gebhart/patrepeval huggingface dataset:
Targeting of Liposomes to Solid Tumors: The Case of Sterically Stabilized Anti-Her2 Immunoliposomes (1997)

Novel therapies for cancer call for a carrier capable of intracellular delivery of systemically administered drugs to cancer cells in solid tumors. Such carrier, sterically stabilized immunoliposomes specific to the cells expressing HER2 protooncogene (anti-HER2 SSL), was designed by conjugating Fab' fragments of a recombinant humanized anti-HER2 MAb to the distal termini of poly(ethylene glycol) chains on the surface of unilamellar liposomes (size 90-100 nm) of phosphatidylcholine, cholesterol, and poly(ethylene glycol)-derivatized phosphatidylethanolamine. Anti-HER2 SSL avidly and specifically bound to cultured HER2-overexpressing cancer cells (8,000-23,000 vesicles per cell) and became endocytosed (ke=0.022–0.033 min.-1) via the coated pit pathway. Anti-HER2 SSL showed prolonged circulation lifetime in rats (blood MRT approx. 24 hours) and significantly increased antitumor activity of encapsulated doxorubicin against HER2-overexpressing human breast cancer xenografts in nude mice. Although the accumulation of anti-HER2 SSL in HER2-overexpressing tumor xenografts was not increased over that of non-targeted SSL, microscopic examination revealed abundance of anti-HER2 SSL in the interstitial spaces, as well as within the cytoplasm of cancer cells, while identical liposomes lacking anti-HER2 Fab' were located predominantly within tumor-resident macrophages. Anti-HER2 SSL, a targeted vehicle capable of in vivo intracellular delivery of substances to HER2-overexpressing solid cancers, enhances the potential for tumor targeting and opens new avenues for better treatment of cancer.
Single analyzer precursor scans using an ion trap (2016)

Secular frequency scanning is a nonconventional method of mass scanning that in combination with product ion ejection enables precursor scans in single ion traps. This phenomenon is demonstrated here for a miniature linear ion trap, but the concepts described also apply to quadrupole mass filters. Copyright © 2016 John Wiley & Sons, Ltd.
A subspace approach for blind estimation of time-varying channels under STBC transmissions (2008)

In this paper we consider the problem of blind estimation of time-varying multiple-input multiple-output (MIMO) channels under space-time block coded (STBC) transmissions. Firstly, the time-varying channel is deterministically represented by means of a basis expansion model (BEM), which reduces the number of parameters to be estimated. Secondly, the STBC structure is exploited to blindly recover the channel parameters by means of a subspace technique, which reduces to the solution of a generalized eigenvalue problem (GEV). Unlike previous approaches, the proposed method provides very accurate results even for non-orthogonal STBCs and high Doppler frequencies, which is illustrated by means of some numerical examples.
Rapid Antimanic Effect of Risperidone Monotherapy: A 3-Week Multicenter, Double-Blind, Placebo-Controlled Trial (2004)

Risperidone monotherapy was significantly more efficacious than placebo in the treatment of acute mania and demonstrated a rapid onset of action. Risperidone was well tolerated by patients in this study.
STORING UP TROUBLE: DOES ACCUMULATION OF INTRAMYOCELLULAR TRIGLYCERIDE PROTECT SKELETAL MUSCLE FROM INSULIN RESISTANCE? (2008)

1. Insulin resistance occurs when normal amounts of insulin are inadequate to produce a normal insulin response from cells. This is important in the context of whole-body glucose homeostasis because skeletal muscle is the main tissue for insulin-stimulated glucose disposal. 2. In obesity, lipid deposition in peripheral tissues, such as skeletal muscle, is linked to the activation of stress kinases and the development of insulin resistance. Accumulation of intramyocellular triglyceride (IMTG) is positively associated with insulin resistance; however, it is unknown whether IMTG causes insulin resistance or protects cells from insulin resistance by preventing the accrual of bioactive lipid metabolites. 3. The role of IMTG in the development of insulin resistance is not resolved. Stable overexpression of the triglyceride lipase adipose triglyceride lipase (ATGL) reduced IMTG content in myotubes, but resulted in a concomitant increase in diacylglycerol (DAG) and ceramide and caused insulin resistance. Increasing TG content by muscle-specific overexpression of diacylglycerol acyltransferase (DGAT) 1 protected mice from insulin resistance. Conversely, overexpression of DGAT2 in glycolytic muscle resulted in accumulation of TG and ceramide and insulin resistance in these tissues. This was sufficient to induce whole-body insulin and glucose insensitivity. 4. It is unlikely that IMTG causes cause insulin resistance directly. Instead, it appears as though TG accumulates in skeletal muscle to sequester fatty acids and to protect from the deleterious actions of lipids, such as ceramide and DAG. Whether lipase inhibitors are viable therapeutics to prevent obesity induced insulin resistance is unknown, but future studies examining tissue-specific ATGL/hormone-sensitive lipase knockouts will hopefully resolve this question.
Curcumin Derivatives Inhibit or Modulate Beta-Amyloid Precursor Protein Metabolism (2007)

Curcumin-derived oxazoles and pyrazoles were synthesized in order to minimize the metal chelation properties of curcumin. The reduced rotational freedom and the absence of stereoisomers was anticipated to enhance the inhibition of gamma-secretase. Accordingly, the replacement of the 1,3-dicarbonyl moiety by isosteric heterocycles turned curcumin analogue oxazoles and pyrazoles into potent gamma-secretase inhibitors. Compounds 4a-i were found to be potent inhibitors of gamma-secretase and displayed activity in the low micromolar range.
Mutants of the RNA-Dependent Protein Kinase (PKR) Lacking Double-Stranded RNA Binding Domain I Can Act as Transdominant Inhibitors and Induce Malignant Transformation (1995)

Recently we reported that introduction of catalytically inactive PKR molecules into NIH 3T3 cells causes malignant transformation and the development of tumors in nude mice. We have proposed that PKR may be a tumor suppressor gene possibly because of its translational inhibitory properties. We have now designed and characterized a number of PKR mutants encoding proteins that retain their catalytic competence but are mutated in their regulatory double-stranded RNA (dsRNA) binding domains (RBDs). RNA binding analysis revealed that PKR proteins either lacking or with point mutations in the first RBD (RBD-1) bound negligible amounts of dsRNA activator or adenovirus VAI RNA inhibitor. Despite the lack of binding, such variants remained functionally competent but were much less active than wild-type PKR. PKR variants completely lacking RBD-1 were largely unresponsive to dsRNA in activation assays but could be activated by heparin. To complement these studies, we evaluated the effects of point mutations in RBD-1 or the removal of either RBD-1 or RBD-2 on the proliferation rate of mouse 3T3 cells. We were unsuccessful at isolating stably transformed cells expressing RBD-1 point mutants or RBD-2-minus mutants. In contrast, NIH 3T3 cells, which constitutively expressed PKR proteins that lacked RBD-1, were selected. These cells displayed a transformed phenotype and caused tumors after inoculation in nude mice. Further, levels of endogenous eIF-2 alpha phosphorylation in RBD-1-minus cell lines were reduced, suggesting that such mutants act in a dominant negative manner to inhibit the function of endogenous PKR. These results emphasize the importance of RBD-1 in PKR control of cell growth and provide additional evidence for the critical role played by PKR in the regulation of malignant transformation.
Role of cAMP in regulating cytotoxic T lymphocyte adhesion and motility (1993)

We investigated the functional role of the cAMP pathway in human cytotoxic T lymphocyte (CTL)-target interaction. Pharmacological increase of intracellular cAMP concentration ([cAMP]i) inhibits killing, especially at low effector-to-target ratios, suggesting an inhibitory effect on CTL recycling. We show that this inhibitory effect is primarily at the level of conjugate formation. Pharmacological increase in [cAMP]i, as well as treatment with cytochalasin D, results in a "rounding up" of the CTL and inhibition of the dramatic changes in shape that occur when a CTL forms a conjugate, even with an irrelevant target. In addition, pharmacological increase in [cAMP]i affects the cytoskeleton of the CTL since it induces a decrease of filamentous actin, as detected by flow cytometry on phalloidin-stained CTL, and a stabilization of microtubules, as detected by increased resistance to the disrupting action of nocodazole. In mature CTL (but not in their immature precursors), T cell receptor triggering by specific targets results in a measurable increase in cAMP levels and strongly synergizes with adenylyl cyclase activators such as prostaglandin E2, cholera toxin and forskolin. We suggest that T cell receptor triggering may induce accumulation of cAMP that interferes with cytoskeleton function and, thus, terminates CTL secretion and adhesion. These effects of cAMP are rapidly reversible and may regulate CTL recycling.
Rapid prototyping using field-programmable logic devices (2000)

Traditionally, undergraduates in electrical and computer engineering study the design and implementation of a simple computer and then develop their own designs. In recent years, computer design courses have for the most part taken a simulation-only approach. Rapid prototyping techniques and a new generation of large field-programmable logic devices (FPLDs) enabled an educational approach that combines modeling with hardware description languages (HDLs), extensive simulation, synthesis, and final verification on a hardware prototype. The author describes an undergraduate computer engineering curriculum using a rapid prototyping approach to simulate, synthesize, and implement digital system and computer architectures.
STUDIES IN EXPERIMENTAL EXTRACORPOREAL THROMBOSIS (1927)

The effects of environmental temperature on thrombosis in circulating blood were tested in the extracorporeal loop by the method previously described. Cold (7 degrees to 15 degrees C.) about the collodion tube retards the clotting of circulating blood. Obstruction of the arterial cannula occurs after from 15 to 25 minutes. Heat (40 degrees and 55 degrees C.) tends to hasten clotting; obstruction by red clot takes place after from 4 to 6 minutes and from 2 to 4 minutes, respectively. In the latter case no characteristic thrombus structure may be seen. These results were what might be expected. The formation of white thrombi occurs even under the influence of cold, and they continue to form and grow as long as the circulation continues. When the carotid artery is partially occluded and the blood stream slowed, after the injection of the anticoagulant, the blood has a tendency to form red thrombi on the foreign surface of the vascular loop. The thrombi are deposited chiefly in the arterial half of the apparatus, especially at the bottom of the arterial end of the collodion tube, just as in the case of Aschoff's sand experiments. In spite of incoagulability of heparinized blood, red clots, with interwoven fibrin bands, are found. Also very tiny white thrombi may form in other parts of the collodion tube. The effect of complete obstruction of the carotid artery and jugular vein on thrombus formation was studied after the use of anticoagulant. When the carotid artery is obstructed the formation of white thrombi is negligible and sedimentation of erythrocytes and deposition of fibrin appear throughout the apparatus; then the blood, at a standstill, clots very slowly. When the jugular vein is obstructed, dislodgment of platelet thrombi probably results from the pulsating movement, and sedimentation of erythrocytes follows, forming mixed thrombi. The dislodged white thrombi tend to gather in the bottom of the tubes of the widest caliber, especially in the collodion tube.
Concentration and Isolation of DNA from Biological Fluids by Agarose Gel Isotachophoresis (2005)

Isotachophoresis is an electrophoretic method of separation of charged substances. The method is characterized by a discontinuous buffer system, constant velocity of separated molecules, and the distribution of separated components in the form of narrow concentrated bands located one right after another. As a rule, isotachophoresis is not used for the separation of nucleic acids because the mobility of polynucleotides in this system does not depend on their size. However, this circumstance proved to be very useful for the quantitative isolation of heterogeneous DNA fragments from biological fluids, for gene diagnostics of cancer in particular. The proposed method of agarose gel isotachophoresis of DNA has been used for the isolation of blood DNA and its successful PCR analysis.
Optical Design of Intraocular Lenses. II. Off-Axis Performance (1989)

The effect of intraocular lens shape on off-axis performance of model pseudophakic eyes was investigated. Image quality criteria included an optimization procedure, spot diagrams, and the modulation transfer function (MTF). The optimum lens shape varies with lens fitting position, corneal asphericity, and pupil size. An earlier investigation showed that the optimum lens shape for on-axis imagery is approximately plano-convex, with the more curved surface facing the cornea. In this investigation, optimum lens shapes for a 10 degrees off-axis position ranged from near this shape to near the reversed shape, i.e., the more curved surface facing the retina. Because the on-axis case should carry more weight and because conditions favoring the reverse form include small pupils for which image quality is fairly insensitive to variations in lens shape, it is suggested that good forms for intraocular lenses range from plano-convex (curved surface facing cornea) to equi-convex.
Application of the remote photocyclization with a pair system of phthalimide and methylthio groups. A photochemical synthesis of crown ether analogs. (1983)

Based on the regioselective remote photocyclization of a pair system consisting of a phthalimide group and a methylthio group, a homologous series of N-substituted phthalimides (4) possessing a terminal sulfide function in the poly-ether side chain afforded, on irradiation, seven- to fifteen-membered crown ether analogs (5-7) in moderate yields.
A Rapid and Facile Conversion of Primary Amides and Aldoximes to Nitriles and Ketoximes to Amides with Triphenylphosphine and N‐Chlorosuccinimide. (2002)

Abstract For Abstract see ChemInform Abstract in Full Text.
Near-field microwave imaging of biologically-based materials using a monopole transceiver system (1998)

A prototype monopole-transceiver microwave imaging system has been implemented, and initial single and multitarget imaging experiments involving biologically relevant property distributions have been conducted to evaluate its performance relative to a previously developed-waveguide system. A new, simplified, but more effective calibration procedure has also been devised and tested. Results show that the calibration procedure leads to improvements which are independent of the type of radiator used. Specifically, data-model match is found to increase by 0.4 dB in magnitude and 4/spl deg/ in phase for the monopoles and by 0.6 dB in magnitude and 7/spl deg/ in phase for the waveguides (on average) on a per measurement basis when the new calibration procedure is employed. Enhancements are also found in the reconstructed images obtained with the monopole system relative to waveguides. Improvements are observed in: 1) the recovered object shape; 2) the uniformity of the background; 3) edge detection; and 4) target property value recovery. Analyses of reconstructed images also suggest that there is a systematic decrease of approximately 10% in the reconstruction errors for the monopole system over its waveguide counterpart in single-target experiments and as much as a 20% decrease in multitarget cases. Results indicate that these enhancements stem from a better data-model match for the monopoles relative to waveguides which is consistent across the type of calibration procedure used. Comparisons of computations and measurements show an average improvement in data-model match of approximately 0.25 dB in magnitude and near 7/spl deg/ in phase in favor of the monopoles in this regard. Beyond this apparent imaging performance enhancement, the monopole system offers economy-of-space and low construction-cost considerations along with computational advantages (as described herein) which make it a compelling choice as a radiator/receiver element around which to construct a clinically viable near-field microwave imaging system.
Cardiovascular Therapeutic Aspects of Soluble Epoxide Hydrolase Inhibitors (2006)

Soluble epoxide hydrolase (sEH) is an enzyme responsible for the conversion of lipid epoxides to diols by the addition of water. Biological actions on the cardiovascular system that are attributed to epoxides include vasodilation, antiinflammatory actions and vascular smooth muscle cell antimigratory actions. Conversion of arachidonic acid epoxides to diols by sEH diminishes the beneficial cardiovascular properties of these epoxyeicosano-ids. Cardiovascular diseases in animal models and humans have been associated with decreased epoxygenase activity or increased sEH activity and these changes are responsible for the progression of the disease state. More recently, sEH gene polymorphisms in the human population have been associated with increased risk for cardiovascular diseases. Thus the biological actions of epoxyeicosanoids and the sEH enzyme are ideal therapeutic targets for cardiovascular diseases. The rapid development of 1,3-disubstituted urea based sEH inhibitors over the past five years has resulted in a number of studies demonstrating cardiovascular protection. sEH inhibitors have antihypertensive and antiinflammatory actions and have been demonstrated to decrease cerebral ischemic and renal injury in rat models of hypertension. These findings of beneficial actions in animal models of disease position the sEH enzyme as a promising therapeutic target for cardiovascular diseases.
Structures and Properties of Nutshells (1996)

Fracture of tree nuts is not only of economic importance to the horticulture industry, as the most costly operation is extracting the kernels, but also of scientific interests. To date there is still no satisfactory explanation why nuts in general are tough to crack. In the present work, four different tree nuts were studied and it was found that, although whole nuts exhibited considerably different resistance to fracture, nutshells possess approximately the same mechanical and fracture properties. At microscopic scale, nutshells are effectively a class of randomly-orientated discontinuous fibre reinforced composite, comprising of randomly oriented bundles, which consisted of cells of relatively short length with a small aspect ratio. A theoretical model is presented, which provides a good prediction to the total load level required to fracture a nut.
A randomized phase II and pharmacokinetic study of the antisense oligonucleotides ISIS 3521 and ISIS 5132 in patients with hormone-refractory prostate cancer. (2002)

The antisense oligonucleotides ISIS 3521 and ISIS 5132, at these doses and on this schedule, do not possess clinically significant single-agent antitumor activity in HRPC. Protracted stable disease in some patients may indicate a cytostatic effect. Additional work is required to define the optimal role of PKC-alpha or Raf-1 inhibition in the treatment of HRPC.
Recombination in GaAs at the AlAs oxide-GaAs interface (1995)

Interface recombination in GaAs at the GaAs/AlAs interface has been investigated before and after selective ‘‘wet oxidation’’ of the AlAs layer. Time-resolved photoluminescence of the band-edge GaAs emission has been used to characterize the interface recombination. Prior to oxidation, the interface recombination is low. After oxidation, the interface recombination has greatly increased, and is comparable to a free GaAs surface in air. However, isolating the GaAs layer from the oxide by a 30 nm layer of Al0.3Ga0.7As allows the interface recombination to remain low after the oxidation. These results help explain the low threshold currents which have been observed in vertical cavity lasers which use wet oxidation of AlAs for current confinement.
Frequent loss of heterozygosity on chromosome 22 in hepatocellular carcinoma (1993)

We investigated 24 hepatocellular carcinomas in Japan to find loss of heterozygosity with 15 polymorphic DNA markers that detect allelic losses at specific chromosome loci. Loss of heterozygosity on chromosomes 10q, 17p and 22q was detected in 3 of 12 (25%), 9 of 21 (43%) and 5 of 15 (33%) informative cases of hepatocellular carcinoma, respectively. This is the first report of loss of heterozygosity on chromosome 22q in hepatocellular carcinoma; the newly recognized common chromosome loss was considered to exist between D22S9 and D22S10 on 22q11. On the basis of this and other studies, we believe it is likely that such a chromosome loss in hepatocellular carcinoma is a signal for malignant transformation and that loss of unknown genes on chromosomes 10q, 17p and 22q may contribute to tumor progression in hepatocellular carcinoma. (Hepatology 1993;17:794-799.)
High current density GaAs and GaSb photovoltaic cells for laser power beaming (2003)

AlGaAs/GaAs- and GaSb-based laser power PV converters operating at output photocurrent densities up to 100 A/cm/sup 2/ were fabricated. Fill Factor values of 0.85-0.87 at laser power density P/sub laser/=1.0-50 W/cm/sup 2/ and FF=0.80-0.83 at P/sub laser/=100-200 W/cm/sup 2/ were measured in the GaAs-based cells. Open circuit voltage of the GaAs cells increased from 1.15 V at P/sub laser/=5 W/cm/sup 2/ to 1.26 V at 200 W/cm/sup 2/. Efficiency of monochromatic (/spl lambda//sub laser/=820-850 nm) power conversion increased up to 56% with increasing P/sub laser/ up to 50 W/cm/sup 2/, and further decreased by 3-4% at P/sub laser/=200 W/cm/sup 2/. AlGaAs/GaAs converters with internal Bragg reflector ensured the photoresponse increase in the wavelength range of 830-870 nm as well as improvement of radiation resistance. Also, AlGaAsSb/GaSb laser power converters were developed for operation in spectral range of 1300-1680 nm.