gebhart/patrepeval huggingface dataset:
P4‐327: Effects of the novel 5‐HT6 SB‐742457 antagonist and the cholinesterase inhibitor donepezil in models of cognition (2008)

5-hydroxytryptamine (5-HT) is found in many areas of the CNS, and has been implicated in the modulation of learning and memory processes. The 5-HT6 receptor is a member of the seven transmembrane G protein coupled family of receptors and is positively coupled to adenylate cyclase. 5-HT6 receptor antagonists can increase the release of several neurotransmitters in the brain and enhance cognitive processes in rodent models. Several 5-HT6 antagonists are being developed as symptomatic agents for the treatment of memory deficits in Alzheimer's disease and other dementias, including SB-742457. SB-742457 was profiled in standard in vitro binding and functional assays. SB-742457 had high affinity for native 5-HT6 receptors expressed in rat striatum (pKi = 9.56) consistent with its binding affinity and functional potency (cAMP assay) at the recombinant human receptor (pKi = 9.68; pA2 = 9.2). SB-742457 is > 100 fold selective for the human 5-HT6 receptor over all other 5-HT receptors, ion channels and transporters examined apart from 5-HT2a. (pKi 8.0). Following oral administration in rats, SB-742457 exhibited high 5-HT6 receptor occupancy in the striatum (ED50 = 0.3mg/kg from ex vivo binding studies) indicative of good brain penetration. In vivo oral activity of SB-742457 and the cholinesterase inhibitor Donepezil was assessed in a range of neurochemical and animal models of cognition including aged Morris Water Maze and Passive Avoidance. In these studies a sub-chronic administration of SB-742457 or Donepezil (0.03 and 0.3mg/kg) was able to significantly improve the spatial learning ability of aged animals, with SB-742457 (1.5mg/kg) promoting an apparently more prolonged beneficial effect on memory retention. Acute administration of both compounds reversed scopolamine induced amnesia in a passive avoidance paradigm, though with different dose-response profiles. Given its beneficial effects, on learning and memory in preclinical species the 5-HT6 antagonist SB-742457 has the potential to be a new therapeutic agent for the symptomatic treatment of Alzheimer's disease and other dementias.
Revealing genome-scale transcriptional regulatory landscape of OmpR highlights its expanded regulatory roles under osmotic stress in Escherichia coli K-12 MG1655 (2017)

A transcription factor (TF), OmpR, plays a critical role in transcriptional regulation of the osmotic stress response in bacteria. Here, we reveal a genome-scale OmpR regulon in Escherichia coli K-12 MG1655. Integrative data analysis reveals that a total of 37 genes in 24 transcription units (TUs) belong to OmpR regulon. Among them, 26 genes show more than two-fold changes in expression level in an OmpR knock-out strain. Specifically, we find that: 1) OmpR regulates mostly membrane-located gene products involved in diverse fundamental biological processes, such as narU (encoding nitrate/nitrite transporter), ompX (encoding outer membrane protein X), and nuoN (encoding NADH:ubiquinone oxidoreductase); 2) by investigating co-regulation of entire sets of genes regulated by other stress-response TFs, stresses are surprisingly independently regulated among each other; and, 3) a detailed investigation of the physiological roles of the newly discovered OmpR regulon genes reveals that activation of narU represents a novel strategy to significantly improve osmotic stress tolerance of E. coli. Thus, the genome-scale approach to elucidating regulons comprehensively identifies regulated genes and leads to fundamental discoveries related to stress responses.
Supplementary Figure Legends 1-2 from Comparison of Neuropathy-Inducing Effects of Eribulin Mesylate, Paclitaxel, and Ixabepilone in Mice (2023)

Supplementary Figure Legends 1-2 from Comparison of Neuropathy-Inducing Effects of Eribulin Mesylate, Paclitaxel, and Ixabepilone in Mice
Generation of 10-W average-power, 40-TW peak-power, 24-fs pulses from a Ti:sapphire amplifier system (1999)

We developed a compact, three-stage, multipass Ti:sapphire laser amplifier system that generates &gt;40-TW pulses, with 24-fs pulse duration, at a repetition rate of 10 Hz, and with an average power of 10 W. Output intensities in excess of 1×1019 W cm-2 were produced. The technique of frequency-resolved optical gating was used to fully characterize the output pulses and to carefully compare theoretical models with experiment. High dynamic range frequency-resolved optical-gating measurements were performed, for the first time to our knowledge, to characterize the temporal wings of the output pulses.
GaAS MOLECUIaAR BEAM EPITAXY MONOLITHIC POWEK AMPLIFIERS AT U- BAND (1989)

a device of 0.8-mm width. This relatively larger sized gate width is used to achieve The design. fabrication, and measure- high output power without using a multicom ments for 44-GHz band molecular beam epibiner scheme, which can contribute to sub taxy (MBE) monolithic power amplifiers are stantial circuit loss that degrades output described. A five-stage balanced amplifier power. provided a linear gain of 15.1 dB and maximum output power of 500 mW at 42.5 GHz. These results may represent the highest power and gain achieved from a MIMlC in the 44-GHz band.
Supplementary Figure S1 from A Clinical PET Imaging Tracer ([<sup>18</sup>F]DASA-23) to Monitor Pyruvate Kinase M2–Induced Glycolytic Reprogramming in Glioblastoma (2023)

&lt;p&gt;[18F]DASA-23 Radiosynthesis&lt;/p&gt;
Supplementary Figures S1 - S9 from Combination Targeted Therapy to Disrupt Aberrant Oncogenic Signaling and Reverse Epigenetic Dysfunction in <i>IDH2</i>- and <i>TET2</i>-Mutant Acute Myeloid Leukemia (2023)

&lt;p&gt;Supplementary Figure S1. Response of Tet2-/- Flt3ITD leukemia model to 5-Aza therapy Tet2-/-Flt3ITD leukemia model treated with vehicle or 5-Aza (n=5). Supplementary Figure S2. Idh2R140QFlt3ITD leukemia model phenotype. Supplementary Figure S3. Idh2R140QFlt3ITD leukemia model treatment response to AG-221 Idh2R140QFlt3ITD leukemia model treated with vehicle or AG-221 (n=6). Supplementary Figure S4. Genomic methylation analysis of Idh2R140Q Flt3ITD leukemia model response to AG-221 therapy. Supplementary Figure S5. GSEA analysis of 5-Aza and AG-221 response. Supplementary Figure S6. Response of Tet2-/-Flt3ITD leukemia model to 5-Aza and AC220 therapy. Supplementary Figure S7. Idh2R140QFlt3ITD and Tet2-/-Flt3ITD leukemia model response to combination therapy. Supplementary Figure S8. Methylation and expression response of Tet2-/-Flt3ITD and Idh2R140QFlt3ITD leukemia model to combination therapy. Supplementary Figure S9. Response of Tet2-/- Flt3ITD and Idh2R140QFlt3ITD leukemia model to combination therapy.&lt;/p&gt;
Sample preparation free tissue imaging using Laser Desorption – Rapid Evaporative Ionisation Mass spectrometry (LD-REIMS) (2023)

Laser desorption ionisation (LDI) is generally considered to be an inferior ionisation modality to matrix assisted LDI (MALDI), providing information solely on lipids with low sensitivity. The current study demonstrates that the combination of ambient LDI with in-source surface-induced declustering provides sensitivity and chemical coverage comparable to MALDI. The setup was characterised for infrared laser desorption using two different laser systems and was successfully used for ambient mass spectrometric imaging. 20 µm spatial resolution was achieved with oversampling, approaching single-cell resolution, while metabolites and lipids ranging from amino acids through carbohydrates and nuclear bases to complex glycolipids were successfully detected. The technique was also tested as a platform for MS-guided surgery, raising the possibility of using a single technique for generating histological and in-vivo data. The results suggest that the new method can form the basis for a new histological classification system for surgery and pathology environments closing this 150 year old diagnostic gap.
Inhibitory Effects of Manassantin A and B Isolated from the Roots ofSaururus chinensison PMA-Induced ICAM-1 Expression (2003)

Cell adhesion inhibitors were isolated from the methanol extract of Saururus chinensis roots by bioactivity-guided fractionation. The active compounds were identified as manassantin A ( 1) and B ( 2), dineolignan compounds. Compounds 1 and 2 inhibited PMA-induced ICAM-1/LFA-1-mediated homotypic aggregation of the HL-60 cells without cytotoxicity with MIC values of 1.0 and 5.5 nM, respectively. Even though 1 and 2 did not affect the adhesion of ICAM-1 to LFA-1, these compounds inhibited PMA-induced ICAM-1 expression in HL-60 cells in a dose-dependent fashion. These results suggest that 1 and 2 inhibit cell aggregation through down-regulation of ICAM-1 expression.
Graph convolutional regression of cardiac depolarization from sparse\n endocardial maps (2020)

Electroanatomic mapping as routinely acquired in ablation therapy of\nventricular tachycardia is the gold standard method to identify the\narrhythmogenic substrate. To reduce the acquisition time and still provide maps\nwith high spatial resolution, we propose a novel deep learning method based on\ngraph convolutional neural networks to estimate the depolarization time in the\nmyocardium, given sparse catheter data on the left ventricular endocardium,\nECG, and magnetic resonance images. The training set consists of data produced\nby a computational model of cardiac electrophysiology on a large cohort of\nsynthetically generated geometries of ischemic hearts. The predicted\ndepolarization pattern has good agreement with activation times computed by the\ncardiac electrophysiology model in a validation set of five swine heart\ngeometries with complex scar and border zone morphologies. The mean absolute\nerror hereby measures 8 ms on the entire myocardium when providing 50\\% of the\nendocardial ground truth in over 500 computed depolarization patterns.\nFurthermore, when considering a complete animal data set with high density\nelectroanatomic mapping data as reference, the neural network can accurately\nreproduce the endocardial depolarization pattern, even when a small percentage\nof measurements are provided as input features (mean absolute error of 7 ms\nwith 50\\% of input samples). The results show that the proposed method, trained\non synthetically generated data, may generalize to real data.\n
OPTICAL AND MAGNETO-OPTICAL PERFORMANCE OF OPTIMIZED DISK STRUCTURES (1991)

We explore the relative magneto-optic readback performance of three magnetic materials for erasable optical data storage. We modeled the system signal-to-noise ratio (SNR) of optimal film structures incorporating either TbFeCo, a Co/Pt multilayer, or BiDy-substituted FeGa garnet as a function of the wavelength of the reading light beam. The complex indices of refraction and Voigt parameters of the three magnetic storage materials were determined experimentally over the spectral range 300-800 nm by regression fitting of data from variable angle of incidence ellipsometry and normal incidence Kerr spectroscopy to an appropriate optical model. Making specific comparisons of the read back performance at 450, 550, and 800 nm, we find that for the MO materials we have characterized, the performance of TbFeCo is superior to that of either Co/Pt or the garnet at 550 and 800 nm. Only at 450 nm did the Co/Pt give slightly higher SNR than the TbFeCo. The garnet showed improving SNR in passing from 800 nm to the shorter wavelengths, but it had lower performance than the metal films.
TRANSPORT PROPERTIES UNDER PRESSURE OF THE ORGANIC CONDUCTORS (TMTTF)2X; X = PF6, C104, Br (1983)

International audience
ChemInform Abstract: Microbial Deracemization of 1‐Aryl and 1‐Heteroaryl Secondary Alcohols. (2002)

Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.
Practical Aspects of Aerosol Characterization in an Environment of Controlled Temperature and Relative Humidity (1988)

AbstractIn the fields of environmental and pharmaceutical aerosols it is of importance to create atmospheres of controlled temperature and relative humidity for the investigation of airborne particulate behavior. Close control of humidity, especially where relative humidity sensing is used, also requires close temperature control because of the dependence of relative humidity on temperature. Unique designs of apparatus have been employed, in many cases, without considering the implications of the level of control required to obtain statistically acceptable data. This paper describes a novel apparatus, contrasts it with those in the literature and states specifically the level of control which can be achieved practically and how this compares with theoretical expectations.
Rice–Ramsperger–Kassel–Marcus (RRKM) Theory (2016)

This document contains recommendations for terminology in mass spectrometry. Development of standard terms dates back to 1974 when the IUPAC Commission on Analytical Nomenclature issued recommendations on mass spectrometry terms and definitions. In 1978, the IUPAC Commission on Molecular Structure and Spectroscopy updated and extended the recommendations and made further recommendations regarding symbols, acronyms, and abbreviations. The IUPAC Physical Chemistry Division Commission on Molecular Structure and Spectroscopy’s Subcommittee on Mass Spectroscopy revised the recommended terms in 1991 and appended terms relating to vacuum technology. Some additional terms related to tandem mass spectrometry were added in 1993 and accelerator mass spectrometry in 1994. Owing to the rapid expansion of the field in the intervening years, particularly in mass spectrometry of biomolecules, a further revision of the recommendations has become necessary. This document contains a comprehensive revision of mass spectrometry terminology that represents the current consensus of the mass spectrometry community.
The RP105/MD-1 complex is indispensable for TLR4/MD-2-dependent proliferation and IgM-secreting plasma cell differentiation of marginal zone B cells (2012)

Marginal zone (MZ) B cells mount rapid T-cell-independent (T-I) immune responses against microbial components such as LPS. While Toll-like receptor 4 (TLR4) is essential for LPS responses, MZ B cells uniquely express high levels of another LPS sensor Radioprotective 105 (RP105). However, little is known about how RP105 is used by MZ B cells. In this study, we investigated TLR4- or RP105-dependent MZ B cell responses by utilizing agonistic monoclonal antibodies (mAbs) to each receptor. Cross-linking TLR4 and RP105 at the same time with the mAbs induced robust IgM-secreting plasma cell generation as lipid A moiety of LPS. In contrast, stimulation with either mAb alone did not elicit such responses. RP105-deficient MZ B cells failed to produce IgM-secreting plasma cells in response to lipid A. TLR4 or lipid A stimulation of MZ B cells up-regulated their B lymphocyte-induced maturation protein 1 (Blimp-1) and X-box-binding protein 1 (Xbp-1) mRNA expression. RP105 stimulation alone did not give these responses and in fact decreased TLR4-mediated their expression. Compared with wild-type (WT) MZ B cells, RP105-deficient MZ B cells exhibited increased levels of Blimp-1 and Xbp-1 mRNA expression in response to lipid A. Lipid A or TLR4 plus RP105 stimulation induced massive proliferation and expression of Bcl-xL and c-Myc in WT but not RP105-deficient MZ B cells. These responses contributed to TLR4-mediated anti-apoptotic responses in MZ B cells. Thus, RP105 contributes in a unique way to the TLR4-dependent survival, proliferation and plasma cell generation of MZ B cells.
Experimental and theoretical understanding of Forming, SET and RESET operations in Conductive Bridge RAM (CBRAM) for memory stack optimization (2014)

In this paper, we deeply investigate for the 1 <sup xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">st</sup> time at our knowledge the impact of the CBRAM memory stack on the Forming, SET and RESET operations. Kinetic Monte Carlo simulations, based on inputs from ab-initio calculations and taking into account ionic hopping and chemical reaction dynamics are used to analyse experimental results obtained on decananometric devices. We propose guidelines to optimize the CBRAM stack, targeting Forming voltage reduction, improved trade-off between SET speed and disturb immunity (time voltage dilemma) and window margin increase (RESET efficiency).
MUC5B expression and location in surfactant protein C mutations in children (2015)

MUC5B may play a role in the development of fibrosis in patients with SFTPC mutations, especially in patients with BRICHOS mutations. Understanding the role of MUC5B in adult and pediatric lung diseases may lead to a better understanding of the etiology of fibrotic lung disease as well as development of novel therapies.
Contributions of T-Type Voltage-Gated Calcium Channels to Postsynaptic Calcium Signaling within Purkinje Neurons (2010)

Low threshold voltage-gated T-type calcium channels have long been implicated in the electrical excitability and calcium signaling of cerebellar Purkinje neurons although the molecular composition, localization, and modulation of T-type channels within Purkinje cells have only recently been addressed. The specific functional roles that T-type channels play in local synaptic integration within Purkinje spines are also currently being unraveled. Overall, Purkinje neurons represent a powerful model system to explore the potential roles of postsynaptic T-type channels throughout the nervous system. In this review, we present an overview of T-type calcium channel biophysical, pharmacological, and physiological characteristics that provides a foundation for understanding T-type channels within Purkinje neurons. We also describe the biophysical properties of T-type channels in context of other voltage-gated calcium channel currents found within Purkinje cells. The data thus far suggest that one specific T-type isoform, Ca(v)3.1, is highly expressed within Purkinje spines and both physically and functionally couples to mGluR1 and other effectors within putative signaling microdomains. Finally, we discuss how the selective potentiation of Ca(v)3.1 channels via activation of mGluR1 by parallel fiber inputs affects local synaptic integration and how this interaction may relate to the overall excitability of Purkinje neuron dendrites.
Dose Optimization in TOF-PET/MR Compared to TOF-PET/CT (2015)

The new TOF-PET/MR device requires significantly less activity to generate PET-images with good-to-excellent image quality, due to improvements in detector geometry and detector technologies. The theoretically achievable dose reduction accounts for up to 65% but cannot be fully translated into clinical routine based on the coils within the FOV and MR-sequences applied at the same time. The clinically realistic reduction in activity is slightly more than 50%. Further studies in a larger number of patients are needed to confirm our findings.
The Counteracting Effects of Capillary Porosity and of Unhydrated Clinker Grains on the Macroscopic Strength of Hydrating Cement Paste–A Multiscale Model (2013)

Strength of cement pastes increases overlinearly with decreasing capillary porosity, such as suggested by the gel-space ratio model of Freyssinet (1933). This model, however, cannot explain that strength of mature sub-stoichiometric cement pastes increases with decreasing w/c-ratio, such as observed by Fagerlund (1972). The latter observation might well stem from a strengthening effect of unhydrated clinker grains, but until very recently an etiological model for quantification of this effect was out of reach. This provides the motivation for the present study, where we envision that the strength of microscopic cement hydrates is the limiting factor for the load carrying capacity of macroscopic cement paste samples. In more detail, we envision a stress-based strength criterion for microscopic hydrate needles, whereby the involved hydrate strength constant is determined from the results of nanoindentation experiments on low-density C-S-H, performed by Constantinides and Ulm (2006). Strength upscaling is performed within the framework of continuum micromechanics (Pichler et al., 2008-2013). Model-predicted macrostrength values of cement pastes (exhibiting different compositions and different maturities) agree very well with strength values measured at three different laboratories. The validated model confirms that strength of cement pastes is strongly influenced by capillary porosity, and that unhydrated clinker grains act as significantly strengthening reinforcements for mature substoichiometric pastes (Pichler et al. 2013).
Licensed shared access (LSA) and three-tier spectrum sharing models: regulation, business and technology perspectives (2017)

Spectrum sharing is an important enabler for future mobile broadband systems to meet the growing end user data traffic needs. Considering spectrum sharing from regulation, business and technology perspectives is the key for the successful development of sharing models that can be deployed in practical systems. This chapter studies recent spectrum sharing concepts from regulatory, business and technology perspectives. We present the European Licensed Shared Access (LSA) spectrum sharing concept covering its regulatory, business, and technical aspects with a focus on the LSA case example of sharing between LTE and incumbent program making and special events (PMSE) services in the 2.3-2.4 GHz band. The LSA evolution including more dynamic sharing toward the US three-tier spectrum sharing model for Citizen Broadband Radio Service (CBRS) based on Spectrum Access System (SAS) is depicted in terms of its ecosystem, business benefits, and technical approaches. Future outlook is given to envisage the development of sharing models for the mobile broadband.
Erythromycin-induced ribosome stall in the ermA leader: a barricade to 5'-to-3' nucleolytic cleavage of the ermA transcript (1989)

The Staphylococcus aureus ermA gene, whose product confers resistance to the macrolide-lincosamide-streptogramin B family of antibiotics, is induced at the level of translation by nanomolar concentrations of erythromycin. Erythromycin also specifically stabilizes ermA transcripts, and the induced stabilization requires in-phase translation of at least one of two small leader peptides in the 5' leader region of the transcript. Erythromycin-induced mRNA stabilization was tested in three constructions in which the ermA transcript was elongated by making insertions at the ermA transcription start. Whereas mRNA downstream of the leader peptide is stabilized by erythromycin, mRNA upstream is not. In the presence of erythromycin, specific mRNA decay intermediates in both the extended ermA genes and the wild-type ermA gene were detected by both Northern blotting and S1 nuclease mapping. The 5' ends of the intermediates map to the sequences that encode each of the two ermA leader peptides, suggesting that the intermediates are produced by stalled erythromycin-bound ribosomes acting as barricades to degradation by 5'-to-3' RNases. In addition, whereas erythromycin was found previously to stabilize ermA transcripts only physically, an ermC-cat-86 hybrid transcript was stabilized both physically and functionally by erythromycin.