gebhart/patrepeval huggingface dataset:
5-Amino-2-Aroylquinolines as Highly Potent Tubulin Polymerization Inhibitors (2010)

A series of aroylquinoline derivatives were synthesized and evaluated for anticancer activity. 5-Amino-6-methoxy-2-aroylquinoline 15 showed more potent antiproliferative activity (IC(50) values ranging from 0.2 to 0.4 nM) as compared to 1a (combretastatin A-4) (IC(50) = 1.9-835 nM) against various human cancer cell lines and a MDR-resistant cancer cell line. Compound 15 (IC(50) = 1.6 microM) exhibited more potent inhibition of tubulin polymerization than 1a (IC(50) = 2.1 microM) and showed strong binding property to the colchicine binding site of microtubules.
Small molecule matrix‐assisted laser desorption/ionization time‐of‐flight mass spectrometry using a polymer matrix (2004)

We have employed a light-absorbing electrically conductive polymer as a matrix to determine the molecular mass of small organic molecules using matrix-assisted laser desorption/ionization time-of-flight (MALDI-TOF) mass spectrometry. This method, which is in contrast to the usual MALDI strategy for matrix selection in which a small molecule matrix is used with a high molecular mass analyte, addresses the problem of matrix interference which limits the usefulness of MALDI-TOF for small molecule analysis. Use of negative ion mode offers advantages for this application. Using this approach, we have obtained clean molecular ion mass spectra of small organic molecules in the mass range 100-300 Da.
Basement Membranes: Cell Scaffoldings and Signaling Platforms (2010)

Basement membranes are widely distributed extracellular matrices that coat the basal aspect of epithelial and endothelial cells and surround muscle, fat, and Schwann cells. These extracellular matrices, first expressed in early embryogenesis, are self-assembled on competent cell surfaces through binding interactions among laminins, type IV collagens, nidogens, and proteoglycans. They form stabilizing extensions of the plasma membrane that provide cell adhesion and that act as solid-phase agonists. Basement membranes play a role in tissue and organ morphogenesis and help maintain function in the adult. Mutations adversely affecting expression of the different structural components are associated with developmental arrest at different stages as well as postnatal diseases of muscle, nerve, brain, eye, skin, vasculature, and kidney.
Information Dropout: Learning Optimal Representations Through Noisy Computation (2016)

The cross-entropy loss commonly used in deep learning is closely related to the defining properties of optimal representations, but does not enforce some of the key properties. We show that this can be solved by adding a regularization term, which is in turn related to injecting multiplicative noise in the activations of a Deep Neural Network, a special case of which is the common practice of dropout. We show that our regularized loss function can be efficiently minimized using Information Dropout, a generalization of dropout rooted in information theoretic principles that automatically adapts to the data and can better exploit architectures of limited capacity. When the task is the reconstruction of the input, we show that our loss function yields a Variational Autoencoder as a special case, thus providing a link between representation learning, information theory and variational inference. Finally, we prove that we can promote the creation of disentangled representations simply by enforcing a factorized prior, a fact that has been observed empirically in recent work. Our experiments validate the theoretical intuitions behind our method, and we find that information dropout achieves a comparable or better generalization performance than binary dropout, especially on smaller models, since it can automatically adapt the noise to the structure of the network, as well as to the test sample.
NAD in Skin: Therapeutic Approaches for Niacin (2009)

The maintenance and regulation of cellular NAD(P)(H) content and its influence on cell function involves many metabolic pathways, some of which remain poorly understood. Niacin deficiency in humans, which leads to low NAD status, causes sun sensitivity in skin, indicative of deficiencies in responding to UV damage. Animal models of niacin deficiency demonstrate genomic instability and increased cancer development in sensitive tissues including skin. Cell culture models of niacin deficiency have allowed the identification of NAD-dependent signaling events critical in early skin carcinogenesis. Niacin restriction in immortalized keratinocytes leads to an increased expression and activity of NADPH oxidase resulting in an accumulation of ROS, providing a potential survival mechanism as has been shown to occur in cancer cells. Niacin deficient keratinocytes are more sensitive to photodamage, as both poly(ADP-ribose) polymerases and Sirtuins are inhibited by the unavailability of their substrate, NAD+, leading to unrepaired DNA damage upon photodamage and a subsequent increase in cell death. Furthermore, the identification of the nicotinic acid receptor in human skin keratinocytes provides a further link to niacin's role as a potential skin cancer prevention agent and suggests the nicotinic acid receptor as a potential target for skin cancer prevention agents. The new roles for niacin as a modulator of differentiation and photo-immune suppression and niacin status as a critical resistance factor for UV damaged skin cells are reviewed here.
Role of histamine in natural killer cell-mediated resistance against tumor cells. (1990)

The formation of lung metastases by i.v.-injected B16 melanoma (F1 and F10 strain) cells in Swiss albino, C57BL/6, and BALB/c mice was reduced by a single dose of histamine given 24 h before tumor cell inoculation. The antimetastatic effect of histamine was specifically mediated by histamine H2-receptors (H2R): it was blocked by the H2R antagonist ranitidine and mimicked by dimaprit, a specific H2R agonist but not by an H2R-inactive structural analog of this compound, nor-dimaprit, or the H1R agonist 2-thiazolyl-ethylamide. A single dose of any of the H2R antagonists ranitidine, tiotidine, famotidine, or cimetidine drastically augmented metastasis. Effects of H2R-interactive compounds on B16 metastasis required intact NK cells, as judged by the inability of histamine or ranitidine to affect B16 metastasis after NK cell depletion in vivo using antibodies to asialo-GM1. NK-cell-mediated lysis of YAC-1 lymphoma cells in vivo was enhanced by histamine and reduced by ranitidine within 4 h after inoculation of tumor cells. The antimetastatic effect of IL-2 was potentiated by histamine; in some experiments, combined treatment with a low dose of IL-2 (6000 U/kg) and histamine completely eliminated metastasis, whereas concomitant treatment with ranitidine abrogated antimetastatic effects of IL-2; animals treated with ranitidine and IL-2 displayed the same level of enhanced metastasis as those treated with ranitidine alone. The presented data are suggestive of an earlier unrecognized role for histamine in NK cell-mediated resistance against metastatic tumor cells.
Effect on the semiconductor laser intensity noise spectrum of propagation in dispersive optical fiber (1996)

Summary form only given. In the application of semiconductor lasers to fiber communications, the dependence of dispersion-induced pulse distortion (for digital systems) and modulation response changes (for analog systems) on the frequency modulation or chirp of the laser is a basic issue that often limits system performance. This has consequences for applications in which the laser intensity noise is the limiting factor in the system signal-to-noise ratio.
Tables for Cascaded Homogeneous Quarter-Wave Transformers (Correction) (1960)

Leo Young, the author of "Tables for Cascaded Homogeneous Quarter- Wave Transformers," which appeared on pages 233-237 in the April, 1959 issue of these Transactions, has requested that the following revisions be made in his paper.
β-Tricalcium Phosphate Coating on Titanium (1991)

Bioactive β-tricalcium phosphate (β-TCP) coating onto titanium was studied. It is shown that the β-TCP adhered to the surface of a titanium plate by the use of a frit, which was composed of CaO, TiO2, P2O5 and a few mol% Na2O. The frit as a coated layer resulted in the formation of β-TCP and CaTi4(PO4)6 phases by a thermal treatment at 800°C for 24h.
Tumor angiogenesis and interstitial hypertension. (1996)

Due to the high permeability of tumor vessels to fluids and plasma proteins, the microvascular pressure (MVP) is the principal driving force for interstitial hypertension in solid tumors; as a result, hydrostatic pressures between the microvascular and interstitial space are close to equilibrium. Based on these observations, we hypothesized that the tumor interstitial fluid pressure (IFP) should increase following the onset of angiogenesis. To this end, the relationship between IFP and tumor neovascularization was determined in the human colon adenocarcinoma (LS174T) and the murine carcinoma (MCaIV) implanted in a transparent dorsal skin fold chamber in severe combined immunodeficient mice. Three stages in the development of the tumor neovasculature were characterized by intravital microscopy. Stage I tumors were avascular, stage II was characterized by vascular sprouts and loops, and in stage III, the tumor vasculature was completely developed and blood flow was obvious. The IFP was measured with micropipettes and a servo-null system. For both tumor types, the IFP in stage I tumors was close to 0 mm Hg, and IFP increased significantly from one stage to the next. To further confirm that interstitial hypertension was associated with the development of the tumor vasculature, IFP was measured in LS174T spheroids. The mean pressure in spheroids was 0.2 +/- 0.3 mm Hg. In stage III tumors, the IFP was compared to the MVP. In MCaIV, the MVP was comparable to the IFP; however, in LS174T the MVP was significantly higher than the IFP. In conclusion, the results demonstrate that avascular tumors have atmospheric pressures and that tumor interstitial hypertension is associated with the development of the neovasculature.
Sultan II. Abdülhamit Döneminde bir “Çerkes Tarihi” Yazılması Girişimi (2008)

Kafkaslar, 1774 Küçük Kaynarca Antlaşması’ndan itibaren Çarlık Rusyası ile Osmanlı İmparatorluğu arasında şiddetli bir mücadele alanı haline gelmiştir. Bu mücadelede Çerkesler, Osmanlı tarafını tutarak, Ruslara karşı amansız bir savaşım içine girmişlerdir. Kırım Savaşı’ndan sonra ise Ruslar, Kafkaslar yönünde kararlı şekilde ilerlemişler, diğer Kafkas kavimleri ile birlikte Çerkesleri de hâkimiyetleri altına almışlardır. Bunun üzerine yurtlarından ayrılmak zorunda kalan Çerkesler, Osmanlı İmparatorluğu’nun çeşitli yerlerine yerleştirilmişler, buralarda ulusal varlıklarını korumaya çalışmışlardır. İşte bu ortamda, 1882 yılında kaleme aldıkları kapsamlı bir Çerkes Tarihi tasarısı, gerek Osmanlı tarih yazımı gerekse Çerkes tarih yazımı açısından önemli bir girişimdir. Bu girişim, geleneksel Osmanlı tarih yazımı çizgisinde ve ümmetçi-milletçi nitelikte bir tarih anlayışının ürünü sayılabilir
Reflectance Difference Spectroscopy Characterization of AlxGa1xN-Compound Layers (1999)

We report reflectance-difference spectroscopy characterization of AlxGa1—xN-compound layers grown on sapphire and 6H-SiC. We observe interference features below the bandgap, a derivative feature at the bandgap, and no signal or a broad feature above the bandgap. We present simulations of the data which are based on the assumption that the c-axis is tilted with respect to the surface normal, which results in an apparent bulk anisotropy in the hexagonal layers in normal-incidence reflectance measurements. We discuss implications with respect to a model by Tersoff [1], who suggested the formation of macrosteps during epitaxy.
Phosphatidylinositol 4-Kinase: Gene Structure and Requirement for Yeast Cell Viability (1993)

Phosphatidylinositol (PtdIns) 4-kinase catalyzes the first step in the biosynthesis of PtdIns-4,5-bisphosphate (PtdIns[4,5]P2). Hydrolysis of PtdIns[4,5]P2 in response to extracellular stimuli is thought to initiate intracellular signaling cascades that modulate cell proliferation and differentiation. The PIK1 gene encoding a PtdIns 4-kinase from the yeast Saccharomyces cerevisiae was isolated by polymerase chain reaction (PCR) with oligonucleotides based on the sequence of peptides derived from the purified enzyme. The sequence of the PIK1 gene product bears similarities to that of PtdIns 3-kinases from mammals (p110) and yeast (Vps34p). Expression of PIK1 from a multicopy plasmid elevated PtdIns 4-kinase activity and enhanced the response to mating pheromone. A pik1 null mutant was inviable, indicating that PtdIns4P and presumably PtdIns[4,5]P2 are indispensable phospholipids.
Enterprise Systems Architecture/370: An architecture for multiple virtual space access and authorization (1989)

The Enterprise Systems Architecture/370™ provides a significant step in the IBM System/370 evolution by providing new capabilities for virtual addressing and program linkage across multiple address spaces. This paper reviews the evolution that led to this advance and illuminates the goals, such as eliminating growth constraints and improving security, integrity, reliability, and performance, that have guided it. The major architectural capabilities are discussed, along with the system environments in which they are useful. The rationale for design choices is presented and related to issues of performance, access authorization, and constraints relief.
Effect of Gallium-Porphyrin Analogue ATX-70 on Nitroxide Formation from a Cyclic Secondary Amine by Ultrasound: On the Mechanism of Sonodynamic Activation (1995)

Sonodynamic therapy is a promising new modality for cancer treatment based on the synergistic effect on tumor cell killing by combination of a drug (typically a photosensitizer) and ultrasound. The mechanism of sonodynamic action was suggested to involve photoexcitation of the sensitizer by sonoluminescent light, with subsequent formation of singlet oxygen. In this work we studied the aqueous sonochemical reactions of the gallium-porphyrin derivative ATX-70, one of the most active sonodynamic agents found, using 50 kHz ultrasound. The experiments were carried out in the presence of 2,2,6,6-tetramethyl-4-piperidone hydrochloride (TMP), which reacts with singlet oxygen or .OH radicals to give the EPR-detectable nitroxide 2,2,6,6-tetramethyl-4-piperidone-N-oxyl (TMP-NO). Recently it has been suggested that the enhancement of TMP-NO yields in the presence of aqueous solutions of ATX-70 exposed to ultrasound was evidence for the formation of singlet oxygen in the system. Our results show that the surfactant cetyltrimethylammonium bromide (CTAB) can mimic the ATX-70-induced increase in the TMP-NO signal, but it fails to reproduce the behavior of ATX-70 in D2O: while the yields of TMP-NO in the presence of ATX-70 increase in D2O, the opposite effect was found with the surfactant CTAB. However, our data show that the increased TMP-NO yields in D2O are paralleled by an increased concentration of ATX-70 dimer, a form that is inactive in the photochemical generation of singlet oxygen. Our finding that the ATX-70-dependent enhancement of the TMP-NO signal was highest at approximately 20% O2, in both N2/O2 and argon/O2 mixtures, and decreased with increasing oxygen concentration is not compatible with the singlet oxygen mechanism. Finally, our results on the temperature dependence of the ATX-70-induced formation of TMP-NO are not consistent with the photochemical excitation of ATX-70 by sonoluminescent light: the ATX-70-dependent enhancement of TMP-NO signal increased with temperature in the range 10-25 degrees C, while the intensity of sonoluminescence of aqueous solutions both in multiple-bubble fields and in single-bubble experiments is known to decrease with increasing temperature.
Aptamers : the new frontier in drug development? (2007)

Often called chemical antibodies, aptamers are poised to take on the monoclonal antibodies in therapeutics, diagnostics, and drug development. Stability, low toxicity and immunogenicity, and, perhaps, a higher safety profile - not to mention low-cost advantages - are drawing the attention of big pharma and biotech.
Magnetic Properties of Cube-Textured 6–81.3 Mo—Permalloy (1964)

A study was made of the magnetic properties of Mo—Permalloy sheets containing 5.3%–6.8% Mo and 79.5%–82.5% Ni that had been cold rolled and annealed to obtain a nearly perfect (100)[001] texture. Square hysteresis loops were obtained only in compositions of about 81.3% Ni quenched from temperatures greater than 500°C, in hydrogen. Magnetic properties of spiral cores made of insulated 0.05 mm thick 6–81.3 Mo—Permalloy tapes were as follows: (a) When annealed at 1150°C to prevent secondary recrystallization, a square loop with μm=1200 000, μ0≤10 000, Hc=0.004 Oe, and Mr/Ms=0.92 was obtained. (b) When annealed at 1170°C, secondary recrystallization occurred; the μ0 of the core was increased to 160 000.
Propulsion Utilizing Laser-Driven Ponderomotive Fields for Deep-Space Missions (2009)

The generation of large amplitude electric fields in plasmas by high‐power lasers has been studied for several years in the context of high‐energy particle acceleration. Fields on the order of GeV/m are generated in the plasma wake of the laser by non‐linear ponderomotive forces. The laser fields generate longitudinal and translational electron plasma waves with phase velocities close to the speed of light. These fields and velocities offer the potential to revolutionize spacecraft propulsion, leading to extended deep space robotic probes. Based on these initial calculations, plasma acceleration by means of laser‐induced ponderomotive forces appears to offer significant potential for spacecraft propulsion. Relatively high‐efficiencies appear possible with proper beam conditioning, resulting in an order of magnitude more thrust than alternative concepts for high ISP (>105 s) and elimination of the primary life‐limiting erosion phenomena associated with conventional electric propulsion systems. Ponderomotive propulsion readily lends itself to beamed power which might overcome some of the constraints of power‐limited propulsion concepts. A preliminary assessment of the impact of these propulsion systems for several promising configurations on mission architectures has been conducted. Emphasizing interstellar and interstellar‐precursor applications, performance and technical requirements are identified for a number of missions. The use of in‐situ plasma and gas for propellant is evaluated as well.
The Intact Central Nervous System of the Newborn Opossum in Long-Term Culture: Fine Structure and Gaba-Mediated Inhibition of Electrical Activity (1991)

1. The entire central nervous system (CNS) of the newly born, South American opossum (Monodelphis domestica) was isolated and maintained in basal medium, Eagle's (BME) with 0.2% foetal calf serum and antibiotics. Isolated CNS preparations remained electrically excitable for up to 10 days. The fine structure of the spinal cord was normal after 5 days in culture: axons, synapses, dendrites and glia were virtually unchanged. Signs of degeneration were evident only in dorsal areas of the spinal cord, which had been denervated by removal of the dorsal root ganglia during dissection. 2. Amino acid transmitters such as glycine, glutamate, N-methyl-D-aspartate (NMDA) and gamma-aminobutyric acid (GABA), applied to the bathing fluid, rapidly and reversibly inhibited synaptic transmission in cervical segments of the spinal cord. GABA (10-100 mumol l-1) produced a dose-dependent reduction in the magnitude of ventral root responses evoked by dorsal root stimulation. GABA also inhibited synaptically activated compound action potentials produced by spinal cord stimulation. Dose-response curves for GABA obtained in different preparations were highly reproducible. 3. Both GABAA and GABAB receptors were reversibly activated by selective agonists and inhibited by specific antagonists. The actions of GABA were potentiated by benzodiazepines, competitively antagonised by bicuculline (a selective GABAA antagonist) and mimicked by muscimol (a GABAA agonist). Baclofen (a specific GABAB agonist) also inhibited electrical activity and was competitively antagonised by the GABAB antagonist, CGP 35348. 4. After 5 days of culture in BME or minimal essential medium (MEM), GABA dose-response curves were unchanged from those observed immediately after removal of the CNS. The inhibitory potency of baclofen was also unaffected by culture in BME. By contrast, after 5 days of culture in MEM, baclofen no longer inhibited electrical activity. This difference between BME and MEM could be attributed to the higher content of L-histidine in MEM. Thus, addition of 150 mumol l-1 L-histidine to BME produced similar results to culture in MEM: the inhibitory action of baclofen was virtually abolished after 3-5 days. L-Histidine had no effect on freshly dissected preparations. Chronic application of L-histidine did not affect glycine or glutamate responses after 5 days. Addition of D-histidine or other amino acids, such as arginine, to BME did not abolish the responses to baclofen. 5. These results show that the isolated CNS of the newborn opossum survives well in long-term culture and that it provides a useful preparation to study receptor development and plasticity of an intact mammalian CNS in vitro.(ABSTRACT TRUNCATED AT 400 WORDS)
Robust Regression Computation Using Iteratively Reweighted Least Squares (1990)

Several variants of Newton’s method are used to obtain estimates of solution vectors and residual vectors for the linear model $Ax = b + e = b_{true} $ using an iteratively reweighted least squares criterion, which tends to diminish the influence of outliers compared with the standard least squares criterion. Algorithms appropriate for dense and sparse matrices are presented. Solving Newton’s linear system using updated matrix factorizations or the (unpreconditioned) conjugate gradient iteration gives the most effective algorithms. Four weighting functions are compared, and results are given for sparse well-conditioned and ill-conditioned problems.