gebhart/patrepeval huggingface dataset:
Novel Carbamates as Potent Histamine H3Receptor Antagonists with Highin Vitroand Oralin VivoActivity, (1996)

The known histamine H3 receptor antagonists burimamide, thioperamide, clobenpropit, and a related homohistamine thioamide derivative were taken as templates in search for new leads. Novel histamine H3 receptor antagonists structurally described as carbamate derivatives of 3-(1H-imidazol-4-yl)propanol were prepared in high yields by treatment of the alcohol with corresponding isocyanates or carbamoyl chlorides and investigated for their H3 receptor antagonist activity. Different chain lengths and various substituents possessing different electronic and steric parameters were introduced and structure-activity relationships established. In different functional tests, the new antagonists showed high H3 receptor antagonist potencies in vitro (-log Ki values of 6.4-8.4) at synaptosomes of rat cerebral cortex and low activities at histamine H1 and H2 receptor subtypes. They were also screened for their central in vivo activity in mice after peroral administration. The most promising compounds (2, 16, 19) showed ED(50) values of about 1-2 mg/kg and thus are potential drugs for the therapy of H3 receptor dependent diseases. Some of the novel carbamate derivatives are H3 receptor selective compounds with high in vitro and in vivo activity.
Intra-Golgi Transport Inhibition by Megalomicin (1996)

Megalomicin (MGM) is a macrolide antibiotic which has been demonstrated previously to cause an anomalous glycosylation of viral proteins. Here we show that MGM produces profound alterations on Golgi morphology and function. The addition of MGM at 50 microM for 1 h caused a dilation of the Golgi detected by immunofluorescence staining for medial- and trans-Golgi markers. The effect of MGM was clearly more intense on the trans-side of the Golgi, as evidenced in electron microscope preparations. The effect on Golgi morphology was reversible and correlated with an impairment of glycoprotein processing in the trans-Golgi. Thus, although the vesicular stomatitis virus G protein was processed in the presence of MGM to an endoglycosidase H-resistant form, it was poorly sialylated. The sialylation of cellular proteins was also inhibited, resulting in cells with low level of sialylation on the cell surface. However MGM did not inhibit the activities of the galactosyl- or sialyltransferase as measured in vitro. MGM inhibited cis- to medial-, and more strongly, medial- to trans-Golgi transport of vesicular stomatitis virus G protein in an in vitro system, suggesting that the impairment in glycoprotein maturation observed in vivo is the result of intra-Golgi transport inhibition.
What Is the Effective Charge of TGA-Stabilized CdTe Nanocolloids? (2005)

The surface charge of semiconductor nanoparticles, Q, is an important parameter which determines their electrokinetic behavior, stability in water and polar solvents, functions of optical and electronic devices, self-assembly properties, and interactions with cell membranes. We have developed a simple method for quantitative determination of Q in their native aqueous environment. The method does not require the knowledge of exact atomic structure or make assumptions about effects of drying on charge distribution. The method is based on titration of nanoparticle dispersion with a solution of oppositely charged polyelectrolyte. The point of complete neutralization is recognized as an inflection point on the dependence of fluorescence intensity on the amount of polyelectrolyte added. Thioglycolic acid-stabilized CdTe nanoparticles 2 nm in diameter were found to carry an average Q from -2.6 to -5.5 for pH 7.5 to 10, respectively. This charge is found to be smaller than that calculated theoretically for an analogous structure (i.e., Q = -8), presumably due to adsorption of Cd(2+) ions on the stabilizer shell and on Te atoms with unsaturated valence located on the side planes of CdTe tetrahedrons.
Effects of Optical Combiner and IPD Change for Convergence on Near-Field Depth Perception in an Optical See-Through HMD (2015)

Many error sources have been explored in regards to the depth perception problem in augmented reality environments using optical see-through head-mounted displays (OST-HMDs). Nonetheless, two error sources are commonly neglected: the ray-shift phenomenon and the change in interpupillary distance (IPD). The first source of error arises from the difference in refraction for virtual and see-through optical paths caused by an optical combiner, which is required of OST-HMDs. The second occurs from the change in the viewer's IPD due to eye convergence. In this paper, we analyze the effects of these two error sources on near-field depth perception and propose methods to compensate for these two types of errors. Furthermore, we investigate their effectiveness through an experiment comparing the conditions with and without our error compensation methods applied. In our experiment, participants estimated the egocentric depth of a virtual and a physical object located at seven different near-field distances (40∼200 cm) using a perceptual matching task. Although the experimental results showed different patterns depending on the target distance, the results demonstrated that the near-field depth perception error can be effectively reduced to a very small level (at most 1 percent error) by compensating for the two mentioned error sources.
Ultrafast ablation with high-pulse-rate lasers. Part I: Theoretical considerations (1999)

We propose a novel ultrafast pulsed laser deposition (PLD) technique, which eliminates the well-known problem of contamination of the films produced by PLD with particulates ejected from the target. The method uses low energy, picosecond duration laser pulses delivered onto a target at rates of several tens of MHz and thus differs from conventional the PLD method which utilizes high energy, nanosecond duration pulses delivered at low (≈10 Hz) repetition rates. In this article we present the theoretical background justifying the method and define the optimal conditions for efficient evaporation of a target with given thermodynamic properties. By reducing the laser pulse energy while maintaining optimum evaporation, the number of atoms evaporated by each pulse is reduced to the point where it becomes impossible for macroscopic lumps of material to be ejected with the available laser energy, thus preventing the source of particle contamination in the film. To achieve high evaporation rate, the laser pulse repetition rate is increased. We compare our theoretical predictions with literature reports of optimal evaporation in a number of experiments, while in part II of this article we describe a specific experimental study where the method is applied to the production of amorphous carbon thin films.
ChemInform Abstract: CARBOXYLATION OF 2‐HYDROXYPICOLINES (1978)

Abstract Die Carboxylierung der Hydroxypicoline (I) bzw. (V) liefert die Carbonsäuren (II) bzw. (VI), die unabhängig auch ausgehend von den Aminen (IV) bzw. (VIII) durch Hydrolyse der aus diesen erhältlichen Nitrile (III) bzw. (VII) (gleiche Reaktionsfolge) dargestellt werden.
Domain 5 of high molecular weight kininogen (kininostatin) down-regulates endothelial cell proliferation and migration and inhibits angiogenesis (2000)

We have demonstrated that high molecular weight kininogen (HK) binds specifically on endothelial cells to domain 2/3 of the urokinase receptor (uPAR). Inhibition by vitronectin suggests that kallikrein-cleaved HK (HKa) is antiadhesive. Plasma kallikrein bound to HK cleaves prourokinase to urokinase, initiating cell-associated fibrinolysis. We postulated that HK cell binding domains would inhibit angiogenesis. We found that recombinant domain 5 (D5) inhibited endothelial cell migration toward vitronectin 85% at 0.27 microM with an IC(50) (concentration to yield 50% inhibition) = 0.12 microM. A D5 peptide, G486-K502, showed an IC(50) = 0.2 microM, but a 25-mer peptide from a D3 cell binding domain only inhibited migration 10% at 139 microM (IC(50) > 50 microM). D6 exhibited weaker inhibitory activity (IC(50) = 0.50 microM). D5 also potently inhibited endothelial cell proliferation with an IC(50) = 30 nM, while D3 and D6 were inactive. Using deletion mutants of D5, we localized the smallest region for full activity to H441-D474. To further map the active region, we created a molecular homology model of D5 and designed a series of peptides displaying surface loops. Peptide 440-455 was the most potent (IC(50) = 100 nM) in inhibiting proliferation but did not inhibit migration. D5 inhibited angiogenesis stimulated by fibroblast growth factor FGF2 (97%) in a chicken chorioallantoic membrane assay at 270 nM, and peptide 400-455 was also inhibitory (79%). HK D5 (for which we suggest the designation, "kininostatin") is a potent inhibitor of endothelial cell migration and proliferation in vitro and of angiogenesis in vivo. (Blood. 2000;95:543-550)
Regulation and Functions of the IL-10 Family of Cytokines in Inflammation and Disease (2011)

The IL-10 family of cytokines consists of nine members: IL-10, IL-19, IL-20, IL-22, IL-24, IL-26, and the more distantly related IL-28A, IL-28B, and IL-29. Evolutionarily, IL-10 family cytokines emerged before the adaptive immune response. These cytokines elicit diverse host defense mechanisms, especially from epithelial cells, during various infections. IL-10 family cytokines are essential for maintaining the integrity and homeostasis of tissue epithelial layers. Members of this family can promote innate immune responses from tissue epithelia to limit the damage caused by viral and bacterial infections. These cytokines can also facilitate the tissue-healing process in injuries caused by infection or inflammation. Finally, IL-10 itself can repress proinflammatory responses and limit unnecessary tissue disruptions caused by inflammation. Thus, IL-10 family cytokines have indispensable functions in many infectious and inflammatory diseases.
Differential regulation of human thymosin beta 15 isoforms by transforming growth factor beta 1 (2009)

We recently identified an additional isoform of human thymosin beta 15 (also known as NB-thymosin beta, gene name TMSB15A) transcribed from an independent gene, and designated TMSB15B. The purpose of this study was to investigate whether these isoforms were differentially expressed and functional. Our data show that the TMSB15A and TMSB15B isoforms have distinct expression patterns in different tumor cell lines and tissues. TMSB15A was expressed at higher levels in HCT116, DU145, LNCaP, and LNCaP-LN3 cancer cells. In MCF-7, SKOV-3, HT1080, and PC-3MLN4 cells, TMSB15A and TMSB15B showed approximately equivalent levels of expression, while TMSB15B was the predominant isoform expressed in PC-3, MDA-MB-231, NCI-H322, and Caco-2 cancer cells. In normal human prostate and prostate cancer tissues, TMSB15A was the predominant isoform expressed. In contrast, normal colon and colon cancer tissue expressed predominantly TMSB15B. The two gene isoforms are also subject to different transcriptional regulation. Treatment of MCF-7 breast cancer cells with transforming growth factor beta 1 repressed TMSB15A expression but had no effect on TMSB15B. siRNA specific to the TMSB15B isoform suppressed cell migration of prostate cancer cells to epidermal growth factor, suggesting a functional role for this second isoform. In summary, our data reveal different expression patterns and regulation of a new thymosin beta 15 gene paralog. This may have important consequences in both tumor and neuronal cell motility.
Oncofetal fibronectins in oral carcinomas: (1994)

Different isoforms of fibronectin are derived from a single gene by alternative processing of the primary RNA transcript or by posttranslational modifications. We have previously demonstrated that an oncofetal fibronectin (FN) isoform derived by O-glycosylation is highly associated with malignancy in breast and oral tumors. Another oncofetal FN isoform containing the ED-B sequence is derived by alternative splicing, and FN containing ED-B has been found to be a stromal marker of malignancies in various tissues. Here we report a comparative study by immunohistology of the distribution of the ED-B-containing isoform and the oncofetal FN isoform derived by O-glycosylation, in oral squamous cell carcinomas, premalignant lesions, and normal oral mucosa. A selective expression of the ED-B-containing isoform was demonstrated in close relation to the invading carcinoma (38/38), whereas there was virtually no staining in submucosa underlying premalignant lesions (1/11) and normal epithelium (0/5). The ED-B-containing FN showed close co-distribution and staining pattern with the oncofetal isoform derived by O-glycosylation. These results demonstrate that accumulation of FN adjacent to oral carcinomas includes both the ED-B-containing isoform and the isoform derived by O-glycosylation. Although both the change in primary structure and glycosylation of FN create conformational and immunologically detectable changes, the functional consequences in association with invasive carcinoma are poorly understood at present. Diagnostic implications especially of borderline lesions as well as evaluation of tumor aggressiveness may, however, be important.
The ISO/MPEG Unified Speech and Audio Coding Standard—Consistent High Quality for All Content Types and at All Bit Rates (2013)

In early 2012 the ISO/IEC JTC1/SC29/WG11 (MPEG) finalized the new MPEG-D Unified Speech and Audio Coding standard. The new codec brings together the previously separated worlds of general audio coding and speech coding. It does so by integrating elements from audio coding and speech coding into a unified system. The present publication outlines all aspects of this standardization effort, starting with the history and motivation of the MPEG work item, describing all technical features of the final system, and further discussing listening test results and performance numbers which show the advantages of the new system over current state-of-the-art codecs. Copyright
Melanoma genetics and the development of rational therapeutics (2005)

Melanoma is a cancer of the neural crest-derived cells that provide pigmentation to skin and other tissues. Over the past 4 decades, the incidence of melanoma has increased more rapidly than that of any other malignancy in the United States. No current treatments substantially enhance patient survival once metastasis has occurred. This review focuses on recent insights into melanoma genetics and new therapeutic approaches being developed based on these advances.
Derivate der Zucker‐mercaptale, XVIII. Synthese und Derivate der 2.5‐Didesoxy‐D‐ribose (1959)

Abstract Das 2‐Desoxy‐ D ‐ribose‐dimethylmercaptal wird mit Tosylchlorid in Pyridin partiell zum 5‐Tosyl‐2‐desoxy‐ D ‐ribose‐dimethylmercaptal tosyliert, welches sich mit LiAlH 4 zum kristallisierten 2.5‐Didesoxy‐ D ‐ribose‐dimethylmercaptal reduzieren läßt. Daraus gewinnt man durch Abspalten von Mercaptan die 2.5‐Didesoxy‐ D ‐ribose. Das 2.5‐Didesoxy‐ D ‐ribose‐mercaptal kann in ein kristallisiertes Bis‐phenylurethan und in das 3.4‐Diacetyl‐2.5‐didesoxy‐ D ‐ribose‐mercaptal übergeführt werden. Letzteres ergibt nach Abspalten von Mercaptan die 3.4‐Diacetyl‐2.5‐didesoxy‐ al ‐ D ‐ribose. Die 1.3‐Diacetyl‐2.5‐didesoxy‐ D ‐ribofuranose wird durch Acetylieren der 2.5‐Didesoxy‐ D ‐ribose gewonnen.
Dirt cheap web-scale parallel text from the Common Crawl (2013)

Parallel text is the fuel that drives modern machine translation systems. The Web is a comprehensive source of preexisting parallel text, but crawling the entire web is impossible for all but the largest companies. We bring web-scale parallel text to the masses by mining the Common Crawl, a public Web crawl hosted on Amazon 19s Elastic Cloud. Starting from nothing more than a set of common two-letter language codes, our open-source extension of the STRAND algorithm mined 32 terabytes of the crawl in just under a day, at a cost of about \$500. Our large-scale experiment uncovers large amounts of parallel text in dozens of language pairs across a variety of domains and genres, some previously unavailable in curated datasets. Even with minimal cleaning and filtering, the resulting data boosts translation performance across the board for five different language pairs in the news domain, and on open domain test sets we see improvements of up to 5 BLEU. We make our code and data available for other researchers seeking to mine this rich new data resource.
Microlens diffusers for efficient laser speckle generation (2007)

Laser Speckle is the optical phenomena resulting from the random interference of coherent light. This phenomenon can be utilized to measure the Modulation Transfer Function (MTF) of detector arrays. Common devices used for speckle generation, such as integrating spheres and ground glass, suffer from low efficiencies less than 20%. Microlens diffusers are shown to be more efficient alternatives for speckle generation. An analysis of the statistical behavior of microlens diffusers is presented with emphasis on their application to MTF testing of detector arrays in the visible spectrum.
Monoclonal Antibodies to Human Cell Surface Antigens (2008)

Many of the leukocyte cell surface molecules are known by "CD" numbers. In this Appendix, a short introduction describes the history and the use of CD nomenclature and provides a few key references to enable access to the wider literature. This is followed by a table that lists all human molecules with approved CD names, tabulating alternative names, key structural features, cellular expression, major known functions, and usefulness of the molecules or antibodies against them in research or clinical applications.
Ga-As (808 nm) Laser Irradiation Enhances ATP Production in Human Neuronal Cells in Culture (2007)

Laser application to NHNP cells significantly increases ATP production in these cells. These findings may explain the beneficial effects of low-level laser therapy (LLLT) in stroked rats. Tissue culture of NHNP cells might offer a good model to study the mechanisms associated with promotion of ATP production in the nervous system by LLLT.
Human autoreactive T cells recognize CD1b and phospholipids (2015)

In contrast with the common detection of T cells that recognize MHC, CD1a, CD1c, or CD1d proteins, CD1b autoreactive T cells have been difficult to isolate in humans. Here we report the development of polyvalent complexes of CD1b proteins and carbohydrate backbones (dextramers) and their use in identifying CD1b autoreactive T cells from human donors. Activation is mediated by αβ T-cell receptors (TCRs) binding to CD1b-phospholipid complexes, which is sufficient to activate autoreactive responses to CD1b-expressing cells. Using mass spectrometry and T-cell responses to scan through the major classes of phospholipids, we identified phosphatidylglycerol (PG) as the immunodominant lipid antigen. T cells did not discriminate the chemical differences that distinguish mammalian PG from bacterial PG. Whereas most models of T-cell recognition emphasize TCR discrimination of differing self and foreign structures, CD1b autoreactive T cells recognize lipids with dual self and foreign origin. PG is rare in the cellular membranes that carry CD1b proteins. However, bacteria and mitochondria are rich in PG, so these data point to a more general mechanism of immune detection of infection- or stress-associated lipids.
Effect(s) of the Demineralization Process on the Osteoinductivity of Demineralized Bone Matrix (1997)

The relationships between residual calcium levels and particle size of ground demineralized bone matrix and its osteoinductive potential were investigated using in vitro and in vivo assays. The effects of variable residual calcium levels, variable particle sizes, and donor age and gender were studied using a tissue culture-based bioassay (in vitro) as well as an athymic mouse (in vivo) bioassay. The osteoinductive potential of the bone-derived biomaterial was assessed by measuring the degree of new bone formation (change in percent calcium content after 4 weeks of implantation) in the in vivo assay and levels of alkaline phosphatase activity associated with cultures of human periosteal cells (HPO cells) in the in vitro assay, respectively. Slightly demineralized bone matrix and overly demineralized bone matrix possessed a degree of osteoinductive potential whereas bone demineralized to levels of approximately 2% residual calcium provided for maximum osteoinductive potential in both assay systems. The osteoinductive potential of ground demineralized bone varied relative to the particle size such that DBM particles ranging from 500 to 710 microns provided for the highest level of calcium deposition (increase of 8.1 weight percent calcium) after 4 weeks of implantation in muscle pouches of an athymic mouse, whereas explanted particles less than 250 microns showed the lowest level of calcium deposition (increase of only 2.8 weight percent calcium). In the donor age and gender study, DBM from different donors were divided into 5 age groups for both female and male donor derived bone: less than 20, 21 to 30, 31 to 40, 41 to 50, and 51 to 60 year old age groups. This study indicated that DBM from female donors in the 31 to 40 years old age group and male donors in the 41 to 50 year age group possess the highest osteoinductive potential, whereas DBM derived from donor bone from both female and male donors in the 51 to 60 year age group presented the lowest osteoinductive potential. DBM derived from male and female donors did not in general show significant differences in osteoinductive potential.
Internal Oxidosqualenes: Determination of Absolute Configuration and Activity as Inhibitors of Purified Pig Liver Squalene Epoxidase (1995)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTInternal Oxidosqualenes: Determination of Absolute Configuration and Activity as Inhibitors of Purified Pig Liver Squalene EpoxidaseJose-Luis Abad, Josefina Casas, Francisco Sanchez-Baeza, and Angel MesseguerCite this: J. Org. Chem. 1995, 60, 12, 3648–3656Publication Date (Print):June 1, 1995Publication History Published online1 May 2002Published inissue 1 June 1995https://pubs.acs.org/doi/10.1021/jo00117a014https://doi.org/10.1021/jo00117a014research-articleACS PublicationsRequest reuse permissionsArticle Views313Altmetric-Citations12LEARN 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 (2)»Supporting Information Supporting Information Get e-Alerts