gebhart/patrepeval huggingface dataset:
Chelation of Intracellular Calcium Prevents Stimulation of Glucose Transport by Insulin and Insulinomimetic Agents in the Adipocyte. Evidence for a Common Mechanism* (1987)

Vanadate, concanavalin A (Con A), H2O2, and the phorbol ester, 12-O-tetradecanoyl phorbol 13-acetate (TPA), seemingly unrelated compounds, have effects on cellular metabolism similar to those of insulin. The mechanism(s) by which these diverse compounds act and their relevance to insulin action remain unclear. The hypothesis that increased intracellular calcium ([Ca2+]i) may provide the common basis for the stimulatory effects of these agents on glucose uptake in adipocytes was tested. This was accomplished by preincubating cells with the membrane-permeant ester, quin2-AM (2-[(2-bis[carboxymethyl] amino-5-methylphenoxy]-6-methoxy-8-bis[carboxymethyl]- aminoquinolinetetrakis [acetoxymethyl] ester), which is rapidly accumulated and hydrolyzed by esterases to form the impermeant tetracarboxylate chelator form, quin2. Vanadate, Con A, H2O2, and TPA stimulate D-glucose uptake in adipocytes approximately 3-, 3-, 2-, and 0.6-fold, respectively, compared to the 5- to 10-fold stimulation of D-glucose uptake obtained with insulin. Preincubation with quin2-AM produced a dose-dependent inhibitory effect only on the stimulated portion of glucose transport without affecting basal (unstimulated) transport. The concentrations for half-maximal inhibition (IC50) of stimulated glucose transport by quin2-AM were 26, 35, 25, 14, and 34 microM for insulin, vanadate, Con A, H2O2, and TPA, respectively. Quin2-AM maximally inhibited stimulated glucose uptake by greater than 85% for all of the insulin mimetic agents. In contrast the maximal inhibition of insulin-stimulated glucose transport by quin2-AM was 55 +/- 4%. Therefore, stimulation of glucose transport by insulin and other diverse compounds appears to involve at least one common calcium-dependent intermediate step.
2-Substituted estra-1,3,5(10)-trienes as anti-cancer agents: D-ring SAR and in vivo activity (2007)

A282 2-Substituted estradiol-3-O-sulfamates (E2MATEs) and 3,17-O,O-bis-sulfamates (E2bisMATEs) are potent anti-angiogenic and anti-proliferative agents which are differentiated from the corresponding estradiol derivatives by their superior activity and oral bioavailability. The ability of these molecules to inhibit the Taxol promoted polymerisation of tubulin underlies their pro-apoptotic effects:- G2M cell cycle arrest, p53 induction, BCL-2 phosphorylation and activation of various caspases are all observed in cancer cells treated with these compounds. Sequestration by red blood cells, through a reversible interaction of the sulfamate group with carbonic anhydrase, combined with the blockage of both deleterious conjugation and 17β-HSD II metabolism by C-17 substitution likely confer high oral bioavailability. Modification at C-17 of the D-ring (e.g. incorporation of a 17-O-sulfamate group) has provided for enhanced activity, with SAR studies indicating that H-bond acceptor ability of the C-17-substituent is requisite for activity.  A series of compounds was elaborated to further interrogate the C-17 SAR in the hope of discovering compounds with higher activity against the proliferation of DU-145 prostate cancer cells than the E2bisMATEs 1 & 2 (GI50 340 & 210 nM respectively). Various H-bond acceptors were thus linked to C-17 via carbon linkers. Of the two-carbon linked H-bond acceptors in the 2-methoxy-3-O-sulfamate series, ketone 3 (GI50 89 nM) proved especially active, with good activity also observed for the corresponding secondary alcohol (143 nM). Larger H-bond acceptors and non-sulfamoylated compounds displayed significantly reduced activity. Abbreviation of the linker to a single carbon afforded numerous novel compounds with activities in the low nanomolar range amongst which the 17β-acyl compounds proved particularly noteworthy. 2-Methoxy-17β-acyl-estra-1,3,5(10)-trien-3-ol 4 with a GI50 300 nM is 4-fold more active against DU-145 proliferation than the clinical agent 2-MeOE2, thus emphasising the likely importance of interactions around C-17. The 3-O-sulfamoylated 2-ethyl- and 2-methoxy- 17β-acyl compounds 5 & 6 were exceptionally potent (GI50’s 62 and 46 nM respectively), with alcohol and ether derivatives also displaying excellent activity. Thus, a number of novel, highly active, anti-proliferative agents were discovered by varying both H-bond acceptor group and C-17-alkyl linker to fine tune activity.  Translation of this in vitro activity to the in vivo context was studied in a mouse Matrigel model of angiogenesis in which 3 and 5 were evaluated at 20mg/kg/day p.o. for 4 days. Results obtained confirm the in vivo anti-angiogenic effects of these molecules and the oral bioavailability that they display and justify further development of this general compound class.
Low-level light therapy for zymosan-induced arthritis in rats (2007)

It has been known for many years that low level laser (or light) therapy (LLLT) can ameliorate the pain, swelling and inflammation associated with various forms of arthritis. Light is absorbed by mitochondrial chromophores leading to an increase in ATP, reactive oxygen species and/or cyclic AMP production and consequent gene transcription via activation of transcription factors. However, despite many reports about the positive effects of LLLT in medicine, its use remains controversial. Our laboratory has developed animal models designed to objectively quantify response to LLLT and compare different light delivery regimens. In the arthritis model we inject zymosan into rat knee joints to induce inflammatory arthritis. We have compared illumination regimens consisting of a high and low fluence (3 J/cm<sup>2</sup> and 30 J/cm<sup>2</sup>), delivered at a high and low irradiance (5 mW/cm2 and 50 mW/cm<sup>2</sup>) using 810-nm laser light daily for 5 days, with the effect of conventional corticosteroid (dexamethasone) therapy. Results indicated that illumination with 810-nm laser is highly effective (almost as good as dexamethasone) at reducing swelling and that longer illumination time was more important in determining effectiveness than either total fluence delivered or irradiance. Experiments carried out using 810-nm LLLT on excisional wound healing in mice also confirmed the importance of longer illumination times. These data will be of value in designing clinical trials of LLLT.
Structural and mutational studies of the recognition of the arginine tRNA-specific major identity element, A20, by arginyl-tRNA synthetase (2001)

Arginyl-tRNA synthetase (ArgRS) recognizes two major identity elements of tRNA(Arg): A20, located at the outside corner of the L-shaped tRNA, and C35, the second letter of the anticodon. Only a few exceptional organisms, such as the yeast Saccharomyces cerevisiae, lack A20 in tRNA(Arg). In the present study, we solved the crystal structure of a typical A20-recognizing ArgRS from Thermus thermophilus at 2.3 A resolution. The structure of the T. thermophilus ArgRS was found to be similar to that of the previously reported S. cerevisiae ArgRS, except for short insertions and a concomitant conformational change in the N-terminal domain. The structure of the yeast ArgRS.tRNA(Arg) complex suggested that two residues in the unique N-terminal domain, Tyr(77) and Asn(79), which are phylogenetically invariant in the ArgRSs from all organisms with A20 in tRNA(Arg)s, are involved in A20 recognition. However, in a docking model constructed based on the yeast ArgRS.tRNA(Arg) and T. thermophilus ArgRS structures, Tyr(77) and Asn(79) are not close enough to make direct contact with A20, because of the conformational change in the N-terminal domain. Nevertheless, the replacement of Tyr(77) or Asn(79) by Ala severely reduced the arginylation efficiency. Therefore, some conformational change around A20 is necessary for the recognition. Surprisingly, the N79D mutant equally recognized A20 and G20, with only a slight reduction in the arginylation efficiency as compared with the wild-type enzyme. Other mutants of Asn(79) also exhibited broader specificity for the nucleotide at position 20 of tRNA(Arg). We propose a model of A20 recognition by the ArgRS that is consistent with the present results of the mutational analyses.
Maximization of mutual information for offline Thai handwriting recognition (2006)

This paper aims to improve the performance of an HMM-based offline Thai handwriting recognition system through discriminative training and the use of fine-tuned feature extraction methods. The discriminative training is implemented by maximizing the mutual information between the data and their classes. The feature extraction is based on our proposed block-based PCA and composite images, shown to be better at discriminating Thai confusable characters. We demonstrate significant improvements in recognition accuracies compared to the classifiers that are not discriminatively optimized.
Optical Cross Correlator in a Silicon Waveguide (2012)

Get PDF Email Share Share with Facebook Tweet This Post on reddit Share with LinkedIn Add to CiteULike Add to Mendeley Add to BibSonomy Get Citation Copy Citation Text M. Fridman, Y. Okawachi, S. Clemmen, M. Menard, M. Lipson, and A. L. Gaeta, "Optical Cross Correlator in a Silicon Waveguide," in Conference on Lasers and Electro-Optics 2012, OSA Technical Digest (online) (Optica Publishing Group, 2012), paper CF2L.2. Export Citation BibTex Endnote (RIS) HTML Plain Text Citation alert Save article
Description and analysis of novelties introduced in DCASE Task 4 2022 on the baseline system (2022)

The aim of the Detection and Classification of Acoustic Scenes and Events Challenge Task 4 is to evaluate systems for the detection of sound events in domestic environments using an heterogeneous dataset. The systems need to be able to correctly detect the sound events present in a recorded audio clip, as well as localize the events in time. This year's task is a follow-up of DCASE 2021 Task 4, with some important novelties. The goal of this paper is to describe and motivate these new additions, and report an analysis of their impact on the baseline system. We introduced three main novelties: the use of external datasets, including recently released strongly annotated clips from Audioset, the possibility of leveraging pre-trained models, and a new energy consumption metric to raise awareness about the ecological impact of training sound events detectors. The results on the baseline system show that leveraging open-source pretrained on AudioSet improves the results significantly in terms of event classification but not in terms of event segmentation.
Deferoxamine, a promising bifunctional chelating agent for labeling proteins with gallium: Ga-67 DF-HSA: concise communication. (1982)

A new efficient method has been developed for the labeling of various biologically important proteins with radiogallium, using deferoxamine (DF) as a bifunctional chelating agent. Human serum albumin (HSA) was chosen for studying the DF coupling reaction by a glutaraldehyde two-step method. The DF-HSA conjugate obtained was then easily labeled with Ga-67 with high efficiency and reproducibility. High stability of the Ga-67 DF-HSA was observed both in vitro and in vivo. In rats the half-time of blood clearance at the first phase was 234 min for the Ga-67 DF-HSA, whereas most conventional I-131 HSA gives 121 min. The excellent pharmacological and physiological properties were assessed by plasma clearance and plasma volume measurements in normal volunteers. Even at 2 hr after injection, (90.0 +/- 3.0)% of Ga-67 DF-HSA was retained within the vascular space. The mean plasma volume per kilogram of body weight, measured with Ga-67 DF-HSA, was 46.6 +/- 3.4 ml/kg, compared with 52.2 +/- 2.4 ml/kg as determined with I-131 HSA in the same men.
Semiconducting Copolymers with Naphthalene Imide/Amide π‐Conjugated Units: Synthesis, Crystallography, and Systematic Structure‐Property‐Mobility Correlations (2022)

Abstract In a series of n‐type semiconducting naphthalene tetracarboxydiimide ( NDI )‐dithiophene ( T2 ) copolymers, structural and electronic properties trends are systematically evaluated as the number of NDI carbonyl groups is reduced from 4 in NDI to 3 in NBL (1‐amino‐4,5‐8‐naphthalene‐tricarboxylic acid‐1,8‐lactam‐4,5‐imide) to 2 in NBA (naphthalene‐bis(4,8‐diamino‐1,5‐dicarboxyl)‐amide). As the NDI ‐ T2 backbone torsional angle falls the LUMO energy rises. However, the thienyl attachment regiochemistry also plays an important role in less symmetric NBL and NBA . Electron mobility is greatest for N2200 (0.17 cm 2 V −1 s −1 ) followed by PNBL‐3,8‐T2 and PNBA‐2,6‐T2 (0.11 cm 2 V −1 s −1 ), 0.02 cm 2 V −1 s −1 in PNBL‐4,8‐T2 , and negligible in PNBA‐3,7‐T2 . Charge transport reflects a delicate balance between electronic backbone communication (optimum for N2200 and PNBL‐4,8‐T2 ), backbone planarity (optimum for PNBA‐2,6‐T2 and PNBL‐3,8‐T2 ), LUMO energy (optimum for N2200 ), π–π stacking distance (optimum for PNBA‐2,6‐T2 ), and film crystallinity (optimum for PNBA‐2,6‐T2 and N2200 ). These results offer generalizable insight into semiconducting copolymer design.
A simple, scalable and provably stable explicit rate computation scheme for flow control in communication networks (2001)

Abstract This paper describes fast rate computation (FASTRAC), an explicit rate flow control algorithm for available bit rate (ABR) traffic. Using digital control theory, we develop a simple rate controller for the ABR flow control process. We prove that the controller is stable, fair to all participating sources and configurable with respect to responsiveness. The analysis presented shows that stability of the flow control process depends primarily on two factors, the control update rate and the feedback delay. The implementation of the proposed algorithm is much simpler than other fair rate allocation algorithms. The proposed algorithm demonstrates the ability to scale with speed, distance, different feedback delays, number of users, and number of nodes while remaining robust, efficient, and fair under stressing and dynamic traffic conditions. Copyright © 2001 John Wiley &amp; Sons, Ltd.
Noninvasive Color Doppler Inspection of Small‐Diameter Vascular Grafts Implanted in Canine Carotid and Femoral Arteries (1992)

To noninvasively evaluate a small-diameter vascular graft (approx. 4 mm in diameter) developed for coronary artery bypass application, a state-of-the-art color Doppler flow mapping system was applied to inspect various grafts implanted in 5 canines. The grafts, including Denaflex, Gore-Tex ePTFE, and Bioflow, were implanted interpositionally in the carotid and femoral arteries. Inspections were conducted with a 5 MHz linear vascular transducer at 6 weeks postimplantation and 12 weeks postimplantation, immediately prior to retrieval. In the carotid artery position, all 5 Denaflex grafts were patent throughout the implantation period while 2 of the 5 Gore-Tex grafts were occluded at 6 weeks, and 1 more was occluded at 12 weeks. In the femoral artery position, all 5 Denaflex grafts were patent at 6 weeks; however 2 were occluded at 12 weeks. For the Bioflow grafts at 6 weeks, 3 were patent, and 2 were occluded. The same results were observed at 12 weeks. The color Doppler inspection results indicated a higher patency rate in the carotid artery position than in the femoral artery position. Furthermore, the volumetric flow rate and the wall shear stress measured with the pulsed Doppler in the carotid artery were greater than in the femoral artery. These findings suggest that the hemodynamic "environment" in which the graft was implanted may affect the graft patency rate. The Doppler inspection results obtained at 12 weeks, identical with those observed after retrieval, demonstrated that color Doppler flow mapping is a reliable method to noninvasively inspect blood flow through small-diameter vascular grafts.
"Laser like" spatial coherence of a high-flux, ultrashort-pulse, EUV source (2003)

Summary form only given. High-harmonic generation is a convenient method for generating coherent light in the extreme-ultraviolet (EUV) region of the spectrum, using a small-scale ultrafast laser-based apparatus. Recent advances in using hollow waveguides for HHG have demonstrated conversion efficiency of >10/sup -5/ into a well-collimated EUV beam. In this work, we demonstrate that this beam exhibits full spatial coherence to the limits of our measurement capability, making this source the most coherent light source ever in this region of the spectrum. This contrasts with previous measurements of the coherence of HHG radiation generated in a gas-jet geometry, which measured substantially-degraded spatial coherence. We also demonstrate a new and simple technique for measuring the spectrum of this EUV emission by deconvolution of a double-slit interference pattern for the first time.
Thiotepa‐based versus total body irradiation‐based myeloablative conditioning prior to allogeneic stem cell transplantation for acute myeloid leukaemia in first complete remission: a retrospective analysis from the Acute Leukemia Working Party of the European Group for Blood and Marrow Transplantation (2015)

Thiotepa is an alkylating compound with an antineoplastic and myeloablative activity and can mimic the effect of radiation. However, it is unknown whether this new regimen could safely replace the long-established ones. This retrospective matched-pair analysis evaluated the outcome of adults with acute myeloid leukaemia in first complete remission who received myeloablative conditioning either with a thiotepa-based (n = 121) or a cyclophosphamide/total body irradiation-based (TBI; n = 358) regimen for allogeneic hematopoietic stem cell transplantation from an HLA-matched sibling or an unrelated donor. With a median follow-up of 44 months, the outcome was similar in both groups. Acute graft-versus-host disease grade II-IV was observed in 25% after thiotepa-containing regimen versus 35% after TBI (P = 0.06). The 2-yr cumulative incidence of chronic graft-versus-host disease was 40.5% for thiotepa and 41% for TBI (P = 0.98). At 2 yrs, the cumulative incidences of non-relapse mortality and relapse incidence were 23.9% (thiotepa) vs. 22.4% (TBI; P = 0.66) and 17.2% (thiotepa) vs. 23.3% (TBI; P = 0.77), respectively. The probabilities of leukaemia-free and overall survival at 2 yrs were not significantly different between the thiotepa and TBI groups, at 58.9% vs. 54.2% (P = 0.95) and 61.4% vs. 58% (P = 0.72), respectively. Myeloablative regimens using combinations including thiotepa can provide satisfactory outcomes, but the optimal conditioning remains unclear for the individual patient in this setting.
Generation of Large Insert YAC Libraries (2003)

The introduction of yeast artificial chromosomes (YACs) as cloning vectors in 1987 has significantly advanced the analysis of complex genomes (1). The capability of cloning large DNA (100–2000 kb) as YACs has accelerated the construction of physical maps and contig building (a contiguous set of overlapping clones). YAC contigs now cover entire human chromosomes (i.e., Y and 21) (2,3) and small genomes (i.e., Schizosaccharomyces pombe) (4), and large YAC contigs cover much of the human genome (5). The main advantages of YACs over prokaryotic-based cloning systems are their large insert capacity and ability to maintain sequences that are unstable or not well represented in bacteriophage or cosmid genomic libraries (6). Therefore, YACs complement existing cloning vectors (cosmids, bacteriophage) and new cloning vectors (P1 bacteriophage [P1], bacterial artificial chromosomes [BACs], and P1-derived artificial chromosomes [PACs]; for review, see ref. 7) in mapping and chromosome walking projects (6, 8).
Human monoclonal natural autoantibodies against the T‐cell receptor inhibit interleukin‐2 production in murine T cells (2002)

Natural autoantibodies (NAAbs) specific for the T-cell receptor (TCR) are present in all human sera, but individuals with rheumatoid arthritis (RA) generally produce higher titres of immunoglobulin M (IgM) isotype autoantibodies (AAbs) against Vbeta TCR epitopes. To investigate possible correlations between the specificity of such AAbs and their role in immunomodulation, we generated seven B-cell hetero-hybridomas, secreting monoclonal IgM NAAbs, from the synovial tissue and peripheral blood of patients with RA. Here we report three anti-TCR monoclonal autoantibodies (mAAbs)--OR2, OR5 and Syn 2H-11--with the ability to bind subsets of murine T cells, including the ovalbumin-specific DO-11.10 clone. These antibodies did not induce apoptosis in vitro, but prevented interleukin-2 (IL-2) production by antigen-specific T cells. These findings suggest an immunomodulatory function for NAAbs to TCR V-region epitopes and serve as the foundation for testing human anti-TCR mAAbs in animal models with the eventual goal of using them as therapeutic agents in human disease.
High-drive CMOS buffer for large capacitive loads (1991)

A new CMOS buffer circuit for high capacitive loads is presented. The objective of the design is a high-power, area-efficient buffer to be used in very large scale analogue applications. The buffer can deliver a slew rate of 1.2 V/μs to capacitive loads in excess of 5000 pF. It has a total harmonic distortion of less than 3% at 20kHz. At stand by, it consumes only 125 μA (0.625mW). The buffer occupies 100mils2 of die area in a 3 μm technology.
FUS binds the CTD of RNA polymerase II and regulates its phosphorylation at Ser2 (2012)

Mutations in the RNA-binding protein FUS (fused in sarcoma)/TLS have been shown to cause the neurodegenerative disease amyotrophic lateral sclerosis (ALS), but the normal role of FUS is incompletely understood. We found that FUS binds the C-terminal domain (CTD) of RNA polymerase II (RNAP2) and prevents inappropriate hyperphosphorylation of Ser2 in the RNAP2 CTD at thousands of human genes. The loss of FUS leads to RNAP2 accumulation at the transcription start site and a shift in mRNA isoform expression toward early polyadenylation sites. Thus, in addition to its role in alternative RNA splicing, FUS has a general function in orchestrating CTD phosphorylation during RNAP2 transcription.
DIAMEX Counter‐Current Extraction Process for Recovery of Trivalent Actinides from Simulated High Active Concentrate (2007)

Abstract The partitioning of trivalent actinides was demonstrated with a new version of the French DIAMEX (DIAMide EXtraction) process. A continuous counter‐current experiment using a 16‐stage centrifugal extractor battery was tested using 1 mol/L N,N′-dimethyl‐N,N′-dioctyl‐hexylethoxy‐malonamide (DMDOHEMA) in TPH as the extractant. A high active concentrate (HAC), obtained after concentration and denitration of a high active raffinate (HAR) with a concentration factor of 10, was used as a feed. Based on results from cold and hot batch extraction experiments and computer code calculations, a flowsheet was developed and a full test was carried out using a simulated HAC solution spiked with radionuclides (241Am, 244Cm, 152Eu, and 134Cs). In the DIAMEX process, five extraction stages were sufficient to obtain Am and Cm (feed/raffinate) greater than 5000 and for the coextracted lanthanides decontamination factors between 1100 and 4500. Co‐extraction of zirconium, molybdenum, and palladium was prevented by using oxalic acid and HEDTA. The back extraction comprising 4 stages was also efficient and the recoveries of actinides were greater than 99.8%, which can be further improved by a minor process flowsheet optimisation. The experimental steady‐state concentration profiles of important solutes were determined and compared with model calculations and good agreement was generally obtained.