gebhart/patrepeval huggingface dataset:
Synthesis, structure and affinity of novel 3-alkoxy-1,2-dihydro-3H-1,4-benzodiazepin-2-ones for CNS central and peripheral benzodiazepine receptors (2009)

A series of novel 3-alkoxy-1,2-dihydro-3H-1,4-benzodiazepin-2-ones (7-15) was synthesized and their in vitro affinity for both the central benzodiazepine receptor (CBR) and the peripheral benzodiazepine receptor (PBR) of rat brain was studied. Racemic mixture of 7-bromo-3-(2-methoxy)ethoxy-5-phenyl-1,2-dihydro-3H-1,4-benzodiazepin-2-one (13) was separated into enantiomers 14, 15 by chiral HPLC. Absolute configuration of R-enantiomer 15 was determined by the method of X-ray diffraction analysis. The affinity of S-enantiomer 14 for CBR ( IC50)=245 nM) is 20-fold higher than the affinity of R-enantiomer 15 (IC50)=4,930 nM). A high selectivity for CBR versus PBR (IC50) (PBR)>10,000 nM) was shown by all reported compounds. Compound 12 was revealed as a potent (IC50)=9 nM) and selective CBR ligand among the synthesized 3-alkoxy-1,2-dihydro-3H-1,4-benzodiazepin-2-ones.
Colloidal Dispersions of Platinum and Palladium Clusters Embedded in the Micelles.Preparation and Application to the Catalysis for Hydrogenation of Olefins (1992)

Abstract Colloidal dispersions of platinum and palladium clusters were prepared by the reduction of the corresponding metal salts in the presence of various surfactants. Hydrogen- and photo-reduction methods were examined for the micellar solution of hexachloroplatinic acid. The photo-reduction was proved to be more suitable than the hydrogen-reduction from the viewpoint of small size and good dispersion in the colloidal clusters. The higher surfactant concentration than the critical micelle concentration (cmc) is favorable for the production of the homogeneous colloidal dispersions. The photo-reduction method is also available for the case of palladium. The colloidal platinum and palladium clusters, thus obtained, act as highly active catalysts for the hydrogenation of olefin in an aqueous solution. The colloidal clusters prepared by the photo-reduction method showed higher activity than those prepared by other methods. The roles of the surfactant micelle for the hydrogenation are not only protecting hydrophobic colloidal particles, but also both solubilizing the hydrophobic substrates in an aqueous solution and assisting their approach toward the active site on the surface of the cluster particles. In the hydrogenation of unsaturated fatty acids, the surfactant micelle surrounding the clusters can control the orientation of the substrates, resulting in novel regioselective hydrogenation.
SU11657 Cooperates with Doxorubicin To Increase Survival of Leukemic Mice. (2006)

Abstract Acute promyelocytic leukemia (APL) is characterized by t(15,17) resulting in fusion of RARα to PML; in rare cases, RARα may be fused to other partners. The PML-RARα fusion initiates APL-like disease in mice, including a response to ATRA. FLT3, a receptor tyrosine kinase, is mutated in a large number of human AMLs and roughly 40% of cases of human APL. In our mouse model of APL, we previously introduced activated FLT3 (ITD mutation) into bone marrow of PML-RARα transgenic mice and observed rapid development of AML. This disease is transplantable into sublethally irradiated mice with onset of disease between 3–6 weeks, creating a system suitable for therapeutic study. There has been considerable effort focused on the development of small molecule inhibitors of FLT3 as therapeutics for hematological malignancies, in particular, AML; some of these inhibitors are currently in clinical trials. SU11657 is a multi-targeted inhibitor of class III/V receptor tyrosine kinases, including FLT3. We previously observed a synergistic effect of SU11657 in combination with ATRA in our PML-RARα/FLT3 model. We set out to use this model to assess the effectiveness of anthracycline chemotherapy in combination with SU11657. This model is in vivo resistant to the maximum tolerated dose of doxorubicin (3 mg/kg/day). We found that the median survival of untreated and doxorubicin-treated mice with PML-RARα/FLT3 leukemia was not significantly different (42 and 45 days, respectively). SU11657 increased the median of survival to 55 days, whereas the combination therapy increased median survival to 62 days (P=0.003). Neither agent alone or in combination significantly increased survival of mice with PML-RARα leukemia lacking activated FLT3. These results suggest that the use of targeted therapeutics, such as a FLT3 inhibitor, can overcome chemoresistance to traditional therapies in AMLs.
Comparative Analysis of Medaka Genes (2005)

報告番号: ; 学位授与年月日: 2006-03-23 ; 学位の種別: 修士; 学位の種類: 修士(科学) ; 学位記番号: 修創域第1905号 ; 研究科・専攻: 新領域創成科学研究科情報生命科学専攻
A physical layer solution for Tomlinson-Harashima precoding in the framework of LTE-Advanced (2012)

Tomlinson-Harashima precoding (THP), as a suboptimal realization of dirty paper coding, has attracted extensive attentions in recent years. However, in numerous studies, only a few of them considered the limitations and restrictions in reality. In this paper, we first point out three main limitations and restrictions of THP when implementing it in the framework of a real industrial system, i.e., the Long Term Evolution Advanced (LTE-A). Then, we propose a physical layer solution for THP in LTE-A, which mainly involves the precoding schemes for Physical Downlink Shared Channel (PDSCH), User Equipment (UE) specific Reference Signal (RS), and the receiver schemes. These schemes are then evaluated by simulations. The simulation result of linear precoding zero-forcing beamforming (ZF-BF) is also provided. The result shows that THP outperforms ZF-BF mainly in high correlation scenario. In low correlation scenario, ZF-BF is better than THP in the high Signal-Noise Ratio (SNR) region.
Gene transfer into the hematopoietic system. (1994)

Efficient transfer of heterologous genes into long-term reconstituting stem cells remains difficult to achieve in large animal models and humans. Long-term expression of introduced gene sequences in hematopoietic cells after gene transfer and bone marrow transplantation procedures is usually seen in less than 5% of cells. Retroviral vectors remain the standard tool for this technology, but these vectors have distinct disadvantages, such as the requirement for cycling target cells, random integration into the infected cell genome, and problems with long-term gene expression in long-term reconstituting stem cells. Novel retroviral vectors and producer cell lines that may address some of these problems have been constructed. In addition, modifications of the retroviral infection protocol and the use of alternative stem cell sources such as cord blood or mobilized peripheral blood cells have been tested with some promise. Recent data suggest that adeno-associated virus-based vector might prove an alternative to retroviral vectors in some cases.
Dapoxetine: A novel, fast-acting serotonin reuptake inhibitor (2005)

Dapoxetine (Alza/Ortho-McNeil) is a novel oral medication undergoing FDA review for premature ejaculation, one of the most common disorders of sexual dysfunction in men. Dapoxetine is a fast-acting inhibitor of the serotonin reuptake transporter. It has a short half-life and is structurally related to the antidepressant fluoxetine, allowing for on-demand dosing. Recent phase 3 clinical trials in patients with premature ejaculation have shown dapoxetine to be effective in improving the time to ejaculation without any major adverse events, except nausea. If approved, dapoxetine would be the first drug specifically indicated for premature ejaculation, and it may offer patients a safer and more tolerable alternative compared to traditional selective serotonin reuptake inhibitors (SSRIs), which are currently used off-label to treat this condition.
On vortex formation from a cylinder. Part 2. Control by splitter-plate interference (1988)

Control of vortex formation from a circular cylinder by a long plate in its wake is examined over the Reynolds number range 140 < Re < 3600. There are two basic flow regimes: a pre-vortex formation regime, in which the plate precludes formation of a large-scale vortex upstream of the tip of the plate; and a post-vortex formation regime in which one or more large-scale vortices are formed upstream of the edge. The unsteady pressure loading at the tip of the plate increases by over an order of magnitude during transition from the pre- to post-vortex formation regime. If the plate is located near the cylinder, it is possible to more than double the vortex formation length, relative to the case of the free wake. Moreover, these observations suggest that: there is a minimum streamwise lengthscale for development of the absolute instability of the near wake and thereby the large-scale vortex; and the vortex formation length may also be influenced by the downstream vorticity dynamics. When the plate is located downstream of the initially formed vortex, effective control is possible when the near-wake fluctuation level and mean base pressure of the corresponding free (non-impinging) wake are sufficiently small. This occurs in the low and moderate subcritical regimes; the substantial control by the wake-plate interaction in this range of Reynolds number implies low strength of the absolute instability of the near wake. However, in the pure von Kármán regime, selfcontrol of the near wake dominates that imposed by the wake-edge interaction, suggesting a strong absolute instability of the near wake.
Real-Time Estimation of Transmitted Torque on Each Clutch for Ground Vehicles With Dual Clutch Transmission (2014)

This paper mainly focuses on the robust separate estimation of transmitted torque on each clutch of the dual clutch transmission-the task that has not yet been accomplished by previously published efforts. In order to estimate the torque on individual clutches, the observer system is composed of a shaft model-based observer, unknown input observers, and a model reference PI observer. The estimations obtained by each subcomponents are processed together to provide online torque estimation of high accuracy. The proposed estimator requires the following information: speed measurements of engine, input shafts, and wheels, and nominal engine torque information obtained as a function of driver inputs and engine speed. These are already available in the current production cars; hence, no further modification or addition to the vehicle hardware is necessary. To validate the effectiveness of the proposed estimator, experiments using an actual vehicle are conducted with various scenarios. With detailed analysis of the results obtained by the experiments, the proposed dual clutch transmission torque estimator is shown to be apt for real car application.
Tumor-specific idiotype vaccines. II. Analysis of the tumor-related network response induced by the tumor and by internal image antigens (Ab2 <i>beta</i>). (1987)

In this study the tumor-specific immuneresponse induced by irradiated tumor cells (L1210/GZL) and by anti-idiotype antibodies was analyzed. The anti-idiotype antibodies (Ab2) were made against the paratope of a monoclonal antitumor antibody (11C1) that recognizes a tumor-associated antigen which cross-reacts with the mouse mammary tumor virus-encoded envelope glycoprotein 52. Two Ab2, 2F10 and 3A4, induced idiotypes expressed by the monoclonal antitumor antibodies 11C1 and 2B2. Cytotoxic T cells, generated by immunization with irradiated tumor cells, lyse 2F10 and 3A4 hybridoma cells. Furthermore, immunization with Ab2 induces tumor-specific cytotoxic T lymphocytes. The frequency of tumor-reactive cytotoxic T lymphocyte was found to be similar in mice immunized with Ab2 or irradiated tumor cells when examined at the precursor level. However, only 2F10 induces protective immunity against the growth of L1210/GZL tumor cells. The depletion of a L3T4+ T cell population from 2F10 immune mice was found to increase the effectiveness of transferred T cells to induce inhibition of tumor growth. The inability of 3A4 to induce antitumor immunity could be correlated with the presence of a population of Lyt2+ regulatory T cells. Collectively, these results demonstrate the existence of a regulatory network controlling the expression of effective tumor immunity. Our results demonstrate that selection of binding site-related Ab2 may not be a sufficient criteria for the development of an idiotype vaccine. A better understanding of the regulatory interactions induced by anti-idiotypes is needed for the design of effective antitumor immunotherapy.
21.5 A current-mode wireless power receiver with optimal resonant cycle tracking for implantable systems (2016)

Continuous health monitoring has become feasible, largely due to miniature implantable sensor systems such as [1]. To recharge batteries of such systems, wireless power transfer is a popular option since it is non-invasive. However, there are two main challenges: 1) strict safety regulations of incident power on human tissue; 2) small coil size for better biocompatibility. These issues reduce the received power at the coil, make it difficult to obtain sufficient power for implanted devices, and call for high power-efficiency (ηP)-transfer techniques, especially at very low received power levels.
Micromonospora RNA polymerase activity changes during stationary phase (1992)

RNA polymerase was isolated from Micromonospora echinospora and from Streptomyces lividans. In vitro transcription of a DNA fragment containing multiple tandem promoters from Micromonospora followed the pattern of expression observed previously for in vivo studies. RNA polymerase was prepared from cultures of Micromonospora that were harvested during the growing phase and during the stationary phase. Promoters that were utilized in Micromonospora only during the stationary phase were utilized in vitro only when RNA polymerase was purified from a stationary-phase culture, and not when RNA polymerase was purified from growing cells.
Acoustic sound from the electric guitar using DSP techniques (2002)

The electric guitar has been developed to withstand electric amplification and utilize (mostly analog) signal processing in order to create a multitude of timbres and sound types. Sometimes it would be desirable to play the same electric guitar, yet with a sound that resembles a good acoustic guitar or some other member of the plucked string instrument family. In this study we have investigated DSP techniques that can be used to shape the magnetic pickup output of the electric guitar to simulate acoustic instruments. This includes linear filtering for body simulation, time-varying modulation to generate beating of the harmonic components, and techniques to simulate the general temporal envelope of the plucked notes.
Integrating Cognitive Models Based on Different Computational Methods (2005)

The mind integrates cognitive and perceptual processes that are currently best modeled using many different computational mechanisms.These are difficult to integrate into a single cognitive model and are thus a challenge to developing a unified model of human cognition.This paper presents two computational principles that identify common elements among these mechanisms and uses these principles, together with empirical findings about human cognition, to motivate a theory of human cognitive architecture.This theory has been embodied in the Polyscheme cognitive architecture, which enables models based on qualitatively different computational mechanisms, including Bayesian Networks, search and production systems, to be integrated into a single cognitive model and thus provides an explanation of how the mind integrates multiple cognitive structures and processes.
Evolutionary conservation of the transcribed spacer sequences of the rDNA repeat unit in three species of the genus Aspergillus. (1994)

We have cloned and sequenced the two intervening transcribed spacers in the rDNA repeat unit of three Aspergillus species--A. nidulans, A. awamori and A. wentii. The A. wentii and A. awamori spacers are almost identical and share a high degree of homology with the A. nidulans spacers. All spacers have a high G-C content (66%-76%) and the potential of forming complex secondary structures, which may indicate that they play a role in the maturation of pre-rRNA molecules.
A 2-V 2-GHz Si-bipolar direct-conversion quadrature modulator (1996)

A 2-GHz Si-bipolar direct-conversion quadrature modulator with a wide bandwidth is described. It operates at a low supply-voltage of 2 V and features a "current-folded" double-balanced mixer with a two-stacked-transistor configuration, and a tunable RC/CR 90/spl deg/ phase shifter that reduces the amplitude imbalance and the phase error over a wide bandwidth (0.8 to 2 GHz). The modulator is implemented using 18-GHz Si-bipolar technology and dissipates only 68 mW at 2 V. The image ratio at 2 GHz is about -37 dBc, corresponding to a phase error of 1.6/spl deg/. Moreover, both second-order and third-order products, and local signal leakage are less than -40 dBc.
HIGH POWER RF WINDOW AND WAVEGUIDE COMPONENT. DEVELOPMENT AND TESTING ABOVE 100 MW AT X-BAND (1992)

SLAC is committed to developing an X-band source _ capable of producing 100~MW, I-ps pulses to power the
Generation of a Zebrafish P1 Artificial Chromosome Library (1999)

We have constructed a genomic P1 artificial chromosome library from the zebrafish. The library has been arrayed and archived in two hundred seventy-one 384-well microtiter dishes. It encompasses four to five genome equivalents with an average insert size of approximately 115 kb and is readily accessible to the scientific community. The library has been used by numerous investigators in the community and shown to be a useful reagent for chromosomal walking and positional cloning.
Effect of <i>Salacia reticulata</i> W. and <i>Clitoria ternatea</i> L. on the cognitive and behavioral changes in the streptozotocin-induced young diabetic rats (2017)

SRCT, a herbal formula, when used in combination, has a more potent effect in preventing the deleterious effects of juvenile diabetes on cognitive and behavioral changes.
A Stapled p53 Helix Targets HDMX to Overcome Nutlin-3 Resistance and Reactivate the p53 Tumor Suppressor Pathway in Cancer (2008)

Abstract p53 is a transcription factor that induces cell cycle arrest or apoptosis in response to DNA damage and cellular stress, and thereby plays a critical role in protecting cells from malignant transformation. The E3 ubiquitin ligase HDM2 controls p53 levels through a direct binding interaction that neutralizes the transactivation activity of p53 and targets it for degradation via the ubiquitylation-proteasomal pathway. Whereas the HDM2-homologue HDMX lacks ubiquitin ligase function, it participates in regulating the p53 axis by heterodimerizing with HDM2 and sequestering p53 through protein interaction. Loss of p53 activity, either by deletion, mutation, or HDM2/HDMX overexpression, is the most common defect in human cancer. Tumors expressing wild type p53 are rendered vulnerable by pharmacologic approaches that stabilize and upregulate p53. In this context, HDM2 and HDMX have emerged as independent therapeutic targets for restoring p53 activity and resensitizing cancer cells to apoptosis in vitro and in vivo. The small molecule nutlin-3 is an effective antagonist of the p53-HDM2 interaction. However, several studies have demonstrated the inability of nutlin-3 to disrupt the p53-HDMX complex, rendering tumor cells that overexpress HDMX nutlin-3-resistant. We have previously described the synthesis and characterization of a hydrocarbon-stapled alpha-helical p53 peptide (SAH-p53-8) that binds HDM2 with low nanomolar affinity, targets HDM2 in situ, and reactivates the p53 tumor suppressor pathway in HDM2-overexpressing osteosarcoma cells. We now report that SAH-p53-8 binds HDMX with even higher affinity, co-immunoprecipitates with endogenous HDMX, and induces apoptosis and cell cycle arrest in nutlin-3-resistant cancer cells that overexpress HDMX. Thus, by inserting a chemical staple into a peptide fragment of the p53 transactivation domain, we have generated the first bifunctional inhibitor of HDM2 and HDMX, enabling the investigation and pharmacologic modulation of both targets in human cancer.
Production of thin, uniform toner layers through use of a contact blade with mono-component development systems (1991)

The authors focus on the effects of contaminants on the uniformity of the toner layers resulting from the direct observation of the toner flow and metering phenomena. The authors have improved earlier observation methods to observe directly and analyze the toner transportation and toner behavior in the layer thickness control area. Using the improved method, they have experimented with the various kinds of toner transportations and layer thickness control systems. They concentrated on disruption of toner layers by contaminant infiltration and found that static toner and friction force against the toner on the developing sleeve are most important in preventing a contaminant from entering the metering area. Based on these results, they found a highly stable layer-forming method, called the contact blade method. which minimizes the effects of infiltration by contaminants.< <ETX xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">></ETX>
Self-contained spatial input device for wearable computers (2004)

In this paper, we present a pen-shaped input device forwearable computers which reproduce and recognizethree-dimensional (3D) hand motions with no externalreferences. The input device is equipped with inertialsensors. The inertial sensors measure accelerations andangular velocities produced by a user's handwritingmotion in 2D/3D spaces. The measurements fromgyroscopes are integrated once to produce the attitude ofthe system and are consequently used to remove theeffects of the gravity and the inclination of the system.The compensated acceleration measurements are doublyintegrated to yield the position of the system. Due to theintegration processes involved in reproducing thehandwriting trajectory, the accuracy of the positionmeasurement significantly deteriorates along with time.To reproduce handwriting trajectory of a stroke on asurface and even in the air, we propose algorithms tosegment a stroke, to compensate the integration errors,and to reconstruct 2D trajectory on the x-y plane from 3Dtrajectory in the air. Real experimental results areincluded to show the effectiveness and feasibility of theproposed algorithms. The proposed methods provide anew approach for implementing a small, user-friendlykeyboard alternative input device for wearable computers.
Inhibition of Hepatic Chylomicron Remnant Uptake by Gene Transfer of a Receptor Antagonist (1994)

The low density lipoprotein receptor-related protein (LRP) has been proposed to mediate in concert with the LDL receptor (LDLR) the uptake of dietary lipoproteins into the hepatocytes. This hypothesis was tested by transient inactivation of LRP in vivo. Receptor-associated protein (RAP), a dominant negative regulator of LRP function, was transferred by an adenoviral vector to the livers of mice lacking LDLR (LDLR-/-). The inactivation of LRP by RAP was associated with a marked accumulation of chylomicron remnants in LDLR-/- mice and to a lesser degree in normal mice, suggesting that both LDLR and LRP are involved in remnant clearance.
Stem loops in HIV and prion protein mRNAs. (1990)

Tat-dependent trans-activation in HIV requires presentation of a CUGGG pentanucleotide at the end of a stem loop within the tar site of the viral long terminal repeat. A tandem repeat within the open reading frame of the prion protein (PrP) mRNA is able to form similar stem loop structures with which the HIV tat protein could interact, disturbing PrP translation. Self-amplification of such a disturbance has been suggested as the cause of the scrapie group of diseases, including the scrapie-like human dementiae. The same mechanism may underly AIDS encephalopathy.