gebhart/patrepeval huggingface dataset:
Chymotrypsin‐like proteases contribute to human monocytic THP‐1 cell as well as human microglial neurotoxicity (2005)

Activated microglia have been observed in various neurodegenerative diseases, including Alzheimer's disease (AD), Parkinson's disease (PD), amyotrophic lateral sclerosis, and multiple sclerosis. They may exacerbate neuronal damage by secreting various toxic molecules. The list of candidate toxins includes proteases. Since it is currently not known which, if any, proteases are involved in human microglia neurotoxicity, we studied the effects of a panel of protease inhibitors on the toxicity of cell-free supernatants of stimulated human microglia and THP-1 monocytic cells to human SH-SY5Y cells. Five structurally distinct inhibitors that are known to inhibit chymotrypsin-like proteases were partially protective. They included chymostatin, AEBSF (Pefabloc SC), alpha1-antichymotrypsin, bromoenol lactone, and 3,4-dichloroisocoumarin. The data suggest that certain protease inhibitors could inhibit microglial-mediated toxicity. They might represent a novel class of drugs with benefit in diseases where overactivity of microglia contributes to the pathogenesis.
Highlight Scene Detection And Video Summarization for PVR-Enabled High-Definition Television Systems (2007)

We describe an implementation of our previously developed highlight scene detection and video summarization system, on a PVR-enabled high-definition television system. The implementation poses significant challenges such as consuming minimal computational resources so as to avoid disrupting any of the existing functionalities. The target platform poses challenges such as the absence of a DSP which differ significantly from our previous PVR platform. Our implementation successfully addresses the aforementioned challenges by adapting techniques such as limited buffering and error concealment for dropped frames to the target platform.
Involvement of ERCC1 in the pathogenesis of osteoarthritis through the modulation of apoptosis and cellular senescence (2014)

DNA damage is a cause of age related pathologies, including osteoarthritis (OA). Excision repair cross complementation group 1 (ERCC1) is an endonuclease required for DNA damage repair. In this study we investigated the function of ERCC1 in chondrocytes and its association with the pathophysiology of OA. ERCC1 expression in normal and osteoarthritic cartilage was assessed, as were changes in ERCC1 expression in chondrocytes under catabolic stress. Inhibiting ERCC1 in chondrocytes under interleukin-1β stimulation using small interfering RNA (siRNA) was also evaluated. Finally, cellular senescence and apoptosis were examined in relation to ERCC1 function. ERCC1 expression was decreased in OA cartilage and increased within 4 h of exposure to interleukin (IL)-1β, but decreased after 12 h. The inhibition of ERCC1 by siRNA increased the expression of matrix metallopeptidase 13 and decreased collagen type II. ERCC1 inhibition also increased the number of apoptotic and senescent cells. The inhibition of ERCC1 in chondrocytes increased their expression of OA related proteins, apoptosis, cellular senescence, and hypertrophic-like changes which suggest that ERCC1 is critical for protecting human chondrocytes (HCs) from catabolic stresses and provides insights into the pathophysiology of OA and a potential target for its treatment. (191)
Serum GP88 as a predictive biomarker for hepatocellular carcinoma in patients with viral hepatitis C after direct-acting antiviral agents (2021)

Sustained high concentrations of serum GP88 in patients treated with direct-acting antiviral agents are correlated with the risk of developing hepatocellular carcinoma.
A new papadopoulos multiaxial fatigue criterion accounting for grain flow orientation in forged components (2007)

International audience
Comparative proteomic analysis of glomerular proteins in primary and bucillamine-induced membranous nephropathy (2022)

Between the pMN and BCL-induced sMN groups, we observed common and different alterations in protein levels such as known disease-associated proteins and potential disease marker proteins.
MRI-powered biomedical devices (2017)

Magnetic resonance imaging (MRI) is beneficial for imaging-guided procedures because it provides higher resolution images and better soft tissue contrast than computed tomography (CT), ultrasound, and X-ray. MRI can be used to streamline diagnostics and treatment because it does not require patients to be repositioned between scans of different areas of the body. It is even possible to use MRI to visualize, power, and control medical devices inside the human body to access remote locations and perform minimally invasive procedures. Therefore, MR conditional medical devices have the potential to improve a wide variety of medical procedures; this potential is explored in terms of practical considerations pertaining to clinical applications and the MRI environment. Recent advancements in this field are introduced with a review of clinically relevant research in the areas of interventional tools, endovascular microbots, and closed-loop controlled MRI robots. Challenges related to technology and clinical feasibility are discussed, including MRI based propulsion and control, navigation of medical devices through the human body, clinical adoptability, and regulatory issues. The development of MRI-powered medical devices is an emerging field, but the potential clinical impact of these devices is promising.
Supplementary Figure 6 from Cabozantinib Eradicates Advanced Murine Prostate Cancer by Activating Antitumor Innate Immunity (2023)

&lt;p&gt;Cabozantinib-mediated tumor clearance is independent of NK and T cells.&lt;/p&gt;
Key Fuel Injection System Features for Efficiency Improvement in Future Diesel Passenger Cars (2019)

&lt;div class="section abstract"&gt;&lt;div class="htmlview paragraph"&gt;Diesel will continue to be an indispensable energy carrier for the car fleet CO&lt;sub&gt;2&lt;/sub&gt; emission targets in the short-term. This is particularly relevant for heavy-duty vehicles as for mid-size cars and SUVs. Looking at the latest technology achievements on the after-treatment systems, it can be stated that the concerning about the NOx emission gap between homologation test and real road use is basically solved, while the future challenge for diesel survival is to keep its competitiveness in the CO&lt;sub&gt;2&lt;/sub&gt; vs cost equation in comparison to other propulsion systems.&lt;/div&gt;&lt;div class="htmlview paragraph"&gt;The development of the combustion system design still represents an important leverage for further efficiency and emissions improvements while keeping the current excellent performance in terms of power density and low-end torque.&lt;/div&gt;&lt;div class="htmlview paragraph"&gt;The paper describes the results achieved in developing a new diesel combustion system for car application that, leveraging on the high flexibility of the latest fuel injection technology, combines outstanding power and fuel efficiency with low pollutant emissions in ultralight engine designed for lower maximum peak cylinder pressure. The study has been carried out on a 0.5l single-cylinder engine on which an advanced and last generation common rail system, capable of very high injection pressure, has been installed.&lt;/div&gt;&lt;div class="htmlview paragraph"&gt;Through an extensive DoE-based test campaign in which all engine operating parameters have been carefully parametrized, the capability to achieve high power density and excellent fuel economy with low engine-out pollutant emissions has been demonstrated and discussed in the paper.&lt;/div&gt;&lt;/div&gt;
Silicon interposer with embedded microfluidic cooling for high-performance computing systems (2015)

A silicon interposer platform utilizing microfluidic cooling is proposed to address the off-chip signaling and cooling challenges facing future high-performance computing systems. A test vehicle with microfluidic I/Os and a micropin-fin heat sink was used to evaluate microfluidic cooling performance. De-ionized water (~20 °C) was used as the coolant. At a flow rate of 50 mL/min, the measured temperature was 55.9 °C for a power density of 97.0 W/cm <sup xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">2</sup> . Compared to air cooling, microfluidic cooling significantly improves cooling performance and thermal isolation. Moreover, 3-D integration of two silicon dice with microfluidic I/Os on a silicon interposer is demonstrated.
Phase II study of perifosine in metastatic renal cell carcinoma (RCC) progressing after prior therapy (Rx) with a VEGF receptor inhibitor (2009)

5034 Background: Perifosine, a synthetic alkylphospholipid, inhibits or modulates a number of different signal transduction pathways (AKT, MAPK and JNK). In a prior trial, 15 RCC patients (pts) were enrolled in a randomized dose finding study, 9 were evaluable for response and 3 (33%) had a partial response (PR). Thus phase II trials were begun for pts who had been treated with one prior VEGFr inhibitor (Group A) or with a prior VEGFr inhibitor and prior mTOR inhibitor (Group B). We report the results of Group A (closed), and Group B (enrollment open). Methods: To measure the objective response rate (RECIST) and PFS to single agent perifosine (100 mg qhs with food) after 3 mos of Rx; Prior Rx with vaccine therapy, bevacizumab and/or cytokines was permitted. Normal organ/marrow function was required. Results: From 12/07–12/08, 46 pts (31 Group A/ 15 Group B) were treated at 13 sites. Median age 64 (range 46–80) and 36 were male; Median prior Rx was 2 (range 1 - 5); Clear cell = 37, non clear cell = 6, data n/a = 3. Prior sunitinib = 35, prior sorafenib = 10, 1 unknown due to blinded study. Prior mTOR; Tem = 9 and Rad001 = 6. As of 12/08, 44 pts were evaluable for response and PFS (two pts not eval; 1 withdrew consent, 1 toxicity &lt; 5 days on Rx). Results listed in the table below. As of 12/08, 12/44 pts (5 Group A/ 7 Group B) remain on treatment. Median survival; not reached. Most common toxicity was grade 1 &amp; 2 nausea (56%), arthralgia (47%), vomiting (36%), fatigue (33%) and cognitive changes (28%). Grade 3 &amp; 4 toxicity was uncommon; arthralgia (14%) and hyperuricemia/gout (8%). Conclusions: Perifosine, similar to mTOR inhibitors, appears to have clinical benefit in mRCC as reflected by the PR rate and a 15 wk median overall PFS. This is most notably in patients who failed both a prior VEGFr and mTOR inhibitor where 7/14 remain on study as of 12/08. Randomized studies are under consideration to further evaluate perifosine's clinical benefit as 2 nd or 3 rd line therapy of mRCC. [Table: see text] [Table: see text]
Single-molecule view of basal activity and activation mechanisms of the G protein-coupled receptor β 2 AR (2015)

Binding of extracellular ligands to G protein-coupled receptors (GPCRs) initiates transmembrane signaling by inducing conformational changes on the cytoplasmic receptor surface. Knowledge of this process provides a platform for the development of GPCR-targeting drugs. Here, using a site-specific Cy3 fluorescence probe in the human β2-adrenergic receptor (β2AR), we observed that individual receptor molecules in the native-like environment of phospholipid nanodiscs undergo spontaneous transitions between two distinct conformational states. These states are assigned to inactive and active-like receptor conformations. Individual receptor molecules in the apo form repeatedly sample both conformations, with a bias toward the inactive conformation. Experiments in the presence of drug ligands show that binding of the full agonist formoterol shifts the conformational distribution in favor of the active-like conformation, whereas binding of the inverse agonist ICI-118,551 favors the inactive conformation. Analysis of single-molecule dwell-time distributions for each state reveals that formoterol increases the frequency of activation transitions, while also reducing the frequency of deactivation events. In contrast, the inverse agonist increases the frequency of deactivation transitions. Our observations account for the high level of basal activity of this receptor and provide insights that help to rationalize, on the molecular level, the widely documented variability of the pharmacological efficacies among GPCR-targeting drugs.
2D Plasmonics for Enabling Novel Light-Matter Interactions (2015)

The physics of light-matter interactions is strongly constrained by both the small value of the fine-structure constant and the small size of the atom. Overcoming these limitations is a long-standing challenge. Recent theoretical and experimental breakthroughs have shown that two dimensional systems, such as graphene, can support strongly confined light in the form of plasmons. These 2D systems have a unique ability to squeeze the wavelength of light by over two orders of magnitude. Such high confinement requires a revisitation of the main assumptions of light-matter interactions. In this letter, we provide a general theory of light-matter interactions in 2D systems which support plasmons. This theory reveals that conventionally forbidden light-matter interactions, such as: high-order multipolar transitions, two-plasmon spontaneous emission, and spin-flip transitions can occur on very short time-scales - comparable to those of conventionally fast transitions. Our findings enable new platforms for spectroscopy, sensing, broadband light generation, and a potential test-ground for non-perturbative quantum electrodynamics.
Tunable-Bandwidth Filter System (2006)

A tunable-bandwidth filter system (TBFS), now undergoing development, is intended to be part of a remote-sensing multispectral imaging system that will operate in the visible and near infrared spectral region (wavelengths from 400 to 900 nm). Attributes of the TBFS include rapid tunability of the pass band over a wide wavelength range and high transmission efficiency. The TBFS is based on a unique integration of two pairs of broadband Raman reflection holographic filters with two rotating spherical lenses. In experiments, a prototype of the TBFS was shown to be capable of spectral sampling of images in the visible range over a 200-nm spectral range with a spectral resolution of .30 nm. The figure depicts the optical layout of a prototype of the TBFS as part of a laboratory multispectral imaging system for the spectral sampling of color test images in two orthogonal polarizations. Each pair of broadband Raman reflection holographic filters is mounted at an equatorial plane between two halves of a spherical lens. The two filters in each pair are characterized by steep spectral slopes (equivalently, narrow spectral edges), no ripple or side lobes in their pass bands, and a few nanometers of non-overlapping wavelength range between their pass bands. Each spherical lens and thus the filter pair within it is rotated in order to rapidly tune its pass band. The rotations of the lenses are effected by electronically controlled, programmable, high-precision rotation stages. The rotations are coordinated by electronic circuits operating under overall supervision of a personal computer in order to obtain the desired variation of the overall pass bands with time. Embedding the filters inside the spherical lenses increases the range of the hologram incidence angles, making it possible to continuously tune the pass and stop bands of the filters over a wider wavelength range. In addition, each spherical lens also serves as part of the imaging optics: The telephoto lens focuses incoming light to a field stop that is also a focal point of each spherical lens. A correcting lens in front of the field stop compensates for the spherical aberration of the spherical lenses. The front surface of each spherical lens collimates the light coming from the field stop. After the collimated light passes through the filter in the spherical lens, the rear surface of the lens focuses the light onto a charge-coupled-device image detector.
Synthetic peptides corresponding to protective epitopes of Escherichia coli digalactoside-binding pilin prevent infection in a murine pyelonephritis model. (1988)

Synthetic peptides corresponding to five segments of a globoside (Gal-Gal)-binding pilin sequence [residues 5-12 (R5-12), R65-75, R93-104, R103-116, and R131-143], cyanogen bromide fragment II (CNBr-II, R53-163), and purified, intact Gal-Gal pili were prepared as vaccines and tested for their efficacy in a BALB/c murine model of pyelonephritis. Intact Gal-Gal pili, CNBr-II, and synthetic peptides R5-12 and R65-75 engendered antibodies that bound the homologous pilin protein and prevented urine and renal colonization in most vaccine recipients. Protection correlated with serum anti-pilus IgG ELISA titers greater than or equal to 1:250. The efficacy afforded by synthetic peptides R5-12 and R65-75 in vaccinated mice indicates that linear "antigenic" determinants in separate cyanogen bromide fragments encode "protective" epitopes. Peptides R93-104, R103-116, and R131-143 lacked efficacy, indicating that not all regions of the sequence are serologically equivalent. The crossreactivity of the peptide antisera for different Gal-Gal pilins was also assessed and correlated with the sequence homology of the corresponding regions. Antiserum to peptide R65-75, which corresponds to a region of unconserved sequence in heterologous pilins, bound only the homologous pilin. Thus, it specifies a type-specific protective epitope. Antiserum to synthetic peptide R5-12, which corresponds to a region of conserved sequence, bound Gal-Gal pilins from seven of eight pyelonephritis strains, indicating that it specifies a crossreacting protective epitope.
ChemInform Abstract: First Total Synthesis of 11‐Thia Steroids. (2000)

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.
Recruiting Cytotoxic T Cells to Folate‐Receptor‐Positive Cancer Cells (2013)

Antikörperhelfer: Ein (anti-CD3 Fab)-Folat-Konjugat rekrutiert zytotoxische T-Zellen zu folatrezeptorpositiven (FR+) Tumoren und bewirkt so eine effiziente Abtötung von Tumorzellen durch aktivierte T-Zellen. Der chemische Ansatz zur Synthese bispezifischer Antikörper unter Verwendung von nichtnatürlichen Aminosäuren mit orthogonaler chemischer Reaktivität liefert in hohen Ausbeuten homogene Konjugate mit einer präzisen Kontrolle über die relative Geometrie der Antikörperbindestellen. As a service to our authors and readers, this journal provides supporting information supplied by the authors. Such materials are peer reviewed and may be re-organized for online delivery, but are not copy-edited or typeset. Technical support issues arising from supporting information (other than missing files) should be addressed to the authors. Please note: The publisher is not responsible for the content or functionality of any supporting information supplied by the authors. Any queries (other than missing content) should be directed to the corresponding author for the article.
Analysis of daily business reports based on sequential text mining method (2005)

This paper proposes a new method that discovers characteristic sequential patterns in textual data. The data are composed of three kinds of information: time information, attributes, and text. The method gathers items of the data with the same attribute values, arranges the gathered items in order of the time, and generates sequences. The method also extracts events from each text by using a text mining method. Finally, the method discovers characteristic sequential patterns, composed of sets of events, from sequences by a sequential mining method. In this paper, we apply the method to business reports collected by our sales force automation system and try to discover characteristic sequential patterns. We verify whether the patterns are valid by investigating texts relating to the patterns.
Thyronamines Inhibit Plasma Membrane and Vesicular Monoamine Transport (2007)

Thyroid hormone has long been known to have important transcriptional regulatory activities. Recently, however, the presence of endogenous derivatives of thyroid hormone, thyronamines, has been reported in various mammalian tissues. These derivatives have potent in vitro activity with a class of orphan G-protein-coupled receptors, the trace amine-associated receptors, and profound in vivo effects when administered to mice. We report here a novel neuromodulatory role for thyronamines. In synaptosomal preparations and heterologous expression systems, thyronamines act as specific dopamine and norepinephrine reuptake inhibitors. Thyronamines also inhibit the transport of monoamines into synaptic vesicles. These observations expand the nontranscriptional role of thyroid hormone derivatives and may help to explain the pharmacological effects of thyronamines in vivo.
Shoulder Arthroplasty for Proximal Humeral Fractures (1999)

Depending on the patient’s age, a shoulder prosthesis may be indicated in displaced or dislocated three or four-part fractures of the proximal humerus. Neer was the first author to emphasize the frequency of humeral head necrosis and to propose, in 1951, a replacement of the humeral head by a non-constrained prosthesis associated with a reconstruction of the tuberosities [26]. However, apart from Charles Neer who obtained 80 to 90% excellent or good results with shoulder prosthesis for fractures [27, 28], most authors achieved rather inferior results [10–15, 18, 19, 22, 25, 30, 31, 34, 36, 39]. Considering these ambiguous results, some surgeons have even opted for conservative treatment (or even no treatment at all) rather than surgical treatment for these complexe upper extremity fractures [40, 42].
Combination of Withaferin-A and CAPE Provides Superior Anticancer Potency: Bioinformatics and Experimental Evidence to Their Molecular Targets and Mechanism of Action (2020)

We have earlier reported anticancer activity in Withaferin A (Wi-A), a withanolide derived from Ashwagandha (<i>Withania somnifera</i>) and caffeic acid phenethyl ester (CAPE), an active compound from New Zealand honeybee propolis. Whereas Wi-A was cytotoxic to both cancer and normal cells, CAPE has been shown to cause selective death of cancer cells. In the present study, we investigated the efficacy of Wi-A, CAPE, and their combination to ovarian and cervical cancer cells. Both Wi-A and CAPE were seen to activate tumor suppressor protein p53 by downregulation of mortalin and abrogation of its interactions with p53. Downregulation of mortalin translated to compromised mitochondria integrity and function that affected poly ADP-ribose polymerase1 (PARP1); a key regulator of DNA repair and protein-target for Olaparib, drugs clinically used for treatment of breast, ovarian and cervical cancers)-mediated DNA repair yielding growth arrest or apoptosis. Furthermore, we also compared the docking capability of Wi-A and CAPE to PARP1 and found that both of these could bind to the catalytic domain of PARP1, similar to Olaparib. We provide experimental evidences that (i) Wi-A and CAPE cause inactivation of PARP1-mediated DNA repair leading to accumulation of DNA damage and activation of apoptosis signaling by multiple ways, and (ii) a combination of Wi-A and CAPE offers selective toxicity and better potency to cancer cells.