gebhart/patrepeval huggingface dataset:
Specificities of Cell Permeant Peptidyl Inhibitors for the Proteinase Activities of μ-Calpain and the 20 S Proteasome (1997)

Cell-permeant peptidyl aldehydes and diazomethylketones are frequently utilized as inhibitors of regulatory intracellular proteases. In the present study the specificities of several peptidyl inhibitors for purified human mu-calpain and 20 S proteasome were investigated. Acetyl-LLnL aldehyde, acetyl-LLM aldehyde, carbobenzyloxy-LLnV aldehyde (ZLLnVal), and carbobenzyloxy-LLY-diazomethyl ketone produced half-maximum inhibition of the caseinolytic activity of mu-calpain at concentrations of 1-5 x 10(-7) M. In contrast, only ZLLnVal was a reasonably potent inhibitor of the caseinolytic activity of 20 S proteasome, producing 50% inhibition at 10(-5) M. The other inhibitors were at least 10-fold less potent, producing substantial inhibition only at near saturating concentrations in the assay buffer. Further studies with ZLLnVal demonstrated that its inhibition of the proteasome was independent of casein concentration over a 25-fold range. Proteolysis of calpastatin or lysozyme by the proteasome was half-maximally inhibited by 4 and 22 microM ZLLnVal, respectively. Thus, while other studies have shown that ZLLnVal is a potent inhibitor of the hydrophobic peptidase activity of the proteasome, it appears to be a much weaker inhibitor of its proteinase activity. The ability of the cell permeant peptidyl inhibitors to inhibit growth of the yeast Saccharomyces cerevisiae was studied because this organism expresses proteasome but not calpains. Concentrations of ZLLnVal as high as 200 microM had no detectable effect on growth rates of overnight cultures. However, yeast cell lysates prepared from these cultures contained 2 microM ZLLnVal, an amount which should have been sufficient to fully inhibit hydrophobic peptidase activity of yeast proteasome. Degradation of ubiquitinylated proteins in yeast extracts by endogenous proteasome was likewise sensitive only to high concentrations of ZLLnVal. The higher sensitivity of the proteinase activity of calpains to inhibition by the cell permeant inhibitors suggests that calpain-like activities may be targets of these inhibitors in animal cells.
Bi-directional recurrent neural networks for speech recognition (1996)

While many possible network architectures have been used to estimate conditional probabilities of class membership, recurrent neural networks (RNNs) have been most successful for speech recognition. In the past optimal results were achieved by merging the outputs of two RNNs trained in each time direction. Merging outputs of different experts to form one resulting opinion is theoretically difficult - a direct combination of the experts during training would be desirable. This paper presents a bi-directional neural network (BRNN) structure which can be trained in both time directions simultanously and hence avoids the difficult merging process. 1. INTRODUCTION Almost all current large vocabulary speech recognition systems are based on Hidden Markov Models (HMMs) with parametric observation density distributions. As the kernels for the distributions usually Gaussians are chosen. The parameters of the distributions can easily be estimated with maximum likelihood methods. For optimal resu...
Short communication Inhibition of export of fibroblast growth factor-2 (FGF-2) from the prostate cancer cell lines PC3 and DU145 by Anvirzel and its cardiac glycoside component, oleandrin (2001)

Anvirzel is an extract of Nerium oleander currently undergoing Phase I clinical evaluation as a potential treatment for cancer. Two of the active components of Anvirzel are the cardiac glycosides oleandrin and oleandrigenin. Previous studies have demonstrated that, in vitro, cardiac glycosides may inhibit fibroblast growth factor-2 (FGF-2) export through membrane interaction with the Na 1 ,K 1 -ATPase pump. In continuing research on the antitumor activity of this novel plant extract, the relative abilities of oleandrin and oleandrigenin to inhibit FGF-2 export from two human prostate cancer cell lines, DU145 and PC3, were examined. An ELISA assay was utilized to determine the FGF-2 concentration in the cell culture medium before and after exposure to cardiac glycosides or the parent extract material Anvirzel. Both cell lines were exposed to non-cytotoxic concentrations of oleandrin (0.05 and 0.1 ng/mL) for up to 72 hr. Studies also were conducted with Anvirzel and ouabain. Oleandrin (0.1 ng/mL) produced a 45.7% inhibition of FGF-2 release from PC3 cells and a 49.9% inhibition from DU145 cells. Non-cytotoxic concentrations (100 ng/mL) of Anvirzel produced a 51.9 and 30.8% inhibition of FGF-2 release, respectively, in the two cell lines. The decrease in FGF-2 release from cells required continuous incubation for 48 ‐72 hr; shorter incubation times were not effective. These results demonstrate that Anvirzel, like oleandrin, inhibited FGF-2 export in vitro from PC3 and DU145 prostate cancer cells in a concentration- and time-dependent fashion and may, therefore, contribute to the antitumor activity of this novel treatment for cancer. © 2001 Elsevier Science Inc. All rights reserved.
Fundamentals of Ergonomic Exoskeleton Robots (2008)

This thesis is the first to provide the fundamentals of ergonomic exoskeleton design. The fundamental theory as well as technology necessary to analyze and develop ergonomic wearable robots interacting with humans is established and validated by experiments and prototypes. The fundamentals are (1) a new theoretical framework for analyzing physical human robot interaction (pHRI) with exoskeletons, and (2) a clear set of design rules of how to build wearable, portable exoskeletons to easily and smoothly interact with varying users in a haptic telemanipulation scenario. The fundamentals aim at providing the basis for truly human compatible exoskeleton design from a human as well as technological perspective.
Origin of the Low-Viscosity of [emim][(FSO<sub>2</sub>)<sub>2</sub>N] Ionic Liquid and Its Lithium Salt Mixture: Experimental and Theoretical Study of Self-Diffusion Coefficients, Conductivities, and Intermolecular Interactions (2010)

The temperature-dependent viscosity, ionic conductivity, and self-diffusion coefficients of an ionic liquid, 1-ethyl-3-methylimidazolium bis(fluorosulfonyl)amide ([emim][FSA]), and its Li salt mixture were studied with reference to emim bis(trifluoromethyl-sulfonyl)amide ([emim][TFSA]) systems. The stabilization energies for the formation of the FSA(-) complexes with emim(+) and Li(+) were calculated by the MP2/6-311G** level ab initio method. The stabilization energies calculated for the FSA(-) complexes with emim(+) and Li(+) (-77.0 and -134.3 kcal/mol) were smaller than those for the corresponding TFSA(-) complexes (-78.8 and -137.2 kcal/mol). The weaker electrostatic and induction interactions are the causes of the smaller interaction energies for the FSA(-) complexes. The weaker interaction between the FSA(-) and emim(+) can be one of the causes of the lower viscosity of the [emim][FSA] ionic liquid compared with that of the [emim][TFSA] ionic liquid. The weaker interaction between the FSA(-) and Li(+) compared with that between the TFSA(-) and Li(+) explains the fact that the addition of Li salt to the [emim][FSA] ionic liquid induces a little increase of the viscosity and a little decrease of the ionic conductivity and self-diffusion coefficients of ions. The FSA(-) in the Li[FSA] complex prefers the cis form due to the stronger attraction and smaller deformation energy of the cis-FSA(-) compared with the trans-FSA(-).
A 21-ns 32 K×8 CMOS static RAM with a selectively pumped p-well array (1987)

The design and performance of a 32 K/spl times/8-b CMOS static RAM (SRAM) are presented. The design features a selectively pumped p-well array. Using this array technology, high-impedance polysilicon resistor loads can be used to reduce the array standby current by three orders of magnitude, and the device characteristics can be optimized to achieve high speed in the peripheral circuits. A unique divided-word-line architecture with shared sense amplifiers is used to achieve high-speed read operation. The read speed is further enhanced by a novel quasistatic equalization that minimizes peak current. A high-speed write circuit with a write-to-read transition detection is used to achieve a fast write operation. An advanced 1.2-/spl mu/m double-level-metal CMOS technology was used to fabricate the devices. The access time is 21 ns and the active power is 330 mW at 22 MHz.
Noncollaborative telepresentations come of age (1997)

At this moment, thousands of people are criss-crossing the globe to attend business presentations. Most of them will spend more time traveling to the presentation than they would in the presentation itself. Also at this moment, thousands of people are not at presentations they need or want to attend due to scheduling conflicts, crises, or budget constraints. Similarly, presenters are busy re-presenting the same material to people who could not attend their last presentation. Now technology
Thermally and electrically isolated single crystal silicon structures in CMOS technology (1994)

Thermally and electrically isolated single crystal silicon structures have been fabricated using a post-processing anisotropic tetramethyl ammonium hydroxide (TMAH) electrochemical etch. The process was carried out on CMOS circuits fabricated by a commercial foundry. Since the etch consists of a single micromachining step performed on packaged and bonded dice, this technique has the potential for cost-effective prototyping and production of integrated sensors and circuits.< <ETX xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">&gt;</ETX>
Excited State Relaxation in Cyanine Dyes:  A Remarkably Efficient Reverse Intersystem Crossing from Upper Triplet Levels (1997)

The upper triplet states of Merocyanine 540 and related cyanine dyes have been generated by a two-color, two-pulse method. The decay of this state partitions between internal conversion to T1 and remarkably efficient reverse intersystem crossing to the singlet manifold. Thus, UV or visible laser generation of the T1 state (either directly or by a sensitized route) followed by excitation with a 640 nm pulse ultimately results in fluorescence and isomerization from the lowest excited singlet state (S1), as evidenced by the production of the ground state photoisomer absorption and emission coincident with the second laser pulse. Since identical behavior (isomerization and fluorescence) is observed for direct excitation into the singlet manifold, we conclude that both the singlet and triplet states are of the same geometry and that isomerization does not occur directly from either T1 or Tn.
New methods and reagents in organic synthesis. 3. Diethyl phosphorocyanidate: a new reagent for C-acylation (1978)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTNew methods and reagents in organic synthesis. 3. Diethyl phosphorocyanidate: a new reagent for C-acylationTakayuki Shioiri and Yasumasa HamadaCite this: J. Org. Chem. 1978, 43, 18, 3631–3632Publication Date (Print):September 1, 1978Publication History Published online1 May 2002Published inissue 1 September 1978https://pubs.acs.org/doi/10.1021/jo00412a058https://doi.org/10.1021/jo00412a058research-articleACS PublicationsRequest reuse permissionsArticle Views506Altmetric-Citations30LEARN 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
Abrogation of α-adrenergic vasoactivity in chronically inflamed rat knee joints (2001)

It has previously been shown that chronic inflammation causes a reduction in sympathetic nerve-mediated vasoconstriction in rat knees. To determine whether this phenomenon is due to an alteration in smooth muscle adrenoceptor function, the present study compared the alpha-adrenoceptor profile of blood vessels supplying the anteromedial capsule of normal and chronically inflamed rat knee joints. While the rats were under urethan anesthesia, the alpha(1)-adrenoceptor agonists methoxamine and phenylephrine and the alpha(2)-adrenoceptor agonist clonidine (0.1-ml bolus; dose range 10(-12)-10(-7) mol) were applied to exposed normal rat knees, resulting in a dose-dependent fall in capsular perfusion. Comparison of drug potencies indicated that alpha(2)-adrenergic effects > alpha(1)-vasoactivity. One week after intra-articular injection of Freund's complete adjuvant to induce chronic joint inflammation, the vasoconstrictor effects of methoxamine, phenylephrine, and clonidine were all significantly attenuated compared with normal controls. These findings show that the preponderance of sympathetic adrenergic vasoconstriction in the anteromedial capsule of the rat is carried out by postjunctional alpha(2)-adrenoceptors. Chronic joint inflammation compromises alpha(1)- and alpha(2)-adrenoceptor function, and this change in alpha-adrenergic responsiveness may help explain the perfusion changes commonly associated with inflammatory arthritis.
High-speed resonant cavity enhanced Ge photodetectors on reflecting Si substrates for 1550-nm operation (2004)

We have designed and fabricated high-speed resonant cavity enhanced germanium (Ge) Schottky photodetectors on a silicon-on-insulator substrate. These back-illuminated detectors have demonstrated 3-dB bandwidths of more than 12 GHz at 3-V reverse bias and a peak quantum efficiency of 59% (R=0.73 A/W) at the resonant wavelength of /spl sim/1540 nm. Time domain measurements of our Ge photodetectors with diameters of up to 48 μm show transit-time limited impulse responses corresponding to bandwidths of at least 6.7 GHz, making these detectors compatible with 10-Gb/s data communication systems.
A novel graphics processor architecture based on partial stream rewriting (2013)

Although individual stages of current graphics processing units (GPU) are programmable via shaders, the pipeline still contains fixed blocks and the data flow cannot be adjusted arbitrary. To overcome these limitations, we propose a novel graphics processor architecture, which substantially improves reconfigurability of the rendering pipeline. For this purpose, we model the complete rendering pipeline as a functional program, which is then represented as a stream of tokens and iteratively modified by a set of rewriting rules. Our proposed architecture enables dynamic thread creation, lock-free synchronization and light-weight scheduling based on pattern matching. Reconfigurability and scalability of the novel processor architecture are demonstrated by complex examples running on an FPGA prototype.
Toward Fully Synthetic Glycoproteins by Ultimately Convergent Routes:  A Solution to a Long-Standing Problem (2004)

A method is disclosed for the convergent synthesis of multiply glycosylated peptides. The approach centers on a convergent technique for generating masked, complex glycopeptide-containing C-terminal acyl donors. Activation of the latent donor in situ and use directly in segment coupling with a second peptide bearing a complex carbohydrate produces a completely unprotected, bifunctional glycopeptide. The system demonstrates a minimum level of hydrolysis and epimerization at the C-terminal amino acid residue of the acyl donor during fully convergent segment coupling and is therefore a powerful tool for the synthesis of glycoproteins.
Adjunctive high-dose glycine in the treatment of schizophrenia (2001)

Glycine is an agonist at brain N-methyl-D-aspartate receptors and crosses the blood-brain barrier following high-dose oral administration. In a previous study, significant improvements in negative and cognitive symptoms were observed in a group of 21 schizophrenic patients receiving high-dose glycine in addition to antipsychotic treatment. This study evaluated the degree to which symptom improvements might be related to alterations in antipsychotic drug levels in an additional group of 12 subjects. Glycine treatment was associated with an 8-fold increase in serum glycine levels, similar to that observed previously. A significant 34% reduction in negative symptoms was observed during glycine treatment. Serum antipsychotic levels were not significantly altered. Significant clinical effects were observed despite the fact that the majority of subjects were receiving atypical antipsychotics (clozapine or olanzapine). As in earlier studies, improvement persisted following glycine discontinuation.
Intratumoral injection of interleukin‐2 augments the local and abscopal effects of radiotherapy in murine rectal cancer (2011)

Recent studies have suggested that tumor shrinkage in response to radiotherapy (RT) is greatly dependent on the host immune response. A Balb/c mouse model of simultaneous subcutaneous tumor and liver metastasis of Colon26 was prepared and, after irradiation of the subcutaneous tumor (2 Gy × 5 day × 2 cycles), interleukin-2 (IL-2) (2 × 10(4) U) was injected intra-tumorally, and the fate of both the subcutaneous tumor and liver metastatic lesions was evaluated. Intratumoral injection of IL-2 greatly enhanced the anti-tumor effects of RT and completely eradicated the established subcutaneous tumor. Interestingly, although RT was given locally to the subcutaneous tumor, liver metastasis formation was also inhibited in mice receiving only local RT. More impressively, the combination of RT + IL-2 completely inhibited liver metastasis formation. Splenocytes in mice receiving RT + IL-2 contained a higher percentage of CD4(+) T cells, but lower percentages of CD4(+)CD25(+) regulatory T cells and CD11b(+) Gr-1(+) myeloid-derived suppressor cells. Immunohistochemical investigation of human rectal cancer revealed that the density of CD8(+) cells infiltrating into irradiated rectal tumor was positively associated with a lower frequency of distant metastasis as well as histological response grade. Local administration of IL-2 not only enhances shrinkage of the irradiated tumor itself, but can also suppress the development of distant metastasis located outside the RT field, possibly though the induction of a systemic T cell response. Augmentation of T-cell-mediated antitumor immunity during RT might be critical for improvement of the clinical efficacy of neoadjuvant RT for the treatment of advanced rectal cancer.
Neuronal nicotinic receptors: functional correlates of ligand binding sites (1991)

Conference Article| February 01 1991 Neuronal nicotinic receptors: functional correlates of ligand binding sites S. Wonnacott S. Wonnacott 1Department of Biochemistry, University of Bath, Bath BA2 7AY, U.K. Search for other works by this author on: This Site PubMed Google Scholar Biochem Soc Trans (1991) 19 (1): 121–124. https://doi.org/10.1042/bst0190121 Article history Received: September 27 1990 Views Icon Views Article contents Figures & tables Video Audio Supplementary Data Peer Review Share Icon Share Facebook Twitter LinkedIn Email Cite Icon Cite Get Permissions Citation S. Wonnacott; Neuronal nicotinic receptors: functional correlates of ligand binding sites. Biochem Soc Trans 1 February 1991; 19 (1): 121–124. doi: https://doi.org/10.1042/bst0190121 Download citation file: Ris (Zotero) Reference Manager EasyBib Bookends Mendeley Papers EndNote RefWorks BibTex toolbar search Search Dropdown Menu toolbar search search input Search input auto suggest filter your search All ContentAll JournalsBiochemical Society Transactions Search Advanced Search Keywords: nAChR, nicotinic acetylcholine receptor © 1991 Biochemical Society1991 Article PDF first page preview Close Modal You do not currently have access to this content.
Software Engineering Education in the Associate-Degree-Level Vocational/Technical Computer Science Program (1990)

The need for software engineers has grown with the increased use of software and computers in our society. Presently, formal education of software engineers is being conducted at the graduate degree level. There are pressures to extend this education to other academic levels; in fact, many baccalaureate degree programs today include one or more software engineering courses. Difficulties confronting software engineering education at the associate degree level include: limited educational and experience backgrounds of the students; faculty whose own education did not include software engineering; and severe time and content constraints imposed on such two-year programs. The author concludes that the two-year associate-degree-level vocational/technical computer science program should continue to focus on producing graduates with sound programming and problem solving skills. Once these graduates gain entry-level employment, they can then build upon these fundamental skills, with experience and further education, toward a software engineering career. Software engineering education in the two-year vocational/technical program, therefore, should be restricted to that which directly enhances the development of these basic skills; specific recommendations are offered for consideration.