gebhart/patrepeval huggingface dataset:
Motilin and motilin receptors: characterization and functional significance. (2001)

In order to get more insight into the mechanism of action of the gastrointestinal peptide, motilin, and its role in human physiology, we aimed at characterizing motilin and motilin receptors. Motilin. Sequence analysis of the motilin precursor from several species indicated that the N- and C-terminal regions of the motilin precursor have evolved at different rates. Sequence analysis of the motilin precursor in brain tissue of rabbit and man and motilin radioimmunoassay on tissue extracts, proved that motilin is a brain-gut peptide. Plasma motilin levels are increased in patients with ulcerative colitis or Crohn's disease. A weak correlation between the motilin genotype and the susceptibility to inflammatory bowel disease was demonstrated. Motilin receptors. Motilin receptors are expressed early postnatally and can be regulated by changes in its plasma level. The pharmacophore of motilin consists of the aromatic rings from Phe1 and Tyr7 and the aliphatic side chains from Val2 and Ile4. In vivo and in vitro studies showed that in the rabbit and human antrum, smooth muscle and neuronal motilin receptors exist which have different characteristics. In the rabbit duodenum motilin's action depends upon the influx of extra- and intracellular Ca2+. Nevertheless, in primary smooth muscle cultures, Ca2+ influx through L-type Ca2+ channels is the major transduction mechanism. The existence of central motilin receptors was demonstrated by autoradiography. Receptor binding studies allowed the identification of two binding sites. In contrast to antral smooth muscle cells, the response to motilin in the human TE671 medulloblastoma cell line, expressing the motilin receptor, relies on intracellular IP3-sensitive Ca2+ stores. The antibiotic erythromycin-A (EM-A) binds to the motilin receptor and induces contractions with the same regional and species specificity as motilin. This interaction was supported by the discovery of motilin antagonists. Structure activity studies led to the development of more powerful erythromycin derivatives, which lack antibiotic properties and which are now in clinical trial for treatment of hypomotility disorders. Conclusion and perspectives. The physiological role of motilin and its receptors in the brain requires further investigation. Erythromycin and its derivatives act as motilin agonists with clinically useful prokinetic potential. The motilin receptor has recently been cloned and has substantial structural homology with the growth hormone secretagogue receptor. This may not only lead to the further characterization of motilin receptor subtypes and aid the development of safe and selective motilin receptor agonists and antagonists, useful for the treatment of GI disorders, but may also give a new dimension to the role of motilin in human physiology.
Glycosylation Reactions with a (4-Alkoxypentadienyl)oxy Leaving Group Linking the Glycosyl Donor and the Acceptor Moiety (1999)

ADVERTISEMENT RETURN TO ISSUEPREVNoteNEXTGlycosylation Reactions with a (4-Alkoxypentadienyl)oxy Leaving Group Linking the Glycosyl Donor and the Acceptor MoietyGötz Scheffler and Richard R. SchmidtView Author Information Fakultät Chemie, Universität Konstanz, Fach M 725, D-78457 Konstanz, Germany Cite this: J. Org. Chem. 1999, 64, 4, 1319–1325Publication Date (Web):January 22, 1999Publication History Received24 September 1997Published online22 January 1999Published inissue 1 February 1999https://pubs.acs.org/doi/10.1021/jo971778ehttps://doi.org/10.1021/jo971778ebrief-reportACS PublicationsCopyright © 1999 American Chemical SocietyRequest reuse permissionsArticle Views419Altmetric-Citations16LEARN 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 SUBJECTS:Aromatic compounds,Carbohydrates,Ethers,Free radicals,Solvents Get e-Alerts
Synergism between distinct enhanson domains in viral induction of the human beta interferon gene. (1990)

This study demonstrates distinct virus-inducible enhanson properties for three regions of the human beta interferon (IFN-beta) promoter; maximum virus inducibility required syngerism among all three enhansons. Expression of the IRF-1 transcription factor differentially increased the expression of plasmids containing (AAGTGA)4 or PRDIII (-94 to -78) motifs but was inefficient in the induction of the intact IFN-beta promoter. The human T-cell lymphotropic virus type I Tax protein was a strong positive activator of PRDII (-64 to -55)-containing plasmids but was also unable to stimulate the IFN-beta promoter. Induction of the intact IFN-beta promoter linked to a reporter plasmid was achieved in lymphoid and epithelioid cellular backgrounds by a triple transfection with IRF-1 and Tax expression plasmids or a combination of IRF-1 and phorbol ester, indicating that at least two trans-activating events and the association of two proteins on the promoter template are required for IFN-beta activation.
Ellipticine derivatives (1975)

Several acyloxy and alkyl derivatives of ellipticine have been prepared. In addition, a modified synthesis leading to the hitherto unobtainable 8,9-dimethoxy- and 8,9-methylenedioxyellipticines is described. Some of the derivatives described herein exhibit antitumor activity. However, none of the compounds showed activity superior to that of the naturally occurring pyridocarbazoles, ellipticine and 9-methoxyellipticine.
Self-Indexing RDF Archives (2016)

Although Big RDF management is an emerging topic in the so-called Web of Data, existing techniques disregard the dynamic nature of RDF data. These RDF archives evolve over time and need to be preserved and queried across it. This paper presents v-RDFCSA, an RDF archiving solution that extends RDFCSA (an RDF self-index) to provide version-based queries on top of compressed RDF archives. Our experiments show that v-RDFCSA reduces space requirements up to 35 - 60 times over a state-of-the-art baseline, and gets more than one order of magnitude ahead over it for query resolution.
Thin-Film Optical Constants Determined from Infrared Reflectance and Transmittance Measurements (1989)

A general method based upon reflectance and transmittance measurements in the infrared region has been developed for the determination of the optical constants n( v) and k( v) of thin films deposited on any substrate (transparent or not). The corresponding computer program, written in FORTRAN 77, involves three main parts: (1) a matrix formalism to compute reflection and transmission coefficients of multilayered systems; (2) an iterative Newton-Raphson method to estimate the optical constants by comparison of the calculated and experimental values; and (3) a fast Kramers-Krönig transform to improve the accuracy of calculating the refractive index. The first part of this program can be used independently to simulate reflection and transmission spectra of any multilayered system using various experimental conditions. Two practical examples are given for illustration. Simulation of reflection spectra at grazing incidence for thin films deposited on a metal surface and determination of the optical constants for thin CaF 2 layers deposited on a silicon substrate are presented.
Stability Analysis and Improvement for SSCB With Single-Gate Controlled Series-Connected SiC MOSFETs (2020)

Silicon carbide-based solid-state circuit breaker (SSCB) exhibits superior performance in dealing with the interruption of dc short-circuit current compared with the mechanical switch. The blocking voltage of commercially available SiC devices still cannot meet the voltage requirements. Series-connected SiC mosfets providing higher blocking voltage based SSCB with the single-gate driver has been proposed previously. However, the sustained oscillation phenomenon, unacceptable false gate-trigger, and severely unbalanced voltage distribution have been observed after the energy-absorbing stage in the circuit. These phenomena are mainly caused by the capacitor coupling mechanism among the two series-connected devices due to specific circuit configuration. This article elaborates on the mechanism of the oscillation by establishing the small-signal models. Based on the stability criterion analysis, an effective damping method is proposed to improve the stability of the SSCB. Simulation and experimental tests have been conducted to verify the effectiveness of the proposed damping method.
Performance of closed-loop power control for a multiple-channel mobile station in the cdma2000 system (2003)

We investigate the reverse link power control of the cdma2000 system where multiple traffic channel signals of different data rates are code-multiplexed and transmitted in a multipath Rayleigh fading environment. In particular, we evaluate the performance of a closed-loop power control scheme utilizing one power control command for all traffic channels. Simulation results show that the use of one common power control command may not be optimal for all code-multiplexed channel signals of different data rates. This is largely due to the different variations in the effective bit signal-to-interference-plus-noise ratios (SINRs) for a given fading rate in a multipath fading channel. With an observation of the performance improvement by more than 1 dB, we propose to use independent power control for each channel signal.
Structure of the Murine <i>lck</i> Gene and Its Rearrangement in a Murine Lymphoma Cell Line (1988)

The lck gene encodes a lymphocyte-specific protein-tyrosine kinase that is implicated in neoplastic transformation. We have determined the germ line organization of the murine lck gene and have isolated and characterized a rearranged lck allele in the murine lymphoma cell line LSTRA. The overall exon-intron organization of the normal lck gene is almost identical to that of avian c-src. In LSTRA DNA, an internally rearranged Moloney murine leukemia virus genome is interposed between two distinct promoters that normally generate lck transcripts differing only in 5' untranslated regions. The rearrangement appears to have been selected to permit splicing of transcripts that initiate from the Moloney virus promoter to an acceptor site located within the first exon 3' to the downstream promoter, thus generating an lck mRNA with a novel 5' untranslated region that may be more efficiently translated.
AdipoRon, the first orally active adiponectin receptor activator, attenuates postischemic myocardial apoptosis through both AMPK-mediated and AMPK-independent signalings (2015)

Adiponectin (APN) is a cardioprotective molecule. Its reduction in diabetes exacerbates myocardial ischemia/reperfusion (MI/R) injury. Although APN administration in animals attenuates MI/R injury, multiple factors limit its clinical application. The current study investigated whether AdipoRon, the first orally active molecule that binds APN receptors, may protect the heart against MI/R injury, and if so, to delineate the involved mechanisms. Wild-type (WT), APN knockout (APN-KO), and cardiomyocyte specific-AMPK dominant negative (AMPK-DN) mice were treated with vehicle or AdipoRon (50 mg/kg, 10 min prior to MI) and subjected to MI/R (30 min/3-24 h). Compared with vehicle, oral administration of AdipoRon to WT mice significantly improved cardiac function and attenuated postischemic cardiomyocyte apoptosis, determined by DNA ladder formation, TUNEL staining, and caspase-3 activation (all P < 0.01). MI/R-induced apoptotic cell death was significantly enhanced in mice deficient in either APN (APN-KO) or AMPK (AMPK-DN). In APN-KO mice, AdipoRon attenuated MI/R injury to the same degree as observed in WT mice. In AMPK-DN mice, AdipoRon's antiapoptotic action was partially inhibited but not lost. Finally, AdipoRon significantly attenuated postischemic oxidative stress, as evidenced by reduced NADPH oxidase expression and superoxide production. Collectively, these results demonstrate for the first time that AdipoRon, an orally active APN receptor activator, effectively attenuated postischemic cardiac injury, supporting APN receptor agonists as a promising novel therapeutic approach treating cardiovascular complications caused by obesity-related disorders such as type 2 diabetes.
QoS-Aware Task Offloading in Distributed Cloudlets with Virtual Network Function Services (2017)

Pushing the cloud frontier to the network edge has attracted tremendous interest not only from cloud operators of the IT service/software industry but also from network service operators that provide various network services for mobile users. In particular, by deploying cloudlets in metropolitan area networks, network service providers can provide various network services through implementing virtualized network functions to meet the demands of mobile users. In this paper we formulate a novel task offloading problem in a metropolitan area network, where each offloaded task requests a specific network function with a maximum tolerable delay and different offloading requests may require different network services. We aim to maximize the number of requests admitted while minimizing their admission cost within a finite time horizon. We first show that the problem is NP-hard, and then devise an efficient algorithm through reducing the problem to a series of minimum eight maximum matching in auxiliary bipartite graphs. We also consider dynamic changes of offloading request patterns over time, and develop an effective prediction mechanism to release and/or create instances of network functions in different cloudlets for cost savings. We finally evaluate the performance of the proposed algorithms through experimental simulations. Experimental results indicate that the proposed algorithms are promising.
Increasing design changeability using dynamical partial reconfiguration (2009)

Recent questions of physics lead to the construction of high energy physic experiments like ALICE at CERN or CBM at FAIR. Since research goals evolve over the lifetime of such experiments, it must be possible to change the functionality of filters and other processing units after their installation. Hence, it has been common for years, to utilize reconfigurable FPGAs for data filtering and data forwarding. This paper illustrates how a dynamical partial reconfiguration framework can help to significantly increase the changeability of these FPGAs regarding typical data acquisition applications and algorithms, which finally leads to a better capacity utilization and thus enables cost and energy savings.
Nylon coil actuator operating temperature range and stiffness (2015)

Components in automotive and aerospace applications require a wide temperature range of operation. Newly discovered thermally active Baughman muscle potentially provides affordable and viable solutions for driving mechanical devices by heating them from room temperature, but little is known about their operation below room temperature. We study the mechanical behavior of nylon coil actuators by testing elastic modulus and by investigating tensile stroke as a function of temperature. Loads that range from 35 MPa to 155 MPa were applied. For the nylon used and the coiling conditions, active thermal contraction totals 19.5 % when the temperature is raised from -40 °C to 160 °C. The thermal contraction observed from -40 °C to 20°C is only ~2 %, whereas between 100 and 160 °C the contraction is 10 %. A marked increase in thermal contraction is occurs in the vicinity of the glass transition temperature (~ 45°C). The elastic modulus drops as temperature increases, from ~155 MPa at – 40 °C to 35 MPa at 200 °C. Interestingly the drop in active contraction with increasing load is small and much less than might be expected given the temperature dependence of modulus.
Vasopressin Antagonists as Anxiolytics and Antidepressants: Recent Developments (2008)

A compelling case for the potential utility of vasopressin (AVP) antagonists as a novel therapeutic class for the treatment of stress-related affective illness has emerged based on observations in depressed individuals, findings in animal models of anxiety and depression, and an understanding of changes in hypothalamic-pituitary-adrenal (HPA) axis regulation under chronic stress. The scientific bases for vasopressin antagonists as a pharmacotherapy for anxiety and depression include: 1) the neuroadaptation and dysregulation of HPA function that accompanies chronic stress in affected humans and in animal models of anxiety and depression, 2) recognition that AVP, not corticotrophin releasing factor (CRF), drives HPA function associated with chronic psychological stress, 3) the CNS localization of vasopressin V1a and V1b receptors in limbic system regions involved in HPA regulation and control of social behaviors, and 4) preclinical data showing efficacy in animal models employed as screens for anxiolytic and antidepressant activity. The public health need for new pharmaceutical treatments for stress-related affective illness is well documented. In the United States alone, anxiety and depression affect some 40 million people each year and carry a conservatively estimated annual total economic burden of at least $125 billion. Existing pharmacotherapies for both indications are not uniformly effective and frequently have undesirable side effects. These limitations demonstrate that a new treatment approach through vasopressin receptor antagonism in the CNS may offer significant opportunities for improved outcomes. In this review, the development of compounds in this class since 2005 is considered. The most advanced clinical candidates and newer compounds described in recent patents are presented.
Part-of-speech tagging using a Variable Memory Markov model (1994)

We present a new approach to disambiguating syntactically ambiguous words in context, based on Variable Memory Markov (VMM) models. In contrast to fixed-length Markov models, which predict based on fixed-lenth histories, variable memory Markov models dynamically adapt their history length based on the training data, and hence may use fewer parameters. In a test of a VMM based tagger on the Brown corpus, 95.81% of tokens are correctly classified.
Autonomic consequences of cerebral hemisphere infarction. (1994)

Power spectral analysis of heart rate variability can detect autonomic consequences of stroke. The spectral data predict that, to the degree that cardiac arrhythmia is produced by unbalanced cardiac autonomic activity favoring the sympathetic system, such arrhythmias could be seen after stroke of either hemisphere and would be more common after cerebral infarction on the right. This is consistent with evidence from the recent literature.
Efficacy of epidermal growth factor receptor targeting in advanced chordoma: case report and literature review (2011)

We report the fourth case of advanced chordoma treated with an EGFR inhibitor. We also review the literature concerning the rationale and potential of EGFR targeting in chordoma.
The retinoblastoma protein: a master tumor suppressor acts as a link between cell cycle and cell adhesion (2014)

<i>RB1</i> was the first tumor suppressor gene discovered. Over four decades of work have revealed that the Rb protein (pRb) is a master regulator of biological pathways influencing virtually every aspect of intrinsic cell fate including cell growth, cell-cycle checkpoints, differentiation, senescence, self-renewal, replication, genomic stability and apoptosis. While these many processes may account for a significant portion of <i>RB1</i>'s potency as a tumor suppressor, a small, but growing stream of evidence suggests that <i>RB1</i> also significantly influences how a cell interacts with its environment, including cell-to-cell and cell-to-extracellular matrix interactions. This review will highlight pRb's role in the control of cell adhesion and how alterations in the adhesive properties of tumor cells may drive the deadly process of metastasis.
A policy for leishmaniasis with respect to the prevention and control of drug resistance (2001)

At the moment no country has a policy designed to control or prevent drug resistance in leishmaniasis. The risk of resistance is high in areas of anthroponotic visceral leishmaniasis, for example North Bihar, India, where the rate in some areas is 60%. Post-epidemic Sudan is also at risk. Zoonotic areas in which HIV co-infection is common could also be at risk as sandflies can become infected from co-infected individuals. Many factors determine the choice of drug for the treatment of visceral leishmaniasis, and drug resistance may not be the over-riding priority. In anthroponotic areas reduction in transmission through public health measures will be important, but the use of two drugs in combination should be seriously considered. Pharmacokinetic and other features of the drugs available, relevant to their use in combination are discussed and tentative suggestions made concerning trials of possible combinations. These include miltefosine plus paromomycin and allopurinol plus an azole. Lessons may be learnt from the experiences of similar problems in malaria, leprosy and tuberculosis. Guidelines are offered for the introduction of policies to use drugs in combination, which differ between anthroponotic and zoonotic areas of transmission.
IL-3 expression by myeloma cells increases both osteoclast formation and growth of myeloma cells (2003)

Macrophage inflammatory protein-1 alpha (MIP-1 alpha) gene expression is abnormally regulated in multiple myeloma (MM) owing to imbalanced expression of the acute myeloid leukemia-1A (AML-1A) and AML-1B transcription factors. We hypothesized that the increased expression ratios of AML-1A to AML-1B also induced abnormal expression of other hematopoietic and bone-specific genes that contribute to the poor prognosis of MM patients with high levels of MIP-1 alpha. We found that interleukin-3 (IL-3) was also induced by the imbalanced AML-1A and AML-1B expression in myeloma. IL-3 mRNA levels were increased in CD138+ purified myeloma cells with increased AML-1A-to-AML-1B expression from MM patients, and IL-3 protein levels were significantly increased in freshly isolated bone marrow plasma from MM patients (66.4 +/- 12 versus 22.1 +/- 8.2 pg/mL; P = .038). IL-3 in combination with MIP-1 alpha or receptor activator of nuclear factor-kappa B ligand (RANKL) significantly enhanced human osteoclast (OCL) formation and bone resorption compared with MIP-1 alpha or RANKL alone. IL-3 stimulated the growth of interleukin-6 (IL-6)-dependent and IL-6-independent myeloma cells in the absence of IL-6, even though IL-3 did not induce IL-6 expression by myeloma cells. These data suggest that increased IL-3 levels in the bone marrow microenvironment of MM patients with imbalanced AML-1A and AML-1B expression can increase bone destruction and tumor cell growth.