitor K-252a. These findings reveal that CPP and CMS are induced by different doses of AMPH and are associated with TrkB changes in particular brain regions. Moreover, Trk receptors in the hippocampus are critical mediators of the neuronal changes necessary for inducing both forms of conditioning. Thus, although these two conditioning models are distinct, because they are commonly regulated by the hippocampal Trk system, these receptors may be a therapeutic target for attenuating the significance of contextual cues that otherwise strengthen the addictive properties of abused drugs.
A Light-Inactivated Antibiotic (1999)

Sodium 7beta-[(R)-2-(N(b)()-o-nitrobenzyloxycarbonyl)hydrazino-3-pheny lpropa namido]cephalosporanate (1) is described as a new type of beta-lactam antibiotic, which undergoes light-induced destruction of its beta-lactam moiety and hence becomes biologically inactive. This type of antibiotic holds the promise of self-destruction over a number of hours of exposure to light, so that it would not allow selection of resistance in the environment.
Single Mode Air-Clad Single Crystal Sapphire Optical Fiber (2017)

The observation of single mode propagation in an air-clad single crystal sapphire optical fiber at wavelengths at and above 783 nm is presented for the first time. A high-temperature wet acid etching method was used to reduce the diameter of a 10 cm length of commercially-sourced sapphire fiber from 125 micrometers to 6.5 micrometers, and far-field imaging provided modal information at intervals as the fiber diameter decreased. Modal volume was shown to decrease with decreasing diameter, and single mode behavior was observed at the minimum diameter achieved. While weakly-guiding approximations are generally inaccurate for low modal volume optical fiber with high core-cladding refractive index disparity, consistency between these approximations and experimental results was observed when the effective numerical aperture was measured and substituted for the theoretical numerical aperture in weakly-guiding approximation calculations. With the demonstration of very low modal volume in sapphire at fiber diameters much larger than anticipated by legacy calculations, the resolution of sapphire fiber distributed sensors may be increased and other sensing schemes requiring very low modal volume, such as fiber Bragg gratings, may be realized in extreme environment applications.
GaN HEMT and MOS monolithic integration on silicon substrates (2011)

Abstract A process for monolithically integrating MOS and AlGaN/GaN HFETs has been developed using a windowed epitaxy technique. AlGaN/GaN HFET devices display a forward current greater than 0.8 A/mm and a break‐down voltage larger than 200 V. Field‐plated devices have also been demonstrated. Enclosed MOS devices based on a 900 °C thermal oxide have been produced showing promising characteristics. (© 2011 WILEY‐VCH Verlag GmbH & Co. KGaA, Weinheim)
Thermodynamic properties and molar heat capacity of Er-2(Asp)(2)(Im)(8)(ClO4)(6)center dot 10H(2)O (2011)

A complex of erbium perchloric acid coordinated with l-aspartic acid and imidazole, er-2(asp)(2)(im)(8)(clo4)(6)center dot 10h(2)o was synthesized for the first time. it was characterized by ir and elements analysis. the heat capacity and thermodynamic properties of the complex were studied with an adiabatic calorimeter (ac) from 80 to 390 k and differential scanning calorimetry (dsc) from 100 to 300 k. glass transition and phase transition were discovered at 220.45 and 246.15 k, respectively. the glass transition was interpreted as a freezing-in phenomenon of the reorientational motion of clo4- ions and the phase transition was attributed to the orientational order/disorder process of clo4- ions. the thermodynamic functions [h (t) - h (298.15)] and [s (t) - s (298.15)] were derived in the temperature range from 80 to 390 k with temperature interval of 5 k. thermal decomposition behavior of the complex in nitrogen atmosphere was studied by thermogravimetric (tg) analysis and differential scanning calorimetry (dsc).
Conversion of α-Aminoadipic Acid to L-Pipecolic Acid by Aspergillus nidulans<sup>*</sup> (1962)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTConversion of α-Aminoadipic Acid to L-Pipecolic Acid by Aspergillus nidulans*Anita J. Aspen and Alton MeisterCite this: Biochemistry 1962, 1, 4, 606–612Publication Date (Print):July 1, 1962Publication History Published online1 May 2002Published inissue 1 July 1962https://pubs.acs.org/doi/10.1021/bi00910a010https://doi.org/10.1021/bi00910a010research-articleACS PublicationsRequest reuse permissionsArticle Views128Altmetric-Citations22LEARN 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
Collective Loops – Multimodal Interactions Through Co-located Mobile Devices and Synchronized Audiovisual Rendering Based on Web Standards (2017)

International audience
Association of Genome-Wide Variation With the Risk of Incident Heart Failure in Adults of European and African Ancestry (2010)

We identified 2 loci that were associated with incident HF and exceeded genome-wide significance. The findings merit replication in other community-based settings of incident HF.
ChemInform Abstract: An Enantio‐ and Stereocontrolled Synthesis of (‐)‐Mycestericin E via Cinchona Alkaloid Catalyzed Asymmetric Baylis—Hillman Reaction. (2002)

Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.
Hydrogenolysis of Higher Fatty Ester to Higher Alcohol using Fe-based Catalyst (1968)

The anthers previously reported that Fe-Cu-O catalyst had high activity to catalytic hydrogenolysis of higher fatty ester to higher alcohol. After that, it was found that Fe-Cu-AI-O catalyst had higher activity when proper amount of Al was contained as third component. Hydrogenolysis of methyl ricinoleate to 1, 12-octadecanediol was studied using the catalyst. The yield was 77%. But when triglyceride was used as raw material, the yield was 50%. Preparation of unsaturated higher alcohol using Fe-Cu-Cd-O, which was prepared newly, was studied, but 65% of unsaturation on the product vanished when 93% of the ester was hydrogenolzyed. From the study of X-ray defraction on these catalysts before and after the reduction, it was recognized that, as to Fe, Fe304 was of active from in the reduction.
Isolation, physicochemical properties, and folding of octopine dehydrogenase from <i>Pecten jacobaeus</i> (1984)

Two types (isoenzymes) of octopine dehydrogenase (A and B) from Pecten jacobaeus adductor muscle were purified to homogeneity, applying affinity chromatography as an efficient final step of purification. Both forms of the enzyme differ in their electrophoretic mobility. All other physico-chemical and enzymatic properties, as well as the folding behaviour were found to be identical. Interconversion of one form into the other was not detectable. Sedimentation equilibrium, gel permeation chromatography, and NaDodSO4/polyacrylamide gel electrophoresis yield a relative molecular mass of 45000 +/- 1500 for both native and denatured enzyme. The unfolding transition at varying guanidine X HCl concentrations is characterized by a two-step profile: at 0.4-0.8 M, partial unfolding is parallelled by inactivation; at 2.0-2.4 M the residual structure is destroyed in a second unfolding step. Beyond 2.8 M no further changes in fluorescence emission and dichroic absorption are observed. At 0.4-1.8 M guanidine X HCl, partial unfolding is superimposed by aggregation. The emission maximum of the intrinsic protein fluorescence at 327 nm is shifted to 352 nm upon denaturation in 6 M guanidine X HCl. Changes in the far-ultraviolet circular dichroism indicate complete loss of the overall backbone structure in this denaturant, including the native helix content of about 33%. Denaturation in 6 M guanidine X HCl, as monitored by the decrease of protein fluorescence, is fast (less than 8s). Upon reactivation after short denaturation, about 25% of the activity is recovered in a fast initial phase (less than 20s). The product of this phase has a similar stability towards destabilizing additives or proteases as the native enzyme. The slow phase of reactivation, which predominates after long-term denaturation, is determined by a single first-order reaction characterized by tau = 29 +/- 3 min (20 degrees C). This reaction must be a relatively late event on the folding pathway, preceded by the fast formation of a structured intermediate, as indicated by the immediate recovery of the native fluorescence. The structural rearrangements, which are rate-limiting for reactivation after long-term denaturation, are characterized by a high energy of activation (112 +/- 8 kJ/mol). The slow reactivation step is compatible in rate with the first-order folding reactions involved in the reconstitution of several oligomeric dehydrogenases [c.f. R. Jaenicke and R. Rudolph (1983) Colloq. Ges. Biol. Chem. Mosbach 34, 62-90].