gebhart/patrepeval huggingface dataset:
Low-affinity penicillin-binding protein associated with beta-lactam resistance in Staphylococcus aureus (1984)

Methicillin resistance in Staphylococcus aureus has been associated with alterations in the penicillin-binding proteins (PBPs). An intriguing property of all methicillin-resistant staphylococci is the dependence of resistance on the pH value of the growth medium. Growth of such bacteria at pH 5.2 completely suppressed the expression of methicillin resistance. We have examined the PBP patterns of methicillin-resistant staphylococci grown at pH 7.0. We detected a high-molecular-weight PBP (PBP-2a; approximate size, 78,000 daltons) that was only present in the resistant bacteria but not in the isogenic sensitive strain. In cultures grown at pH 5.2, the extra PBP was not detectable.
Aerobic Energy Cost and Sensation Responses During Submaximal Running Exercise - Positive Effects of Wearing Compression Tights (2006)

This study aimed to examine the effects of wearing compression compared to classic elastic tights and conventional shorts (control trial) on oxygen cost and sensation responses during submaximal running exercise. In part I, aerobic energy cost was evaluated in six trained runners at 10, 12, 14, and 16 km x h(-1). In part II, the increase in energy cost over time (i. e., slow component expressed as difference in VO2 values between min 2 and end-exercise) was determined in six trained runners at a constant running pace corresponding to 80% of maximal VO2 for 15 min duration. All tests were performed on a 200-m indoor track with equivalent thermal stress conditions. VO2 was determined with a portable metabolic system (Cosmed K4b2, Rome, Italy) during all testing sessions. Runners were asked their ratings of perceived exertion (RPE) and perceptions for clothing sweating, comfort, and whole thermal sensations following each trial. Results showed in part I a significant lower energy cost only at 12 km x h(-1) by wearing compression and elastic tights compared to conventional shorts. During part II, wearing compression tights decreased significantly VO2 slow component by 26 and 36% compared to elastic tights and conventional shorts, respectively. There were no differences in sweating and comfort sensations, RPE, and for whole thermal sensation between clothing conditions in parts I and II. Wearing compression tights during running exercise may enhance overall circulation and decrease muscle oscillation to promote a lower energy expenditure at a given prolonged submaximal speed.
On Multiphysics Discrete Element Modeling of Powder-Based Additive Manufacturing Processes (2016)

Physically accurate modeling of powder-based additive manufacturing (AM) processes can play an enabling role for both the certification and qualification as well as the functional tailoring of materials produced by these processes. In an effort to address these needs in a computationally efficient and physically realistic manner, this paper presents the initial efforts towards the development of a methodology for simulating polydisperse particle-based AM processes by the use of the Multiphysics Discrete Element Method (MDEM). We discuss the formulation of a DEM framework for addressing the unique multiphysics behavior of AM materials and processes. In particular, we focus on coupled thermo-mechanical effects that result in residual strains and deformation. The MDEM approach is demonstrated on several test problems involving laser sintering of metal powders. The paper concludes with a discussion on how this approach may be generalized to broader classes of AM systems, and details are given regarding future work that must be accomplished in order to further develop the present methodology.
The Adaptor Protein APPL2 Inhibits Insulin-Stimulated Glucose Uptake by Interacting With TBC1D1 in Skeletal Muscle (2014)

Insulin stimulates glucose uptake by promoting the trafficking of GLUT4 to the plasma membrane in muscle cells, and impairment of this insulin action contributes to hyperglycemia in type 2 diabetes. The adaptor protein APPL1 potentiates insulin-stimulated Akt activation and downstream actions. However, the physiological functions of APPL2, a close homolog of APPL1, in regulating glucose metabolism remain elusive. We show that insulin-evoked plasma membrane recruitment of GLUT4 and glucose uptake are impaired by APPL2 overexpression but enhanced by APPL2 knockdown. Likewise, conditional deletion of APPL2 in skeletal muscles enhances insulin sensitivity, leading to an improvement in glucose tolerance. We identified the Rab-GTPase-activating protein TBC1D1 as an interacting partner of APPL2. Insulin stimulates TBC1D1 phosphorylation on serine 235, leading to enhanced interaction with the BAR domain of APPL2, which in turn suppresses insulin-evoked TBC1D1 phosphorylation on threonine 596 in cultured myotubes and skeletal muscle. Substitution of serine 235 with alanine diminishes APPL2-mediated inhibition on insulin-dependent TBC1D1 phosphorylation on threonine 596 and the suppressive effects of TBC1D1 on insulin-induced glucose uptake and GLUT4 translocation to the plasma membrane in cultured myotubes. Therefore, the APPL2-TBC1D1 interaction is a key step to fine tune insulin-stimulated glucose uptake by regulating the membrane recruitment of GLUT4 in skeletal muscle.
Sound Bite News: Television Coverage of Elections, 1968–1988 (1992)

Based on samples of network evening news broadcasts from each presidential election from 1968 through 1988, this article shows that the average sound bite has declined from 43 to 9 seconds. This change is interpreted as part of a general shift in the style of television news toward a more mediated, journalist-centered form of journalism. Three factors help explain this change: (a) the evolution of television “know-how,” (b) the weakening of political consensus and authority during the last 20 years, and (c) changes in the economics of the industry. This change has significant consequences for journalism in the 1990s.
Myeloid-Derived Suppressor Cells Confer Tumor-Suppressive Functions on Natural Killer Cells via Polyinosinic:Polycytidylic Acid Treatment in Mouse Tumor Models (2013)

Polyinosinic:polycytidylic acid (poly I:C), a synthetic double-stranded RNA, acts on myeloid cells and induces potent antitumor immune responses including natural killer (NK) cell activation. Myeloid-derived suppressor cells (MDSCs) systemically exist in tumor-bearing hosts and have strong immunosuppressive activity against antitumor effector cells, thereby dampening the efficacy of cancer immunotherapy. Here we tested what happened in MDSCs in poly I:C-treated mice. NK-sensitive syngenic tumor (B16)-bearing C57BL/6 mice were employed for this study. Intraperitoneal poly I:C treatment induced MDSC activation, driving CD69 expression and interferon (IFN)-γ production in NK cells. IFN-γ directly inhibited proliferation of B16 cells. This NK cell priming led to growth retardation of B16 tumors, although no direct tumoricidal activity was induced in NK cells. Mechanistic analysis using KO mice and function-blocking monclonal antibody revealed that MDSCs produced IFN-α via the mitochondrial antiviral signaling protein (MAVS) pathway after in vivo administration of poly I:C, and activated NK cells through the IFNAR pathway. MDSC-mediated NK cell priming was reconstituted by IFN-α in a coculture system. Either the MAVS or IFNAR signaling pathway was required for activation of MDSCs that led to growth retardation of B16 tumor in vivo. The results infer that MDSC is a target of poly I:C to prime NK cells, which exert antitumor activity to NK-sensitive tumor cells.
Mass Transfer in Polymeric Packaging Systems: Sorption, Diffusion, Permeation, and Shelf Life (2015)

No AccessPlastics PackagingJan 2016Mass Transfer in Polymeric Packaging Systems: Sorption, Diffusion, Permeation, and Shelf LifeSusan E.M. Selke, John D. CulterSusan E.M. Selke, John D. Culterhttps://doi.org/10.3139/9783446437197.014SectionsAboutPDF ToolsAdd to FavoritesDownload CitationTrack CitationsCopy LTI LinkPDF key 'share (en)' returned an object instead of string.FacebookTwitterEmailLinkedIn previous chapternext chapter FiguresReferencesRelatedDetails 2015Pages: 353-393Print ISBN: 978-3-446-40790-9eISBN: 978-3-446-43719-7 Copyright & Permissions© 2016 Carl Hanser Verlag GmbH & Co. KGPDF downloadLoading ...
A short and unequivocal synthesis of 5‐aminotetrazolo[1,5‐a]‐quinazoline as a tricyclic analogue of 4‐(3‐bromoanilino)‐6,7‐dimethoxyquinazoline (PD 153035) (1997)

Abstract The discovery of 4‐(3‐bromoanilino)‐6,7‐dimethoxyquinazoline (PD 153035) as an extremely potent inhibitor of the tyrosine kinase activity of the epidermal growth factor receptor led to the preparation of several fused tricyclic quinazoline analogues. The present paper reports a new tricyclic derivative: 5‐(3‐bromoanilino)‐7,8‐dimethoxytetrazolo[1,5‐ a ]quinazoline. This compound was synthesized by two different pathways via a 1,3‐dipolar cycloaddition of an azide at carbon 2 of the quinazoline ring.
Impact of hydroxychloroquine therapy on chronic urticaria: chronic autoimmune urticaria study and evaluation (2004)

Immunomodulation with hydroxychloroquine is safe and appears to offer some efficacy as an intervention in CU.
Light‐Triggered Self‐Assembly of a Spiropyran‐Functionalized Dendron into Nano‐/Micrometer‐Sized Particles and Photoresponsive Organogel with Switchable Fluorescence (2009)

Abstract The synthesis, self‐assembly, and spectroscopic investigations of spiropyran (SP)‐functionalized dendron 1 are reported. Under UV light irradiation, assembly of 1 into nano‐/microparticles occurs due to the transformation of the closed form of SP into the open merocyanine (MC) form. The formation of these nano‐/microparticles is confirmed by transmission electron microscopy (TEM) and dynamic light scattering (DLS) experiments in addition to the confocal laser scanning microscopy (CLSM) measurements. These nano‐/microparticles exhibit relatively strong red emission. It is interesting to note that the direct cooling of the toluene/benzene solution of 1 to 0 °C leads to gel formation. Multivalent π–π interactions due to the dendron in 1 may be the driving‐force for the gelation. The UV light irradiation cannot destroy the gel phase, and in fact, the gel–gel transition is successfully realized. The purple‐blue gel exhibits relatively strong red fluorescence; moreover, the fluorescence can be reversibly switched by alternating UV and visible light irradiation. The results clearly indicate that the MC form after aggregation becomes more stable and fluorescent.
Measurement of the Beta Decay of 26P to Determine Classical Nova 26Al Production in the Milky Way (2015)

Observation across the Milky Way of a 1809-keV -ray characteristic of 26 Al decay provides direct evidence for ongoing nucleosynthetic production of 26 Al. Although massive stars and supernovae are likely to be the primary sites for 26 Al production, classical novae may also contribute a significant portion of the total amount of Galactic 26 Al. At peak nova temperatures of approximately 0.4 GK, the rate of the 25 Al(p,) 26 Si reaction, which bypasses 26 Al production and therefore places an upper limit on the amount of 26 Al contributed by novae to Galactic abundances, is likely dominated by a single 3 + resonance. Constraining the energy and strength of this resonance is therefore critical to determining the 25 Al(p,) 26 Si reaction rate. We have used a radioactive 26 P beam produced at the National Superconducting Cyclotron Laboratory to populate the 3 + state via beta decay, and have observed first evidence for its decay branch, the last piece of information needed to calculate the resonance strength. We find the 3 + state to have a resonance energy of E r = 414.9 0.6 (stat) 0.3 (syst) 0.6 (lit.) keV and a resonance strength of = 23 6 (stat) +11 -10 (lit.) meV. We have also used hydrodynamic nova simulations to model 26 Al production and we find that novae may contribute up to 0.6 solar masses of the Galactic 26 Al -38% of the total Galactic 26 Al abundance.
Thermodynamic evaluation for a small scale compressed air energy storage system by integrating renewable energy sources (2015)

The present work aims to store renewable energy from wind and sun in the form of compressed air. Several scenarios to find the best operating conditions for a small scale compressed air energy storage system has been analyzed in this paper. The results show a primary efficiency of 52% to 68% for a configuration in which the heat extracted from the air during compression is returned to it during expansion. While for a configuration in which the heat is used for other purposes the theoretical primary efficiency has been found between 37% and 51%, but in this configuration the system it's able to provide an important amount of hot and cold. According to consumer needs the current system can be configured to deliver hot, cold and electricity or only electricity.
Programmed Assembly of Binary Nanostructures in Solution (2002)

Near size-monodisperse silver nanocrystals and silica nanospheres have been prepared and surface-modified with the [2]pseudorotaxane recognition motifs, dibenzo[24]crown-8 and dibenzylammonium cation, respectively. The silver nanocrystals, 7 nm in diameter, are shown to recognize and bind to the silica nanospheres, 180 nm in diameter, via pseudorotaxane formation. The result is the templated assembly of silver nanocrystals at the surface of the larger silica nanosphere core. This composite material exhibits optical properties that are a consequence of localizing silver nanocrystals at the surface of the silica nanospheres. The templating process is also shown to be reversible. This noncovalent recognition-directed templating strategy represents a novel metallization process resulting in the formation of composite media whose collective properties can be controlled.
The Solubility of Hen Lysozyme in Ethylammonium Nitrate/H2O Mixtures and a Novel Approach to Protein Crystallization (2010)

We report on the solubility of hen lysozyme (HEWL) in aqueous ethylammonium nitrate (EAN) as a function of water content. We find the solubility behavior to be complex, exhibiting both a maximum (400 mg/mL) at very high EAN content) and a minimum at intermediate EAN content. We exploit this solubility profile in a novel approach to generating crystals of hydrophilic proteins, based on rehydration of a high concentration protein solution. We describe the production of crystals of X-ray diffraction quality. Two related ionic liquid solvent systems, with the same solubility profiles but different effective pH characteristics, are identified for future evaluation.
Protein Phosphatase 2A Inhibitors, I1PP2A and I2PP2A, Associate with and Modify the Substrate Specificity of Protein Phosphatase 1 (2000)

Recombinant I(1)(PP2A) and I(2)(PP2A) did not affect the activity of the catalytic subunit of protein phosphatase 1 (PP1(C)) with (32)P-labeled myelin basic protein, histone H1, and phosphorylase when assayed in the absence of divalent cations. However, in the presence of Mn(2+), I(1)(PP2A) and I(2)(PP2A) stimulated PP1(C) activity by 15-20-fold with myelin basic protein and histone H1 but not phosphorylase. Half-maximal stimulation occurred at 2 and 4 nM I(1)(PP2A) and I(2)(PP2A), respectively. Moreover, I(1)(PP2A) and I(2)(PP2A) reduced the Mn(2+) requirement by about 30-fold to 10 microM. In contrast, PP1(C) activity was unaffected by I(1)(PP2A) and I(2)(PP2A) in the presence of Co(3+) (0.1 mM), Mg(2+) (2 mM), Ca(2+) (0.5 mM), and Zn(2+) (0.1 mM). Following gel filtration chromatography on Sephacryl S-200 in the presence of Mn(2+), PP1(C) coeluted with I(1)(PP2A) and I(2)(PP2A) in the void volume. However, when I(1)(PP2A) and I(2)(PP2A) or Mn(2+) were omitted, PP1(C) emerged with a V(e)/V(0) of approximately 1.6. The results demonstrate that I(1)(PP2A) and I(2)(PP2A) associate with and modify the substrate specificity of PP1(C) in the presence of physiological concentrations of Mn(2+). A novel role is suggested for I(1)(PP2A) and I(2)(PP2A) in the reciprocal regulation of two major mammalian serine/threonine phosphatases, PP1 and PP2A.
Interpreting the Randomized Clinical Trial of Constraint-Induced Movement Therapy (2007)

JAMA Effect of Constraint-Induced Movement Therapy on Upper Extremity Function 3 to 9 Months After Stroke: The EXCITE Randomized Clinical Trial Steven L. Wolf, PhD, PT; Carolee J. Winstein, PhD, PT; J. Philip Miller, AB; Edward Taub, PhD; Gitendra Uswatte, PhD; David Morris, PhD, PT; Carol Giuliani, PhD, PT; Kathye E. Light, PhD, PT; Deborah Nichols-Larsen, PhD, PT; for the EXCITE Investigators Context: Single-site studies suggest that a 2-week program of constraint-induced movement therapy (CIMT) for patients more than 1 year after stroke who maintain some hand and wrist movement can improve upper extremity function that persists for at least 1 year. Objective: To compare the effects of a 2-week multisite program of CIMT vs usual and customary care on improvement in upper extremity function among patients who had a first stroke within the previous 3 to 9 months. Design and Setting: The Extremity Constraint Induced Therapy Evaluation (EXCITE) trial, a prospective, single-blind, randomized, multisite clinical trial conducted at 7 US academic institutions between January 2001 and January 2003. Participants: Two hundred twenty-two individuals with predominantly ischemic stroke. Interventions: Participants were assigned to receive either CIMT (n = 106; wearing a restraining mitt on the less-affected hand while engaging in repetitive task practice and behavioral shaping with the hemiplegic hand) or usual and customary care (n = 116; ranging from no treatment after concluding formal rehabilitation to pharmacologic or physiotherapeutic interventions); patients were stratified by sex, prestroke dominant side, side of stroke, and level of paretic arm function. Main Outcome Measures: The Wolf Motor Function Test (WMFT), a measure of laboratory time and strength-based ability and quality of movement (functional ability), and the Motor Activity Log (MAL), a measure of how well and how often 30 common daily activities are performed. Results: From baseline to 12 months, the CIMT group showed greater improvements than the control group in both the WMFT Performance Time (decrease in mean time from 19.3 seconds to 9.3 seconds [52% reduction] vs from 24.0 seconds to 17.7 seconds [26% reduction]; between-group difference, 34% [95% confidence interval {CI}, 12%-51%]; P P Conclusion: Among patients who had a stroke within the previous 3 to 9 months, CIMT produced statistically significant and clinically relevant improvements in arm motor function that persisted for at least 1 year. Trial Registration: clinicaltrials.gov Identifier:NCT00057018
An ISA-retargetable framework for embedded software analysis (2004)

Industry requires new advanced tools and methodologies for the design of complex system-on-chip platforms. In STMicroelectronics we developed an innovative retargetable technology for the analysis and optimization of embedded software. In this paper we provide an overview of our retargetable tool chain which consists of: a specification reader a disassembler a code analyzer and a functional simulator. Their capabilities, specific features and limitations are described in detail.
Determination of Kinase Inhibitor Potencies in Cell Extracts by Competition Binding Assays and Isobaric Mass Tags (2011)

Chemical proteomics offers a unique approach for target identification of small molecule inhibitors directly from cell extracts, thus enabling characterization of target proteins under close to physiological conditions. Here, we describe a competition binding procedure that is based on affinity enrichment of potential target proteins on a probe matrix in the presence of increasing amounts of free test compound in solution. Reduced binding of target proteins to the probe matrix as a function of test compound concentration can be measured and thus, enables calculation of IC(50) values. The method employs quantitative mass spectrometry using isobaric mass tags which enables determination of potency for a large number of target proteins in a single analysis.
Development of a new method for measuring total urinary protein using acid violet 6B pigment (2003)

We have developed a new method for measuring total urinary protein using acid violet 6B (AV6B) pigment. Nine purified components of human urinary proteins and urine samples collected randomly from 123 diabetic outpatients were used. There were 62, 36, and 25 cases of prenephropathy, early nephropathy, and overt nephropathy, respectively. All samples were measured by Coomassie brilliant blue G 250 (CBB), pyrogallol red-molybdate (PRM), and AV6B methods using an optical photometer. In healthy subjects, the major components of urinary proteins, such as gamma-globulins, IgG, IgA Tamm-Horsfall protein, and transferrin, the reactivity values of the AV6B and PRM methods were similar. The CBB method was the least sensitive of the three methods. In the urine samples from diabetic patients, the urinary protein values measured by the AV6B method were higher than those measured by the CBB method in the prenephropathy stage. The values obtained by the AV6B method (y) correlated well with those from the CBB method (x) (y=1.243x+3.61, r=0.904). When the values from the AV6B method (y) were compared to those from the PRM method (x), correlation was low (y=1.406x-29.15, r=0.786). In conclusion, the AV6B method was more useful than the CBB and PRM methods for low levels of urinary protein.
Kinetic Isotope Effect Characterization of the Transition State for Oxidized Nicotinamide Adenine Dinucleotide Hydrolysis by Pertussis Toxin (1997)

Pertussis toxin from Bordatella pertussis catalyzes the ADP ribosylation of several G-proteins, using NAD+ as a substrate. In the absence of an acceptor protein, the toxin acts as a NAD+ glycohydrolase. Pertussis toxin is one of the virulent factors for whooping cough and therefore a target for site-specific inhibitors based on the transition state structure. A family of kinetic isotope effects was determined for the hydrolysis reaction, using NAD+ labeled with 3H, 14C, and 15N as substrates. Primary isotope effects were 1.021 +/- 0.001 for [1'N-14C]NAD+ and 1.021 +/- 0.004 for [1N-15N]NAD+, and the double-primary effect of [1'N-14C,1N-15N]NAD+ was 1.049 +/- 0.004. Secondary kinetic isotope effects were 1.207 +/- 0.010 for the [1'N-3H]-, 1.144 +/- 0.005 for the [2'N-3H]-, 0.989 +/- 0.001 for the [4'N-3H]-, and 1.019 +/- 0.004 for the [5'N-3H]NAD+, respectively. Commitment to catalysis was excluded by isotope trapping experiments, and the experimental kinetic isotope effects were independent of pH. The measured isotope effects are therefore intrinsic. The isotope effects are remarkable because they indicate an oxocarbenium-like ribose ring at the transition state but a stiffer than expected vibrational environment for C1' at the reaction center. On the basis of these isotope effects, a bond order vibrational analysis was performed to locate a transition state structure consistent with the isotope effects. The kinetic isotope effects predict a residual bond order to the nicotinamide leaving group of 0.11, corresponding to a distance of 2.14 A. Participation of the water nucleophile is weak, consistent either with an S(N)1-like transition state with no water interaction or with the water oxygen no closer than 3.5 A from the reaction center. The positive charge of the ribose oxocarbenium is stabilized by delocalization between the C1'-O4' and C1'-C2' bonds. The enzyme contacts restrict the vibrational environment of the reaction coordinate requiring increased bonding force constants for the enzyme-stabilized transition state. NAD+ analogues with the nicotinamide ribose replaced by an iminoribitol ring, mimicking the flattened ribose ring of the transition state, are expected to be transition state inhibitors.