gebhart/patrepeval huggingface dataset:
Characterization of l‐[3H]Nicotine Binding in Human Cerebral Cortex: Comparison Between Alzheimer's Disease and the Normal (1986)

Putative nicotine receptors in the human cerebral cortex were characterized with L-[3H]nicotine, L-[3H]Nicotine binding was enhanced by the addition of Ca2+ and abolished in the presence of Na3EDTA. Association and dissociation of the ligand were rapid at 25 degrees C with t1/2 values of 2 and 3 min, respectively. Saturation binding analysis revealed an apparent single class of sites with a dissociation constant of 5.6 nM and a Hill coefficient of 1.05. There was no effect of postmortem interval on the density of binding sites assayed up to 24 h in rat frontoparietal cortex. Nicotine binding in human cortical samples was also unaltered by increasing sampling delay. In human cortical membranes, binding site density decreased with normal aging. Receptor affinity and concentration in samples of frontal cortex (Brodmann area 10) from patients with Alzheimer's disease were comparable to age-matched control values. Samples of infratemporal cortex (Brodmann area 38) from patients with Alzheimer's disease had a 50% reduction in the number of L-[3H]nicotine sites. Choline acetyltransferase activity was significantly decreased in both cortical areas. Enzyme activities in the temporal pole were reduced to 20% of control values. These data indicate that postsynaptic nicotine receptors are spared in the frontal cortex in Alzheimer's disease. In the infratemporal cortex, significant numbers of receptors remain despite the severe reduction in choline acetyltransferase activity. Replacement therapy directed at these sites may be warranted in Alzheimer's disease.
Chemical vapor deposition of titanium, zirconium, and hafnium nitride thin films (1991)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTChemical vapor deposition of titanium, zirconium, and hafnium nitride thin filmsRenaud Fix, Roy G. Gordon, and David M. HoffmanCite this: Chem. Mater. 1991, 3, 6, 1138–1148Publication Date (Print):November 1, 1991Publication History Published online1 May 2002Published inissue 1 November 1991https://pubs.acs.org/doi/10.1021/cm00018a034https://doi.org/10.1021/cm00018a034research-articleACS PublicationsRequest reuse permissionsArticle Views2745Altmetric-Citations205LEARN 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
Synthesis and Biological Evaluation of Low Molecular Weight Fluorescent Imaging Agents for the Prostate-Specific Membrane Antigen (2012)

Targeted near-infrared (NIR) optical imaging can be used in vivo to detect specific tissues, including malignant cells. A series of NIR fluorescent ligands targeting the prostate-specific membrane antigen (PSMA) was synthesized and each compound was tested for its ability to image PSMA+ tissues in experimental models of prostate cancer. The agents were prepared by conjugating commercially available active esters of NIR dyes, including IRDye800CW, IRDye800RS, Cy5.5, Cy7, or a derivative of indocyanine green (ICG) to the terminal amine group of (S)-2-(3-((S)-5-amino-1-carboxypentyl)ureido)pentanedioic acid 1, (14S,18S)-1-amino-8,16-dioxo-3,6-dioxa-9,15,17-triazaicosane-14,18,20-tricarboxylic acid 2 and (3S,7S)-26-amino-5,13,20-trioxo-4,6,12,21-tetraazahexacosane-1,3,7,22-tetracarboxylic acid 3. The K(i) values for the dye-inhibitor conjugates ranged from 1 to 700 pM. All compounds proved capable of imaging PSMA+ tumors selectively to varying degrees depending on the choice of fluorophore and linker. The highest tumor uptake was observed with IRDye800CW employing a poly(ethylene glycol) or lysine-suberate linker, as in 800CW-2 and 800CW-3, while the highest tumor to nontarget tissue ratios were obtained for Cy7 with these same linkers, as in Cy7-2 and Cy7-3. Compounds 2 and 3 provide useful scaffolds for targeting of PSMA+ tissues in vivo and should be useful for preparing NIR dye conjugates designed specifically for clinical intraoperative optical imaging devices.
Bending losses of trench-assisted few-mode optical fibers (2016)

A semianalytical method based on the perturbation theory is developed to calculate the bending losses of individual modes of few-mode fibers (FMFs); it is applicable for optical fibers with arbitrary circularly symmetric index profile, especially for trench-assisted fibers. The bending performance of trench-assisted step-index FMFs and parabolic-index FMFs are investigated with three key parameters (i.e., the refractive index difference of trench-cladding, the width of the trench, and the distance of the core-trench). Then, a performance index is defined to estimate the bending performance for FMFs. It is shown that changing the distance of the trench-core, for each order of mode, there is a minimum bending loss, which can be used for fiber optimization. This optimization position (core-trench distance) decreases as the mode order increases. It is found that the bending performance of parabolic-index FMFs is better than that of step-index FMFs with fixed core radius and cutoff wavelength. The conclusions are helpful for understanding the mechanism of bending loss for FMFs, and make contributions to designing and manufacturing of few-mode bend-insensitive fibers.
Hexa-arginine enhanced uptake and residualization of selective high affinity ligands by Raji lymphoma cells (2009)

The incorporation of a hexa-D-arginine peptide into the linker of the SHAL (DvLPBaPPP)2LLDo enhanced both the uptake and residualization of the SHAL analog by Raji cells. In contrast to the abundant cell surface binding observed with Lym-1 antibody, the majority of (DvLPBaPPP)2LArg6AcLLDo and the parent SHAL were internalized. Some of the internalized hexa-arginine SHAL analog was also associated with the nucleus. These results demonstrate that several important SHAL properties, including uptake, internalization, retention and possibly intracellular distribution, can be enhanced or modified by conjugating the SHALs to a short polypeptide.
Cooperative site specific binding of oligonucleotides to duplex DNA (1989)

Cooperative interactions between DNA binding ligands are critical to their specificity, affinity, and biological activity. Triple helix formation by oligonucleotides is the most powerful chemical approach to date for the sequence-specific recognition of double helical DNA. Hoogsteen hydrogen bonded base triplets, TAT and C+GC, result from pyrimidine oligonucleotides binding site specifically to purine duplex sequences. In the triple helical model, a binding site size of 18 purine base pairs affords 36 discrete sequence-specific hydrogen bonds for recognition of DNA in the major groove. As a possible mechanism for improving the specificity of triple helix formation, we tested whether oligonucleotides could cooperatively bind to a double-stranded DNA&#13;\ntemplate.
Design of Novel Synthetic Peptides Including Cyclic Conformationally and Topgraphically Constrained Analogs (2003)

The properties of a peptide in biological systems are dependent on its structure. Thus, our ability to use rational design for the generation of useful peptides is dependent on our commensurate ability to determine the specific relationships of molecular structure to biological activity. The ability to recognize these relationships is complicated by a variety of uncertainties, both in the assay systems and in the interpretation of data. One major complicating factor is the difficulty in ascertaining the three-dimensional structure of the peptide itself. Most peptides are inherently flexible and, thus, assume many conformations in solution. It is difficult to determine which of these conformations is responsible for the observed activity of the peptide, and many peptides may be active in more than one conformation. The use of conformational constraints has been helpful in elucidating these structure-function relationships. The logic is that if the peptide is restricted to a particular conformation or closely related family of conformations, then the activity measured will reflect that structure. Although a perfectly rigid molecule is impossible, by creating analogs with prescribed structural motifs, one can begin to ascribe certain biological activities to their causal structures. In favorable cases, knowledge of requirements for peptide activity at receptor- and enzyme-active sites can be obtained.
Automatic testing of the digital micromirror device/sup TM/ (DMD/sup TM/) (1996)

The DMD is basically a special static RAM (SRAM) of a CMOS design capped with a multilevel metal process to produce the digital micromirror light modulating superstructure. Consequently, to properly test the DMD requires dc current, CMOS SRAM memory, plus specialized electro-optical testing. Texas Instruments has maintained a rigorous test development activity during its DMD development and preproduction phase that has resulted in the ability to automatically characterize a wide range of DMD devices, including defect states, contrast ratios, and mirror array reflection efficiencies.
Exogenous Cross-Linking Increases the Stability of Spinal Motion Segments (2006)

By reducing the neutral zone, exogenous cross-linking may help combat the progression of instability in degenerative disc disease.
Migraine: Pathophysiology, Pharmacology, Treatment and Future Trends (2003)

Migraine treatment has evolved into the scientific arena, but it seems still controversial whether migraine is primarily a vascular or a neurological dysfunction. Irrespective of this controversy, the levels of serotonin (5-hydroxytryptamine; 5-HT), a vasoconstrictor and a central neurotransmitter, seem to decrease during migraine (with associated carotid vasodilatation) whereas an i.v. infusion of 5-HT can abort migraine. In fact, 5-HT as well as ergotamine, dihydroergotamine and other antimigraine agents invariably produce vasoconstriction in the external carotid circulation. The last decade has witnessed the advent of sumatriptan and second generation triptans (e.g. zolmitriptan, rizatriptan, naratriptan), which belong to a new class of drugs, the 5-HT1B/1D/1F receptor agonists. Compared to sumatriptan, the second-generation triptans have a higher oral bioavailability and longer plasma half-life. In line with the vascular and neurogenic theories of migraine, all triptans produce selective carotid vasoconstriction (via 5-HT1B receptors) and presynaptic inhibition of the trigeminovascular inflammatory responses implicated in migraine (via 5-HT1D/5-ht1F receptors). Moreover, selective agonists at 5-HT1D (PNU-142633) and 5-ht1F (LY344864) receptors inhibit the trigeminovascular system without producing vasoconstriction. Nevertheless, PNU-142633 proved to be ineffective in the acute treatment of migraine, whilst LY344864 did show some efficacy when used in doses which interact with 5-HT1B receptors. Finally, although the triptans are effective antimigraine agents producing selective cranial vasoconstriction, efforts are being made to develop other effective antimigraine alternatives acting via the direct blockade of vasodilator mechanisms (e.g. antagonists at CGRP receptors, antagonists at 5-HT7 receptors, inhibitors of nitric oxide biosynthesis, etc). These alternatives will hopefully lead to fewer side effects.
Electrode shapes for a cylindrical electron beam (1955)

The problem of obtaining the electrode shapes which will maintain a cylindrical beam of space-charge limited current reduces to the problem of solving Laplace's equation for the electrostatic potential outside the space-charge region, with the appropriate boundary conditions on the surface of the beam. A new approximate analytical solution of the Laplace equation has been obtained, and numerical tables have been developed for designing the electrode shapes. A plot of the electrode shapes, which is applicable to either hollow or solid beams, has been drawn up. The shape of the outside electrodes is the same for either type of beam, but the hollow beam requires an additional set of electrodes located inside the beam. The shape of the outside electrodes agrees fairly well with that obtained previously by Pierce,(1) Harrison,(2) and Kuo Chu Ho and Moon.(3)
Synthesis and reactions of 1,2,3,4,5,6-hexahydro-3,6-dimethyl-2,6-methano-3-benzazocin-11-one (2,5-dimethyl-9-oxo-6,7-benzomorphan); a new route to 3-benzazocines (1983)

In second-order Beckmann reactions oximes of the title compound (1) and 1-[2-(N,N-dimethylamino)ethyl]-3,4-dihydro-1-methylnaphthalen-2(1H)-one (14) gave 1,2,3,4-tetrahydro-3,6-dimethyl-3-benzazocine-2-carbonitrile (8) and (E)-2-[o-(2-cyanoethyl)phenyl]-4-dimethylaminobut-2-ene (15), respectively. The benzazocine-2-carbonitrile (8) was hydrolysed to the corresponding carboxylic acid (10), which was converted into its ethyl (11) and methyl esters (12) and reduced to the 2-aminomethyl-3-benzazocine (13). An attempt to prepare the ethyl ester (11) in hot 10% aqueous ethanol saturated with hydrogen chloride resulted in ring contraction, to give 1-methyl-2-(N-methylaminomethyl)naphthalene (17). In a Pinner reaction in ethanol the benzazocine-2-carbonitrile (8) gave the corresponding amide (9) instead of the ethyl imidate.An evaluation of the May and Murphy synthesis of the title compound (1) is given. 1-[2-(N-Benzyl-N-methylamino)ethyl]-3,4-dihydro-1-methylnaphthalen-2(1H)-one (20), prepared from 1-[2-(N,N-dimethylamino)ethyl]-3,4-dihydro-1-methylnaphthalen-2(1H)-one and benzyl chloride, was converted into its ethylene acetal (31; R = CH2Ph) and removal of the benzyl group followed by hydrolysis of the deprotected acetal gave the 2,3,5,9b-tetrahydrobenz[e]indole (23; R = H), a key intermediate in the Takeda-style synthesis of the title compound. 1-[2-(N-Chloro-N-methylamino)ethyl]-3,4-dihydro-1-methylnaphthalen-2(1H)-one ethylene acetal (31; R = Cl) was prepared but failed to cyclise under various conditions.Under the same conditions 1-[2-(N-benzyl-N-methylamino)ethyl]-3,4-dihydro-1-methylnaphthalen-2(1H)-one (20; R = CH2Ph) failed to brominate whilst the corresponding 1-[2-(N-ethoxycarbonyl-N-methylamino)ethyl] compound (22; R1= Et, R2= H) gave its 3,3-dibromo derivative (28).
Inhibitory effects of fusarochromanone on melanoma growth (2007)

Fusarochromanone is a toxic metabolite produced by Fusarium equiseti, a fungus present in decaying cereal plants in northern latitudes; it has been detected in various food grains. Fusarochromanone has been shown to have both stimulatory and inhibitory effects on various mammalian cells, depending on the concentration used. Whether these cytotoxic effects can be used in the clinical treatment of tumors remains to be established. Here, we evaluated the effects of fusarochromanone on the growth of human melanoma cells both in vitro and in vivo. In vitro, low concentrations (0.1-1 nmol/l) of fusarochromanone were found to be cytotoxic to many melanoma cell lines. In contrast, growth of normal melanocytes was inhibited only at much higher fusarochromanone concentrations (100-200 nmol/l). In vivo, the growth of melanoma cells implanted subcutaneously in immuno-compromised mice was significantly (P<0.05) reduced by daily administration of fusarochromanone. Immunohistological analyses indicated a significant (P<0.05) increase in the expression of active caspase-3 in tumor masses of mice treated with fusarochromanone, compared with controls. Together, these observations show that fusarochromanone increased apoptosis of tumor cells and reduced tumor growth in vivo. Therefore, the effects of fusarochromanone warrant further investigation as an adjuvant molecule to prevent growth and recurrence of melanomas.
Involvement of a plasmid in the invasive ability of Shigella flexneri (1982)

Representative Shigella flexneri strains were studied to determine whether plasmids are involved in their virulence. All invasive S. flexneri strains, irrespective of serotype, were found to harbor a large plasmid of approximately 140 megadaltons in size, although some strains carried additional plasmid species. Spontaneous variants of strains of serotypes 1, 2, and 5 had lost this 140-megadalton plasmid and had concomitantly become avirulent, i.e., could neither invade HeLa cell monolayers nor produced keratoconjunctivitis in guinea pigs. To monitor plasmid transfer, the 140-megadalton plasmid of strain M90T (serotype 5) was tagged with the kanamycin resistance transposon Tn5. This tagged plasmid, pWR110, was not self-transmissible, but was mobilized by one of several different conjugative plasmids into avirulent derivatives of the heterologous serotypes 1 and 2 which had lost the comparable large plasmid. Transconjugants of both serotypes which had received pWR110 regained virulence. These data directly demonstrate that this large S. flexneri plasmid encodes or regulates some function(s) required for epithelial cell penetration.
Thermostable D-amino acid aminotransferase from a thermophilic Bacillus species (1989)

D-Amino acid aminotransferase was found in several thermophilic Bacillus species and purified to homogeneity from the best producer, Bacillus sp. YM-1, which was newly isolated from a sauna dust. The enzyme has a molecular weight of about 62,000 and consists of two subunits identical in molecular weight (30,000). It catalyzes transamination between various D-amino acids and alpha-keto acids, although the substrate specificity is narrower than the enzyme from the mesophile, Bacillus sphaericus (Yonaha, K., Misono, H., Yamamoto, T., and Soda, K. (1975) J. Biol. Chem. 250, 6983-6989). The Bacillus sp. YM-1 enzyme is most active at 60 degrees C and stable at high temperatures. Automated Edman degradation provided the N-terminal sequence of the first 20 amino acids, and carboxypeptidase Y digestion provided the C-terminal sequence of the last 3 amino acids. The amino acid sequence in the vicinity of the lysyl residue, Lys(Pxy), that binds pyridoxal 5'-phosphate was determined as Cys-Asp-Ile-Lys(Pxy)-Ser-Leu-Asn-Leu-Leu-Gly-Ala-Val-Leu-Ala-Lys- from the pyridoxyl peptide obtained by digestion with trypsin. The active site sequence is markedly different from those of L-amino acid aminotransferases and other pyridoxal 5'-phosphate-dependent enzymes.
Synthesis of Conformationally Preorganized and Cell-Permeable Guanidine-Based γ-Peptide Nucleic Acids (γGPNAs) (2009)

A general method for preparing optically pure guanidine-based gamma-peptide nucleic acid (gammaGPNA) monomers for all four natural nucleobases (A, C, G, and T) is described. These second-generation gammaGPNAs differ from the first-generation GPNAs in that the guanidinium group is installed at the gamma- instead of the alpha-position of the N-(2-aminoethyl)glycine backbone unit. This positional switch enables GPNAs to be synthesized from relatively cheap L- as opposed to D-amino acids. Unlike their alpha-predecessors, which are randomly folded, gammaGPNAs prepared from L-amino acids are preorganized into a right-handed helix and bind to DNA and RNA with exceptionally high affinity and sequence selectivity and are readily taken up by mammalian cells.
Identification of a novel serine/threonine kinase and a novel 15-kD protein as potential mediators of the gamma interferon-induced cell death. (1995)

Programmed cell death is often triggered by the interaction of some cytokines with their cell surface receptors. Here, we report that gamma interferon (IFN-gamma) induced in HeLa cells a type of cell death that had cytological characteristics of programmed cell death. In this system we have identified two novel genes whose expression was indispensable for the execution of this type of cell death. The rescue was based on positive growth selection of cells after transfection with antisense cDNA expression libraries. The antisense RNA-mediated inactivation of the two novel genes protected the cells from the IFN-gamma-induced cell death but not from the cytostatic effects of the cytokine or from a necrotic type of cell death. One of those genes (DAP-1) is expressed as a single 2.4-kb mRNA that codes for a basic, proline-rich, 15-kD protein. The second is transcribed into a single 6.3-kb mRNA and codes for a unique 160-kD calmodulin-dependent serine/threonine kinase (DAP kinase) that carries eight ankyrin repeats. The expression levels of the two DAP proteins were selectively reduced by the corresponding antisense RNAs. Altogether, it is suggested that these two novel genes are candidates for positive mediators of programmed cell death that is induced by IFN-gamma.
The multistable charge-controlled memory effect in SOI MOS transistors at low temperatures (1990)

A phenomenon called the MCCM (multistable charge-controlled memory) effect is observed in SOI MOS transistors working at lot temperatures. This MCCM effect essentially results in a controllable setting of the transistor threshold voltage by applying adequate voltage pulses (or up-down voltage sweeps) to one or more electrodes of the structure. A change in threshold voltage of several volts can be obtained. Stability on the order of hours and longer, depending on temperature and operational conditions, is observed. The physics behind the MCCM effect is discussed, and a simple analytical model is proposed. Some new applications based on the MCCM effect are briefly highlighted.< <ETX xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">&gt;</ETX>
Reduction of Myocardial Ischemia-Reperfusion Injury by Mechanical Tissue Resuscitation Using Sub-Atmospheric Pressure (2010)

Treatment of ischemic myocardium with MTR, for a controlled period of time during reperfusion, successfully reduced the extent of myocardial death after acute myocardial infarction. These data provide evidence that MTR using subatmospheric pressure may be a simple, efficacious, nonpharmacological, mechanical strategy for decreasing cardiomyocyte death following myocardial infarction, which can be delivered in the operating room.