gebhart/patrepeval huggingface dataset:
Aminomethyl spectinomycins as therapeutics for drug-resistant respiratory tract and sexually transmitted bacterial infections (2015)

The antibiotic spectinomycin is a potent inhibitor of bacterial protein synthesis with a unique mechanism of action and an excellent safety index, but it lacks antibacterial activity against most clinically important pathogens. A series of N-benzyl-substituted 3'-(R)-3'-aminomethyl-3'-hydroxy spectinomycins was developed on the basis of a computational analysis of the aminomethyl spectinomycin binding site and structure-guided synthesis. These compounds had ribosomal inhibition values comparable to spectinomycin but showed increased potency against the common respiratory tract pathogens Streptococcus pneumoniae, Haemophilus influenzae, Legionella pneumophila, and Moraxella catarrhalis, as well as the sexually transmitted bacteria Neisseria gonorrhoeae and Chlamydia trachomatis. Non-ribosome-binding 3'-(S) isomers of the lead compounds demonstrated weak inhibitory activity in in vitro protein translation assays and poor antibacterial activity, indicating that the antibacterial activity of the series remains on target against the ribosome. Compounds also demonstrated no mammalian cytotoxicity, improved microsomal stability, and favorable pharmacokinetic properties in rats. The lead compound from the series exhibited excellent chemical stability superior to spectinomycin; no interaction with a panel of human receptors and drug metabolism enzymes, suggesting low potential for adverse reactions or drug-drug interactions in vivo; activity in vitro against a panel of penicillin-, macrolide-, and cephalosporin-resistant S. pneumoniae clinical isolates; and the ability to cure mice of fatal pneumococcal pneumonia and sepsis at a dose of 5 mg/kg. Together, these studies indicate that N-benzyl aminomethyl spectinomycins are suitable for further development to treat drug-resistant respiratory tract and sexually transmitted bacterial infections.
Real-Time Terahertz Imaging System for the Detection of Concealed Objects (2007)

We have demonstrated for the first time a novel, real-time terahertz imaging system using a single fiber laser to generate THz radiation by DFM and an uncooled microbolometer array to image the THz signal.
Development of antibodies that interfere with the collagen-VWF-GPIb axis as new antithrombotics. (2005)

The epitope and the antithrombotic effect of 6B4, an antibody that inhibits GPIb, the receptor for von Willebrand Factor (VWF) on blood platelets, and of 82D6A3, an antibody against VWF that prevents the binding of VWF to collagen, were characterised. By using canine-human chimeras, alanine-scans, phage display, mutant analysis and modeling both the epitope of 6B4 in the N-terminal domain of GPIb, and of 82D6A3 in the VWF-A3 domain, could be mapped. As both epitopes furthermore are part of the ligand binding sites, this at once also explained the mechanism of the inhibition by the antibodies. Next both antibodies were tested in a thrombosis model in a stenosed artery in baboons, where they showed potent antithrombotic activities, without a noteworthy prolongation of the bleeding time. With this we thus could reveal two new strategies to prevent arterial thrombosis, which presumably may be safer than the currently available antiplatelet agents.
Integration of transistors, microoptics and vertical-cavity surface-emitting lasers (1993)

We report the flip-chip integration of heterojunction bipolar transistors (HBTs) and microlenses with vertical-cavity surface-emitting lasers (VCSELs). In addition, we present modeled light-out vs voltage characteristics for field-effect transistors (FETs) integrated with VCSELs and describe our efforts to integrate the two. HBT/VCSEL and FET/VCSBL devices exhibit lasing thresholds of 65-μΑ (experimental) and 1.0 volt (modeled), respectively. In addition, we use microlenses to produce diffraction limited one-to-one imaging of 10-degree far field VCSEL outputs. This integrated devices are ideally suited for free-space optical interconnection of multichip modules; optical neural networks; multichannel-multiwavelength fiberoptic communication; and print and scan heads for digital laser printing, scanning, and optical memory. These are just a few of the sophisticated functions and applications on the horizon of this breakthrough technology.1
Synchronization of Micromechanical Oscillators Using Light (2012)

Synchronization, the emergence of spontaneous order in coupled systems, is of fundamental importance in both physical and biological systems. We demonstrate the synchronization of two dissimilar silicon nitride micromechanical oscillators, that are spaced apart by a few hundred nanometers and are coupled through an optical cavity radiation field. The tunability of the optical coupling between the oscillators enables one to externally control the dynamics and switch between coupled and individual oscillation states. These results pave a path toward reconfigurable synchronized oscillator networks.
ViLDAR - Visible Light Sensing Based Speed Estimation using Vehicle's Headlamps (2018)

The introduction of light emitting diodes (LED) in automotive exterior lighting systems provides opportunities to develop viable alternatives to conventional communication and sensing technologies. Most of the advanced driver-assist and autonomous vehicle technologies are based on Radio Detection and Ranging (RADAR) or Light Detection and Ranging (LiDAR) systems that use radio frequency or laser signals, respectively. While reliable and real-time information on vehicle speeds is critical for traffic operations management and autonomous vehicles safety, RADAR or LiDAR systems have some deficiencies especially in curved road scenarios where the incidence angle is rapidly varying. In this paper, we propose a novel speed estimation system so-called the Visible Light Detection and Ranging (ViLDAR) that builds upon sensing visible light variation of the vehicle's headlamp. We determine the accuracy of the proposed speed estimator in straight and curved road scenarios. We further present how the algorithm design parameters and the channel noise level affect the speed estimation accuracy. For wide incidence angles, the simulation results show that the ViLDAR outperforms RADAR/LiDAR systems in both straight and curved road scenarios. A provisional patent (US#62/541,913) has been obtained for this work.
Using Magnetic Levitation for Three Dimensional Self‐Assembly (2011)

Magnetic levitation (MagLev) enables 3D self-assembly of diamagnetic objects with control over many aspects of position and orientation. This work demonstrates the ability of MagLev to position and align components, such as mirrors, filters, lenses, and soft objects, without mechanical support. Detailed facts of importance to specialist readers are published as ”Supporting Information”. Such documents are peer-reviewed, but not copy-edited or typeset. They are made available as submitted by the authors. Please note: The publisher is not responsible for the content or functionality of any supporting information supplied by the authors. Any queries (other than missing content) should be directed to the corresponding author for the article.
Antineoplastic agents. 214. Isolation and structure of cephalostatins 7-9 (1992)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTAntineoplastic agents. 214. Isolation and structure of cephalostatins 7-9George R. Pettit, Yoshiaki Kamano, Masuo Inoue, Claude Dufresne, Michael R. Boyd, Cherry L. Herald, Jean M. Schmidt, Dennis L. Doubek, and Nigel D. ChristieCite this: J. Org. Chem. 1992, 57, 2, 429–431Publication Date (Print):January 1, 1992Publication History Published online1 May 2002Published inissue 1 January 1992https://pubs.acs.org/doi/10.1021/jo00028a007https://doi.org/10.1021/jo00028a007research-articleACS PublicationsRequest reuse permissionsArticle Views138Altmetric-Citations44LEARN 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-AlertscloseSupporting Info (1)»Supporting Information Supporting Information Get e-Alerts
Phenotypic characterization of circulating tumor cells (CTCs) from neuroendocrine prostate cancer (NEPC) and metastatic castration-resistant prostate cancer (mCRPC) patients to identify a novel diagnostic algorithm for the presence of NEPC. (2015)

197 Background: NEPC is an aggressive variant of prostate cancer that most commonly arises in later stages of mCRPC, especially with visceral metastases in the setting of a low PSA. There are no reliable serum markers to identify patients that are transforming to NEPC and incidence of CTCs in these patients is unknown. Detection of NEPC has clinical implications as these patients are often treated with platinum chemotherapy rather than with androgen receptor (AR) targeted therapies such as abiraterone or enzalutamide. We sought to determine if phenotypic characterization of CTCs could differentiate NEPC from mCRPC. Methods: 24 pts (16 pts with tissue confirmed NEPC and 8 pts with mCRPC) had blood collection for CTC analysis utilizing the Epic Sciences platform. Epic analysis included identification of traditional CTCs (CK+, CD45- cells, with intact nuclei, morph distinct), CK- CTCs (CK-, CD45-, intact nuclei, morph distinct), small CTCs (CK+, CD45-, intact nuclei, small cell size), and CTC clusters. We examined CTCs at the single cell level for CTC size, shape, epithelial and AR expression. Advanced digital pathology algorithms measured size and shape measurements of CTCs. Results: CTCs from NEPC patients demonstrated strong statistical differentiation from mCRPC patients, with unique CTC morphology and protein chemistry that was not seen in mCRPC CTCs. NEPC CTCs had increase prevalence of unique CTC phenotypes including: small size, AR negativity, and presence of nucleoli. Unique cell types enabled a multivariate biomarker that is strongly associated with CTCs exclusive to tissue confirmed NEPC. Conclusions: CTCs from NEPC have unique phenotypes compared with those from mCRPC. If confirmed, the utilization of a liquid biopsy to diagnose NEPC may enable earlier identification of patients prone to visceral metastasis, and intervention to cytotoxic therapeutics. Additionally, identification of patients with NEPC could help for patient selection for AR vs. NEPC targeted therapeutics. [Table: see text]
Flexibility Reserve in Power Systems: Definition and Stochastic Multi-Fidelity Optimization (2020)

Summary form only given. This paper defines flexibility reserve trajectory as a single reserve product that not only supplies the energy imbalance in real-time operation but also the resulting ramping requirements by embedding the flexible ramping trajectories as time derivative of the reserve trajectories. Further, a stochastic optimization model is proposed for multi-fidelity co-optimization of energy and flexibility reserve in day-ahead power systems operation. The proposed model integrates operation decisions with different levels of modeling fidelity in a single stochastic optimization problem. More specifically, day-ahead energy trajectories, day-ahead flexibility reserve capacity trajectories, and real-time flexibility reserve deployment trajectories are modeled by Bernstein polynomials with different degrees as required to match the load and renewable generation with different levels of variability in day-ahead and real-time operations. The proposed model is implemented on the IEEE reliability test system using load and solar generation data of California ISO, where the numerical results demonstrate that the proposed model schedules a reserve capacity that more accurately matches the real-time energy imbalance and ramping requirements of net-load, while reducing the total operation cost of the system.
Protection of fiber function by para‐Axial fluid flow in interstitial laser therapy of malignant tumors (1990)

In the past, interstitial laser therapy frequently has failed because of the damage to the bare fiber tip due to intense heat generated at the point of contact. Using a rat mammary tumor model, we describe a method of placing a 600 micron fiber inside a gauge 19 needle cannula after its insertion into the tumor. With this device continuous wave Nd:YAG laser is delivered to the target tumor while 0.9% saline flows para-axially into the tumor. Significant coagulation necrosis was induced with 500 joules at 5 watts, 100 seconds and 1 cc per minute of saline while the needle-fiber is pulled out of the tumor by 10 mm. The mean transmission loss after 500 joules was 2% in ten experiments. The tumor edema due to 1.5 ml of saline was transient. We conclude that successful hyperthermic coagulation necrosis by Nd:YAG laser can be achieved with minimal transmission loss by employing the above technique.
Learning Motion in Feature Space: Locally-Consistent Deformable Convolution Networks for Fine-Grained Action Detection (2018)

Fine-grained action detection is an important task with numerous applications in robotics and human-computer interaction. Existing methods typically utilize a two-stage approach including extraction of local spatio-temporal features followed by temporal modeling to capture long-term dependencies. While most recent papers have focused on the latter (long-temporal modeling), here, we focus on producing features capable of modeling fine-grained motion more efficiently. We propose a novel locally-consistent deformable convolution, which utilizes the change in receptive fields and enforces a local coherency constraint to capture motion information effectively. Our model jointly learns spatio-temporal features (instead of using independent spatial and temporal streams). The temporal component is learned from the feature space instead of pixel space, e.g. optical flow. The produced features can be flexibly used in conjunction with other long-temporal modeling networks, e.g. ST-CNN, DilatedTCN, and ED-TCN. Overall, our proposed approach robustly outperforms the original long-temporal models on two fine-grained action datasets: 50 Salads and GTEA, achieving F1 scores of 80.22% and 75.39% respectively.
Detection of Toxoplasma gondii antigens by a dot-immunobinding technique (1985)

A sensitive assay for the detection of antigens of Toxoplasma gondii by spotting samples directly onto nitrocellulose paper was developed. The sensitivity ranged from 10 to 40 pg of antigen diluted in phosphate-buffered saline and 40 to 130 pg of antigen diluted in normal mouse serum, normal human serum, or human cerebrospinal fluid. T. gondii antigen in serum samples taken from mice infected with T. gondii was detectable by day 2 of infection. Antigen was also detectable in cerebrospinal fluid samples taken from four of six infants congenitally infected with T. gondii and in serum samples from two of these infants.
SHG nanoprobes: Advancing harmonic imaging in biology (2012)

Second harmonic generating (SHG) nanoprobes have recently emerged as versatile and durable labels suitable for in vivo imaging, circumventing many of the inherent drawbacks encountered with classical fluorescent probes. Since their nanocrystalline structure lacks a central point of symmetry, they are capable of generating second harmonic signal under intense illumination - converting two photons into one photon of half the incident wavelength - and can be detected by conventional two-photon microscopy. Because the optical signal of SHG nanoprobes is based on scattering, rather than absorption as in the case of fluorescent probes, they neither bleach nor blink, and the signal does not saturate with increasing illumination intensity. When SHG nanoprobes are used to image live tissue, the SHG signal can be detected with little background signal, and they are physiologically inert, showing excellent long-term photostability. Because of their photophysical properties, SHG nanoprobes provide unique advantages for molecular imaging of living cells and tissues with unmatched sensitivity and temporal resolution.
Synthetic Studies of Imidazole C‐Nucleoside Derivatives: Their Application to Histamine H<sub>3</sub>‐ and H<sub>4</sub>‐Ligands (2003)

Abstract For Abstract see ChemInform Abstract in Full Text.
Silver Beta‐Alumina as a Potentiometric Gas Sensor for Arsenic Oxides, AsO x (1990)

A potentiometric solid‐state sensor for measuring gaseous arsenic oxides and/or arsine was constructed by using a silver β‐alumina solid electrolyte with Ag metal as the reference electrode. The operation of this sensor depends on thein situ formation of at the surface of the electrolyte and can be represented by the following galvanic cell
Electroless Palladium Plating from an Ethylenediamine Complex Bath using Phosphite as a Reducing Agent (1996)

SUMMARYElectroless palladium plating was investigated from palladium-ethylenediamine complex solutions containing sodium phosphite as a reducing agent.The deposition process proceeded autocatalytically as with hypophosphite, but the phosphorus content in the deposits was much lower.From the experimental results on solderability and electric contact resistance, it was suggested that electroless palladium plating could be utilized as an alternative to gold plating on electrical contacts and to solder or the preflux coat for ensuring good solderability.
Negative Impact of β-Arrestin-1 on Post-Myocardial Infarction Heart Failure via Cardiac and Adrenal-Dependent Neurohormonal Mechanisms (2013)

β-Arrestin (βarr)-1 and β-arrestin-2 (βarrs) are universal G-protein-coupled receptor adapter proteins that negatively regulate cardiac β-adrenergic receptor (βAR) function via βAR desensitization and downregulation. In addition, they mediate G-protein-independent βAR signaling, which might be beneficial, for example, antiapoptotic, for the heart. However, the specific role(s) of each βarr isoform in cardiac βAR dysfunction, the molecular hallmark of chronic heart failure (HF), remains unknown. Furthermore, adrenal βarr1 exacerbates HF by chronically enhancing adrenal production and hence circulating levels of aldosterone and catecholamines. Herein, we sought to delineate specific roles of βarr1 in post-myocardial infarction (MI) HF by testing the effects of βarr1 genetic deletion on normal and post-MI cardiac function and morphology. We studied βarr1 knockout (βarr1KO) mice alongside wild-type controls under normal conditions and after surgical MI. Normal (sham-operated) βarr1KO mice display enhanced βAR-dependent contractility and post-MI βarr1KO mice enhanced overall cardiac function (and βAR-dependent contractility) compared with wild type. Post-MI βarr1KO mice also show increased survival and decreased cardiac infarct size, apoptosis, and adverse remodeling, as well as circulating catecholamines and aldosterone, compared with post-MI wild type. The underlying mechanisms, on one hand, improved cardiac βAR signaling and function, as evidenced by increased βAR density and procontractile signaling, via reduced cardiac βAR desensitization because of cardiac βarr1 absence, and, on the other hand, decreased production leading to lower circulating levels of catecholamines and aldosterone because of adrenal βarr1 absence. Thus, βarr1, via both cardiac and adrenal effects, is detrimental for cardiac structure and function and significantly exacerbates post-MI HF.
Combining Multiple Clusterings by Soft Correspondence (2006)

Combining multiple clusterings arises in various important data mining scenarios. However, finding a consensus clustering from multiple clusterings is a challenging task because there is no explicit correspondence between the classes from different clusterings. We present a new framework based on soft correspondence to directly address the correspondence problem in combining multiple clusterings. Under this framework, we propose a novel algorithm that iteratively computes the consensus clustering and correspondence matrices using multiplicative updating rules. This algorithm provides a final consensus clustering as well as correspondence matrices that gives intuitive interpretation of the relations between the consensus clustering and each clustering from clustering ensembles. Extensive experimental evaluations also demonstrate the effectiveness and potential of this framework as well as the algorithm for discovering a consensus clustering from multiple clusterings.
Flagellin, a Novel Mediator of <i>Salmonella</i> -Induced Epithelial Activation and Systemic Inflammation: IκBα Degradation, Induction of Nitric Oxide Synthase, Induction of Proinflammatory Mediators, and Cardiovascular Dysfunction (2001)

Gram-negative sepsis is mediated by the actions of proinflammatory genes induced in response to microbes and their products. We report that flagellin, the monomeric subunit of flagella, is a potent proinflammatory species released by Salmonella. Flagellin (1 microgram/ml) induces IkappaBalpha degradation, NF-kappaB nuclear translocation, and inducible NO synthase expression in cultured intestinal epithelial cells (IEC). Aflagellic Salmonella mutants do not induce NF-kappaB activation or NO production by cultured IEC. Antiserum to flagellin blocks NO production in IEC induced by medium conditioned by a variety of motile Gram-negative enteric pathogens (Escherichia coli, Salmonella muenchen, Serratia marcescens, Proteus mirabilis, and Proteus vulgaris). Flagellin, when injected systemically (approximately 10 microgram/mouse), induces systemic inflammation characterized by the systemic expression of a range of proinflammatory cytokines and chemokines and of inducible NO synthase. At higher doses (approximately 300 microgram/mouse), flagellin induces shock, characterized by hypotension, reduced vascular contractility in mice, and death. The effects of flagellin do not diminish in C3H/HeJ LPS-resistant mice, indicating that the Toll-like receptor-4 receptor is not involved in flagellin's actions. In LPS-resistant mice, i.p. injection of S. dublin flagellin or medium conditioned by wild-type S. dublin induces serum IFN-gamma and TNF-alpha, whereas medium conditioned by aflagellic mutants has no effect. Flagellin can be detected in the blood of rats with septic shock induced by live bacteria at approximately 1 microg/ml. We propose that flagellin released by Gram-negative pathogens may contribute to the inflammatory response by an LPS- and Toll-like receptor-4-independent pathway.