gebhart/patrepeval huggingface dataset:
Topical Caspofungin for Treatment of Keratitis Caused by Candida albicans in a Rabbit Model (2005)

Candida albicans is the most frequent cause of fungal keratitis in temperate regions. Caspofungin has potent activity against Candida spp. in a variety of clinical settings. Little is known, however, about its activity against fungal keratitis. We compared the efficacy of topical caspofungin with that of topical amphotericin B (AMB) in a rabbit model of experimental keratomycosis. Keratitis was induced with a standardized inoculum of Candida albicans (SC 5314) placed on the debrided cornea. Twenty-four hours after infection, animals were randomly assigned to treatment with 0.15% caspofungin, 0.5% caspofungin, 0.15% AMB, and a saline control (n = 12 rabbits in each group). For the first 12 h, treatment was repeated every 30 min and, after a 12-h pause, was resumed at hourly intervals for another 12 h. The animals were examined and killed 12 h after administration of the last dose. Treatment effects were evaluated by clinical assessment, fungal culture, and histopathology. Drug treatment significantly reduced corneal fungal recovery from 3.78 log10 CFU in saline-treated animals to 2.97, 1.76, and 1.18 log10 CFU in animals treated with 0.15% caspofungin, 0.5% caspofungin, and 0.15% AMB, respectively. By histopathology, the mean hyphal density was significantly lower in the corneas of treated animals than in those of the controls; there was no difference in hyphal densities between the different treatment groups. The depth of corneal invasion was not significantly reduced by the antifungal treatments. By clinical assessment, keratitis progressed in animals treated with saline, whereas disease progression was inhibited by all drug treatment regimens. In our rabbit model, 0.5% caspofungin was as effective as 0.15% AMB for the topical treatment of Candida keratitis. The potential clinical efficacy of caspofungin awaits further investigation.
Turbo coded OFDM system with peak power reduction (2003)

We propose three turbo coded Orthogonal frequency-division multiplexing (OFDM) systems which can mitigate the peak to average power ratio (PAPR) problem.For the first, we use long maximum-length sequences as test sequences to increase the capability of PAPR reduction and use a short code to protect the side information.Sufficient protection of the side information is obtained by increasing the power of subcarriers corresponding to the short code.For the second, we use several distinct interleavers to yield output symbols with various PAPR and then select the one with the lowest PAPR.In this way, no side information is needed.For the third, a combination of test sequences and interleavers are used.Simulation results show that all the three systems can achieve significant PAPR reduction and satisfactory error performance over AWGN channels.
Identification of preferred hTBP DNA binding sites by the combinatorial method REPSA (1997)

Here we describe the application of a novel combinatorial method, restriction endonuclease protection selection and amplification (REPSA), to identification of a consensus DNA binding site for the TATA binding subunit (hTBP) of the human general transcription factor TFIID. Unlike most combinatorial methods, REPSA is based on inhibition of an enzymatic template inactivation process by specific ligand-DNA complexes. The mild conditions of this method allow examination of proteins with atypical binding characteristics (e.g. limited discrimination between specific and non-specific binding sites), such as those found with hTBP. Analysis of 57 emergent sequences identified 47 sequences containing consensus 6 bp TATA elements as previously defined. However, further examination of these sequences indicated that a larger consensus, 5'-TATAAATA-3', could be supported by the data. Studies of the binding affinities and transcriptional activities of these four consensus TATA sequences demonstrated that hTBP binding affinity correlated directly with transcriptional activity in vitro and that the TATAAATA sequence was the best among the TATA sequences investigated.
MicroRNA Gene Expression Deregulation in Human Breast Cancer (2005)

MicroRNAs (miRNAs) are a class of small noncoding RNAs that control gene expression by targeting mRNAs and triggering either translation repression or RNA degradation. Their aberrant expression may be involved in human diseases, including cancer. Indeed, miRNA aberrant expression has been previously found in human chronic lymphocytic leukemias, where miRNA signatures were associated with specific clinicobiological features. Here, we show that, compared with normal breast tissue, miRNAs are also aberrantly expressed in human breast cancer. The overall miRNA expression could clearly separate normal versus cancer tissues, with the most significantly deregulated miRNAs being mir-125b, mir-145, mir-21, and mir-155. Results were confirmed by microarray and Northern blot analyses. We could identify miRNAs whose expression was correlated with specific breast cancer biopathologic features, such as estrogen and progesterone receptor expression, tumor stage, vascular invasion, or proliferation index.
The Eye and Visual Optical Instruments (1997)

There is a wide variety of optical instruments where the human eye forms an integral part of the overall system. This book provides a detailed description of the visual ergonomics of such instruments. The book begins with a section on image formation and basic optical components. The various optical instruments that can be adequately described using geometrical optics are then discussed, followed by a section on diffraction and interference, and the instruments based on these effects. There are separate sections devoted to ophthalmic instruments and aberration theory, with a final section covering visual ergonomics in depth. Containing many problems and solutions, this book will be of great use to undergraduate and graduate students of optometry, optical design, optical engineering, and visual science, and to professionals working in these and related fields.
Discovery of the Dual Orexin Receptor Antagonist [(7R)-4-(5-Chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the Treatment of Insomnia (2010)

Despite increased understanding of the biological basis for sleep control in the brain, few novel mechanisms for the treatment of insomnia have been identified in recent years. One notable exception is inhibition of the excitatory neuropeptides orexins A and B by design of orexin receptor antagonists. Herein, we describe how efforts to understand the origin of poor oral pharmacokinetics in a leading HTS-derived diazepane orexin receptor antagonist led to the identification of compound 10 with a 7-methyl substitution on the diazepane core. Though 10 displayed good potency, improved pharmacokinetics, and excellent in vivo efficacy, it formed reactive metabolites in microsomal incubations. A mechanistic hypothesis coupled with an in vitro assay to assess bioactivation led to replacement of the fluoroquinazoline ring of 10 with a chlorobenzoxazole to provide 3 (MK-4305), a potent dual orexin receptor antagonist that is currently being tested in phase III clinical trials for the treatment of primary insomnia.
The p50 subunit of NF-kappa B associates with the NF-IL6 transcription factor. (1992)

The NF-kappa B-p50 polypeptide, a member of the Rel family of transcription factors, was produced as a fusion protein containing amino-terminal peptide additions that facilitate purification and detection with a monoclonal antibody and specific radiolabeling by phosphorylation in vitro. The 32P-labeled NK-kappa B-p50 fusion polypeptide was used as the probe in Western blotting experiments and in screenings of a bacteriophage expression library to isolate cDNAs encoding interacting protein domains. As expected, cDNAs encoding proteins of the Rel family were identified. Surprisingly, the 32P-labeled NF-kappa B protein also specifically bound to proteins encoded by cDNAs for the human NF-IL6 transcription factor. The NF-kappa B-p50 and NF-IL6 proteins directly interact, and the Rel homology domain and leucine-zipper motif, respectively, are important for this interaction. Since induction of the NF-kappa B and NF-IL6 factors are important events in immune and acute-phase responses, this interaction could permit coregulation of genes.
Role of Leukotriene B4Receptors in the Development of Atherosclerosis: Potential Mechanisms (2003)

The effects of LTB4 in atherosclerosis are likely mediated through the high-affinity BLT-1 and the low-affinity BLT-2 receptors. LTB4 promotes atherosclerosis by chemo-attracting monocytes, by providing an amplification loop of monocyte chemotaxis via CCL2 production, and by converting monocytes to foam cells by enhanced expression of CD36 and fatty acid accumulation.
Hexamethylene-1,6-bis-t-amines in Which Part of the Six Carbon Chain is also Part of a Six-membered Ring (1956)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTHexamethylene-1,6-bis-t-amines in Which Part of the Six Carbon Chain is also Part of a Six-membered RingFreeman H. McMillan, Kenneth A. Kun, Carol B. McMillan, and John A. KingCite this: J. Am. Chem. Soc. 1956, 78, 16, 4077–4081Publication Date (Print):August 1, 1956Publication History Published online1 May 2002Published inissue 1 August 1956https://pubs.acs.org/doi/10.1021/ja01597a058https://doi.org/10.1021/ja01597a058research-articleACS PublicationsRequest reuse permissionsArticle Views145Altmetric-Citations6LEARN 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
A Frame-Based Language in Information Retrieval (1988)

With the advent of the information society, many researchers are turning to artificial intelligence techniques to provide effective retrieval over large bodies of textual information. Yet any AI system requires a formalism for encoding its knowledge about the objects of its knowledge, the world, and the intelligence that it is designed to manifest. In the CODER system, the mission of which is to provide an environment for experiments in applying AI to information retrieval, that formalism is provided by a single well defined factual representation language. Designed as a flexible tool for retrieval research, the CODER factual representation language is a hybrid AI language involving a system of strong types for attribute values, a frame system, and a system of Prolog-like relational structures. Inheritance is enforced throughout, and the semantics of type subsumption and object matching formally defined. A collection of type and object managers called the knowledge administration complex implements this common language for storing knowledge and communicating it within the system. Of the three types of knowledge structures in the language, the frame facility has proven most useful in the retrieval domain. The factual representation language is implemented in Prolog as a set of predicates accessible to all system modules. Each level of knowledge representation (elementary primitives, frames, and relations) has a type manager; the frame and relation levels also have object managers. Storage of complete knowledge objects (statements in the factual representation language) is supported by a system or external knowledge bases. One paper discusses the frame construct itself, the implementation of the knowledge administration complex and external knowledge bases. and the use of the construct in retrieval research. The paper closes with a discussion of the utility of the language in experiments.
Dysbiosis in the Gut Microbiota of Patients with Multiple Sclerosis, with a Striking Depletion of Species Belonging to Clostridia XIVa and IV Clusters (2015)

The pathogenesis of multiple sclerosis (MS), an autoimmune disease affecting the brain and spinal cord, remains poorly understood. Patients with MS typically present with recurrent episodes of neurological dysfunctions such as blindness, paresis, and sensory disturbances. Studies on experimental autoimmune encephalomyelitis (EAE) animal models have led to a number of testable hypotheses including a hypothetical role of altered gut microbiota in the development of MS. To investigate whether gut microbiota in patients with MS is altered, we compared the gut microbiota of 20 Japanese patients with relapsing-remitting (RR) MS (MS20) with that of 40 healthy Japanese subjects (HC40) and an additional 18 healthy subjects (HC18). All the HC18 subjects repeatedly provided fecal samples over the course of months (158 samples in total). Analysis of the bacterial 16S ribosomal RNA (rRNA) gene by using a high-throughput culture-independent pyrosequencing method provided evidence of a moderate dysbiosis in the structure of gut microbiota in patients with MS. Furthermore, we found 21 species that showed significant differences in relative abundance between the MS20 and HC40 samples. On comparing MS samples to the 158 longitudinal HC18 samples, the differences were found to be reproducibly significant for most of the species. These taxa comprised primarily of clostridial species belonging to Clostridia clusters XIVa and IV and Bacteroidetes. The phylogenetic tree analysis revealed that none of the clostridial species that were significantly reduced in the gut microbiota of patients with MS overlapped with other spore-forming clostridial species capable of inducing colonic regulatory T cells (Treg), which prevent autoimmunity and allergies; this suggests that many of the clostridial species associated with MS might be distinct from those broadly associated with autoimmune conditions. Correcting the dysbiosis and altered gut microbiota might deserve consideration as a potential strategy for the prevention and treatment of MS.
The utility of the microcrystalline cellulose sphere as a particulate embolic agent: an experimental study. (2000)

Because CELPHERE beads are easy to handle, highly biocompatible, and have few adverse effects, they are suitable for intravascular applications.
Gastrin-releasing peptide receptor expression in non-cancerous bronchial epithelia is associated with lung cancer: a case-control study (2012)

GRPR expression in non-cancerous bronchial epithelium was significantly associated with the presence of lung cancer in never and former smokers. The association in never and former smokers was found in males and females. Association with lung cancer did not differ by sex in any smoking group.
Remediation of Cr(VI) and Pb(II) Aqueous Solutions Using Supported, Nanoscale Zero-valent Iron (2000)

Borohydride reduction of an aqueous iron salt in the presence of a support material gives supported zero-valent iron nanoparticles that are 10−30 nm in diameter. The material is stable in air once it has dried and contains 22.6% iron by weight. The supported zero-valent iron nanoparticles (“Ferragels”) rapidly separate and immobilize Cr(VI) and Pb(II) from aqueous solution, reducing the chromium to Cr(III) and the Pb to Pb(0) while oxidizing the Fe to goethite (α-FeOOH). The kinetics of the reduction reactions are complex and include an adsorption phase. About 10% of the iron in the material appears to be located at active surface sites. Once these sites have been saturated, the reduction process continues but at a much lower rate, which is likely limited by mass transfer. Rates of remediation of Cr(VI) and Pb(II) are up to 30 times higher for Ferragels than for iron filings or iron powder on a (Fe) molar basis. Over 2 months, reduction of Cr(VI) was 4.8 times greater for Ferragels than for an equal weight of commercial iron filings (21 times greater on the basis of moles of iron present). The higher rates of reaction, and greater number of moles of contaminant reduced overall, suggest that Ferragels may be a suitable material for in situ remediation.
Low-temperature (≤200 °C) plasma enhanced atomic layer deposition of dense titanium nitride thin films (2012)

Titanium nitride (TiN) has been widely used in the semiconductor industry for its diffusion barrier and seed layer properties. However, it has seen limited adoption in other industries in which low temperature (&amp;lt;200 °C) deposition is a requirement. Examples of applications which require low temperature deposition are seed layers for magnetic materials in the data storage (DS) industry and seed and diffusion barrier layers for through-silicon-vias (TSV) in the MEMS industry. This paper describes a low temperature TiN process with appropriate electrical, chemical, and structural properties based on plasma enhanced atomic layer deposition method that is suitable for the DS and MEMS industries. It uses tetrakis-(dimethylamino)-titanium as an organometallic precursor and hydrogen (H2) as co-reactant. This process was developed in a Veeco NEXUS™ chemical vapor deposition tool. The tool uses a substrate rf-biased configuration with a grounded gas shower head. In this paper, the complimentary and self-limiting character of this process is demonstrated. The effects of key processing parameters including temperature, pulse time, and plasma power are investigated in terms of growth rate, stress, crystal morphology, chemical, electrical, and optical properties. Stoichiometric thin films with growth rates of 0.4–0.5 Å/cycle were achieved. Low electrical resistivity (&amp;lt;300 μΩ cm), high mass density (&amp;gt;4 g/cm3), low stress (&amp;lt;250 MPa), and &amp;gt;85% step coverage for aspect ratio of 10:1 were realized. Wet chemical etch data show robust chemical stability of the film. The properties of the film have been optimized to satisfy industrial viability as a Ruthenium (Ru) preseed liner in potential data storage and TSV applications.
Changes in Solution Color During Phenol Oxidation by Fenton Reagent (2006)

Fenton reaction is a highly effective treatment for degrading phenolic compounds in an aqueous solution. However, during phenol oxidation, the oxidized water takes on a dark brown color associated with increased toxicity. Then, although phenol can be completely removed, if the oxidation process is not carried out properly, the final wastewater will be brown in color and have higher toxicity, two parameters in which legislation imposes restrictions. This paper analyzes the development of the dark color observed in the solution under oxidation treatment and formulates a reaction mechanism to explain the color generation. The experiments were carried out following the batch-wise procedure, but with the solution pH being kept constant throughout the reaction at its optimum value for phenol removal, i.e., pH 3.0. It is checked experimentally that color is formed at the beginning of the reaction in less than five minutes, and follows the kinetic-path of a reaction intermediate. During the first steps of the reaction phenol is degraded to dihydroxylated rings (catechol, resorcinol, and hydroquinone). These aromatic intermediates generate higher colored compounds such as ortho- and parabenzoquinone. On the other hand the dihydroxylated rings can react with their own quinones to generate charge-transfer complexes (quinhydrone), compounds which take on a dark color at low concentrations. Moreover, when iron reacts with hydrogen peroxide, ferric ions are generated that can be coordinated to benzene rings to produce colored metal complexes. The observed color of the solution is not a fortuitous result depending on trace components of low significance, but depends directly on the main reaction intermediates, so it is concluded that observed color depends on the level of oxidation reached. The maximum color observable during oxidation treatment (A(o)) depends only on initial phenol concentration and not on oxidant or catalyst doses.
Total Synthesis of Chloropeptin II (Complestatin) and Chloropeptin I (2009)

The first total synthesis of chloropeptin II (1, complestatin) is disclosed. Key elements of the approach include the use of an intramolecular Larock indole synthesis for the initial macrocyclization, adopting conditions that permit utilization of a 2-bromoaniline, incorporating a terminal alkyne substituent (-SiEt(3)) that sterically dictates the indole cyclization regioselectivity, and benefiting from an aniline protecting group (-Ac) that enhances the atropdiastereoselectivity and diminishes the strained indole reactivity toward subsequent electrophilic reagents. Not only did this key reaction provide the fully functionalized right-hand ring system of 1 in superb conversion (89%) and good atropdiastereoselectivity (4:1 R:S), but it also represents the first reported example of what will prove to be a useful Larock macrocyclization strategy. Subsequent introduction of the left-hand ring system enlisting an aromatic nucleophilic substitution reaction for macrocyclization with biaryl ether formation completed the assemblage of the core bicyclic structure of 1. Intrinsic in the design of the approach and by virtue of the single-step acid-catalyzed conversion of chloropeptin II (1) to chloropeptin I (2), the route also provides a total synthesis of 2.
Immune Activation by Life-Shortening Wolbachia and Reduced Filarial Competence in Mosquitoes (2009)

Wolbachia strain wMelPop reduces the longevity of its Drosophila melanogaster host and, when introduced into the mosquito Aedes aegypti, halves its life span. We show that wMelPop induces up-regulation of the mosquito's innate immune system and that its presence inhibits the development of filarial nematodes in the mosquito. These data suggest that wMelPop could be used in the global effort to eliminate lymphatic filariasis and possibly for the control of other mosquito-borne parasites where immune preactivation inhibits their development. The cost of constitutive immune up-regulation may contribute to the life-shortening phenotype.
An efficient synthesis of 2-amino-4-(4-fluoro-3-(2-fluoropyridin-3-yl)phenyl)-4-(4-methoxy-3-methylphenyl)-1-methyl-1H-imidazol-5(4H)-one, a potent BACE1 inhibitor (2009)

An efficient method has been developed for the synthesis of 2-amino-4-(4-fluoro-3-(2fluoropyridin-3-yl)phenyl)-4-(4-methoxy-3-methylphenyl)-1-methyl-1H-imidazol-5(4H)-one, a potent BACE1 inhibitor for the potential treatment of Alzheimer's Disease. The new method features a Friedel-Crafts reaction between 3-bromo-4-fluorophenylacetic acid and 2methoxytoluene followed by DMSO mediated -oxidation of the resulting 1,2-diarylethanone to give an -diketone. Subsequent aminohydantoin formation and Suzuki coupling led to the target molecule in greater than 70% overall yield.