gebhart/patrepeval huggingface dataset:
Novel Thiourea Compounds as Dual-Function Microbicides (2000)

Sexually active women represent the fastest growing human immunodeficiency virus (HIV)/acquired immunodeficiency syndrome risk group. In an effort to develop a vaginal microbicidal contraceptive potentially capable of preventing HIV transmission as well as providing fertility control, we previously reported the synthesis of novel nonnucleoside inhibitors (NNIs) of HIV-1 reverse transcriptase with sperm-immobilizing activity (SIA). To gain further insight into the structure-function relationship controlling these two properties of NNIs, we have rationally designed and synthesized 30 novel thiourea compounds and examined them for dual-function, anti-HIV and spermicidal activity. Twelve of the 30 thiourea compounds exhibited potent anti-HIV activity in the nanomolar range (IC(50) = <1-9 nM). Nine of the 30 thiourea derivatives exhibited both anti-HIV and spermicidal activity. Among the phenyl ring-containing thioureas, the 2-fluoro (HI-240) -substituted and 2-chloro (HI-253) -substituted derivatives exhibited potent anti-HIV activity (IC(50) = <1 nM) with SIA (EC(50) = 70 microM and 147 microM). Among the alicyclic ring-containing thioureas, the 5-bromo (HI-346) and 5-chloro (HI-445) functionalized cyclohexenyl ring-substituted thioureas were the most potent dual-function spermicides (EC(50) = 42 and 57 microM), with anti-HIV activity at nanomolar range (IC(50) = 3 nM). Unlike nonoxynol-9 (N-9), none of the potent dual-function thiourea compounds were cytotoxic to normal human vaginal, ectocervical, and endocervical epithelial cells at spermicidal concentrations. We conclude that as potent anti-HIV agents with SIA and reduced cytotoxicity when compared with N-9, the phenyl-substituted and cyclohexenyl-substituted thiourea derivatives, especially compounds HI-253 (N-[2-(2-chlorophenethyl)]-N'-[2-(5-bromopyridyl)-thiourea), HI-346 (N-[2-(5-bromopyridinyl)]-N'-[2-(1-cyclohexenyl)ethyl-thiourea), and HI-445 (N-[2-(5-chloropyridinyl)]-N'-[2-(1-cyclohexenyl)ethyl-thiourea) show unique clinical potential to become the active ingredients of a vaginal contraceptive for women who are at high risk for acquiring HIV by heterosexual vaginal transmission.
<title>Ultrasonic atomic force microscopy with real-time mapping of resonance frequency and Q factor</title> (2002)

Ultrasonic atomic force microscopy (UAFM) is a new scientific tool realizing reliable measurement of nano-scale elasticity from resonance vibration of cantilever in the contact mode AFM. The elasticity is evaluated from the resonance frequency, and the loss modulus may be evaluated from Q the factor. This paper describes recent progress on the theoretical model, subsurface imaging, inverse analysis, nonlinearity due to a dislocation, and theory and experiment of Q control for improving resolution and stability.
A high gain vertical channel controlled thyristor (1977)

A new vertical channel field controlled thyristor structure is described. This device has a surface grid structure with a high channel length to width aspect ratio which simultaneously allows achieving high blocking gains and fast gate turn-off capability. The devices have the capability of blocking more than 1000 volts with an applied grid bias of 32 volts, and simultaneously exhibiting a low forward voltage drop in the on-state. In addition, the surface grid structure allows gate turn-off capability with a cathode current turn-off time of less than 0.5 microseconds.
Bisoxazolidine-Catalyzed Enantioselective Reformatsky Reaction (2011)

A readily available chiral bisoxazolidine catalyzes the asymmetric Reformatsky reaction between ethyl iodoacetate and aldehydes. In the presence of 10 mol % of the ligand, dimethylzinc, and air, this method produces ethyl 3-hydroxy-3-(4-aryl)propanoates in high yields and in 75 to 80% ee at room temperature within 1 h. In contrast to aromatic substrates, relatively low ee's are obtained with aliphatic aldehydes.
Augmented microscopy: real-time overlay of bright-field and near-infrared fluorescence images (2015)

Intraoperative applications of near-infrared (NIR) fluorescent contrast agents can be aided by instrumentation capable of merging the view of surgical field with that of NIR fluorescence. We demonstrate augmented microscopy, an intraoperative imaging technique in which bright-field (real) and electronically processed NIR fluorescence (synthetic) images are merged within the optical path of a stereomicroscope. Under luminance of 100,000 lx, representing typical illumination of the surgical field, the augmented microscope detects 189 nM concentration of indocyanine green and produces a composite of the real and synthetic images within the eyepiece of the microscope at 20 fps. Augmentation described here can be implemented as an add-on module to visualize NIR contrast agents, laser beams, or various types of electronic data within the surgical microscopes commonly used in neurosurgical, cerebrovascular, otolaryngological, and ophthalmic procedures.
Automated Fall Risk Assessment and Detection in the Home: A Preliminary Investigation (2012)

Falls are a major problem for older adults. A continuous unobtrusive in-home monitoring system that provides an accurate automated assessment of fall risk and detects when falls have occurred would allow for timely intervention and prevention allowing individual to remain healthier and independent longer. Sensor networks have been installed in apartments of older adult volunteers at TigerPlace, an independent senior living community. Initial results comparing gait parameters captured with a Microsoft Kinect with ground truth clinical fall risk assessments and GAITRite data are presented.
The Synthesis and Transition Temperatures of Some Fluoro-Substituted 4-Cyanophenyl and 4-Cyanobiphenyl-4′-yl 4-Pentyl- and 4-Butoxy-Benzoates (1989)

Abstract A series of 4-cyanophenyl 4-X-benzoates and a series of 4-cyanobiphenyl-4′-yl 4-X-benzoates (X =pentyl, butoxy) have been prepared without fluoro-substitution and with mono-fluoro to tetra-fluoro-substitution; all possible combinations of substitution patterns at the positions ortho- to the cyano group and ortho- to the carboxylate group have been obtained in an attempt to determine the structural features which are responsible for some members of these series showing very large positive values of dielectric anisotropy. The synthesis of novel precursors required for the preparation of these esters is described and the melting points and transition temperatures of the esters are discussed and an explanation is provided for the variation of TN -1 values with position and extent of fluoro-substitution.
Aryl 1-But-3-ynyl-4-phenyl-1,2,3,6-tetrahydropyridines as Potential Antipsychotic Agents:  Synthesis and Structure−Activity Relationships (1996)

A novel series of aryl 1-but-3-ynyl-4-phenyl-1,2,3,6-tetrahydropyridines with dopaminergic activity is described. The structure-activity relationships of this series were studied by synthesis of analogs and evaluation of their affinities for the dopamine (DA) D2 receptor and inhibition of locomotor activity (LMA) in rodents. The basic amine, alkyne chain length, and aryl groups were varied. Compounds having a 4-phenyl-1,2,3,6-tetrahydropyridine and an aryl group with hydrogen-bonding substituents separated by a butynyl chain were found to have the most potent dopaminergic activity. Several compounds that were found to have exceptional in vivo activity in LMA inhibition in rodents were evaluated for additional pharmacological activity including binding affinities for other DA receptor subtypes as well as effects on brain DA synthesis, DA neuronal firing, and conditioned avoidance responding in squirrel monkeys.
A feasibility study for predicting optimal radiation therapy dose distributions of prostate cancer patients from patient anatomy using deep learning (2017)

With the advancement of treatment modalities in radiation therapy for cancer patients, outcomes have improved, but at the cost of increased treatment plan complexity and planning time. The accurate prediction of dose distributions would alleviate this issue by guiding clinical plan optimization to save time and maintain high quality plans. We have modified a convolutional deep network model, U-net (originally designed for segmentation purposes), for predicting dose from patient image contours of the planning target volume (PTV) and organs at risk (OAR). We show that, as an example, we are able to accurately predict the dose of intensity-modulated radiation therapy (IMRT) for prostate cancer patients, where the average Dice similarity coefficient is 0.91 when comparing the predicted vs. true isodose volumes between 0% and 100% of the prescription dose. The average value of the absolute differences in [max, mean] dose is found to be under 5% of the prescription dose, specifically for each structure is [1.80%, 1.03%](PTV), [1.94%, 4.22%](Bladder), [1.80%, 0.48%](Body), [3.87%, 1.79%](L Femoral Head), [5.07%, 2.55%](R Femoral Head), and [1.26%, 1.62%](Rectum) of the prescription dose. We thus managed to map a desired radiation dose distribution from a patient's PTV and OAR contours. As an additional advantage, relatively little data was used in the techniques and models described in this paper.
A Novel X-ray Microtomography System with High Resolution and Throughput (2004)

The large penetration depth and rich contrast mechanisms of x rays makes it ideal for non-destructive or non-invasive imaging applications. Projection-type x-ray micro-imaging systems are widely used in micro- and nano-technology industries to study the internal structures of manufactured components such as micro-electro-mechanical (MEM) or semiconductor devices. The resolution of these system is typically determined by the size of the x-ray source. As a consequence, a small x-ray source size and high magnification are required to achieve high resolution. Since both factors reduce the detectable flux, a compromise between the resolution and the throughput must be made. Based on its innovative high-resolution detector, Xradia has developed a new system, the microXCT, that solves this problem by using a unique optical design. It is able to acquire images with 1-micormeter resolution in an exposure time of a few seconds. This instrument includes a fully automated tomographic data acquisition and reconstruction capability for an user to study the 3D structure of a sample at micrometer three-dimensional resolution. This system’s unique capability of imaging at high-resolution with minimal compromise in the throughput makes it a valuable tool in non-destructive imaging applications in microtechnology and biotechnology.
Discriminating normal and abnormal left ventricular shapes in four-chamber view 2D echocardiography (2014)

In this paper, we address discrimination between normal and abnormal left ventricular shapes by capturing deviations from the normal appearance through a new parametric distorted elliptic shape model. To apply the parametric description, we automatically locate the left ventricular region in 4-chamber views and extract its bounding contours and pose. The parametric description of the elliptic fit with minimum alignment error with the bounding contour then becomes the shape descriptor for the bounding contour. Labeled vectors from normal and damaged left ventricular regions are separated into two classes using a support vector machine. Results are presented on a large database of normal and abnormal left ventricular images showing the effectiveness of the parametric features for normal/abnormal discrimination.
Off-axis co-sputtered YBCO and CeO/sub 2/ thin films (1997)

We have investigated the properties of off-axis co-sputtered films of YBCO and CeO/sub 2/ having CeO/sub 2/ concentrations up to 43%. Morphology investigations suggest that films with more than 29% CeO/sub 2/ may consist of a new material phase, T/sub c/ and resistance ratio decreased with increasing CeO/sub 2/ concentration. Degradation of T/sub c/, after photoresist processing the films was observed and reversed by a 20 minute oxygen plasma etch. The temperature dependence of the critical current near T/sub c/ showed two power law dependence regions with a crossover near 0.99 T/sub c/ for films having low concentrations of CeO/sub 2/. I/sub C/ 's were decreased by small applied magnetic fields, and for some samples the response was observed to increase at lower temperature. For a sample having 26% CeO/sub 2/, a 40% reduction in critical current was observed for a 2 Gauss applied field. This response indicates that this may be a candidate material for the development of Josephson vortex flow devices.
A simplified method for the synthesis of ceric alkoxides from ceric ammonium nitrate (1985)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTA simplified method for the synthesis of ceric alkoxides from ceric ammonium nitratePeter S. Gradeff, Fred G. Schreiber, Kenneth C. Brooks, and Robert E. SieversCite this: Inorg. Chem. 1985, 24, 7, 1110–1111Publication Date (Print):March 1, 1985Publication History Published online1 May 2002Published inissue 1 March 1985https://pubs.acs.org/doi/10.1021/ic00201a033https://doi.org/10.1021/ic00201a033research-articleACS PublicationsRequest reuse permissionsArticle Views589Altmetric-Citations48LEARN 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
Método para determinar información de tipo geométrico en dispositivos de redes en la banda de ondas milimétricas [METHOD FOR DETERMINING GEOMETRIC INFORMATION OF MMWAVE NETWORK DEVICES] (2020)

A method for determining geometric information of mmWave network devices comprising collecting measures, by at least one of the devices, of signal strength and SNR of a transmission received from another device of the mmWave network; estimating angle information of the received signals to generate a set of informed particles comprising initial values of state of each informed particle and input in a modified particle filter; the modified particle filter evolving the sets of informed particles and past particles to obtain a set of evolved particles which, in turn, is evolved to obtain a set of posterior particles delivered by the modified particle filter. Finally, the modified particle filter delivers as output final values of geometric information of the at least one device extracted from the delivered set of posterior particles.

US Patent Application. Application number: 16/365,953 (27.03.2019)
Development of a codon-optimized sodium/iodide symporter (NIS) for a sensitive imaging reporter gene and an efficient therapeutic gene (2013)

65 Objectives Sodium/iodide symporter (NIS) accounts for radioiodine accumulation in imaging and therapy of differentiated thyroid cancer. Recently, reporter gene imaging and radionuclide gene therapy have been tried in small animal levels. However, the major limitation is relatively low functional expression of NIS. We made a codon-optimized NIS, having efficient translation, and evaluated the expression and activity of this new NIS using in vivo imaging. Methods Human NIS sequence (NM_000453, hNIS) was optimized to have the highest frequency of codons in Homo sapiens and named oNIS. Retroviral vector pMSCV/hNIS or oNIS was transduced in thyroid cancer cell line (FRO) and breast cancer cell line (MDA-MB-231). The expression of NIS mRNA and protein in the cells was measured by real-time PCR and western blot. To evaluate the functional activity of NIS, radioiodine (125I) uptake of the cancer cells was measured. For scintigraphic imaging, 99mTc (0.5 mCi) was injected intraperitoneally to nude mice having the xenografted tumors, and those were imaged using a gamma camera with a pinhole collimater. Results The hNIS and oNIS genes were identical in amino acid sequences, but the Codon Adaptation Index (CAI)—representing the number of effective codons for human expression—was 0.79 and 0.97, respectively. The expression levels of NIS mRNA were similar in all cancer cell lines. However, protein amount of oNIS cells was 4 ~ 5.4 times higher than that of hNIS cells (P Conclusions The oNIS transfected tumors accumulated higher amount of radioiodine and 99mTc-pertechnetate than hNIS tumors in nude mice model. This novel codon-optimized NIS system can improve the experimental imaging and therapy using NIS with the possibility of clinical application in the future.
Seismic vibration source (1979)

A system for vibrating the earth in a location where seismic mapping is to take place is described. A relatively shallow hole formed in the earth, such as a hole 10 feet deep, placing a solid propellant in the hole, sealing a portion of the hole above the solid propellant with a device that can rapidly open and close to allow a repeatedly interrupted escape of gas. The propellant is ignited so that high pressure gas is created which escapes in pulses to vibrate the earth.
The composition of the GABA receptor at the <i>Caenorhabditis elegans</i> neuromuscular junction (2005)

1. The unc-49 gene of the nematode Caenorhabditis elegans encodes three gamma-aminobutyric acid type A (GABA(A)) receptor subunits. Two of these, UNC-49B and UNC-49C, are expressed at high abundance and co-localize at the neuromuscular junction. 2. The UNC-49B subunit is sufficient to form a GABA(A) receptor in vitro and in vivo. Furthermore, all loss-of-function unc-49 alleles lack functional UNC-49B. No mutations specifically inactivate UNC-49C. Thus, UNC-49C appears to be dispensable for receptor function; however, UNC-49C has been conserved among different nematode species, suggesting it plays a necessary role. 3. To ascertain whether UNC-49C is part of the GABA(A) receptor in vivo, we performed patch-clamp electrophysiology on C. elegans muscle cells. Sensitivity to GABA, and to the antagonists picrotoxin and pregnenolone sulfate, matched the UNC-49B/C heteromer rather than the UNC-49B homomer, for both exogenous and synaptically-released GABA. 4. The synaptic localization of UNC-49C requires the presence of UNC-49B, indicative of a physical association between the two subunits in vivo. Thus, the in vivo receptor is an UNC-49B/C heteromer. 5. UNC-49C plays a negative modulatory role. Using the rapid ligand-exchange technique in vitro, we determined that UNC-49C causes accelerated receptor desensitization. Previously, UNC-49C was shown to reduce single-channel conductance in UNC-49B/C heteromers. Thus, the function of UNC-49B is to provide GABA responsiveness and localization to synapses, while the function of UNC-49C is to negatively modulate receptor function and precisely shape inhibitory postsynaptic currents.
Cell-Permeable Parkin Proteins Suppress Parkinson Disease-Associated Phenotypes in Cultured Cells and Animals (2014)

Parkinson's disease (PD) is a neurodegenerative disorder of complex etiology characterized by the selective loss of dopaminergic neurons, particularly in the substantia nigra. Parkin, a tightly regulated E3 ubiquitin ligase, promotes the survival of dopaminergic neurons in both PD and Parkinsonian syndromes induced by acute exposures to neurotoxic agents. The present study assessed the potential of cell-permeable parkin (CP-Parkin) as a neuroprotective agent. Cellular uptake and tissue penetration of recombinant, enzymatically active parkin was markedly enhanced by the addition of a hydrophobic macromolecule transduction domain (MTD). The resulting CP-Parkin proteins (HPM13 and PM10) suppressed dopaminergic neuronal toxicity in cells and mice exposed to 6-hydroxydopamine (6-OHDH) and 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP). These included enhanced survival and dopamine expression in cultured CATH.a and SH-SY5Y neuronal cells; and protection against MPTP-induced damage in mice, notably preservation of tyrosine hydroxylase-positive cells with enhanced dopamine expression in the striatum and midbrain, and preservation of gross motor function. These results demonstrate that CP-Parkin proteins can compensate for intrinsic limitations in the parkin response and provide a therapeutic strategy to augment parkin activity in vivo.
Three-dimensional histo-morphometric features from light sheet microscopy images result in improved discrimination of benign from malignant glands in prostate cancer (2020)

Glandular features play an important role in the evaluation of prostate cancer. There has been significant interest in the use of 2D pathomics (feature extraction) approaches for detection, diagnosis, and characterization of prostate cancer on digitized tissue slide images. With the development of 3D microscopy techniques, such as open-top light-sheet (OTLS), there is an opportunity for rapid 3D imaging of large tissue specimens such as whole biopsies. In this study, we sought to investigate whether 3D features of gland morphology, namely volume and surface curvature, from OTLS images offer superior discrimination between malignant and benign glands compared to the traditional 2D gland features, namely area and curvature, alone. In this study, a cohort of 8 de-identified fresh prostate biopsies comprehensively imaged in 3D via the OTLS platform. A total of 367 glands were segmented from these images, of which 79 were identified as benign and 288 were identified as malignant. Glands were segmented using a 3D watershed algorithm followed by post-processing steps to filter out falsepositive regions. The 2D and 3D features were compared quantitatively and qualitatively. Our experiments demonstrated that a model using 3D features outperformed one using 2D features in differentiating benign and malignant glands. In 3D, both features, gland volume (p = 1.45 × 10<sup>−3</sup>) and surface curvature (p = 3.2 × 10<sup>−3</sup>), were found to be informative whereas in 2D, only gland area (p = 9 × 10<sup>−18</sup>) was found to be discriminating (p = 0.79 for 2D curvature). Notable visual and quantitative differences between 3D benign/malignant glands encourage the development of additional more sophisticated features in the future.
Differential MMSE: new adaptive algorithms for equalization, interference suppression, and beamforming (2002)

This paper provides a reformulation of the linear minimum mean squared error (MMSE) criterion so that it applies to systems in which the quantity to be tracked is the ratio of the data appearing in two successive observations. The resulting differential MMSE criterion leads to a number of novel algorithms for adaptive implementation of the MMSE receiver. Applications include the following: (a) equalization for single user systems in fast fading (b) adaptive multiuser detection, or interference suppression, for direct sequence CDMA systems employing short spreading sequences in fast fading; (c) blind beamforming using a receive antenna array for direct sequence CDMA systems with long spreading sequences. Note that standard MMSE adaptation either fails in fast fading environments such as (a) and (b), or incurs significant overhead in terms of pilot symbols for tracking the fades. Application (c) applies directly to third generation wideband CDMA proposals, and the algorithms we provide perform significantly better than the state of the art.