gebhart/patrepeval huggingface dataset:
How human neuroblastoma cells make morphine (2005)

Recently, our laboratory demonstrated that human neuroblastoma cells (SH-SY5Y) are capable of synthesizing morphine, the major active metabolite of opium poppy. Now our experiments are further substantiated by extending the biochemical studies to the entire morphine pathway in this human cell line. L-[1,2,3-13C3]- and [ring-2',5',6'-2H3]dopa showed high isotopic enrichment and incorporation in both the isoquinoline and the benzyl moiety of the endogenous morphine. [2,2-2H2]Dopamine, however, was exclusively incorporated only into the isoquinoline moiety. Neither the trioxygenated (R,S)-[1,3-13C2]norcoclaurine, the precursor of morphine in the poppy plant, nor (R)-[1,3,4-2H3]norlaudanosoline showed incorporation into endogenous morphine. However, (S)-[1,3,4-2H3]norlaudanosoline furnished a good isotopic enrichment and the loss of a single deuterium atom at the C-9 position of the morphine molecule, indicating that the change of configuration from (S)- to (R)-reticuline occurs via the intermediacy of 1,2-dehydroreticuline. Additional feeding experiments with potential morphinan precursors demonstrated substantial incorporation of [7-2H]salutaridinol, but not 7-[7-2H]episalutaridinol, and [7-2H,N-C2H3]oripavine, and [6-2H]codeine into morphine. Human morphine biosynthesis involves at least 19 chemical steps. For the most part, it is a reflection of the biosynthesis in opium poppy; however, there is a fundamental difference in the formation of the key intermediate (S)-reticuline: it proceeds via the tetraoxygenated initial isoquinoline alkaloid (S)-norlaudanosoline, whereas the plant morphine biosynthesis proceeds via the trioxygenated (S)-norcoclaurine. Following the plant biosynthetic pathway, (S)-reticuline undergoes a change of configuration at C-1 during its transformation to salutaridinol and thebaine. From thebaine, there is a bifurcate pathway leading to morphine proceeding via codeine or oripavine, in both plants and mammals.
Analysis of prostatic fluid: Evidence for the presence of a prospective marker for prostatic cancer (1995)

In an endeavor to identify marker(s) for prostatic cancer, proteins in prostatic fluids were analyzed by two-dimensional (2-D) gel electrophoresis. The fluids were obtained from five males who had no prostate lesions and five patients each with benign prostatic hyperplasia (BPH) and prostatic carcinoma (PCA). The specimens were collected directly over a mixture of protease inhibitors and centrifuged, and the supernatants were lyophilized and solubilized in sodium dodecyl sulfate mix. Identical amounts of proteins were pooled according to donors' prostate disease and the resulting samples were subjected to 2-D gel analysis employing the ISO-DALT system. The electrophoretograms were developed by silver or double stain. The samples of each group exhibited distinctive profiles with the exception of similar relative positions of major protein spots. A predominant protein occurring as several charge variants was consistently present in prostatic fluids of patients with PCA. This protein appeared to be a previously unknown constituent that we have called protein D (molecular weight approximately 22 kDa and isoelectric point approximately 4), and was undetectable in the fluids of "normal" men and patients with BPH. An analysis of pooled, unprocessed urine from PCA patients revealed that perhaps this protein is excreted in urine in very low quantities. These results strongly suggest that the potential of this protein as a marker for prostatic cancer should be further explored.
Properties of binding of Escherichia coli endotoxin to various matrices (1981)

Binding of Escherichia coli O127:B8 endotoxin to a variety of resins and column materials was investigated by measuring the beta-hydroxy myristic acid content (a major component of the lipid A moiety) of endotoxin after hydrolysis by selected ion-monitoring gas chromatography-mass spectrometry. More than 80% of the endotoxin was bound to hydroxylapatite, polystyrene, Dowex 1-X2, and charcoal. The binding of endotoxin to these materials was markedly reduced by the addition of normal or delipidated serum. Phenyl- and octyl-Sepharose bound 56 and 50% of the endotoxin from saline solutions, respectively. Their percent binding was increased significantly in 1 M ammonium sulfate solutions, indicating hydrophobic interactions between endotoxin and phenyl- and octyl-Sepharose. Only 5% of the endotoxin was bound to plastic polymer PSI-HAP-100 beads, and no binding was observed with concanavalin A- and heparin-Sepharose. Study of the in vitro binding of endotoxin to the above material in the presence of serum suggests that the use of these materials in removing circulating endotoxin in vivo is limited.
Antitransforming growth factor-β therapy in fibrosis: recent progress and implications for systemic sclerosis (2008)

Anti-TGF-beta therapies promise to have a major impact in systemic sclerosis. Significant concerns regarding efficacy and safety need to be addresed. The identification of optimal candidates for therapy, and of biomarkers of safety and efficacy, are critical challenges ahead.
The receptor for antidiabetic sulfonylureas controls the activity of the ATP-modulated K+ channel in insulin-secreting cells. (1987)

Sulfonylureas are powerful hypoglycemic drugs that have been used for decades to treat diabetic patients. This paper describes a 86Rb+ flux technique that permits one to study easily the properties of ATP-modulated K+ channels in RINm5F insulinoma cells. Sulfonylureas inhibit this type of K+ channel under conditions of intracellular ATP depletion. The most potent sulfonylureas (glibenclamide, glipizide, and gliquidone) are acting in the nanomolar range of concentration. Inhibition of the single ATP-modulated K+ channels by low concentrations of sulfonylureas was also observed using the patch-clamp technique. The sulfonylurea receptor has been biochemically identified with [3H]glibenclamide. For 10 different sulfonylureas (or sulfonylurea analogs) there was an excellent correlation between efficacy of blockade of ATP-modulated K+ channels and efficacy of binding to the sulfonylurea receptors using the 3H-ligand.
Synthesis of (<i>Z</i>)-3-Deoxy-3-(1,2,3,6-Tetradeoxy-3,6-Imino-L-<i>Arabino</i>-Hexitol-1-<i>C</i>-Ylidene)-D-<i>Xylo</i>-Hexose Derivatives. First Examples Of Homo-(1→3)-<i>C</i>-Linked Iminodisaccharides. (2000)

Cross-aldolisation of 3,6-[(tert-butoxy)carbonyl]imino-2,3,6-trideoxy-4,5-O- isopropylidene-L-arabino-hexose (10) with 1,6-anhydro-2-O-benzyl-3-deoxy-beta-D-erythro-hexopyrano-4-ulose (6) generates, after water elimination, a single enone II that is reduced selectively into an allylic alcohol 12, deprotection of which affords methyl (Z)-3-deoxy-3-(1,2,3,6-tetradeoxy-3,6-imino-L-arabino-hexitol-1-C-yliden e)-beta-D-xylo-hexofuranoside (1) and (Z)-1,6-anhydro-3-deoxy-3-(1,2,3,6-tetradeoxy-3,6-imino-L-arabino-hexito l-1 -C-ylidene)-beta-D-xylo-hexopyranose (14).
Cannabimimetic activity of novel enantiomeric, benzofuran cannabinoids (1990)

The synthesis of the (2R,3R,4S,6R)-7/(2S,3S,4R,6S)-8 enantiomeric pair of benzofuran cannabinoids is reported together with the 1H and 13C NMR spectral parameters. In benzofuran 8 the configurational arrangement of ligated groups at the stereogenic C(3) atom (through which the terpene moiety is connected to the aromatic ring) is very similar to that of the corresponding atom in natural (3R,4R)-delta 1-tetrahydrocannabinol (delta 1-THC), although their respective Cahn-Ingold-Prelog descriptors are different. In drug-discrimination tests in pigeons and rats, benzofuran 8 is as active as delta 1-THC; in the mouse ring test compound 8 is more active than delta 6-THC. Enantiomer 7 is considerably less active than enantiomer 8 in both tests. These results can be explained by the fact that both 7 and 8 have a dimethylheptyl side chain (which is known to enhance cannabimimetic activity) and that delta 1-THC and benzofuran 8 have closely related conformations, as determined by molecular mechanics.
Poly(3,4-ethylenedioxythiophene)−Multiwalled Carbon Nanotube Composite Films: Structure-Directed Amplified Electrochromic Response and Improved Redox Activity (2009)

Composite thin films of poly(3,4-ethylenedioxythiophene) (PEDOT)-enwrapped functionalized multiwalled carbon nanotubes (MWCNTs) have been synthesized over multiple length scales by electropolymerization of the monomer without the use of any other supporting electrolyte. The functionalized MWCNTs are incorporated into the positively charged polymer deposit as counterions during oxidative electropolymerization. The morphology, electrochemistry, and electrochromism of the PEDOT-MWCNT films have been compared with those of control PEDOT films doped by triflate ions. Such a comparison enabled us to demonstrate the profound effect of MWCNTs as counterions, realized in terms of better electropolymerization rate, higher conductivity, faster color-bleach kinetics, higher charge storage capacity, and substantially amplified coloration efficiency (eta = 414 cm(2) C(-1), lambda(max) = 575 nm, E = -1.5 V) in comparison to the values of eta reported to date for PEDOT. The strong interaction between the polymer and MWCNTs, the interconnected nanotubular structures, and the porous framework of the film allow facile charge transport and larger ion uptake during redox switching. Electrochemical investigations on devices based on PEDOT-MWCNT and control PEDOT films established the practical utility of PEDOT-MWCNT films as they show lower charge-transfer resistance, higher diffusional capacitance, and a much smaller amplitude of impedance as compared to control PEDOT films.
A Microfluidic Chip for Liquid Metal Droplet Generation and Sorting (2017)

A liquid metal based microfluidic system was proposed and demonstrated for the generation and sorting of liquid metal droplets. This micro system utilized silicon oil as the continuous phase and Ga66In20.5Sn13.5 (66.0 wt % Ga, 20.5 wt % In, 13.5 wt % Sn, melting point: 10.6 °C) as the dispersed phase to generate liquid metal droplets on a three-channel F-junction generator. The F-junction is an updated design similar to the classical T-junction, which has a special branch channel added to a T-junction for the supplement of 30 wt % aqueous NaOH solution. To perform active sorting of liquid metal droplets by dielectrophoresis (DEP), the micro system utilized liquid-metal-filled microchannels as noncontact electrodes to induce electrical fields through the droplet channel. The electrode channels were symmetrically located on both sides of the droplet channel in the same horizontal level. According to the results, the micro system can generate uniformly spherical liquid metal droplets, and control the flow direction of the liquid metal droplets. To better understand the control mechanism, a numerical simulation of the electrical field was performed in detail in this work.
Monoclonal antibodies to human erythrocyte membrane Ca++-Mg++ adenosine triphosphatase pump recognize an epitope in the basolateral membrane of human kidney distal tubule cells. (1987)

Human calcium transporting tissues were examined to determine whether they contained a protein similar to the Ca++-Mg++ adenosine triphosphatase (Ca++-Mg++ATPase) pump of the human erythrocyte membrane. Tissues were processed for immunoperoxidase staining using monoclonal antibodies against purified Ca++-Mg++ATPase. In human kidneys, specific staining was found only along the basolateral membrane of the distal convoluted tubules. Glomeruli and other segments of the nephron did not stain. Staining of erythrocytes in human spleen was readily observed. Human small intestine, human parathyroid, and human liver showed no antigens that crossreacted with the antibodies to Ca++-Mg++ATPase. Specific staining of distal tubule basolateral membranes from the kidney of a chimpanzee was also noted. Our experiments show, for the first time, that basolateral membranes of the human distal convoluted tubule contain a protein that is immunologically similar to the human erythrocyte Ca++-Mg++ATPase. These observations suggest that the cells of the distal convoluted tubules of human kidney may have a calcium pump similar to that of human erythrocyte membranes.
Flavivirus Cell Entry and Membrane Fusion (2011)

Flaviviruses, such as dengue virus and West Nile virus, are enveloped viruses that infect cells through receptor-mediated endocytosis and fusion from within acidic endosomes. The cell entry process of flaviviruses is mediated by the viral E glycoprotein. This short review will address recent advances in the understanding of flavivirus cell entry with specific emphasis on the recent study of Zaitseva and coworkers, indicating that anionic lipids might play a crucial role in the fusion process of dengue virus [1].
Blast-like cell compartment in carcinogen-induced proliferating bile ductules. (1996)

Small non-epithelial cells with morphological features of blast-like cells are found within a proliferating intrahepatic biliary system after institution in rats of a diethylnitrosamine, 2-acetylaminofluorene, partial hepatectomy carcinogenesis protocol. Two to three days after the partial hepatectomy step of the carcinogen protocol, the small blast-like cells are evident beneath a layer of bile ductule epithelial cells that line the walls of the bile ductules. The basally located small cells are not exposed to the bile ductule lumen or to the surrounding basal lamina. They ranged in size from 3.0 to 5.0 microns, exhibit an undifferentiated phenotype, including a high nucleus-to-cytoplasm ratio and no to minimal differentiated cytoplasmic and surface structures. Mitosis of blast-like cells are evident, and their nuclei express proliferating nuclear cell antigen. The ductal blast-like cells do not express cytokeratin 19, oval cell antigen 270.38, or actin immunoreactivity, in contrast to bile ductule epithelial cells. The basal cells, as well as bile ductule epithelial cells, are negative for a panel of T and B lymphocyte surface markers in contrast to lymphocytes present in the connective tissue stroma surrounding the bile ductules and throughout the hepatic parenchyma. Within some segments of the biliary system, some of the ductal blast-like cells increased in size to approximately 10 microns and showed increased amounts of cytoplasmic organelles and plasma membrane filapodia but did not develop the polarized phenotype of bile ductule epithelial cells (ie, apical microvilli, desmosomes, connections to bile ductule cells, and exposure to duct lumen); however, their nuclear morphology was essentially similar to the smaller basal cells. We also found bile ductules to contain two types of polarized epithelial cells, one with the characteristic oval nucleus of the oval/bile ductule epithelial cells and the other, transitional epithelial cells with a rounder nucleus and prominent nucleoli. The transitional cells exhibit a similar apical-basal polarity and antigenic phenotype as the oval/bile ductule epithelial cells. However, transitional cells are larger and have an overall less dense cytoplasm than the bile ductule epithelial/oval cells, and some show apical microvilli changes and small catalase-positive peroxisomes. These observations indicate that a greater diversity of cell types exist within intrahepatic bile ductules of rats treated with carcinogens. Furthermore, the nonpolarized ductal blast-like cells undergo proliferation and are significantly different in phenotype from other hepatic cells previously reported as candidates for liver progenitor cells.
Reboxetine: the first selective noradrenaline re-uptake inhibitor (2000)

Several treatment approaches are available for treatment of depression. However, reboxetine is the first selective noradrenaline re-uptake inhibitor. Whereas formerly only noradrenaline re-uptake inhibitors with a mixed mechanism of action were available. These included action not only at noradrenergic, but also at serotonergic and other neurotransmitter-sites. Thus, reboxetine represents the first of a new class of antidepressant agents with specificity for the noradrenergic system. Reboxetine has been shown to be an effective first-line treatment for patients with all grades of depression, to be effective in the prevention of relapse and recurrence and to offer significant benefits in terms of relieving the impaired social functioning associated with depressive disorders. Reboxetine was significantly superior to the serotonergic compound fluoxetine in improvement of social functioning in both the general depressed population and in those patients who achieved symptomatic remission, indicating a superior quality of remission. Altogether reboxetine was well tolerated during the acute and long-term treatment phase; side-effects such as increased sweating, constipation and dry mouth were the most prominent to be reported. The availability of reboxetine represents a significant addition to the currently available pharmacologic armamentarium for the treatment of depression.
Single Cell Gene Expression in Classical Monocytes Correlates with Treatment Response to Tnf-Alpha Inhibition in Rheumatoid Arthritis (2016)

Restricted accessAbstractFirst published online March 1, 2016Single Cell Gene Expression in Classical Monocytes Correlates with Treatment Response to Tnf-Alpha Inhibition in Rheumatoid ArthritisT Wampler Muskardin, Z Jin, […], JM Dorschner, MA Jensen, T Bongartz, K Wright, T Mason, S Persellin, C Michet, D John, E Matteson, T Niewold, and W Fan+10-10View all authors and affiliationsVolume 64, Issue 4https://doi.org/10.1136/jim-2016-000120.135
Study on Growth and Optical, Scintillation Properties of Thallium Doped Cesium Iodide-Scintillator Crystal (2014)

Oriental Journal of Chemistry is a peer reviewed quarterly research journal of pure and applied chemistry. It publishes standard research papers in almost all thrust areas of current chemistry of academic and commercial importance. It provides a platform for rapid publication of quality research papers, reviews and chemistry letters. Oriental Journal of Chemistry is abstracted and indexed in almost all reputed National and International agencies.
Evidence‐Based Medicine, Heterogeneity of Treatment Effects, and the Trouble with Averages (2004)

Evidence-based medicine is the application of scientific evidence to clinical practice. This article discusses the difficulties of applying global evidence ("average effects" measured as population means) to local problems (individual patients or groups who might depart from the population average). It argues that the benefit or harm of most treatments in clinical trials can be misleading and fail to reveal the potentially complex mixture of substantial benefits for some, little benefit for many, and harm for a few. Heterogeneity of treatment effects reflects patient diversity in risk of disease, responsiveness to treatment, vulnerability to adverse effects, and utility for different outcomes. Recognizing these factors, researchers can design studies that better characterize who will benefit from medical treatments, and clinicians and policymakers can make better use of the results.
Electron scattering and transmission through SCALPEL masks (1998)

Electron scattering in thin solid films used for the fabrication of masks for electron projection lithography, e.g., SCALPEL®, is investigated. We have developed an analytical model to calculate electron transmission through the mask membrane and image contrast due to different scattering properties of the patterned area and the membrane. The model utilizes cross sections for electron elastic and inelastic scattering on an atom with exponentially screened Coulomb potential of the nucleus derived in the first Born approximation. The variety and controversy of theoretical and empirical adjustments of the screening parameter are briefly analyzed and attributed to the misinterpretation of experimental data ignoring the effects mostly due to plural scattering of electrons and dense packing of atoms in thin solid films. This model frees us from the computational limitations of Monte Carlo simulations and proves to be effective for the straightforward characterization of various alternative materials for SCALPEL mask membrane and scatterer. The model includes the appropriate effects of the projection optics and back-focal plane aperture.
Dual-wavelength diode laser with electrically adjustable wavelength distance at 785  nm (2016)

A spectrally adjustable monolithic dual-wavelength diode laser at 785 nm as an excitation light source for shifted excitation Raman difference spectroscopy (SERDS) is presented. The spectral distance between the two excitation wavelengths can be electrically adjusted between 0 and 2.0 nm using implemented heater elements above the distributed Bragg reflector (DBR) gratings. Output powers up to 180 mW at a temperature of 25°C were measured. The spectral width is smaller than 13 pm, limited by the spectrum analyzer. The device is well-suited for Raman spectroscopy, and the flexible spectral distance allows a target-specific adjustment of the excitation light source for shifted excitation Raman difference spectroscopy (SERDS).
Pain control using high‐intensity pulsed magnetic stimulation (1993)

High-intensity pulsed magnetic stimulation (HIPMS) non-invasively depolarizes neurones, which can be deeply embedded in local tissues. Trans- or subcutaneous electrical stimulation can produce analgesia. To test the hypothesis that similar analgesia could be obtained using HIPMS, analgesia was determined in ten blinded subjects following HIPMS. Analgesia was consistently produced in all subjects with long-lasting pain relief occurring in half of the cases.
Exploiting parallelism in high performance embedded system scheduling (2002)

This paper defines a new paradigm for high performance embedded systems. We present a model of distributed embedded control system software to capture the real-time computing requirements of complex computer-based systems. The hierarchical software architecture defines the notion of a software path the construct identified by studying embedded real-time applications. We present a technique for dynamic scheduling of sporadic paths. The novel feature of the approach is to enhance schedulability through high performance concurrent computing.
A pattern search method for putative anchor residues in T cell epitopes (1993)

The binding affinity between an antigenic peptide and its particular major histocompatibility complex (MHC) molecule seems to be largely determined by only a few residues. These residues have been called "anchors" because of their property of fitting into "pockets" inside the groove of the MHC molecule. To predict natural antigenic epitopes within a longer sequence, it therefore appears to be important to know the motif or pattern describing the anchors, i.e. the anchors amino acid residue preference and the distance between anchor residues. A large set of MHC class I-restricted peptides has been described. Peptide sequences vary in length and lack an obvious common sequence motif. For a list of peptides belonging to one type of MHC class I molecule, we describe a method to find the most prominent sequence motif with at least two anchor residues. Briefly, antigenic sequences are aligned, and two anchor positions are searched for, where all anchor residues share a high similarity. The alignments are scored according to the similarity of their anchor residues. We show that the motifs predicted for the MHC alleles A2.1, B27, Kb, Kd, Db are in substantial agreement with experimental data. We derive binding motifs for the MHC class I alleles HLA-A1, A11, B8, B14, H-2Ld and for the MHC class II alleles I-Ab and I-As. In some cases, higher scores were obtained by allowing a slight variation in the number of residues between anchors. Therefore, we support the view that the length of epitopes belonging to a particular class I MHC is not uniform. This method can be used to predict the natural short epitope inside longer antigenic peptides and to predict the epitopes anchor residues. Anchor motifs can be used to search for antigenic regions in sequences of infectious viruses, bacteria and parasites.