gebhart/patrepeval huggingface dataset:
Pharmacokinetics of flupirtine in elderly volunteers and in patients with moderate renal impairment (1988)

The pharmacokinetics of flupirtine after a single oral dose of 100mg have been studied in patients with moderate renal impairment and in healthy elderly subjects aged 66-83 years. Mean elimination half-life of flupirtine was higher in elderly patients than in younger normal subjects, and this was associated with an increased maximum serum concentration and reduced clearance. The mean half-life in patients with renal impairment was higher than in normal subjects. There was no correlation between observed elimination half-life and degree of renal impairment, but the creatinine clearance of most patients fell in a narrow range between 43 and 60 ml/min. In the light of these results and until further information is available, it would be prudent to start treatment of patients who are elderly or have evidence of renal impairment with half the dose of flupirtine recommended for younger patients with normal renal function.
Effect of an alpha-blocking agent (phenoxybenzamine) in the management of premature ejaculation. (1986)

Phenoxybenzamine has been extremely effective in treating patients with vesical dysfunctions, its minimal side effects include anejaculation and delay and difficulty in ejaculation. Fifteen men were treated with phenoxybenzamine (PBZ) for premature ejaculation. Eight patients reported a subjective improvement of the time from penetration to ejaculation. PBZ is a well tolerated drug. The only side effect of the treatment was dry ejaculation. The Authors suggest its use in selected patients.
The Promoters for Human and Monkey Poliovirus Receptors (1997)

The cellular receptors for poliovirus (PVR) are glycoproteins belonging to the immunoglobulin superfamily. Functional receptors for poliovirus are only expressed by primates; known rodent homologues lack the ability to bind virus due to amino acid differences. Human poliovirus infections are targeted to the gastrointestinal tract and, rarely, to motor neurons in the central nervous system. Available evidence suggests that poliovirus uses only one cellular receptor, implying that the tissue tropism of poliovirus is likely to be related to the expression of the human PVR (hPVR). However, low levels of expression of hPVR-specific mRNAs can be detected in many human tissues other than the apparent target cells. The nonpathogenic function of hPVR is unknown. For a study of the transcriptional control of hPVR expression, we have isolated and characterized the promoter of the hPVR gene. Deletion analysis defined an approximately 280 base pair minimal promoter fragment that: 1) lacks TATA- and CAAT-like elements, 2) is distinguished by a high GC content, and 3) promotes transcription at multiple start sites. The pattern of activity caused by transfection of serial 5'- and 3'-promoter deletions is almost identical in HEp2, HeLa, COS-1, and mouse L929 cells, indicating a similar transcriptional regulation of the hPVR promoter in these cell lines. However, on transfection of Raji cells, a Burkitt's lymphoma cell line harboring a transcriptionally inactive hPVR gene, all promoter reporter constructs tested exerted only residual activity. These results suggest that the cis-element(s) governing cell type-specific hPVR expression resides in the minimal promoter region. We also report the sequences of the promoters of two monkey homologues to hPVR (AGMalpha1 and AGMalpha2). Transcripts encoding the monkey poliovirus receptors originate from a region analogous to that identified for hPVR transcripts.
ChemInform Abstract: Application of a New Combination of Palladium and CaCO<sub>3</sub> for an Aerobic Heck Reaction Using Arenediazonium‐Salts. (1999)

Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.
Ropporin, a sperm-specific binding protein of rhophilin, that is localized in the fibrous sheath of sperm flagella (2000)

The small GTPase Rho; functions as a molecular switch that regulates various cellular processes such as cell adhesion, motility, gene expression and cytokinesis. We previously isolated several putative Rho; targets including rhophilin which bound selectively to the GTP-bound form of Rho;. Rhophilin is expressed highly in testis and is localized specifically in sperm flagella. The presence of a PDZ domain at the carboxy terminus of rhophilin suggested that rhophilin works as an adaptor molecule. To test this hypothesis, we employed a yeast two hybrid system using the rhophilin PDZ domain as a bait, and screened a mouse testis cDNA library. We isolated several positive clones containing the same insert. The open reading frame of the cDNA encoded a novel protein of 212 amino acids designated as ropporin from a Japanese word 'oppo' (the tail). The amino-terminal 40 amino acid sequence of ropporin showed high homology to that of the regulatory subunit of type II cAMP-dependent protein kinase, which is involved in dimerization and binding to A-kinase anchoring proteins. Consistently, a yeast two hybrid assay and gel filtration of recombinant ropporin indicated that ropporin dimerizes through this domain. Deletion analysis indicated that the carboxy-terminal four amino acids are essential for binding of ropporin to rhophilin, and ropporin and RhoV14 coprecipitated in the presence of rhophilin in vitro. Northern blot analysis showed that ropporin is exclusively expressed in testis, and induced at the late stage of spermatogenesis. This induction paralleled that of rhophilin. Immunocytochemistry using anti-ropporin antibody showed that ropporin is localized in the principal piece and the end piece of sperm flagella. Electronmicroscopy revealed that ropporin is mostly localized in the inner surface of the fibrous sheath while rhophilin is present in the outer surface of the outer dense fiber. These results suggest that rhophilin and ropporin may form a complex in sperm flagella.
Low-profile, Modular, Ultra-Wideband Phased Arrays (2022)

Ultrawideband (UWB) phased antenna arrays are critical to the success of future multi-functional communication, sensing, and countermeasure systems, which will utilize a few UWB phased arrays in place of multiple antennas on a platform. The success of this new systems approach relies in part on the ability to manufacture and assemble low-cost UWB phased arrays with excellent radiation characteristics.This dissertation presents the theory and design of a new class of UWB arrays that is based on unbalanced fed tightly-coupled horizontal dipoles over a ground plane. Practical implementation of this concept leads to two inexpensive wideband array topologies, the Banyan Tree Antenna (BTA) Array, and the Planar Ultrawideband Modular Antenna (PUMA) Array. The key challenge in designing unbalanced-fed tightly-coupled dipole arrays lies in the control of a common mode resonance that destroys UWB performance. This work introduces a novel feeding strategy that eliminates this resonance and results in wideband, wide-angle radiation. More importantly, the new feeding scheme is simple and intuitive, and can be implemented at low-cost in both vertically and planarly-integrated phased array architectures. Another desirable byproduct of this topology is the electrical and mechanical modularity of the aperture, which enables easy manufacturability and assembly. A theoretical framework is presented for the new phased array topologies, which is then applied to the design of innite BTA and PUMA arrays that achieve 4:1 and 5:1 bandwidths,respectively. A practical application of this technology is demonstrated through the full design, fabrication, and measurement of a 7.25-21GHz 16x16 dual-pol PUMA array prototype for SATCOM applications.
Statistical Modeling and Reconstruction of Randoms Precorrected PET Data (2006)

Randoms precorrected positron emission tomography (PET) data is formed as the difference of two Poisson random variables. Its exact probability mass function (PMF) is inconvenient for use in likelihood-based iterative image reconstruction as it contains an infinite summation. The shifted Poisson model is a tractable approximation to this PMF but requires that negative values are truncated, resulting in positively biased reconstructions in low count studies. Here we analyze the properties of the exact PMF and propose a simple but accurate approximation that allows negative valued data. We investigate the properties of this approximation and demonstrate its application to penalized maximum likelihood image reconstruction.
A Second-Order Frequency-Aided Digital Phase-Locked Loop for Doppler Rate Tracking (1980)

A second-order digital phase-locked loop (DPLL) has a finite lock range which is a function of the frequency of the incoming signal to be tracked. For this reason, it is not capable of tracking an input with Doppler rate for an indefinite period of time. In this correspondence, an analytical expression for the hold-in time is derived. In addition, an all-digital scheme to alleviate this problem is proposed based on the information obtained from estimating the input signal frequency.
Structure of product‐bound <scp>SMG</scp>1 lipase: active site gating implications (2015)

Monoacylglycerol and diacylglycerol lipases are industrially interesting enzymes, due to the health benefits that arise from the consumption of diglycerides compared to the traditional triglyceride oils. Most lipases possess an α-helix (lid) directly over the catalytic pocket which regulates the activity of the enzyme. Generally, lipases exist in active and inactive conformations, depending on the positioning of this lid subdomain. However, lipase SMG1, a monoacylglycerol and diacylglycerol specific lipase, has an atypical activation mechanism. In the present study we were able to prove by crystallography, in silico analysis and activity tests that only two positions, residues 102 and 278, are responsible for a gating mechanism that regulates the active and inactive states of the lipase, and that no significant structural changes take place during activation except for oxyanion hole formation. The elucidation of the gating effect provided data enabling the rational design of improved lipases with 6-fold increase in the hydrolytic activity toward diacylglycerols, just by providing additional substrate stabilization with a single mutation (F278N or F278T). Due to the conservation of F278 among the monoacylglycerol and diacylglycerol lipases in the Rhizomucor miehei lipase-like family, the gating mechanism described herein might represent a general mechanism applicable to other monoacylglycerol and diacylglycerol lipases as well. Database: Structural data are available in the Protein Data Bank under the accession numbers 4ZRE (F278D mutant) and 4ZRD (F278N mutant).
Genetic improvement of the microalga Phaeodactylum tricornutum for boosting neutral lipid accumulation (2014)

To obtain fast growing oil-rich microalgal strains has been urgently demanded for microalgal biofuel. Malic enzyme (ME), which is involved in pyruvate metabolism and carbon fixation, was first characterized in microalgae here. Overexpression of Phaeodactylum tricornutum ME (PtME) significantly enhanced the expression of PtME and its enzymatic activity in transgenic P. tricornutum. The total lipid content in transgenic cells markedly increased by 2.5-fold and reached a record 57.8% of dry cell weight with a similar growth rate to wild type, thus keeping a high biomass. The neutral lipid content was further increased by 31% under nitrogen-deprivation treatment, still 66% higher than that of wild type. Transgenic microalgae cells exhibited obvious morphological changes, as the cells were shorter and thicker and contained larger oil bodies. Immuno-electron microscopy targeted PtME to the mitochondrion. This study markedly increased the oil content in microalgae, suggesting a new route for developing ideal microalgal strains for industrial biodiesel production.
A Single Nucleotide Polymorphism in MGEA5 Encoding O-GlcNAc–selective <i>N</i>-Acetyl-β-<scp>d</scp> Glucosaminidase Is Associated With Type 2 Diabetes in Mexican Americans (2005)

Excess O-glycosylation of proteins by O-linked beta-N-acetylglucosamine (O-GlcNAc) may be involved in the pathogenesis of type 2 diabetes. The enzyme O-GlcNAc-selective N-acetyl-beta-d glucosaminidase (O-GlcNAcase) encoded by MGEA5 on 10q24.1-q24.3 reverses this modification by catalyzing the removal of O-GlcNAc. We have previously reported the linkage of type 2 diabetes and age at diabetes onset to an overlapping region on chromosome 10q in the San Antonio Family Diabetes Study (SAFADS). In this study, we investigated menangioma-expressed antigen-5 (MGEA5) as a positional candidate gene. Twenty-four single nucleotide polymorphisms (SNPs), identified by sequencing 44 SAFADS subjects, were genotyped in 436 individuals from 27 families whose data were used in the original linkage report. Association tests indicated significant association of a novel SNP with the traits diabetes (P = 0.0128, relative risk = 2.77) and age at diabetes onset (P = 0.0017). The associated SNP is located in intron 10, which contains an alternate stop codon and may lead to decreased expression of the 130-kDa isoform, the isoform predicted to contain the O-GlcNAcase activity. We investigated whether this variant was responsible for the original linkage signal. The variance attributed to this SNP accounted for approximately 25% of the logarithm of odds. These results suggest that this variant within the MGEA5 gene may increase diabetes risk in Mexican Americans.
Validity of the construct of nonverbal memory: A factor-analytic study in a normal elderly sample (1992)

One problem in evaluating the construct of nonverbal memory is finding a purely nonverbal memory measure. Encouraged by initial research with a new measure, the Visual Spatial Learning Test (VSLT), we examined nonverbal memory in a normal elderly sample. Subjects were 460 community-dwelling individuals between the ages of 55-95. All received neuropsychological batteries which included the Wechsler Adult Intelligence Scale-Revised, the Wechsler Memory Scale-Revised, the Rey Auditory Verbal Learning Test, and the VSLT. Two variable sets were created to avoid overlapping immediate and delayed recall trials for the same stimulus materials. Exploratory factor analyses using two different extraction methods were performed. Across analyses a single general memory factor was observed, no modality or time specific factors were found. If it can be assumed that we used adequate measures of nonverbal memory, our results combine with prior research to challenge the validity of the construct of nonverbal memory as distinct from verbal memory, especially in older normal adult populations.
La empresa digital en la Sociedad de la Información y de las Comunicaciones (2001)

De entre los cambios previsibles en los principios rectores que ha de regir la nueva era, destaca el papel de Internet como instrumento educativo orientado hacia el aprendizaje de la realidad global, siendo la educacion el pilar esencial para lograr un uso mas correcto de la red. 
Ademas del progreso tecnologico, la sociedad digital conlleva un cambio de valores hacia el optimismo tolerante, visiones globales y compromisos locales, fruto de un aprendizaje innovador y anticipativo y viene caracterizada por superar los limites al crecimiento existentes para el entorno industrial previo. Su aplicacion es le factor mas importante del crecimiento y del empleo, dando lugar a la economia.
Der frühhallstättische Hortfund von Schönberg in Steiermark (2017)

[nicht vorhanden / not available]
Molecular Recognition at the Membrane−Water Interface: Controlling Integral Peptide Helices by Off-Membrane Nucleobase Pairing (2010)

The aggregation and organization of membrane proteins and transmembrane peptides is related to the interacting molecular species itself and strongly depends on the lipid environment. Because of the complexity and dynamics of these interactions, they are often hardly traceable and nearly impossible to predict. For this reason, peptide model systems are a valuable tool in studying membrane associated processes since they are synthetically accessible and can be readily modified. To control and study the aggregation of peptide transmembrane domains (TMDs) the interacting interfaces of the TMDs themselves can be altered. A second less extensively studied approach targets the TMD assembly by using interaction and recognition of domains at the membrane outside as frequently found in the membrane protein interplay and protein assembly. In the present study, double helical transmembrane domains were designed and synthesized on the basis of a recently reported d,l-alternating peptide pore motif derived from gramicidin A. The highly hydrophobic and aromatic transmembrane peptide was covalently functionalized with a short peptide nucleic acid (PNA) used as specific outer-membrane recognition unit. The PNA sequences were chosen with high polarity to ensure localization within the aqueous phase. To estimate the impact of the membrane adjacent recognition on the TMD assembly by Förster resonance energy transfer (FRET), fluorescence probes were covalently attached to the side chains of the membrane spanning peptide helices. Dimerization of the TMD-peptide/PNA conjugates within unilamellar lipid vesicles was observed. The dimer/monomer ratio of TMDs can be controlled by temperature variation.
Selective Killing of Dormant Mycobacterium tuberculosis by Marine Natural Products (2017)

The dormant phenotype acquired by <i>Mycobacterium tuberculosis</i> during infection poses a major challenge in disease treatment, since these bacilli show tolerance to front-line drugs. Therefore, it is imperative to find novel compounds that effectively kill dormant bacteria. By screening 4,400 marine natural product samples against dual-fluorescent <i>M. tuberculosis</i> under both replicating and nonreplicating conditions, we have identified compounds that are selectively active against dormant <i>M. tuberculosis</i> This validates our strategy of screening all compounds in both assays as opposed to using the dormancy model as a secondary screen. Bioassay-guided deconvolution enabled the identification of unique pharmacophores active in each screening model. To confirm the activity of samples against dormant <i>M. tuberculosis</i>, we used a luciferase reporter assay and enumerated CFU. The structures of five purified active compounds were defined by nuclear magnetic resonance (NMR) and mass spectrometry. We identified two lipid compounds with potent activity toward dormant and actively growing <i>M. tuberculosis</i> strains. One of these was commercially obtained and showed similar activity against <i>M. tuberculosis</i> in both screening models. Furthermore, puupehenone-like molecules were purified with potent and selective activity against dormant <i>M. tuberculosis</i> In conclusion, we have identified and characterized antimycobacterial compounds from marine organisms with novel activity profiles which appear to target <i>M. tuberculosis</i> pathways that are conditionally essential for dormancy survival.
Partial Sequence Analysis of 130 Randomly Selected Maize cDNA Clones (1993)

As part of a project to identify novel maize (Zea mays L. cv B73) genes functionally, we have partially sequenced 130 randomly selected clones from a maize leaf cDNA library. Data base comparisons revealed seven previously sequenced maize cDNAs and 18 cDNAs with sequence similarity to related maize genes or to genes from other organisms. One hundred five cDNAs show little or no similarity to previously sequenced genes. Our results also establish the suitability of this library for large-scale sequencing in terms of its large insert size, proper insert orientation, and low duplication rate.
Recommending what video to watch next (2019)

In this paper, we introduce a large scale multi-objective ranking system for recommending what video to watch next on an industrial video sharing platform. The system faces many real-world challenges, including the presence of multiple competing ranking objectives, as well as implicit selection biases in user feedback. To tackle these challenges, we explored a variety of soft-parameter sharing techniques such as Multi-gate Mixture-of-Experts so as to efficiently optimize for multiple ranking objectives. Additionally, we mitigated the selection biases by adopting a Wide & Deep framework. We demonstrated that our proposed techniques can lead to substantial improvements on recommendation quality on one of the world's largest video sharing platforms.
Protein Engineering of the Quaternary Sulfiredoxin·Peroxiredoxin Enzyme·Substrate Complex Reveals the Molecular Basis for Cysteine Sulfinic Acid Phosphorylation (2009)

Oxidative stress can damage the active site cysteine of the antioxidant enzyme peroxiredoxin (Prx) to the sulfinic acid form, Prx-SO(2)(-). This modification leads to inactivation. Sulfiredoxin (Srx) utilizes a unique ATP-Mg(2+)-dependent mechanism to repair the Prx molecule. Using selective protein engineering that involves disulfide bond formation and site-directed mutagenesis, a mimic of the enzyme.substrate complex has been trapped. Here, we present the 2.1 A crystal structure of human Srx in complex with PrxI, ATP, and Mg(2+). The Cys(52) sulfinic acid moiety was substituted by mutating this residue to Asp, leading to a replacement of the sulfur atom with a carbon atom. Because the Srx reaction cannot occur, the structural changes in the Prx active site that lead to the attack on ATP may be visualized. The local unfolding of the helix containing C52D resulted in the packing of Phe(50) in PrxI within a hydrophobic pocket of Srx. Importantly, this structural rearrangement positioned one of the oxygen atoms of Asp(52) within 4.3 A of the gamma-phosphate of ATP bound to Srx. These observations support a mechanism where phosphorylation of Prx-SO(2)(-) is the first chemical step.
A New Data Transformation Method for Cbers-02b Multi-Spectral Images (2012)

According to the detailed studies on the data of China-Brazil earth resources satellite-02B (CBERS-02B) and the LBV data transform method proposed by the previous researcher, a new LBV data transformation equations for CBERS-02B data was specially proposed. A transformation experiment on CBERS-02B data showed that the LBV transformed result images were more vivid, and the features of result images were more easily to be classified than the fault color composite images of original bands. In order to evaluate the performance of this proposed method, the maximum likelihood supervised classification method was used. The final classification results showed that the accuracy of the LBV transformed image is obviously better than that of the fault color composite images of original bands, which demonstrated that the proposed LBV transformation method for CBERS-02B has good potential for CBERS-02B data in the future applications.
Cancellation of metal‐induced MRI artifacts with dual‐component paramagnetic and diamagnetic material: Mathematical modelization and experimental verification (1996)

A mathematical model of dual-component paramagnetic and diamagnetic material to cancel metal-induced MRI artifacts was developed and verified experimentally. The magnetization produced by metallic material and then the gradient linearity distortion can be cancelled by using such materials with opposing paramagnetic and diamagnetic properties. This concept of dual-component materials provides a novel solution to the problem of MRI artifacts.
SARS-CoV-2 spike therapeutic antibodies in the age of variants (2021)

Christos Kyratsous, Vice President of Research, Infectious Diseases, and Viral Vector Technologies at Regeneron Pharmaceuticals, and Alina Baum, Associate Director, Infectious Diseases Associate at Regeneron Pharmaceuticals, discuss the development of antibody therapeutics targeting the spike protein of SARS-CoV-2.