gebhart/patrepeval huggingface dataset:
RS‐127445: a selective, high affinity, orally bioavailable 5‐HT2B receptor antagonist (1999)

Efforts to define precisely the role of 5-HT2B receptors in normal and disease processes have been hindered by the absence of selective antagonists. To address this deficiency, we developed a series of naphthylpyrimidines as potentially useful 5-HT2B receptor antagonists. RS-127445 (2-amino-4-(4-fluoronaphth-1-yl)-6-isopropylpyrimidine) was found to have nanomolar affinity for the 5-HT2B receptor (pKi = 9.5+/-0.1) and 1,000 fold selectivity for this receptor as compared to numerous other receptor and ion channel binding sites. In cells expressing human recombinant 5-HT2B receptors, RS-127445 potently antagonized 5-HT-evoked formation of inositol phosphates (pK(B) = 9.5+/-0.1) and 5-HT-evoked increases in intracellular calcium (pIC50 = 10.4+/-0.1). RS-127445 also blocked 5-HT-evoked contraction of rat isolated stomach fundus (pA2 = 9.5+/-1.1) and (+/-)alpha-methyl-5-HT-mediated relaxation of the rat jugular vein (pA2 = 9.9+/-0.3). RS-127445 had no detectable intrinsic activity in these assays. In rats, the fraction of RS-127445 that was bioavailable via the oral or intraperitoneal routes was 14 and 60% respectively. Intraperitoneal administration of RS-127445 (5 mg kg(-1)) produced plasma concentrations predicted to fully saturate accessible 5-HT2B receptors for at least 4 h. In conclusion, RS-127445 is a selective, high affinity 5-HT2B receptor antagonist suitable for use is vivo. The therapeutic potential of this molecule is being further evaluated.
브랜드 쌀의 브랜드자산과 소비자 인식에 관한 연구 (2009)

쌀은 전체 농업생산액의 23%를 차지하여 단일품목으로 생산액이 최대인 품목이며, 전체 농가의 70%이상이 쌀 생산농가이다. 이처럼 한국에서 쌀은 산업으로서 매우 중요한 품목일 뿐만 아니라 정치, 사회적으로도 매우 민감한 품목이다. 본 연구에서는 최근 국민소득의 향상과 문화수준의 발전 등으로 도시를 중심으로 한 현대인들의 식생활 변화에 따라 양에서 질로 바뀌었으며, 또한 농산물시장의 개방으로 인해 우리 농업의 근간인 쌀은 외국브랜드 쌀이 국내 시장에 수입되고 있으며 국제적 수준의 브랜드와 품질 및 가격 면에서 상대적으로 경쟁력을 상실하고 있다. 쌀 상품선택의 폭이 넓어지고 치열해진 시장에서 브랜드가 소비자에게 선택되어지기 위해서는 경쟁제품과의 차별화가 이루어져야 하며, 브랜드마다 구체적인 차별화 전략수립이 필요한 시점에 있다. 본 조사의 핵심인 쌀 브랜드에 대한 속성(브랜드 영향력, 가격, 인지도, 포장 디자인, 쌀 생산지)이 만족도에 어떤 영향을 미치는가를 알아보기 위하여 다중 회귀분석을 실시한 결과 브랜드, 생산지, 인지도의 속성만이 유의수준 0.5수준에서 유의하다고 할 수 있어서 만족도에 영향을 준다고 할 수 있지만 다른 속성인 디자인, 가격은 만족도에 양향을 주지 않은 것으로 나타났다. 따라서 쌀 브랜드는 지역적 브랜드와 인지도를 기반으로 한 브랜드 이미지야 말로 더욱 강건한 브랜드 파워를 형성 할 수 있는 기반이 될 것이다.
The Krüppel-like Factor KLF2 Inhibits Peroxisome Proliferator-activated Receptor-γ Expression and Adipogenesis (2003)

Obesity is an important public health problem associated with a number of disease states such as diabetes and arteriosclerosis. As such, an understanding of the mechanisms governing adipose tissue differentiation and function is of considerable importance. We recently reported that the Krüppel-like zinc finger transcription factor KLF15 can induce adipocyte maturation and GLUT4 expression. In this study, we identify that a second family member, KLF2/Lung Krüppel-like factor (LKLF), as a negative regulator of adipocyte differentiation. KLF2 is highly expressed in adipose tissue, and studies in cell lines and primary cells demonstrate that KLF2 is expressed in preadipocytes but not mature adipocytes. Constitutive overexpression of KLF2 but not KLF15 potently inhibits peroxisome proliferator-activated receptor-gamma (PPARgamma) expression with no effect on the upstream regulators C/EBPbeta and C/EBPdelta. However, the expression of C/EBPalpha and SREBP1c/ADD1 (adipocyte determination and differentiation factor-1/sterol regulatory element-binding protein-1), two factors that feedback in a positive manner to enhance PPARgamma function, was also markedly reduced. In addition, transient transfection studies show that KLF2 directly inhibits PPARgamma2 promoter activity (70% inhibition; p < 0.001). Using a combination of promoter mutational analysis and gel mobility shift assays, we have identified a binding site within the PPARgamma2 promoter, which mediates this inhibitory effect. These data identify a novel role for KLF2 as a negative regulator of adipogenesis.
Complete dissection of the Hb(64-76) determinant using T helper 1, T helper 2 clones, and T cell hybridomas (1992)

We have generated cloned Th1 cells, Th2 cells, and T cell hybridomas specific for the single immunogenic peptide from the beta-chain of murine hemoglobin (Hb(64-76)). The availability of these various types of T cells provided us an unique opportunity to examine and dissect the T cell response to an immunogenic peptide. A panel of altered Hb peptides was made by replacing each amino acid in the Hb peptide (positions 64-76) with a conservative amino acid substitution or an alanine. Although none of the eleven T cell clones and hybridomas tested exhibited the same pattern of reactivity to the substituted Hb peptides, some general features were identified for all T cell responses. The primary T cell contact residue of Hb(64-76) was shown to be asparagine 72. For every Hb(64-76) specific T cell, no activation was observed using a peptide containing the conservative substitution of a glutamine for the asparagine at position 72. The flanking glutamic acid at position 73 was also required for a proliferative response for all of the Th1 and Th2 clones. The Th subtypes were not grossly unique in their responses to the substituted Hb peptides, but exhibited minor differences in fine specificity with the Th1 cells identifying more critical amino acids then did the Th2 cells. For the Th1 cells and also the T cell hybridomas, the phenylalanine at position 71 was critical for a T cell response. Analysis of peptide affinity for IEk molecules indicated that position 71 played a role in peptide binding to MHC. Secondary T cell contact residues, which were important for many but not all of the T cells, were identified at positions 69, 70, and 76. Overall T cell responses were minimally affected by changes in the amino acid residues at positions 64-68, 74, and 75. We have also demonstrated that cloned Th1 cells, Th2 cells and T hybridomas can be generated against the same Hb(64-76) determinant.
Femtosecond real-time probing of reactions. II. The dissociation reaction of ICN (1988)

Experimental results obtained for the dissociation reaction ICN*→[I⋅⋅⋅CN]‡*→I+CN using femtosecond transition-state spectroscopy (FTS) are presented. The process of the I–CN bond breaking is clocked, and the transition states of the reaction are observed in real time. From the clocking experiments, a ‘‘dissociation’’ time of 205±30 fs was measured and was related to the length scale of the potential. The transition states live for only ∼50 fs or less, and from the observed transients we deduce some characteristics of the relevant potential energy surfaces (PES). These FTS experiments are discussed in relation to both classical and quantum mechanical models of the dynamical motion, including features of the femtosecond coherence and alignment of fragments during recoil. The observations are related to the radial and angular properties of the PES.
Specific Antigen in Serum of Patients with Colon Carcinoma (1981)

The binding of monoclonal antibody specific for colon carcinoma was inhibited by serum from patients with adenocarcinoma of the colon but not by serum from patients with other bowel diseases or from healthy volunteers. Of other malignancies studied, serum from two patients with gastric carcinoma and two patients with pancreatic carcinoma also inhibited the specific binding of monoclonal antibody. The levels of carcinoembryonic antigen in these serum samples were not correlated with their levels of binding inhibition. Such monoclonal antibodies may prove useful for the detection of colorectal carcinoma.
Expression of Integrins in Squamous Cell Carcinoma of the Oral Cavity: Correlations with Tumor Invasion and Metastasis (1999)

Integrins are cell adhesion molecules that mediate the cell to extracellular matrix interactions. We sought to determine whether the integrin expression on tumor cells is associated with invasive and metastatic potential. First, in 8 cell lines of oral squamous cell carcinoma, 4 of which were metastatic in nude mice and 4 of which were not, integrin expression was examined. When these cell lines were cultured in vitro or transplanted into the tongues of nude mice, the metastatic cell lines tended to show a stronger expression of alpha 2, alpha 3, alpha 5, and alpha 6 integrins than did the nonmetastatic cell lines. Second, integrin expression was immunohistochemically examined in 65 biopsy specimens of primary oral squamous cell carcinoma. In invasive or metastatic cases, a marked expression of alpha 2, alpha 3, alpha 5, and alpha 6 integrins was frequently observed. The association of integrin expression with the mode of tumor invasion and nodal involvement was found to be statistically significant. These results suggest that integrin expression is closely associated with tumor invasion and nodal involvement in oral squamous cell carcinoma.
An event‐flow model of GUI‐based applications for testing (2007)

Abstract Graphical user interfaces (GUIs) are by far the most popular means used to interact with today's software. The functional correctness of a GUI is required to ensure the safety, robustness and usability of an entire software system. GUI testing techniques used in practice are resource intensive; model‐based automated techniques are rarely employed. A key reason for the reluctance in the adoption of model‐based solutions proposed by researchers is their limited applicability; moreover, the models are expensive to create. Over the past few years, the present author has been developing different models for various aspects of GUI testing. This paper consolidates all of the models into one scalable event‐flow model and outlines algorithms to semi‐automatically reverse‐engineer the model from an implementation. Earlier work on model‐based test‐case generation, test‐oracle creation, coverage evaluation, and regression testing is recast in terms of this model by defining event‐space exploration strategies (ESESs) and creating an end‐to‐end GUI testing process. Three such ESESs are described: for checking the event‐flow model, test‐case generation, and test‐oracle creation. Two demonstrational scenarios show the application of the model and the three ESESs for experimentation and application in GUI testing. Copyright © 2007 John Wiley &amp; Sons, Ltd.
The Role of Nitric Oxide in the Development of Diabetic Angiopathy (2004)

Diabetic angiopathy is the main cause of morbidity and mortality in patients with diabetes mellitus. Clinical manifestations and pathophysiological mechanisms of diabetic angiopathy can be traced back to the development of endothelial cell dysfunction with alterations in the eNOS/NO system production or availability as the primum movens in its natural history. Hyperglycemia per se or through the accumulation of AGEs, increased oxidative stress, leading to NOS uncoupling and NO-quenching by excess superoxide and peroxynitrite, and individual genetic background are thought to be responsible for this NO metabolism imbalance. The complex interplay of these mechanisms results in a perturbation of the physiological properties of NO in the maintenance of endothelial homeostasis, such as vasodilation, anticoagulation, leukocyte adhesion, smooth muscle cell proliferation, and antioxidant capacity. Hence, abnormality in NO availability results in generalized accelerated atherosclerosis, hyperfiltration, glomerulosclerosis, tubulointerstitial fibrosis and progressive decline in glomerular filtration rate, and apoptosis and neovascularization in the retina. Indeed, the parallel development of nephropathy, retinopathy, and macroangiopathy may be considered as manifestations of endothelial dysfunction at distinct vascular sites. Given this scenario, intervention targeting any of the pathways involved in the NOS/NO system cascade may prove potential therapeutic targets in the prevention of long-term diabetic complications.
Temporary forms of occupation – part II: the role oftenancies at will (1995)

In Part I the inherent weaknesses and merits of licence agreements, and their limited specialized use, were considered. Part II considers the particular uses for, and pitfalls of, agreements which create tenancies at will. Highlights the differences, problems and advantages of both forms of temporary occupation.
Satellite broadcasting in Australia (1988)

The operational features of the Australian domestic satellite system, AUSSAT, are discussed, particularly as they relate to broadcasting direct to communities and distribution to transmitters and studio centres of the Australian Broadcasting Corporation, ABC (Aus). Distribution of sound-only broadcasting programs is covered by the use of time-multiplexing using B-MAC. Comprehensive direct broadcasting from satellites is now available to many people living in remote areas of Australia who would otherwise receive minimal service. Initially, for each of the four major regions, ABC (Aus) has provided one television channel with stereophonic sound capability together with three different sound-only services, one of which is stereophonic. In addition to the 'free' services of ABC (Aus), commercial broadcasting satellite services are being progressively introduced to the four regions.< <ETX xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">&gt;</ETX>
LytB protein catalyzes the terminal step of the 2‐C‐methyl‐D‐erythritol‐4‐phosphate pathway of isoprenoid biosynthesis (2002)

Recombinant LytB protein from the thermophilic eubacterium Aquifex aeolicus produced in Escherichia coli was purified to apparent homogeneity. The purified LytB protein catalyzed the reduction of (E)-4-hydroxy-3-methyl-but-2-enyl diphosphate (HMBPP) in a defined in vitro system. The reaction products were identified as isopentenyl diphosphate and dimethylallyl diphosphate. A spectrophotometric assay was established to determine the steady-state kinetic parameters of LytB protein. The maximal specific activity of 6.6+/-0.3 micromol x min(-1) x mg(-1) protein was determined at pH 7.5 and 60 degrees C. The k(cat) value of the LytB protein was 3.7+/-0.2 s(-1) and the K(m) value for HMBPP was 590+/-60 microM.
Cross-Neutralization of 1918 and 2009 Influenza Viruses: Role of Glycans in Viral Evolution and Vaccine Design (2010)

New strains of H1N1 influenza virus have emerged episodically over the last century to cause human pandemics, notably in 1918 and recently in 2009. Pandemic viruses typically evolve into seasonal forms that develop resistance to antibody neutralization, and cross-protection between strains separated by more than 3 years is uncommon. Here, we define the structural basis for cross-neutralization between two temporally distant pandemic influenza viruses--from 1918 and 2009. Vaccination of mice with the 1918 strain protected against subsequent lethal infection by 2009 virus. Both were resistant to antibodies directed against a seasonal influenza, A/New Caledonia/20/1999 (1999 NC), which was insensitive to antisera to the pandemic strains. Pandemic strain-neutralizing antibodies were directed against a subregion of the hemagglutinin (HA) receptor binding domain that is highly conserved between the 1918 and the 2009 viruses. In seasonal strains, this region undergoes amino acid diversification but is shielded from antibody neutralization by two highly conserved glycosylation sites absent in the pandemic strains. Pandemic HA trimers modified by glycosylation at these positions were resistant to neutralizing antibodies to wild-type HA. Yet, antisera generated against the glycosylated HA mutant neutralized it, suggesting that the focus of the immune response can be selectively changed with this modification. Collectively, these findings define critical determinants of H1N1 viral evolution and have implications for vaccine design. Immunization directed to conserved receptor binding domain subregions of pandemic viruses could potentially protect against similar future pandemic viruses, and vaccination with glycosylated 2009 pandemic virus may limit its further spread and transformation into a seasonal influenza.
Properties of a sarcoma‐growth‐factor‐like peptide from cells transformed by a temperature‐sensitive sarcoma virus (1981)

Serum-free conditioned media was collected from three sarcoma virus-transformed cell lines and an untransformed cell line. All three virally transformed lines produced and released growth factors into their serum-free media. The major activity in all cases, whether the cells were transformed by Moloney sarcoma virus (MSV) or Kirsten sarcoma virus (KiSV), or whether they were mouse or rat, was a sarcoma-growth-factor (SGF)-like activity with an apparent molecular weight of 10,000. The SGF-like pools from a Moloney sarcoma virus-transformed mouse 3T3 cell and a Kirsten sarcoma virus-transformed NRK cell were further purified by carboxymethyl cellulose chromatography. The elution profiles of these peptides were very similar. The serum-free conditioned media from the untransformed cells showed no detectable growth stimulating activity. The temperature sensitivity of an SGF-like growth factor from the supernate of a NRK cell transformed by a wild-type Kirsten sarcoma virus (KiSV) was compared with that of the SGF-like activity from the supernates of a NRK cell transformed by a ts-mutant of KiSV that is temperature sensitive with respect to transformation (ts-371 Cl 5). Neither the cells transformed by the wild-type sarcoma virus nor those transformed by the temperature sensitive virus released a SGF-like activity that was temperature sensitive under the conditions of the assays.
Evidence for inhibition of cholinesterases in insect and mammalian nervous systems by the insect repellent deet (2009)

These findings question the safety of deet, particularly in combination with other chemicals, and they highlight the importance of a multidisciplinary approach to the development of safer insect repellents for use in public health.
气候变暖，地球真的“在乎”吗？ (2013)

如今许多有责任感的人都在关心地球遭受的损害。人类燃烧化石燃料产生的二氧化碳正以可怕的速度在大气层中积聚，一个世纪之内，二氧化碳浓度就会翻一番。这种积聚现象可能会把地球的平均温度提高几摄氏度，足以影响气候并加速两极冰盖的融化。
Multiport SOLR calibrations: performance and an analysis of some standards dependencies (2005)

Short-Open-Load-Reciprocal (SOLR) has been used as a calibration technique when the realization of a good thru line is difficult. This may happen in on-wafer environments (e.g., when probes are orthogonal or when two-signal probes are used), in coaxial measurements (when different connector types are involved), or in fixtured measurements. The increasing number of multiport S-parameter measurements has further pushed demand for such an algorithm as probe and connector configurations proliferate. Several issues related to a practical implementation of multiport SOLR measurements are covered in this paper including thoughts on optimal combinations of thrus and reciprocal networks when choice is available, some limits on the behavior of reciprocal networks and how they affect standards choices, and a heuristic analysis of the use of redundant thrus/reciprocals in the multiport environment. Load match benefits the most from true thrus, when available, but transmission tracking seems less sensitive for a wide variety of networks. Thus, a careful selection of standards employed can, in some sense, optimize the multiport calibration in this environment.
Haemophilus influenzae Forms Biofilms on Airway Epithelia (2006)

NTHi formed adherent biofilms on the apical surface airway epithelia with decreased susceptibility to antibiotics, and respiratory cells exhibited inflammatory and host defense responses-evidence of a dynamic host-pathogen interaction. The data presented here have implications both for understanding early CF lung disease pathogenesis and for the treatment of early, asymptomatic colonization of patients with CF with H. influenzae.
Emotional competence and the mediator (2006)

Extract: This article discusses findings from the first phase of a doctoral study which explores the resources on which mediators rely in order to accomplish their demanding role. The study is being conducted at the University of Melbourne, and has also been approved by the ethics committee of the Department of Justice, Victoria. Twenty-three experienced mediators were involved in this initial phase, which included participation in one of three focus groups and the completion of two inventories related to their reported coping behaviours.
Bandwidth compression optical processor using chirped fiber Bragg gratings (2007)

Chirped fiber Bragg gratings are used as low-loss, dispersion compensation modules for telecommunications applications. Here we use them to make an optical processor that compresses the bandwidth of electronic signals before digitization by an analog-to-digital converter.
Use of CD137 to study the full repertoire of CD8+ T cells without the need to know epitope specificities (2008)

CD137 (4-1BB) is a member of the TNFR-family with costimulatory function, triggering prosurvival signals in activated T-cells. Upregulation of CD137 upon stimulation allows identifying and isolating live, human antigen-specific CD8+ T-cells of all phenotypes, and therefore provides a comprehensive detection method. Furthermore responses against antigen mixtures can be easily detected, enabling antigen discovery in a stepwise deconvoluting approach. In this article, we will discuss various aspects of this methodology, including potential pitfalls as well as a variety of applications, as illustrated by examples from our laboratory.
Electrical impedance endo-tomography: imaging tissue from inside (2002)

This paper describes a new method for scanning the conductivity of a tissue or an organ using a multielectrode impedance probe placed at the center of the region of interest. The long-term objective of the study is the evaluation, using an urethral impedance probe, of the lesion produced by ultrasound ablathermy of localized prostate cancer. The probe consists of electrodes placed at the surface of an insulating cylinder. The injected current passes around the cylinder and spreads in the medium surrounding the probe. This paper presents the theoretical bases of this method, the calculated sensitivity distributions of electrode configurations involving a pair of diametrically opposed electrodes and an application in vitro. The experimental set-up consisted of a water tank and a 16-electrode prototype probe 50 mm in diameter. Data sets were collected in the presence of conductivity perturbations produced by small size insulators or conductors and a 7.5% constant perturbation model. The presented images, although reconstructed using a simple retro-projection algorithm, demonstrate the feasibility of the method. Improvements in data collection and image reconstruction are possible.