gebhart/patrepeval huggingface dataset:
Sulfonylthiadiazoles with an Unusual Binding Mode as Partial Dual Peroxisome Proliferator‐Activated Receptor (PPAR) γ/δ Agonists with High Potency and in vivo Efficacy (2011)

Compounds that simultaneously activate the peroxisome proliferator-activated receptor (PPAR) subtypes PPARγ and PPARδ have the potential to effectively target dyslipidemia and type II diabetes in a single pharmaceutically active molecule. The frequently observed side effects of selective PPARγ agonists, such as edema and weight gain, are expected to be overcome by using partial instead of full agonists for this nuclear receptor family. Herein we report the discovery, synthesis, and optimization of a novel series of sulfonylthiadiazoles that are active as partial agonists. The initial compound 6 was discovered by high-throughput screening as a moderate partial PPARδ agonist; its optimization was based on the X-ray crystal structure in complex with PPARδ. In contrast to other PPARδ agonists, this ligand does not interact directly with residues from the activation helix AF-2, which might be linked to its partial agonistic effect. Interestingly, the thiadiazole moiety fills a novel subpocket, which becomes accessible after moderate conformational rearrangement. The optimization was focused on introducing conformational constraints and replacing intramolecular hydrogen bonding interactions. Highly potent molecules with activity as dual partial PPARγ/δ agonists in the low nanomolar range were then identified. One of the most active members, compound 20 a, displayed EC₅₀ values of 1.6 and 336 nM for PPARδ and γ, respectively. The X-ray crystal structure of its complex with PPARδ confirms our design hypothesis. Compound 20 a clearly displayed in vivo activity in two chronic mice studies. Lipids were modified in a beneficial way in normolipidemic mice, and the development of overt diabetes could be prevented in pre-diabetic db/db mice. However, body weight gain was similar to that observed with the PPARγ agonist rosiglitazone. Hence, active compounds from this series can be considered as valuable tools to elucidate the complex roles of dual PPARγ/δ agonists for potential treatment of metabolic syndrome.
Towards dependable data repairing with fixing rules (2014)

research-article Towards dependable data repairing with fixing rules Share on Authors: Jiannan Wang UC Berkeley, Berkeley, CA, USA UC Berkeley, Berkeley, CA, USAView Profile , Nan Tang Qatar Computing Research Institute (QCRI), Doha, Qatar Qatar Computing Research Institute (QCRI), Doha, QatarView Profile Authors Info & Claims SIGMOD '14: Proceedings of the 2014 ACM SIGMOD International Conference on Management of DataJune 2014 Pages 457–468https://doi.org/10.1145/2588555.2610494Online:18 June 2014Publication History 97citation671DownloadsMetricsTotal Citations97Total Downloads671Last 12 Months42Last 6 weeks6 Get Citation AlertsNew Citation Alert added!This alert has been successfully added and will be sent to:You will be notified whenever a record that you have chosen has been cited.To manage your alert preferences, click on the button below.Manage my AlertsNew Citation Alert!Please log in to your account Save to BinderSave to BinderCreate a New BinderNameCancelCreateExport CitationPublisher SiteGet Access
Online detection of unusual events in videos via dynamic sparse coding (2011)

Real-time unusual event detection in video stream has been a difficult challenge due to the lack of sufficient training information, volatility of the definitions for both normality and abnormality, time constraints, and statistical limitation of the fitness of any parametric models. We propose a fully unsupervised dynamic sparse coding approach for detecting unusual events in videos based on online sparse re-constructibility of query signals from an atomically learned event dictionary, which forms a sparse coding bases. Based on an intuition that usual events in a video are more likely to be reconstructible from an event dictionary, whereas unusual events are not, our algorithm employs a principled convex optimization formulation that allows both a sparse reconstruction code, and an online dictionary to be jointly inferred and updated. Our algorithm is completely un-supervised, making no prior assumptions of what unusual events may look like and the settings of the cameras. The fact that the bases dictionary is updated in an online fashion as the algorithm observes more data, avoids any issues with concept drift. Experimental results on hours of real world surveillance video and several Youtube videos show that the proposed algorithm could reliably locate the unusual events in the video sequence, outperforming the current state-of-the-art methods.
Packaged hybrid soliton pulse source results and 270 terabit.km/sec soliton transmission using sliding-frequency guiding filters (2002)

Summary form only given. A fully packaged hybrid soliton pulse source is described. Excellent stability and tuning characteristics are shown. Error free soliton transmission at 10 Gbit/s is achieved over 27,000 km using sliding-frequency guiding filters.
Tradeoffs in Elastographic Imaging (2001)

This paper presents the tradeoffs in elastographic imaging. Elastography is viewed as a new imaging modality and presented in terms of three fundamental concepts that constitute the basis for the elastographic imaging process. These are the tissue elastic deformation process, the statistical analysis of strain estimation and the image characterization. The first concept involves the use of the contrast transfer efficiency (CTE) that describes the mapping of a distribution of local tissue elastic moduli into a distribution of local longitudinal tissue strains. The second concept defines the elastographic system and the relationship between ultrasonic and signal processing parameters. This process is described in terms of a stochastic framework (the strain filter) that provides upper and practical performance bounds and their dependence on the various system parameters. Finally, the output image, the elastogram, is characterized by its image parameters, such as signal-to-noise ratio, contrast-to-noise ratio, dynamic range and resolution. Finite-element simulations are used to generate examples of elastograms that are confirmed by the theoretical prediction tools.
Subjective Analysis of an End-to-end Streaming System (2019)

Measuring Quality of Experience (QoE) and integrating these measurements into video streaming algorithms is a multi-faceted problem that fundamentally requires the design of comprehensive subjective QoE databases and metrics. To achieve this goal, we have recently designed the LIVE-NFLX-II database, a highly-realistic database which contains subjective QoE responses to various design dimensions, such as bitrate adaptation algorithms, network conditions and video content. Our database builds on recent advancements in content-adaptive encoding and incorporates actual network traces to capture realistic network variations on the client device. Using our database, we study the effects of multiple streaming dimensions on user experience and evaluate video quality and quality of experience models. We believe that the tools introduced here will help inspire further progress on the development of perceptuallyoptimized client adaptation and video streaming strategies.
Cascade of Dual LDA opearators for face recognition (2006)

In this paper, we propose a cascade of Dual-LDA (DLDA) operators for Face Recognition. We show that such an approach results in efficient and low-dimensional feature space for face representation with enhanced discriminatory power. Comparative results to classical LDA and cascade of classical LDA algorithms are presented, showing significantly improved performance. A theoretical analysis for Fisher and DLDA is also presented. Experimental evaluation of the proposed FR algorithm, conducted on MPEG test set with over 8000 images of 929 individuals, shows state-of-the-art performance.
Preparation of single crystals of superconducting YBa2Cu3O7−<i>x</i> from CuO melts (1987)

Millimeter size single crystals of superconducting YBa2Cu3O7−x (Tc ∼90 K) were grown by melting a mixture of stoichiometric YBa2Cu3O7−x plus excess CuO at 1150 °C followed by holding at 900 °C for four days. Crystals were in the form of plates with c axis normal to the plate face. Growth of the crystals is believed to be aided by a liquid phase which is present at the holding temperature.
Immunodiagnosis of hepatitis B with high-affinity IgM monoclonal antibodies. (1981)

High-affinity monoclonal IgG and IgM antibodies to hepatitis B surface antigen (HBsAg) have been prepared and their functional capabilities explored by means of solid-phase radioimmunoassays. 125I-labeled HBsAg binding studies indicated that monoclonal IgM antibodies against HBsAg (anti-HBs) coupled to a solid-phase support quantitatively bound more HbsAg at a faster rate than conventionally prepared anti-HBs reagents or other high-affinity IgG monoclonal anti-HBs antibodies. Consequently, IgM anti-HBs was also radiolabeled, and an IgM-IgM radioimmunoassay was developed for the immunodiagnosis of hepatitis B. The lower limit of this assay was approximately 100 pg +/- 30 (SEM) of HBsAg per ml of serum. Compared to available commercial radioassays, preliminary studies have shown the IgM-IgM assay to have increased sensitivity, which improved the detection of a HBsAg-associated determinant in acute hepatitis and post transfusion hepatitis. It is probable that the multivalent interaction between monoclonal IgM anti-HBs and the polydeterminant HBsAg is important in augmenting the performance of this monoclonal assay.
Synthesis of nonreducible bicyclic analogs of somatostatin (1980)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTSynthesis of nonreducible bicyclic analogs of somatostatinRuth F. Nutt, Daniel F. Veber, and Richard SapersteinCite this: J. Am. Chem. Soc. 1980, 102, 21, 6539–6545Publication Date (Print):October 8, 1980Publication History Published online1 May 2002Published inissue 8 October 1980https://pubs.acs.org/doi/10.1021/ja00541a025https://doi.org/10.1021/ja00541a025research-articleACS PublicationsRequest reuse permissionsArticle Views235Altmetric-Citations65LEARN 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
Highly accurate measurement of oxygen using a paramagnetic gas sensor (2006)

The amount fraction of oxygen in oxygen–nitrogen gas mixtures has been measured with a relative uncertainty of ±0.02% within the range 100–1000 mmol mol−1. The method employed uses an auto-null 'dumbbell' type paramagnetic oxygen sensor, which has high resolution (10 µmol mol−1) and excellent linearity. The sensor is used to compare the sample gas mixture with pure oxygen and nitrogen gases, which compensates for drift and pressure change, and avoids the uncertainty from using bottled calibration gas mixtures. The method was verified by measuring primary standard gas mixtures at the National Physical Laboratory. To the authors knowledge the uncertainty achieved is better than any other analytical instrument, within the specified range.
A new tapered double balun for spiral-mode 2 (2007)

The tapered balun (J.W. Duncan and V.P. Minerva, 1960) is an excellent feed for very broadband, balanced antennas, such as spirals and sinuous antennas. Its bandwidth is limited only at the low-frequency end, which can be made arbitrarily low by making the taper longer. Furthermore, it can be easily designed and fabricated in an inexpensive printed circuit medium. A four-arm spiral antenna that operates only in mode 2 (R.G. Corzine and J.A. Mosko, 1990) really has only two electrical terminals since opposite arms theoretically can be connected together. However, practically, it is not obvious how to achieve this connection in a rugged and inexpensive way. A clever tapered coplanar-line balun has been reported (E. Gschwendtner, 1999) but a cavity will interfere with it, and the authors do not discuss how to make it balanced at the feed point. This paper describes a new tapered double balun that solves these issues and provides an improved technique to excite mode 2 for four-arm spirals.
Tension Membrane Water Retaining Structures (2005)

Since the first recorded use of mitre gates in a canal in Milan during the 15th century there is a consistent aspect to all gate styles. Whether the gate style is mitre, flap, or sector, the main structural element is rigid. From the earliest gates that were constructed from structural timber to be followed by iron and currently to steel, gates are all designed to be rigid. Rigid in that the design assumes an elastic deformation, perhaps with plastic design applying appropriate factors of safety with bending moments, shear forces and axial loading: compression and components of beam, struc and/or arch. These fundamental structural components are well established in not only gate design, but also for building design, bridge design, etc. However, there would be an outcry if the design of a sail for a boat were rigid. Sails are flexible to allow their easy storage, maneuvering into position and freedom to best respond to wind loading. As there are fundamental similarities to gas and fluid physics why not use a flexible membrane in a structural context to control water levels in maritime uses such as lock gates? The following sections will consider the established gate forms and their inefficiencies in retaining water levels together with the changing operational maritime environment of such structures. Also to be discusses is the use of an alternative, innovative form of gate structure as a way forward in water retention for maritime uses.
Synthesis and Evaluation of Selected Key Methyl Ether Derivatives of Vancomycin Aglycon (2010)

A select series of methyl ether derivatives of vancomcyin aglycon were prepared and examined for antimicrobial activity against vancomycin-sensitive Staphylococcus aureus and vancomycin-resistant Enterococci faecalis as well as their binding affinity for D-Ala-D-Ala and D-Ala-D-Lac. The intent of the study was to elucidate the role selected key methyl groups may play in the improvement of the in vitro antimicrobial profile of the tetra methyl ether derivative of vancomycin aglycon against vancomycin-resistant Enterococci faecalis previously reported. In these studies, methodology for selective derivatization of the A-, B-, and D-ring was developed that defines the relative reactivity of the four phenols of vancomycin aglycon, providing a foundation for future efforts for site-directed modification of the vancomycin aglycon core.
A passive technique for fingerprinting wireless devices with Wired-side Observations (2013)

In this paper, we introduce GTID, a technique that passively fingerprints wireless devices and their types from the wired backbone. GTID exploits the heterogeneity of devices, which is a function of different device hardware compositions and variations in devices' clock skew. We use statistical techniques to create unique, reproducible device and device type signatures that represent time variant behavior in network traffic and use artificial neural networks (ANNs) to classify devices and device types. We demonstrate the efficacy of our technique on both an isolated testbed and a live campus network (during peak hours) using a corpus of 27 devices representing a wide range of device classes. We collected more than 100 GB of traffic captures for ANN training and classification. We assert that for any fingerprinting technique to be practical, it must be able to detect previously unseen devices (i.e., devices for which no stored signature is available) and must be able to withstand various attacks. GTID is the first fingerprinting technique to detect previously unseen devices and to illustrate its resilience under various attacker models. We measure the performance of GTID by considering accuracy, recall, and processing time and illustrate how it can be used to complement existing authentication systems and to detect counterfeit devices.
The Automated Asphaltene Determinator Coupled with Saturates, Aromatics, and Resins Separation for Petroleum Residua Characterization (2013)

A new fully automated saturates, aromatics, resins, and asphaltenes (SARA) separation for asphalt bitumen and petroleum residua has been developed and optimized. This system performs separations on 2 mg sample portions utilizing four columns packed with different stationary phases. The direction of solvent flow is controlled by automated four-port and six-port switching valves. The asphaltenes precipitate out of solution within a ground polytetrafluoroethylene (PTFE) packed column in an excess of heptane. The heptane-soluble maltenes pass through glass beads, aminopropyl bonded silica, and activated silica packed columns where chromatographic separation of the maltenes occurs. The saturates material is not retained, and it passes through all three adsorption columns. The more highly polar and pericondensed aromatic resins are retained by the glass bead column, and the remaining resins are adsorbed on the aminopropyl silica column. The glass bead column minimizes irreversible adsorption of resins by preventing the more polar resins from reaching the aminopropyl silica column. The aromatics are adsorbed on the activated silica column. In the next step of the method, the asphaltenes are selectively redissolved from the PTFE column with cyclohexane, toluene, and methylene chloride:methanol (98:2 v/v), yielding highly alkyl substituted asphaltene components, less alkyl substituted pericondensed aromatic asphaltenes, and precoke pericondensed aromatic asphaltenes, respectively. In the final steps, the aromatics and resins are eluted from their respective columns. An evaporative light scattering detector is used to quantify the amounts of each fraction, and an optical absorbance detector set at 500 nm records the relative amounts of pericondensed aromatic material with extended π systems that absorb visible light contained within the eluting fractions. The entire system is regenerated to the original column activity with a toluene and heptane solvent flush sequence, prior to the next injection. An automated separation is performed every four hours compared to several days for a corresponding gravimetric manual method.
Calibration-free wavelength-modulation spectroscopy for measurements of gas temperature and concentration in harsh environments (2009)

We present a practical implementation of calibration-free wavelength-modulation spectroscopy with second harmonic detection (WMS-2f) for measurements of gas temperature and concentration in harsh environments. The method is applicable to measurements using lasers with synchronous wavelength and intensity modulation (such as injection current-tuned diode lasers). The key factors that enable measurements without the on-site calibration normally associated with WMS are (1) normalization of the WMS-2f signal by the first harmonic (1f) signal to account for laser intensity, and (2) the inclusion of laser-specific tuning characteristics in the spectral-absorption model that is used to compare with measured 1f-normalized, WMS-2f signals to infer gas properties. The uncertainties associated with the calibration-free WMS method are discussed, with particular emphasis on the influence of pressure and optical depth on the WMS signals. Many of these uncertainties are also applicable to calibrated WMS measurements. An example experimental setup that combines six tunable diode laser sources between 1.3 and 2.0 mum into one probe beam for measurements of temperature, H(2)O, and CO(2) is shown. A hybrid combination of wavelength and frequency demultiplexing is used to distinguish among the laser signals, and the optimal set of laser-modulation waveforms is presented. The system is demonstrated in the harsh environment of a ground-test scramjet combustor. A comparison of direct absorption and 1f-normalized, WMS-2f shows a factor of 4 increase in signal-to-noise ratio with the WMS technique for measurements of CO(2) in the supersonic flow. Multidimensional computational fluid-dynamics (CFD) calculations are compared with measurements of temperature and H(2)O using a simple method that accounts for the influence of line-of-sight (LOS) nonuniformity on the absorption measurements. The comparisons show the ability of the LOS calibration-free technique to gain useful information about multidimensional CFD models.
Discovery of Potent, Nonsteroidal, and Highly Selective Glucocorticoid Receptor Antagonists (2002)

An approach to the computer-assisted, pharmacophore design of nonsteroidal templates for the glucocorticoid receptor (GR) that contained an element of pseudo-C2 symmetry was developed. The enatiomer of the initial design, 1Ra, and not the designed molecule, 1S, showed the desired ligand binding to the GR. The pseudo-C2 symmetry of the template allowed for rapid improvements in GR activity resulting in potent, selective, nonsteroidal GR antagonists, CP-394531 and CP-409069.
Condensation of nucleic acids by intercalating aromatic cations. (1984)

Certain intercalating aromatic cations, such as the fluorochrome acridine orange or the antitumor drug Mitoxantrone, induce condensation of nucleic acids in solutions. The appearance of the condensed form during titration of nucleic acids with these intercalating ligands can be quantitatively monitored by light scatter measurements. The resulting highly reproducible light scatter transition curves are typical of the cooperative processes, and the transitions occur at different critical concentrations of the ligands depending upon both the ligand itself and the primary structure (base and sugar composition) and the secondary structure (single- or double-stranded) of the nucleic acids. The mechanism of condensation of nucleic acids by intercalating cationic ligands is discussed in light of the model of interactions occurring between certain intercalators and single-stranded nucleic acids and compared with the condensation induced by polyvalent "simple" cations such as Co3+ or spermine4+. The described phenomenon can have an application in analytical and preparative biochemistry for characterization of the primary and secondary structure of nucleic acids and for separation of the compounds. The possibility that the condensation plays a role in mutagenic and pharmacological effects of aromatic cations is considered.