gebhart/patrepeval huggingface dataset:
Derivatives of 1- and 2-Tetralones (1966)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTDerivatives of 1- and 2-TetralonesGeorge deStevens and Barbara SmolinskyCite this: J. Med. Chem. 1966, 9, 6, 954–957Publication Date (Print):November 1, 1966Publication History Published online1 May 2002Published inissue 1 November 1966https://pubs.acs.org/doi/10.1021/jm00324a038https://doi.org/10.1021/jm00324a038research-articleACS PublicationsRequest reuse permissionsArticle Views86Altmetric-Citations3LEARN 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
Oligomannoside-type glycopeptides inhibiting adhesion of Escherichia coli strains mediated by type 1 pili: preparation of potent inhibitors from plant glycoproteins (1986)

Various structurally defined glycopeptides of natural origin were tested as inhibitors of guinea pig erythrocyte agglutination by enteropathogenic Escherichia coli strains expressing type 1 pili. Besides hybrid-type glycoasparagines from ovalbumin which were not active, large oligomannoside-type carbohydrate chains from legume storage glycoproteins moderately inhibited hemagglutinations, whereas the short oligomannoside-type glycoasparagine from ovalbumin Man alpha(1----6) [Man alpha(1----3)]Man alpha(1----6)[Man alpha(1----3)] Man beta(1----4)GlcNAc beta(1----4)GlcNAc beta(1----N)Asn exhibited a potent activity. These results strongly suggested that the nonsubstitution of the alpha(1----3)-linked mannosyl residue from the N-linked glycopeptide core structure is the key determinant in the minimal structural requirement specific to this fimbrial lectin. Such Man5GlcNAc2-containing glycopeptides were obtained from larger N-linked carbohydrate chains, occurring abundantly in natural sources. The ability of jack bean alpha-mannosidase to cleave the alpha(1----2)-linked mannoses more rapidly than the others allowed the controlled digestion of large oligomannoside-type glycopeptides from legume storage glycoproteins. Such shortened glycopeptides of plant origin were prepared which strongly inhibited guinea pig erythrocyte agglutinations as well as bacterial adhesion on human buccal cells, thus confirming their similarity (if not identity) with the receptor of type 1 pili on mammalian cells. The importance of this preparation of a receptorlike compound that inhibits bacterial adhesion with regard to the research on the role of type 1 pili in E. coli pathogenicity is discussed.
Is seminal prostatic acid phosphatase a reliable marker for male infertility? (1996)

This project was undertaken to determine whether there is any correlation between sperm counts and motility and the level of prostatic acid phosphatase (PAcP). Fifty-six patients were studied in this series-those with normospermia (Group A,n = 19); mild oligospermia (Group B,n = 18) and very severe oligospermia (Group C,n = 19). Each group was further subdivided into 2 groups-those who were 25-35 years old and those 36 years old and above. The results in this age group are discussed and it was found that individuals with very severe oligospermia (sperm counts 1-20x10(5)/mL) showed a positive correlation (p = 0.009) in the age group 36 years and above. The results have to be treated with caution since a statistically significant result was only displayed in one group, ie, individuals over the age of 35 years and very low sperm counts.
Therapeutic Fc‐Fusion Proteins (2013)

Therapeutic Fc fusion proteins , Therapeutic Fc fusion proteins , کتابخانه مرکزی دانشگاه علوم پزشکی تهران
Interleukin-2 receptor regulates activation of phosphatidylinositol 3-kinase (1991)

Interleukin-2 (IL-2) stimulates proliferation of T lymphocytes and is involved in the activation of both natural killer and lymphokine-activated killer precursor cells. The intracellular messengers which mediate IL-2-dependent events have not yet been identified. IL-2 receptor is not a protein-tyrosine kinase. Activation of a cellular protein-tyrosine kinase and direct association of a protein-tyrosine kinase activity with the IL-2 receptor occurs within minutes of IL-2 stimulation. We investigated the activation of phosphatidylinositol 3-kinase (PI 3-kinase) in IL-2-mediated signal transduction using the IL-2-dependent murine T-cell line, CTLL-2, and human phytohemagglutinin-stimulated peripheral blood lymphocytes (phytohemagglutinin blasts). Within a minute following stimulation of these cells with IL-2, PI 3-kinase activity could be detected in antiphosphotyrosine (anti-P-Tyr) antibody immunoprecipitates. IL-2 triggered a direct association of PI 3-kinase with the IL-2 receptor as detected in immunoprecipitates using anti-IL-2 receptor beta chain antibody. In vivo labeled CTLL-2 cells have a time-dependent increase in D-3-phosphorylated polyphosphoinositides following stimulation with IL-2. This is the first group of second messengers identified in IL-2-mediated signal transduction.
The origin of matrix metalloproteinases and their familial relationships (1991)

New computer comparisons of the sequences of mammalian matrix metalloproteinases have established for the first time strong links with bacterial metalloproteinases. We also propose that there are five groups in the family of matrix metalloproteinases, although only three are as yet well-characterized as proteins, and discuss their origin and relationships with other zinc containing proteases.
Excited states and photochemistry of organic molecules (1996)

Spectroscopy in the visible and UV region absorption spectra of organic molecules optical activity principles of the quantum chemical description of photophysical and photochemical processes photophysical processes photochemical reaction models organic photochemistry.
With a Little Help from Prokaryotes (2013)

Red algae can adapt to extreme conditions through horizontal gene transfer from free-living prokaryotic extremophiles. [Also see Report by Schönknecht et al. ]
Yeast: an Experimental Organism for Modern Biology (1988)

The yeasts Saccharomyces cerevisiae and Schizosaccharomyces pombe have become popular and successful model systems for understanding eukaryotic biology at the cellular and molecular levels. The reasons for this success are experimental tractability, especially in applying classical and molecular genetic methods to associate genes with proteins and functions within the cell.
REDUCED TRANSPLANTABILITY OF SYNGENIC MOUSE TUMORS SUPERINFECTED WITH MEMBRANE VIRUSES IN NU/NU MICE (1976)

Transplantability of mouse tumors superinfected with various kinds of membrane viruses was investigated in syngeneic hosts. Methylcholanthrene-induced fibrosarcomas in BALB/c mice, Meth A, and in C57BL/6 mice, BMT-, superinfected with Friend lymphatic leukemia virus in mice given neonatal injection of the virus, grew more slowly than uninfected tumors. The retardation of growths was not observed in mice that had been given injections of the virus at birth. Similarly, Meth A and a hepatoma in C3H/He mice, MH134, superinfected with Moloney murine sarcoma virus in nu/nu mice, had reduced their transplantability in respective syngeneic mice. Further, Meth A and MH134 superinfected with endogenous rat leukemia virus and human measles virus, respectively, in nu/nu mice also showed reduced transplantability, and some of the former were actually rejected by normal syngeneic hosts. On the other hand, the reduced transplantability was not found in irradiated mice, suggesting that the phenomenon was due to immunological events. However, a myelogenous leukemia in C57BL/6 mice, C1498, superinfected with Moloney sarcoma virus in nu/nu mice grew like uninfected tumor and did not show reduced transplantability at all.
Cytokine Production and Hematopoiesis Supporting Activity of Cord Blood Derived Unrestricted Somatic Stem Cells. (2004)

Abstract Particularly within the last several years cord blood (CB) has become a well established hematopoietic source for unrelated transplantation in children. Assuming, however, a threshold of 2x107 nucleated cells (NC)/kg body weight required for transplantation in adults over 70kg, an average of only 25% of the CB units presently stored in the major CB banks contain sufficient NC to safely engraft patients. Thus far the majority of studies have assessed selective cytokine driven expansion of progenitors for transplantation, which however may be associated with exhaustion of stem cells and an increase of GvHD in adult patients. Therefore, we assessed cytokine production and hematopoiesis supporting stromal activity of CB derived unrestricted somatic stem cells (USSC, Koegler et al. JEM2004: 200: 2: 1–13) in comparison to bone marrow mesenchymal stem cells (BMMSC) and hematopoietic progenitor expansion solely driven by recombinant cytokines. Initiation of USSC generation was initiated from fresh (n=325) and cryopreserved CB (n=66). In the presence of H5100 medium/10−7M dexamethasone, USSC cultures from fresh CB were initiated from 57.1% of CB samples (n= 52 out of 91 CB samples), whereas in DMEM-medium/10−7M dexamethasone the frequency was 31.6% (n=74 out of 234 CB samples). The generation frequency from frozen HES separated CB was only 19.5%. Cytokine production by USSC and BMMSC was determined qualitatively by cytokine mRNA expression array analyses or quantitatively by Luminex or ELISA analyses. To analyze hematopoiesis supporting activity, CB CD34+ cells were expanded in co-cultures with USSC, BMMSC or in the presence of Flt3-L, SCF, TPO. Expansion of CD34+ cells, total cells and colony-forming cells (CFC) were determined after 1, 2, 3 and 4 weeks of culture. USSC constitutively produced SCF, LIF, TGF-1ß, M-CSF, GM-CSF, VEGF, IL-1ß, IL-6, IL-8, IL-11, IL-12, IL-15, SDF-1a and HGF. When USSC were stimulated with IL-1ß, G-CSF was released. Production of SCF (p= 0.0104) and LIF (p= 0.046) was significantly higher in USSC compared to BMMSC. At 1, 2, 3 and 4 weeks, respectively co-cultivation of CD34+ cells on the USSC layer resulted in a 14.62±1.1-fold, 110.1±17.9-fold, 151.8±39.7-fold and 183.6±40.4-fold amplification of total cells and in a 30.56±4.4-fold, 101.4±27.5-fold, 64.67±15.8-fold and 29.4±3.1-fold amplification of CFC. Expansion achieved was significantly higher for USSC compared to BMMSC feeder layers. USSC produce functionally significant amounts of hematopoiesis supporting cytokines and are able to expand CD34+ cells from CB in significantly higher amounts compared to BMMSC. Therefore the USSC is a suitable candidate to direct ex-vivo expansion of hematopoietic CB cells for short term reconstitution.
A single sodium channel mutation produces hyper- or hypoexcitability in different types of neurons (2006)

Disease-producing mutations of ion channels are usually characterized as producing hyperexcitability or hypoexcitability. We show here that a single mutation can produce hyperexcitability in one neuronal cell type and hypoexcitability in another neuronal cell type. We studied the functional effects of a mutation of sodium channel Nav1.7 associated with a neuropathic pain syndrome, erythermalgia, within sensory and sympathetic ganglion neurons, two cell types where Nav1.7 is normally expressed. Although this mutation depolarizes resting membrane potential in both types of neurons, it renders sensory neurons hyperexcitable and sympathetic neurons hypoexcitable. The selective presence, in sensory but not sympathetic neurons, of the Nav1.8 channel, which remains available for activation at depolarized membrane potentials, is a major determinant of these opposing effects. These results provide a molecular basis for the sympathetic dysfunction that has been observed in erythermalgia. Moreover, these findings show that a single ion channel mutation can produce opposing phenotypes (hyperexcitability or hypoexcitability) in the different cell types in which the channel is expressed.
Chemokines Are Associated With Delirium After Cardiac Surgery (2008)

After cardiac surgery, chemokine levels were elevated in patients who developed delirium in the early postoperative period. Because chemokines are capable of disrupting blood-brain barrier integrity in vitro, future studies are needed to define the relationship of these inflammatory mediators to delirium pathogenesis.
Systemic Involvement of High-Mobility Group Box 1 Protein and Therapeutic Effect of Anti–High-Mobility Group Box 1 Protein Antibody in a Rat Model of Crush Injury (2012)

Patients with crush injury often present systemic inflammatory response syndrome and fall into multiple organ failure. The mechanism by which the local tissue damage induces distant organ failure is still unclear. We focused on high-mobility group box 1 protein (HMGB1) as one of the damage-associated molecular pattern molecules that cause systemic inflammation in crush injury. We investigated involvement of HMGB1 and the effects of treatment with anti-HMGB1 antibody in a rat model of crush injury. Both hindlimbs of rats were compressed for 6 h and then released. In the crush injury group, the level of serum HMGB1 peaked at 3 h after releasing compression, followed by the increasing in the serum levels of interleukin 6 and tumor necrosis factor α. Hematoxylin-eosin staining showed substantial damage in the lung 24 h after the crush injury, with upregulation of the expression of receptor for advanced glycation end products, as revealed by immunohistochemical analysis. Intravenous administration of anti-HMGB1 antibody improved survival (n = 20 each group) and significantly suppressed serum levels of HMGB1, interleukin 6, and tumor necrosis factor α compared with the untreated crush injury group (n = 6-9 each group). Histological findings of lung damage were ameliorated, and the expression of receptor for advanced glycation end products was hampered by the treatment. These results indicate that HMGB1 is released in response to damage immediately after crush injury and acts as a proinflammatory mediator. Administration of anti-HMGB1 antibody reduced inflammatory reactions and improved survival by blocking extracellular HMGB1. Thus, HMGB1 appears to be a therapeutic target, and anti-HMGB1 antibody may become a promising novel therapy against crush injury to prevent the progression to multiple organ failure.
布阿松管制量輪詢系統之硏究 (1998)

摘要 輪詢系統包含一個服務者以及多個服務站或等候站，物件由外進入服務站等候服務，而服務者依某一次序至多個服務站做服務。輪詢系統主要的應用範圃是可將通訊網路token ring、token bus、ARQ、TDMA和slotted ring等等以輪詢系統的模式評估其效能。另一方面輪詢系統的模式亦可應用在自動化工程上，如弾性製造系統、機器手臂加工系統、自動倉儲系統以及無人搬運車。本篇研究的是布阿松管制量輪詢系統，其中服務者到達各站時以一個布阿松隨機變數決定他的服務量(要服務的物件數)。假設X i爲服務者到逹服務站i時，所觀察到的人數，我們以X i爲該布阿松隨機變數之參数(平均值)。在這個系統中我們推導出E[X i]之上下界限，同樣地，我們也推導出非純粹守恆定率律中加權平均等待時問總合之上下界限，同時並與二項式管制量等輪詢系統的結果加以比較。
Molecular magnetic resonance imaging (2006)

Molecular MRI (mMRI) is a special implementation of Molecular Imaging for the non-invasive visualisation of biological processes at the cellular and molecular level. More specifically, mMRI comprises the contrast agent-mediated alteration of tissue relaxation times for the detection and localisation of molecular disease markers (such as cell surface receptors, enzymes or signaling molecules), cells (e.g. lymphocytes, stem cells) or therapeutic drugs (e.g. liposomes, viral particles). MRI yields topographical, anatomical maps; functional MRI (fMRI) provides rendering of physiologic functions and magnetic resonance spectroscopy (MRS) reveals the distribution patterns of some specific metabolites. mMRI provides an additional level of information at the molecular or cellular level, thus extending MRI further beyond the anatomical and physiological level. These advances brought by mMRI are mandatory for MRI to be competitive in the age of molecular medicine. mMRI is already today increasingly used for research purposes, e.g. to facilitate the examination of cell migration, angiogenesis, apoptosis or gene expression in living organisms. In medical diagnostics, mMRI will pave the way toward a significant improvement in early detection of disease, therapy planning or monitoring of outcome and will therefore bring significant improvement in the medical treatment for patients.In general, Molecular Imaging demands high sensitivity equipment, capable of quantitative measurements to detect probes that interact with targets at the pico- or nanomolar level. The challenge to detect such sparse targets can be exemplified with cell surface receptors, a common target for molecular imaging. At high expression levels (bigger than 106 per cell) the receptor concentration is approx. 10(15) per ml, i.e. the concentration is in the micromole range. Many targets, however, are expressed in even considerably lower concentrations. Therefore the most sensitive modalities, namely nuclear imaging (PET and SPECT) have always been at the forefront of Molecular Imaging, and many nuclear probes in clinical use today are already designed to detect molecular mechanisms (such as FDG, detecting high glucose metabolism). In recent years however, Molecular Imaging has commanded attention from beyond the field of nuclear medicine. Further imaging modalities to be considered for molecular imaging primarily include optical imaging, MRI and ultrasound.
Global and local instability of flow focusing: The influence of the geometry (2010)

In the flow focusing technique, a liquid flow rate Q is injected through a microcapillary to form a meniscus attached to its edge. The meniscus is stretched until a thin jet tapers from its tip due to the action of a gas stream driven by a pressure drop Δp. Both the liquid jet and the gas stream cross the orifice of a plate located in front of the capillary at a distance H. In the present work, the stability of both the tapering liquid meniscus and the emitted jet is analyzed experimentally. Three regimes are identified: (i) the steady jetting regime, where the liquid meniscus is stable and the jet is convectively unstable; (ii) the local instability regime, where the liquid meniscus is stable and the jet is absolutely unstable; and (iii) the global instability regime, where the liquid meniscus is unstable. The mechanisms responsible for the transitions between those regimes are described. The experiments show the existence of a minimum value Qmin of the flow rate Q below which flow focusing is globally unstable independent of the pressure drop Δp applied to the gas stream. The dependence of the stability threshold Qmin with respect to the capillary-to-orifice distance H is analyzed considering different liquids. If the rest of the geometrical parameters are fixed, there is an optimum value Hopt of the capillary-to-orifice distance H for which the stability threshold Qmin is minimum. We also determine the dependence of Hopt and the corresponding minimum flow rate Qopt with respect to the capillary diameter. In addition, we find that Qmin diverges as the capillary-to-orifice distance H decreases and approaches a certain critical value, at which the transition from flow focusing to “flow blurring” takes place. We confirm our interpretation of the experimental results by conducting numerical simulations for the aforementioned three regimes.
Identification of potent, selective P2Y-purinoceptor agonists: structure-activity relationships for 2-thioether derivatives of adenosine 5'-triphosphate (1993)

Study of P2-purinoceptor subtypes has been difficult due to the lack of potent and selective ligands. With the goal of developing high affinity P2-purinoceptor-selective agonist, we have synthesized a series of analogues of adenine nucleotides modified on the purine ring as chain-extended 2-thioethers or as N6-methyl-substituted compounds. Chemical functionality incorporated in the thioether moiety included cyanoalkyl, nitroaromatic, amino, thiol, cycloalkyl, n-alkyl, and olefinic groups. Apparent affinity of the compounds for P2Y-purinoceptors was established by measurement of P2Y-purinoceptor-promoted phospholipase C activity in turkey erythrocyte membranes and relaxation of carbachol-contracted smooth muscle in three different preparations (guinea pig taenia coli, rabbit aorta, and rabbit mesenteric artery). Activity at P2X-purinoceptors was established by measurement of contraction of rabbit saphenous artery and of the guinea pig vas deferens and urinary bladder. All 11 of the 2-thioethers of ATP stimulated the production of inositol phosphates with K0.5 values of 1.5-770 nM, with an (aminophenyl)ethyl derivative being most potent. Two adenosine diphosphate analogues were equipotent to the corresponding ATP analogues. Adenosine monophosphate analogues were full agonists, although generally 4 orders of magnitude less potent. ATP 2-thioethers displayed pD2 values in the range of 6-8 in smooth muscle assay systems for activity at P2Y-receptors. There was a significant correlation for the 2-thioether compounds between the pK0.5 values for inositol phosphate production and the pD2 values for relaxation mediated via the P2Y-purinoceptors in the guinea pig taenia coli, but not for the vascular P2Y-receptors or for the P2X-receptors. At P2X-receptors, no activity was observed in the rabbit saphenous artery, but variable degrees of activity were observed in the guinea pig vas deferens and bladder depending on distal substituents of the thioether moiety. N6-Methyl-ATP was inactive at P2X-receptors, and approximately equipotent to ATP at taenia coil P2Y-receptors. This suggested that hybrid N6-methyl and 2-thioether ATP derivatives might be potent and selective for certain P2Y-receptors, as was shown for one such derivative, N6-methyl-2-(5-hexenylthio)-ATP.
Characterization of functionally active gene fusions in human papillomavirus related oropharyngeal squamous cell carcinoma (2016)

The Cancer Genome Atlas (TCGA) sequencing analysis of head and neck squamous cell carcinoma (HNSCC) recently reported on gene fusions, however, few human papillomavirus (HPV) positive samples were included, and the functional relevance of identified fusions was not explored. We therefore performed an independent analysis of gene fusions in HPV-positive oropharyngeal SCC (OPSCC). RNA sequencing was performed on 47 HPV-positive OPSCC primary tumors and 25 normal mucosal samples from cancer unaffected controls on an Illumina TruSeq platform. MapSplice2 was used for alignment and identification of fusion candidates. Putative fusions with less than five spanning reads, detected in normal tissues, or that mapped to the same gene were filtered out. Selected fusions were validated by RT-PCR and Sanger sequencing. Within 47 HPV-positive OPSCC tumors, 282 gene fusions were identified. Most fusions (85.1%) occurred in a single tumor, and the remaining fusions recurred in 2-16 tumors. Gene fusions were associated with significant up regulation of 16 genes (including EGFR and ERBB4) and down regulation of four genes (PTPRT, ZNF750, DLG2, SLCO5A1). Expression of these genes followed similar patterns of up regulation and down regulation in tumors without these fusions compared to normal tissue. Five of six gene fusions selected for validation were confirmed through RT-PCR and sequencing. This integrative analysis provides a method of prioritizing functionally relevant gene fusions that may be expanded to other tumor types. These results demonstrate that gene fusions may be one mechanism by which functionally relevant genes are altered in HPV-positive OPSCC.