gebhart/patrepeval huggingface dataset:
Profiling target engagement and cellular uptake of cRGD-decorated clinical-stage core-crosslinked polymeric micelles (2022)

Polymeric micelles are increasingly explored for tumor-targeted drug delivery. CriPec® technology enables the generation of core-crosslinked polymeric micelles (CCPMs) based on thermosensitive (mPEG-b-pHPMAmLac<sub>n</sub>) block copolymers, with high drug loading capacity, tailorable size, and controlled drug release kinetics. In this study, we decorated clinical-stage CCPM with the α<sub>v</sub>β<sub>3</sub> integrin-targeted cyclic arginine-glycine-aspartic acid (cRGD) peptide, which is one of the most well-known active targeting ligands evaluated preclinically and clinically. Using a panel of cell lines with different expression levels of the α<sub>v</sub>β<sub>3</sub> integrin receptor and exploring both static and dynamic incubation conditions, we studied the benefit of decorating CCPM with different densities of cRGD. We show that incubation time and temperature, as well as the expression levels of α<sub>v</sub>β<sub>3</sub> integrin by target cells, positively influence cRGD-CCPM uptake, as demonstated by immunofluorescence staining and fluorescence microscopy. We demonstrate that even very low decoration densities (i.e., 1 mol % cRGD) result in increased engagement and uptake by target cells as compared to peptide-free control CCPM, and that high cRGD decoration densities do not result in a proportional increase in internalization. In this context, it should be kept in mind that a more extensive presence of targeting ligands on the surface of nanomedicines may affect their pharmacokinetic and biodistribution profile. Thus, we suggest a relatively low cRGD decoration density as most suitable for in vivo application.
Simple Near-Infrared Time-Correlated Single Photon Counting Instrument with a Pulsed Diode Laser and Avalanche Photodiode for Time-Resolved Measurements in Scanning Applications (1999)

A simple apparatus for time-correlated single photon counting (TCSPC) measurements in the near-infrared (near-IR) region for scanning-type applications has been constructed and examined. The apparatus consisted of five major components including a pulsed diode laser source (lasing wavelength = 780 nm; repetition rate 80 MHz; power = 5 mW; pulse width = 150 ps), an integrated microscope, a large-photoactive-area avalanche photodiode (APD), a TCSPC PC-board including the electronics, and a Windows-based software package for accumulating the fluorescence decay profiles. The instrument response function (IRF) of this assembly was found to be 460 ps, which is adequate for measuring lifetimes with τ f ⩾ 500 ps. Due to the small size of the device, it also allowed implementation into scanning experiments where lifetimes were measured. To demonstrate this capability, we scanned a three-well microscope slide containing a near-IR dye. The decay profile of the near-IR dye, aluminum 2,3-naphthalocyanine, was collected and analyzed to obtain its lifetime, which was found to be 2.73 ns, in close agreement with the literature value for this particular dye. In addition, a three-dimensional plot showing the decay profiles (time vs. photocounts) and scan position of aluminum 2,3-naphthalocyanine fluorescence was acquired by scanning the microscope head over this three-well glass slide. In the scanning mode, the IRFs as well as the decays of the dyes were found to be very stable. The device demonstrated a concentration detection sensitivity of 0.44 nM; however, the dynamic range was limited due to the slow time constant (passive quenching) associated with the APD.
Zero-forcing throughput maximization for regenerative multi-user relaying (2012)

We provide a computationally inexpensive zero-forcing downlink precoder design for regenerative relaying with multiple users. The design objectives are throughput maximization and rate balancing subject to separate transmit power constraints for the base station and relay. For throughput maximization, we provide also a distributed solution with low signaling overhead. The considered system model consists of a single multi-antenna base station and multi-antenna relay that both serve multiple users with single-antenna receivers. Two-stage transmission is considered, in which the additional interference caused by the over-the-air (OTA) transmission between the base station and relay is taken under consideration. It is shown that proper OTA signaling has major impact on improving the system performance.
Xanthene dye functionalized norbornenes for the use in ring opening metathesis polymerization (2007)

Abstract A convenient synthetic route towards polymerizable fluorescein, dicholorofluorescein, and eosin dyes is presented. Polymerizability was provided by linking 2‐norbornene carboxylic acid, 11‐bromo‐undecyl ester to the dye's carboxylate functionality. Although the monomers bearing dichlorofluorescein and eosin were obtained in high yield, the related fluorescein bearing monomer could only be obtained in low yield. In the latter case, concurring etherification and esterification led to a product mixture of the desired carboxy modified monomer and a double substituted by‐product. The dye‐monomers were used successfully for the preparation of statistical copolymers with endo , exo ‐2,3‐norbornene dicarboxylic acid dimethylester by ROMP. Absorption and luminescence characteristics and, in particular, the acid/base sensitive behavior of the parent dyes were preserved in the monomers and copolymers. The absorption and emission maxima in THF solution and in the solid state were red shifted in comparison to the aqueous samples of the parent dyes. Dye‐copolymers exhibited good film forming properties. Solid state luminescence studies of the copolymers revealed an increasing sensitivity towards NEt 3 vapor in the order fluorescein &lt; dichlorofluorescein &lt; eosin bearing copolymer. © 2007 Wiley Periodicals, Inc. J Polym Sci Part A: Polym Chem 45: 1336–1348, 2007
Software and the Concurrency Revolution (2005)

Concurrency has long been touted as the "next big thing" and "the way of the future," but for the past 30 years, mainstream software development has been able to ignore it. Our parallel future has finally arrived: new machines will be parallel machines, and this will require major changes in the way we develop software. The introductory article in this issue describes the hardware imperatives behind this shift in computer architecture from uniprocessors to multicore processors, also known as CMPs.
Ultrasonic Microelastography to Assess Biomechanical Properties of the Cornea (2018)

Our results demonstrate the principle of using ultrasonic microelastography techniques to image the biomechanical properties of the cornea. Integrating high-resolution ARFI imaging labeled with reconstructed Young's modulus and structural imaging of the cornea can potentially lead to a routinely performed imaging modality in the field of ophthalmology.
5G New Radio Base-Station Sensitivity and Performance (2018)

In this paper, we address and analyze the receiver reference sensitivity requirements for the 5G New Radio (NR) wireless communications systems, which relate to the SNR requirements at the base station to reach 95 % of the maximum throughput defined for fixed reference channels. Based on the latest 3GPP specifications and evaluation assumptions agreed for Release 15, a wide set of different transmission bandwidths and radio interface numerologies are investigated, at sub-6GHz and millimeter-wave frequency ranges, covering both AWGN and fading channel scenarios as well as varying mobility conditions. The performance results in terms of the relative throughput and block error rate using LDPC coding scheme are presented and analyzed, while for comparison purposes also LTE turbo code based results are provided. The results show that in frequency-selective channels, the reference sensitivity and UL radio link performance are systematically better with LDPC code compared to turbo code. The results also indicate that the purely front-loaded demodulation reference signal (DM-RS) based system can outperform the corresponding two DM-RS based system even at higher velocities and high center frequencies, allowing low decoding latency and efficient pipelined receiver processing.
Union-Find Decoders For Homological Product Codes (2021)

Homological product codes are a class of codes that can have improved distance while retaining relatively low stabilizer weight. We show how to build union-find decoders for these codes, using a union-find decoder for one of the codes in the product and a brute force decoder for the other code. We apply this construction to the specific case of the product of a surface code with a small code such as a <mml:math xmlns:mml="http://www.w3.org/1998/Math/MathML"><mml:mo stretchy="false">[</mml:mo><mml:mo stretchy="false">[</mml:mo><mml:mn>4</mml:mn><mml:mo>,</mml:mo><mml:mn>2</mml:mn><mml:mo>,</mml:mo><mml:mn>2</mml:mn><mml:mo stretchy="false">]</mml:mo><mml:mo stretchy="false">]</mml:mo></mml:math> code, which we call an augmented surface code. The distance of the augmented surface code is the product of the distance of the surface code with that of the small code, and the union-find decoder, with slight modifications, can decode errors up to half the distance. We present numerical simulations, showing that while the threshold of these augmented codes is lower than that of the surface code, the low noise performance is improved.
Genetic Risk Score for Serum 25-Hydroxyvitamin D Concentration Helps to Guide Personalized Vitamin D Supplementation in Healthy Finnish Adults (2021)

Background Genetic factors modify serum 25-hydroxyvitamin D [25(OH)D] concentration and can affect the optimal intake of vitamin D. Objectives We aimed to personalize vitamin D supplementation by applying knowledge of genetic factors affecting serum 25(OH)D concentration. Methods We performed a genome-wide association study of serum 25(OH)D concentration in the Finnish Health 2011 cohort (n = 3339) using linear regression and applied the results to develop a population-matched genetic risk score (GRS) for serum 25(OH)D. This GRS was used to tailor vitamin D supplementation for 96 participants of a longitudinal Digital Health Revolution (DHR) Study. The GRS, serum 25(OH)D concentrations, and personalized supplementation and dietary advice were electronically returned to participants. Serum 25(OH)D concentrations were assessed using immunoassays and vitamin D intake using FFQs. In data analyses, cross-sectional and repeated-measures statistical tests and models were applied as described in detail elsewhere. Results GC vitamin D-binding protein and cytochrome P450 family 2 subfamily R polypeptide 1 genes showed genome-wide significant associations with serum 25(OH)D concentration. One single nucleotide polymorphism from each locus (rs4588 and rs10741657) was used to develop the GRS. After returning data to the DHR Study participants, daily vitamin D supplement users increased from 32.6% to 60.2% (P = 6.5 × 10-6) and serum 25(OH)D concentration from 64.4 ± 20.9 nmol/L to 68.5 ± 19.2 nmol/L (P = 0.006) between August and November. Notably, the difference in serum 25(OH)D concentrations between participants with no risk alleles and those with 3 or 4 risk alleles decreased from 20.7 nmol/L to 8.0 nmol/L (P = 0.0063). Conclusions We developed and applied a population-matched GRS to identify individuals genetically predisposed to low serum 25(OH)D concentration. We show how the electronic return of individual genetic risk, serum 25(OH)D concentrations, and factors affecting vitamin D status can be used to tailor vitamin D supplementation. This model could be applied to other populations and countries.
The clinical behavior of „mixed” small cell/large cell bronchogenic carcinoma compared to „pure” small cell subtypes (1982)

Biopsy specimens from 19 previously untreated lung cancer patients were prospectively diagnosed as small cell carcinoma with a large cell component. The patients were thoroughly staged and received intensive combination chemotherapy. They represented 12% of all small cell carcinoma cases eligible for aggressive chemotherapy protocols during a 5.5 year period. To determine whether the clinical behavior of this "mixed" histologic variant differed from the other histologic subtypes of small cell lung cancer, we compared these 19 patients to a concurrent group of 103 patients with only small cell cancer in their diagnostic biopsies given equivalent therapy. The "mixed" histology patients were comparable to the "pure" small cell group in age, performance status, extent of disease, and frequency of bone marrow, liver, bone, and central nervous system metastases. Their complete plus partial response rare (58%) was significantly less than the response rate for the "pure" small cell patients (91%), their complete response rate was also lower (16 versus 46%), and their overall survival was significantly shorter (median, 6 versus 10.5 months) Mixed histology small cell/large cell carcinoma represents a distinct pathologic variant of small cell carcinoma of the lung, associated with lower response rates and shorter survival than the "pure" small cell subtypes. Since combination chemotherapy yields some complete responses and long-term disease-free survival in these patients, however, aggressive treatment with potentially curative intent should be considered in their management.
Effects of Vitis vinifera leaf extracts on inflammation and vascular permeability (2022)

Wine production leads to large amounts of by-products, such as leaves, which are rich in flavonoids that are effective in venous insufficiency [1], [2]. Venous insufficiency results from venous hypertension and leads to edema, skin lesions and eventually venous ulceration. It is characterized by increased vascular leakage, inflammation factors (IL-6, TGF-1), adhesion molecules (sICAM, sVCAM) and metalloproteases (MMP2, MMP9). Here, we investigated the effect of Vitis vinifera leaf extracts on inflammation and vascular permeability. Human endothelial (EA. hy926) and fibroblast (DLF) cell lines were pretreated with six leaf extracts (1 µg/ml). Inflammation was induced by TNA-α (100 ng/ml). Twenty-four hours following TNF-α stimulation, the levels of secreted IL-6, TGF-β1, sVCAM, sICAM and MMP9 levels were quantified with ELISA. The two most effective extracts were tested in the carrageenan (2% w/v)-induced paw edema model and the VEGF (50 ng)-induced vascular leakage model in mice, using the EVANS blue method. The aqueous extract E13 and the enriched phenolic fraction E15 were the most effective in reducing TNF-α induced IL-6, TGF-β1, sICAM, sVCAM and MMP9 in both EA. hy925 and DLF cells. Also, E13 (30 mg/Kg) and E15 (30 mg/Kg) reduced carrageenan-induced edema and E13 (30 mg/Kg and 100 mg/Kg) significantly reduced vascular leakage induced by VEGF. In summary, the aqueous extract E13, effectively reduced inflammation and vascular leakage in vitro and in vivo suggesting it could be further evaluated in humans suffering from venous insufficiency.
Fast Facts: Renal Disorders (2013)

Early detection of renal problems coupled with the appropriate therapeutic strategy can radically reduce the progressive nature of, and complications associated with, chronic kidney disease, and in many instances will result in the successful treatment of acute kidney injury. As many patients will not be seen by nephrologists, it is essential that
Discovery, Synthesis, and Structure–Activity Relationships of Conotoxins (2014)

International audience
Methodology of Echo State Neural Network To Diagnose Human Depression (2015)

Depression is common in working personality due to high tension in the working environment. Symptoms can affect dayto-day life and can become very worrying. With true depression, there is a low mood and other symptoms each day for more than two weeks. Symptoms can also become rigorous enough to interfere with normal day-to-day activities. This paper suggests an Artificial Neural Network (ANN) algorithm approach for quicker learning of psychological depression data. Performance of neural network methods for estimating depression state with Echo State Neural Network (ESNN) is presented. Tentative data were collected from the patients with 21 input variables. One target output is used for training the ESNN. The training and testing patterns are made using the data as per Hamilton Rating Scale.The input patterns are pre-processed and presented to the input layer of ANN. The proposed method proves to be a capable system for diagnosis of depression. Keywords: Depression Data, ESNN, Hamilton Rating Scale
Simultaneous production of isopropanol, butanol, ethanol and 2,3-butanediol by Clostridium acetobutylicum ATCC 824 engineered strains (2012)

Isopropanol represents a widely-used commercial alcohol which is currently produced from petroleum. In nature, isopropanol is excreted by some strains of Clostridium beijerinckii, simultaneously with butanol and ethanol during the isopropanol butanol ethanol (IBE) fermentation. In order to increase isopropanol production, the gene encoding the secondary-alcohol dehydrogenase enzyme from C. beijerinckii NRRL B593 (adh) which catalyzes the reduction of acetone to isopropanol, was cloned into the acetone, butanol and ethanol (ABE)-producing strain C. acetobutylicum ATCC 824. The transformants showed high capacity for conversion of acetone into isopropanol (> 95%). To increase isopropanol production levels in ATCC 824, polycistronic transcription units containing, in addition to the adh gene, homologous genes of the acetoacetate decarboxylase (adc), and/or the acetoacetyl-CoA:acetate/butyrate:CoA transferase subunits A and B (ctfA and ctfB) were constructed and introduced into the wild-type strain. Combined overexpression of the ctfA and ctfB genes resulted in enhanced solvent production. In non-pH-controlled batch cultures, the total solvents excreted by the transformant overexpressing the adh, ctfA, ctfB and adc genes were 24.4 g/L IBE (including 8.8 g/L isopropanol), while the control strain harbouring an empty plasmid produced only 20.2 g/L ABE (including 7.6 g/L acetone). The overexpression of the adc gene had limited effect on IBE production. Interestingly, all transformants with the adh gene converted acetoin (a minor fermentation product) into 2,3-butanediol, highlighting the wide metabolic versatility of solvent-producing Clostridia.
5-Fluoro-2-methyl-N-[4-(5H-pyrrolo[2,1-c]- [1,4]benzodiazepin-10(11H)-ylcarbonyl)-3- chlorophenyl]benzamide (VPA-985):  An Orally Active Arginine Vasopressin Antagonist with Selectivity for V2Receptors (1998)

ADVERTISEMENT RETURN TO ISSUEPREVLetterNEXT5-Fluoro-2-methyl-N-[4-(5H-pyrrolo[2,1-c]- [1,4]benzodiazepin-10(11H)-ylcarbonyl)-3- chlorophenyl]benzamide (VPA-985): An Orally Active Arginine Vasopressin Antagonist with Selectivity for V2 ReceptorsJ. Donald Albright, Marvin F. Reich, Efren G. Delos Santos, John P. Dusza, Fuk-Wah Sum, Aranapakam M. Venkatesan, Joseph Coupet, Peter S. Chan, Xun Ru, Hossein Mazandarani, and Trina BaileyView Author Information Wyeth-Ayerst Research, Pearl River, New York 10965, and Wyeth-Ayerst Research, Princeton, New Jersey 08543-8000 Cite this: J. Med. Chem. 1998, 41, 14, 2442–2444Publication Date (Web):June 16, 1998Publication History Received23 March 1998Published online16 June 1998Published inissue 1 July 1998https://pubs.acs.org/doi/10.1021/jm980179chttps://doi.org/10.1021/jm980179crapid-communicationACS PublicationsCopyright © 1998 American Chemical SocietyRequest reuse permissionsArticle Views1035Altmetric-Citations125LEARN 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 SUBJECTS:Antagonists,Receptors,Rodent models,Screening assays,Selectivity Get e-Alerts
Development of walking analysis system consisting of mobile force plate and motion sensor (2011)

In walking analysis, which is one useful method for efficient physical rehabilitation, the ground reaction force, the center of pressure, and the body orientation data are measured during walking. In the past, these data were measured by a 3D motion analysis system consisting of high-speed cameras and force plates, which must be installed in the floor. However, a conventional 3D motion analysis system can measure the ground reaction force and the center of pressure just on force plates during a few steps. In addition, the subjects' stride lengths are limited because they have to walk on the center of the force plate. These problems can be resolved by converting conventional devices into wearable devices. We used a measuring device consisting of portable force plates and motion sensors. We developed a walking analysis system that calculates the ground reaction force, the center of pressure, and the body orientations and measured a walking subject to estimate this system. We simultaneously used a conventional 3D motion analysis system to compare with our development system and showed its validity for measurements of ground reaction force and the center of pressure.
Structural and magnetic properties of La0.5Ca0.5MnO3 (abstract) (1997)

The nuclear and magnetic structures of the perovskite La0.5Ca0.5MnO3 were studied as a function of temperature. At low temperatures this system exhibits charge ordering and a magnetic structure of a charge exchange-type in the a–c plane with a ferromagnetic component along the b axis. At intermediate temperatures there is a purely ferromagnetic phase. In this intermediate ferromagnetic phase we find charge ordering associated with antiferromagnetic short-range order. We find no evidence that would support the existence of a charge ordered purely ferromagnetic structure.
RETRACTED - Clergy Sexual Abuse and an Ethics of Recognition: An Example of the #ChurchToo Movement in South Korea (2022)

RETRACTION NOTICE: This article has been retracted at the request of its author, David Kwon. The author acknowledges citation irregularities throughout the article as the reason for the retraction. The editors of the journal supports this retraction. The article will only be available with this retraction notice.
Supplemental Figure 8 from Combination Drug Scheduling Defines a “Window of Opportunity” for Chemopotentiation of Gemcitabine by an Orally Bioavailable, Selective ChK1 Inhibitor, GNE-900 (2023)

&lt;p&gt;Pharmacokinetics of GNE-900 in female CD-1 mice or male Sprague-Dawley rats.&lt;/p&gt;