gebhart/patrepeval huggingface dataset:
Identification of Orally Available Naphthyridine Protein Kinase D Inhibitors (2010)

A novel 2,6-naphthyridine was identified by high throughput screen (HTS) as a dual protein kinase C/D (PKC/PKD) inhibitor. PKD inhibition in the heart was proposed as a potential antihypertrophic mechanism with application as a heart failure therapy. As PKC was previously identified as the immediate upstream activator of PKD, PKD vs PKC selectivity was essential to understand the effect of PKD inhibition in models of cardiac hypertrophy and heart failure. The present study describes the modification of the HTS hit to a series of prototype pan-PKD inhibitors with routine 1000-fold PKD vs PKC selectivity. Example compounds inhibited PKD activity in vitro, in cells, and in vivo following oral administration. Their effects on heart morphology and function are discussed herein.
A small-size transfer blackbody cavity for calibration of infrared ear thermometers (2014)

A small-size transfer blackbody cavity for calibration of infrared ear thermometers (IRETs) was developed and characterized at the Korea Research Institute of Standards and Science. This blackbody cavity consists of a reflector exposed to the air and a radiator with three-step curves immersed in a water-bath, and has an angularly uniform emissivity of higher than 0.9993. The radiance temperature of the blackbody cavity was measured with an IRET. We also calculated the effective emissivity by using the software STEEP322, considering the influence of the shape and temperature of the probe-tip of the IRET on the effective emissivity of the blackbody cavity. The measured and calculated radiance temperatures of the blackbody cavity were compared to those of the ASTM-type blackbody cavity and are in good agreement. Uncertainties (k = 1) of the blackbody cavity are estimated to be less than 44 mK in the temperature range 35-42 °C.
Applications of organocatalysed visible-light photoredox reactions for medicinal chemistry (2018)

The focus of this review is to provide an overview of the field of organocatalysed photoredox chemistry relevant to synthetic medicinal chemistry. Photoredox transformations have been shown to enable key transformations that are important to the pharmaceutical industry. This type of chemistry has also demonstrated a high degree of sustainability, especially when organic dyes can be employed in place of often toxic and environmentally damaging transition metals. The sections are arranged according to the general class of the presented reactions and the value of these methods to medicinal chemistry is considered. An overview of the general characteristics of the photocatalysts as well as some electrochemical data is presented. In addition, the general reaction mechanisms for organocatalysed photoredox transformations are discussed and some individual mechanistic considerations are highlighted in the text when appropriate.
Elektronentransfer durch DNA beim radikalinduzierten Strangbruch (1998)

Keinen positiven Effekt hat die Stapelung der Basen der DNA auf den Elektronentransfer. Dies folgt aus Experimenten mit einem neuen DNA-Testsystem, bei dem ein durch Strangbruch erzeugtes Radikalkation von Guaninbasen in derselben DNA reduziert werden kann (der Elektronentransfer ist in der schematischen Abbildung rechts durch Pfeile symbolisiert). Die Distanzabhängigkeit dieses Elektronentransfers wurde aus den chemischen Ausbeuten des Reduktionsproduktes bestimmt.
Clonal hematopoiesis in men living with HIV and association with subclinical atherosclerosis (2022)

Clonal hematopoiesis was more common in PWH and among PWH was associated with the extent of coronary artery disease. Larger studies are needed to further examine the biological and clinical consequences of clonal hematopoiesis in PWH.
Object-based rate allocation with spatio-temporal trade-offs (2002)

This paper describes a bit allocation algorithm that can achieve a constant bit rate when coding multiple video objects (MVOs), while improving the rate-distortion (R-D) performance over the reference method for MPEG-4 object-based rate control. In object-based coding, bit allocation is performed at the object level and temporal rates of different objects may vary. The proposed algorithm in this paper deals with these two issues. We pay particular attention to maintenance of buffer occupancy levels and propose a new method for spatio-temporal trades-offs for object-based coding. In order to improve the coding efficiency, we also consider several new R-D coding modes. These modes are available at the encoder to determine the best R-D performance under different coding conditions and are chosen automatically. Simulation results demonstrate moderate improvements at low and high bit rates. One important key aspect of the proposed algorithm is that the actual coded bits in the proposed algorithm are similar to the target bits over a wide range of bit rates. Consequently, the proposed algorithm has not experienced the buffer overflow/underflow over the entire range of bit rates.
Surface-wave suppression band gap and plane-wave reflection phase band of mushroomlike photonic band gap structures (2008)

Mushroomlike photonic band gap (PBG) structures exhibit two band gap characteristics: surface-wave suppression and in-phase reflectivity. The fundamental electromagnetic properties and the relationship between the surface-wave suppression band gap and the plane-wave reflection phase band are investigated and clarified by a finite-element full-wave analysis. The results of the plane-wave bistatic reflection experiments on mushroomlike PBG plates in an anechoic chamber are in good agreement with those of numerical simulation, confirming the phenomenon of dual in-phase reflection, i.e., dual-resonant behavior, for a transverse magnetic polarization plane wave at oblique incidence on a mushroomlike PBG surface. A modified local resonance cavity cell model of a PBG structure is presented to provide insight into the physical mechanism of dual-resonant behavior.
Metastabiles Salpetersäuretrihydrat in Eiswolken (2016)

Abstract Die Zusammensetzung von hochliegenden Eiswolken ist ein intensiv diskutierter Gegenstand der aktuellen Forschung. Die Bildungsmechanismen und die genaue Phasenzusammensetzung sind, nicht zuletzt aufgrund der schwierigen Zugänglichkeit, noch nicht endgültig aufgeklärt. Hier wird eine lange vermutete, aber strukturell unbekannte Phase vorgestellt. Diese Phase ist alpha‐Salpetersäuretrihydrat (alpha‐NAT), eine metastabile Phase von NAT. Mittels Röntgen‐ und Neutronendiffraktionsexperimenten wurde die Phase analysiert und daraus eine schlüssige Struktur abgeleitet. Schwingungsspektren wurden aufgenommen und mit theoretischen Berechnungen verglichen. Es konnte eine starke Interaktion zwischen Eis und alpha‐NAT beobachtet werden, was die experimentellen Spektren und die Kinetik beim Phasenübergang erklärt. Auf Grundlage der ermittelten Ergebnisse wird ein dreistufiger Prozess zur Bildung von NAT in stratosphärischen Wolken vorgeschlagen.
Indoloazepinone‐Constrained Oligomers as Cell‐Penetrating and Blood–Brain‐Barrier‐Permeating Compounds (2018)

Non-cationic and amphipathic indoloazepinone-constrained (Aia) oligomers have been synthesized as new vectors for intracellular delivery. The conformational preferences of the [l-Aia-Xxx]<sub>n</sub> oligomers were investigated by circular dichroism (CD) and NMR spectroscopy. Whereas Boc-[l-Aia-Gly]<sub>2,4</sub> -OBn oligomers 12 and 13 and Boc-[l-Aia-β<sup>3</sup> -h-l-Ala]<sub>2,4</sub> -OBn oligomers 16 and 17 were totally or partially disordered, Boc-[l-Aia-l-Ala]<sub>2</sub> -OBn (14) induced a typical turn stabilized by C<sub>5</sub> - and C<sub>7</sub> -membered H-bond pseudo-cycles and aromatic interactions. Boc-[l-Aia-l-Ala]<sub>4</sub> -OBn (15) exhibited a unique structure with remarkable T-shaped π-stacking interactions involving the indole rings of the four l-Aia residues forming a dense hydrophobic cluster. All of the proposed FITC-6-Ahx-[l-Aia-Xxx]<sub>4</sub> -NH<sub>2</sub> oligomers 19-23, with the exception of FITC-6-Ahx-[l-Aia-Gly]<sub>4</sub> -NH<sub>2</sub> (18), were internalized by MDA-MB-231 cells with higher efficiency than the positive references penetratin and Arg<sub>8</sub> . In parallel, the compounds of this series were successfully explored in an in vitro blood-brain barrier (BBB) permeation assay. Although no passive diffusion permeability was observed for any of the tested Ac-[l-Aia-Xxx]<sub>4</sub> -NH<sub>2</sub> oligomers in the PAMPA model, Ac-[l-Aia-l-Arg]<sub>4</sub> -NH<sub>2</sub> (26) showed significant permeation in the in vitro cell-based human model of the BBB, suggesting an active mechanism of cell penetration.
Spectral characteristics of the excimer XeCl in the wavelength range 300–311 nm (1987)

An experimental investigation was made of the spontaneous luminescence spectrum of XeCl* in the wavelength range 300<λ<311 nm. A calculation of the luminescence spectrum due to the B→X transition was in satisfactory agreement with the experiments and made it possible to reconstruct the distribution of the XeCl* (B) molecules over the vibrational levels. A calculation of the permittivity of the active medium within the gain band enabled an estimate to be made of the increase in the divergence of the light beam resulting from resonant dispersion.
1.5× Energy-Efficient and 1.4× Operation-Speed Via-Switch FPGA with Rapid and Low-Cost ASIC Migration by Via-Switch Copy (2020)

1.5x energy-efficient and 1.4x operation-speed, nonvolatile via-switch (VS) FPGA with atom switch and a-Si/SiN/a-Si varistor is demonstrated in a 65nm-node for various basic applications. For rapid and low-cost migration from VS-FPGA to ASIC, “hard-via” to replace VS with “ON”, named VS-copy (VSC), is newly proposed. The VSC-ASIC is fabricated by sharing all the photo masks with VS-FPGA excepting one via mask revise and three VS masks skip, realizing an exact design copy with minimum NRE cost and TAT. The VS-FPGA equipped with the VSC gives energy-efficient edge device, e.g., for up-to-date AI inference algorithms, covering a wide range of chip volume with extremely low cost.
ProDisc-C Total Disc Replacement Versus Anterior Cervical Discectomy and Fusion for Single-Level Symptomatic Cervical Disc Disease (2015)

Therapeutic Level I. See Instructions for Authors for a complete description of levels of evidence.
Extracting Energy Band Offsets on Long-Channel Thin Silicon-on-Insulator MOSFETs (2009)

Structural quantum confinement in long-channel thin silicon-on-insulator MOSFETs has been quantified using the temperature dependence of the subthreshold current. The results were compared with the shifts in the threshold voltage. Data were obtained from simulations after initial verification with experimental data. This study demonstrates that, with the temperature dependence of the subthreshold current, shifts in the valence and conduction band edge can be extracted distinctively from changes in mobility and density of states (DOS), making this method more accurate in assessing the impact of structural quantum confinement than the commonly used threshold voltage method. Furthermore, we show that, with additional <i xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">C</i> - <i xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">V</i> data, a possible change in mobility and DOS can be disentangled.
ChemInform Abstract: Fluorine‐Directed Nazarov Cyclizations. Part 2. Regioselective Synthesis of 5‐Trifluoromethyl‐2‐cyclopentenones. (1998)

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.
Synthetic Antimicrobial Peptide Tuning Permits Membrane Disruption and Interpeptide Synergy (2020)

The ribosomally produced antimicrobial peptides of bacteria (bacteriocins) represent an unexplored source of membrane-active antibiotics. We designed a library of linear peptides from a circular bacteriocin and show that pore-formation dynamics in bacterial membranes are tunable via selective amino acid substitution. We observed antibacterial interpeptide synergy indicating that fundamentally altering interactions with the membrane enables synergy. Our findings suggest an approach for engineering pore-formation through rational peptide design and increasing the utility of novel antimicrobial peptides by exploiting synergy.
Sulfonated Thermoresponsive Injectable Gel for Sequential Release of Therapeutic Proteins to Protect Cardiac Function after Myocardial Infarction (2022)

Myocardial infarction causes cardiomyocyte death and persistent inflammatory responses, which generate adverse pathological remodeling. Delivering therapeutic proteins from injectable materials in a controlled-release manner may present an effective biomedical approach for treating this disease. A thermoresponsive injectable gel composed of chitosan, conjugated with poly(<i>N</i>-isopropylacrylamide) and sulfonate groups, was developed for spatiotemporal protein delivery to protect cardiac function after myocardial infarction. The thermoresponsive gel delivered vascular endothelial growth factor (VEGF), interleukin-10 (IL-10), and platelet-derived growth factor (PDGF) in a sequential and sustained manner <i>in vitro</i>. An acute myocardial infarction mouse model was used to evaluate polymer biocompatibility and to determine therapeutic effects from the delivery system on cardiac function. Immunohistochemistry showed biocompatibility of the hydrogel, while the controlled delivery of the proteins reduced macrophage infiltration and increased vascularization. Echocardiography showed an improvement in ejection fraction and fractional shortening after injecting the thermal gel and proteins. A factorial design of experimental study was implemented to optimize the delivery system for the best combination and doses of proteins for further increasing stable vascularization and reducing inflammation using a subcutaneous injection mouse model. The results showed that VEGF, IL-10, and FGF-2 demonstrated significant contributions toward promoting long-term vascularization, while PDGF's effect was minimal.
Supplementary Figure 1 from Identification of the <i>IFITM</i> Family as a New Molecular Marker in Human Colorectal Tumors (2023)

Supplementary Figure 1 from Identification of the &lt;i&gt;IFITM&lt;/i&gt; Family as a New Molecular Marker in Human Colorectal Tumors
Models for the Subjective Effects of Loss, Noise, and Talker Echo on Telephone Connections (1976)

Tests have been conducted at Bell Laboratories within the last 10 years to obtain subjective evaluations of the effects of loss, noise, and talker echo on telephone transmission quality. We use these subjective test results to formulate graphical and analytical models of subjective opinion that can be used in network planning studies to evaluate transmission performance of the network and to study the effects of network changes on performance. These models are based on the concept of a generalized transmission-rating scale. Separate opinion curves for each test take into account differences caused by factors such as subject group, type of test, and range of conditions. We also describe the methods of data analysis used in the formulation of the transmission-rating scale and opinion models, provide a comparison of the test results with the models, and discuss the models in sufficient detail to permit their application in transmission planning studies.
Synergistically Enhanced Osteogenic Differentiation of Human Mesenchymal Stem Cells by Culture on Nanostructured Surfaces with Induction Media (2010)

We have examined the effects of surface nanotopography on in vitro osteogenesis of human mesenchymal stem cells (hMSCs). UV-assisted capillary force lithography was employed to fabricate a scalable (4x5 cm), well-defined nanostructured substrate of a UV curable polyurethane polymer with dots (150, 400, 600 nm diameter) and lines (150, 400, 600 nm width). The influence of osteogenic differentiation of hMSCs was characterized at day 8 by alkaline phosphatase (ALP) assay, RT-PCR, and real-time PCR analysis. We found that hMSCs cultured on the nanostructured surfaces in osteogenic induction media showed significantly higher ALP activity compared to unpatterned PUA surface (control group). In particular, the hMSCs on the 400 nm dot pattern showed the highest level of ALP activity. Further investigation with real-time quantitative RT-PCR analysis demonstrated significantly higher expression of core binding factor 1 (Cbfa1), osteopontin (OP), and osteocalcin (OC) levels in hMSCs cultured on the 400 nm dot pattern in osteogenic induction media. These findings suggest that surface nanotopography can enhance osteogenic differentiation synergistically with biochemical induction substance.
Supplementary figure 1 legend from Efficacy of Anti-mesothelin Immunotoxin RG7787 plus Nab-Paclitaxel against Mesothelioma Patient–Derived Xenografts and Mesothelin as a Biomarker of Tumor Response (2023)

&lt;p&gt;Semiquantitative assessment of mesothelin expression using H-score in mesothelioma patient derived xenografts. (A) NCI-Meso16: tumor with areas of strong membrane staining and intermingling of negative areas (H-score 230). (B) NCI-Meso21: tumor shows only focal membrane positivity (H-score 50). (C) NCI-Meso29: tumor shows nearly uniform strong membrane positivity (H-score 290). Original magnification 400x.&lt;/p&gt;
Endothelial Cell Metabolism (2017)

Endothelial cells (ECs) are more than inert blood vessel lining material. Instead, they are active players in the formation of new blood vessels (angiogenesis) both in health and (life-threatening) diseases. Recently, a new concept arose by which EC metabolism drives angiogenesis in parallel to well-established angiogenic growth factors (e.g., vascular endothelial growth factor). 6-Phosphofructo-2-kinase/fructose-2,6-bisphosphatase-3-driven glycolysis generates energy to sustain competitive behavior of the ECs at the tip of a growing vessel sprout, whereas carnitine palmitoyltransferase 1a-controlled fatty acid oxidation regulates nucleotide synthesis and proliferation of ECs in the stalk of the sprout. To maintain vascular homeostasis, ECs rely on an intricate metabolic wiring characterized by intracellular compartmentalization, use metabolites for epigenetic regulation of EC subtype differentiation, crosstalk through metabolite release with other cell types, and exhibit EC subtype-specific metabolic traits. Importantly, maladaptation of EC metabolism contributes to vascular disorders, through EC dysfunction or excess angiogenesis, and presents new opportunities for anti-angiogenic strategies. Here we provide a comprehensive overview of established as well as newly uncovered aspects of EC metabolism.
Un sistema distribuito per la misura di transitori veloci di tensione (2008)

I transitori di tensione e i loro effetti sono la principale causa di lamentela da parte degli utenti con fornitura in media tensione ed è pertanto naturale che sia le aziende distributrici che le Autorità stiano rivolgendo il proprio interesse a tecniche di misura capaci di fornire informazioni utili a localizzare tali fenomeni e classificarli in base alla loro origine. Sebbene l’attenzione sia spesso concentrata sui buchi di tensione, anche i transitori veloci, quali quelli determinati da fulminazioni o da guasti, vengono adesso trattati con interesse sempre crescente. Alla luce di tali considerazioni, questo lavoro riassume le caratteristiche di un sistema distribuito per la misura di transitori veloci di tensione. Tale sistema, progettato per soddisfare particolari specifiche sull’affidabilità dei risultati forniti, è stato impiegato in una campagna di misura, durata circa un anno, in una rete di media tensione
Principles of conjugating quantum dots to proteins via carbodiimide chemistry (2011)

The covalent coupling of nanomaterials to bio-recognition molecules is a critical intermediate step in using nanomaterials for biology and medicine. Here we investigate the carbodiimide-mediated conjugation of fluorescent quantum dots to different proteins (e.g., immunoglobulin G, bovine serum albumin, and horseradish peroxidase). To enable these studies, we developed a simple method to isolate quantum dot bioconjugates from unconjugated quantum dots. The results show that the reactant concentrations and protein type will impact the overall number of proteins conjugated onto the surfaces of the quantum dots, homogeneity of the protein-quantum dot conjugate population, quantum efficiency, binding avidity, and enzymatic kinetics. We propose general principles that should be followed for the successful coupling of proteins to quantum dots.
Design of HIFU CMUT Arrays for Treatment of Liver and Renal Cancer (2007)

We present the development of a capacitive micromachined ultrasonic transducer (CMUT) array for noninvasive focused ultrasound ablation of lower abdominal cancers under MR‐guidance. While piezoelectric transducers have been traditionally used for HIFU, recent advances in CMUT design have made them highly competitive. Not only are CMUTs cost effective, they allow fabrication flexibility and advantages in efficiency and bandwidth. Current imaging CMUTs have shown capability of HIFU operation through high power and continuous wave operation. In this paper, we will present the development of CMUT membranes designed specifically for HIFU. These membranes are piston‐like membranes fabricated by placing a thick layer of silicon or gold at the center of the membrane. The width of the piston layer is usually 60–85% of the membrane width and allows the membrane mass and elasticity to be controlled independently. It also increases the average displacement and average output pressure of the membrane. We patterned these CMUT membranes into an 8 element, 3.5 cm concentric array. We simulated the heating patterns of this array to show it is capable of producing lesions of 5 mm in diameter within 20–30 seconds, which can be imaged using our MR detection software.
Small PWR Using Coated Particle Fuel of Thorium and Plutonium (2007)

An innovative concept of PFPWR50 for district heating has been studied, which is a small PWR of 50 MWt capability using coated particle fuels with conventional zircaloy cladding.This concept takes advantages of fuel integrity against fission products release of coated particle fuels and a high reliability of PWR technology based on the long history of a successful operation.We have investigated burnup characteristics of fuel rods, assemblies, and reactor cores by the calculation code SRAC95 in order to establish a core concept of long life without on-site refueling.The loading pattern of assemblies with various concentrations of burnable poison is optimized to obtain a flat excess reactivity during the core life in order to eliminate a soluble boron control system.The core life of a cycle is about 8.9 equivalent full power years.And we have also studied the applicability of SiC/SiC composite cladding in place of zircaloy cladding, which is now under development for gas cooled fast reactor fuels.It could be applicable to high burnup fuel rods for a long term operation.From the calculation results, it is found out that the burnup characteristics do not change significantly with SiC cladding and contribute to elongate the core life to 9.2 equivalent full power years.
Design and implementation of the POWER5/spl trade/ microprocessor (2004)

POWER5 offers /spl sim/4/spl times/ performance over the previous design by incorporating simultaneous multithreading, a latency-optimized memory subsystem, extensive reliability, availability and serviceability (RAS), and power management support. The 276M-transistor processor is implemented in a 0.13 /spl mu/m, 8M silicon-on-insulator technology and operates above 1.5 GHz.