gebhart/patrepeval huggingface dataset:
3-(16.beta.-17.beta.-Dihydroxy-3-oxoandrost-4-en-17.alpha.-yl)propionic acid .gamma.-lactone, its preparation and antimineralocorticoid activity (1973)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXT3-(16.beta.-17.beta.-Dihydroxy-3-oxoandrost-4-en-17.alpha.-yl)propionic acid .gamma.-lactone, its preparation and antimineralocorticoid activityLeland J. Chinn and Lorenz M. HofmannCite this: J. Med. Chem. 1973, 16, 7, 839–843Publication Date (Print):July 1, 1973Publication History Published online1 May 2002Published inissue 1 July 1973https://pubs.acs.org/doi/10.1021/jm00265a021https://doi.org/10.1021/jm00265a021research-articleACS PublicationsRequest reuse permissionsArticle Views57Altmetric-Citations7LEARN ABOUT THESE METRICSArticle Views are the COUNTER-compliant sum of full text article downloads since November 2008 (both PDF and HTML) across all institutions and individuals. These metrics are regularly updated to reflect usage leading up to the last few days.Citations are the number of other articles citing this article, calculated by Crossref and updated daily. Find more information about Crossref citation counts.The Altmetric Attention Score is a quantitative measure of the attention that a research article has received online. Clicking on the donut icon will load a page at altmetric.com with additional details about the score and the social media presence for the given article. Find more information on the Altmetric Attention Score and how the score is calculated. Share Add toView InAdd Full Text with ReferenceAdd Description ExportRISCitationCitation and abstractCitation and referencesMore Options Share onFacebookTwitterWechatLinked InRedditEmail Other access optionsGet e-Alertsclose Get e-Alerts
Development of potent autophagy inhibitors that sensitize oncogenic BRAF V600E mutant melanoma tumor cells to vemurafenib (2014)

Autophagy is a dynamic cell survival mechanism by which a double-membrane vesicle, or autophagosome, sequesters portions of the cytosol for delivery to the lysosome for recycling. This process can be inhibited using the antimalarial agent chloroquine (CQ), which impairs lysosomal function and prevents autophagosome turnover. Despite its activity, CQ is a relatively inadequate inhibitor that requires high concentrations to disrupt autophagy, highlighting the need for improved small molecules. To address this, we screened a panel of antimalarial agents for autophagy inhibition and chemically synthesized a novel series of acridine and tetrahydroacridine derivatives. Structure-activity relationship studies of the acridine ring led to the discovery of VATG-027 as a potent autophagy inhibitor with a high cytotoxicity profile. In contrast, the tetrahydroacridine VATG-032 showed remarkably little cytotoxicity while still maintaining autophagy inhibition activity, suggesting that both compounds act as autophagy inhibitors with differential effects on cell viability. Further, knockdown of autophagy-related genes showed no effect on cell viability, demonstrating that the ability to inhibit autophagy is separate from the compound cytotoxicity profiles. Next, we determined that both inhibitors function through lysosomal deacidification mechanisms and ultimately disrupt autophagosome turnover. To evaluate the genetic context in which these lysosomotropic inhibitors may be effective, they were tested in patient-derived melanoma cell lines driven by oncogenic BRAF (v-raf murine sarcoma viral oncogene homolog B). We discovered that both inhibitors sensitized melanoma cells to the BRAF V600E inhibitor vemurafenib. Overall, these autophagy inhibitors provide a means to effectively block autophagy and have the potential to sensitize mutant BRAF melanomas to first-line therapies.
Selective Cancer Therapy by Extracellular Activation of a Highly Potent Glycosidic Duocarmycin Analogue (2013)

Conventional cancer chemotherapy is limited by systemic toxicity and poor selectivity. Tumor-selective activation of glucuronide prodrugs by beta-glucuronidase in the tumor microenvironment in a monotherapeutic approach is one promising way to increase cancer selectivity. Here we examined the cellular requirement for enzymatic activation as well as the in vivo toxicity and antitumor activity of a glucuronide prodrug of a potent duocarmycin analogue that is active at low picomolar concentrations. Prodrug activation by intracellular and extracellular beta-glucuronidase was investigated by measuring prodrug 2 cytotoxicity against human cancer cell lines that displayed different endogenous levels of beta-glucuronidase, as well as against beta-glucuronidase-deficient fibroblasts and newly established beta-glucuronidase knockdown cancer lines. In all cases, glucuronide prodrug 2 was 1000-5000 times less cytotoxic than the parent duocarmycin analogue regardless of intracellular levels of beta-glucuronidase. By contrast, cancer cells that displayed tethered beta-glucuronidase on their plasma membrane were 80-fold more sensitive to glucuronide prodrug 2, demonstrating that prodrug activation depended primarily on extracellular rather than intracellular beta-glucuronidase activity. Glucuronide prodrug 2 (2.5 mg/kg) displayed greater antitumor activity and less systemic toxicity in vivo than the clinically used drug carboplatin (50 mg/kg) to mice bearing human lung cancer xenografts. Intratumoral injection of an adenoviral vector expressing membrane-tethered beta-glucuronidase dramatically enhanced the in vivo antitumor activity of prodrug 2. Our data provide evidence that increasing extracellular beta-glucuronidase activity in the tumor microenvironment can boost the therapeutic index of a highly potent glucuronide prodrug.
Ion pair partition chromatography of organic ammonium compounds (1973)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTIon pair partition chromatography of organic ammonium compoundsStaffan. Eksborg and Goran. SchillCite this: Anal. Chem. 1973, 45, 12, 2092–2100Publication Date (Print):October 1, 1973Publication History Published online1 May 2002Published inissue 1 October 1973https://pubs.acs.org/doi/10.1021/ac60334a019https://doi.org/10.1021/ac60334a019research-articleACS PublicationsRequest reuse permissionsArticle Views235Altmetric-Citations119LEARN ABOUT THESE METRICSArticle Views are the COUNTER-compliant sum of full text article downloads since November 2008 (both PDF and HTML) across all institutions and individuals. These metrics are regularly updated to reflect usage leading up to the last few days.Citations are the number of other articles citing this article, calculated by Crossref and updated daily. Find more information about Crossref citation counts.The Altmetric Attention Score is a quantitative measure of the attention that a research article has received online. Clicking on the donut icon will load a page at altmetric.com with additional details about the score and the social media presence for the given article. Find more information on the Altmetric Attention Score and how the score is calculated. Share Add toView InAdd Full Text with ReferenceAdd Description ExportRISCitationCitation and abstractCitation and referencesMore Options Share onFacebookTwitterWechatLinked InRedditEmail Other access optionsGet e-Alertsclose Get e-Alerts
Formation of semi-insulating 6H-SiC layers by vanadium ion implantations (1996)

Vanadium ion (V+) implantation has been successfully applied to the formation of semiinsulating 6H-SiC layers. The resistivity of V+-implanted layers strongly depended on the conduction type of initial 6H-SiC crystals. The resistivity at room temperature exceeded 1012 Ω cm and 106 Ω cm for p- and n-type samples, respectively. Compensation mechanism is discussed based on the temperature dependence of resistivity. This technique will be useful for device isolation, edge termination, and reduction of parasitic impedance of SiC devices.
INSTRUMENTATION FOR MOISTURE MEASUREMENT-BASES, SUBGRADES, AND EARTH MATERIALS (SENSOR EVALUATION) (1979)

Two types of moisture sensors for long term in situ monitoring of moisture in highway subgrade soils have been developed and field tested. One sensor is based on the relationship between the soil moisture and the dielectric constant of the soil which affects the capacitance as sensed by a pair of embedded electrodes. The other sensor is based on the nuclear magnetic resonance of hydrogen of the water molecules in the soil. Results of the evaluation program show that the tested sensors are capable of determining soil moisture content in the range of 20% to 30% with an accuracy in the field of plus or minus 2% over dray moisture content and a precision of plus or minus 2% oven dry moisture content. The sensors were evaluated in the field for over a year under in-service highways in Arizona and Pennsylvania, and under a test road at the U.S. Army Cold Regions Research Laboratory in New Hampshire. Periodic comparisons were made among the sensor readings and results of other moisture measurements including nuclear probe and gravimetric analysis of borings. Although some discrepancies were observed among the field results, and the field tests were not conclusive, the data obtained with the newly developed sensors appear to be consistent with the indicated moisture conditions. (Author)
A novel compact 35 A/150 ps current pulse generator for a new generation of the laser radars (2002)

A current pulse generator is presented which allows a 35 A current amplitude with a rise time of 150 ps to be achieved across a low-ohmic load. The generator is based on an avalanche transistor matrix with intrinsic switching synchronisation. The front of the pulse is further sharpened by employing sub-nanosecond diode recovery in the first stage and super-fast switching of another diode under pulsed reverse biasing in the second stage. An application of this current pulse for the feeding of a high-power gain-switched semiconductor laser is demonstrated.
[1,4]Benzoxazine-2,3-diones as antiallergic agents (1985)

The synthesis of a series of [1,4]benzoxazine-2,3-diones and a new class of compounds, benzobisoxazinetetrones, is described. These compounds were evaluated for their effect in the rat mast cell (RMC) test passively sensitized in vitro with rat antiovalbumin serum and for their effect in inhibitory passive cutaneous anaphylaxis (PCA) in the rat. Some of these compounds are of the same potency level as disodium cromglycate in the RMC test and some are effective orally in PCA.
Microstructure and properties of high alumina castables containing calcium alumino‐titanate (2018)

Abstract Calcium alumino‐titanate ( CAT )‐containing high alumina castables were prepared using bauxite, CAT , and α‐Al 2 O 3 as starting materials, and subsequently heat treated at various temperatures ranging from 1400°C to 1600°C. The thermo‐mechanical properties of the specimens as a function of the temperature were characterized in terms of linear shrinkage, bulk density, apparent porosity, cold crushing strength ( CCS ), modulus of rupture ( MOR ), residual ratio of MOR , and coefficient of thermal expansion ( CTE ). X‐ray diffraction ( XRD ) and scanning electron microscopy ( SEM ) were used to determine the phase composition and microstructural evolution, respectively. Sintering at temperatures between 1450 and 1500°C promoted normal grain growth, with the formation of a granular surface contact, and abnormal grain growth occurred at higher temperatures (≥ 1550°C). The cold strength of the specimen initially increased and subsequently decreased with temperature, whereas the residual ratio of MOR initially decreased with increasing temperature to 1550°C, then increased above 1550°C. In addition, the CTE of the specimen was only minimally influenced by the firing temperature.
Resource Management in Fog-Enhanced Radio Access Network to Support Real-Time Vehicular Services (2017)

With advances in the information and communication technology (ICT), connected vehicles are one of the key enablers to unleash intelligent transportation systems (ITS). On the other hand, the envisioned massive number of connected vehicles raises the need for powerful communication and computation capabilities. As an emerging technique, fog computing is expected to be integrated with existing communication infrastructures, giving rise to a concept of fog-enhanced radio access networks (FeRANs). Such architecture brings computation capabilities closer to vehicular users, thereby reducing communication latency to access services, while making users capable of sharing local environment information for advanced vehicular services. In the FeRANs service migration, where the service is migrated from a source fog node to a target fog node following the vehicle's moving trace, it is necessary for users to access service as close as possible in order to maintain the service continuity and satisfy stringent latency requirements of real-time services. Fog servers, however, need to have sufficient computational resources available to support such migration. Indeed, a fog node typically has limited resources and hence can easily become overloaded when a large number of user requests arrive, e.g., during peak traffic, resulting in degraded performance. This paper addresses resource management in FeRANs with a focus on management strategies at each individual fog node to improve quality of service (QoS), particularly for real-time vehicular services. To this end, the paper proposes two resource management schemes, namely fog resource reservation and fog resource reallocation. In both schemes, real-time vehicular services are prioritized over other services so that their respective vehicular users can access the services with only one hop. Simulation results show that the proposed schemes can effectively improve one-hop access probability for real-time vehicular services implying low delay performance, even when the fog resource is under heavy load.
A new education model in sustainable energy (2018)

The European Institute for Innovation and Technology (EIT) has selected knowledge and innovation community (KIC) InnoEnergy as the leading engine for innovation and entrepreneurship in sustainable energy in Europe. Since 2010, KIC InnoEnergy Master School has offered Master's degree programs, which are directed at a new type of education in the energy field, aimed at mobilising the innovative and entrepreneurial spirit of the students. Seven Master's programs, accredited by top technical universities in Europe, offer a combination of engineering and entrepreneurship courses. This paper describes a new mechanism for the development of a teaching environment, which creates strong links between education, technology, business and entrepreneurship. The paper also emphasises the main distinguishing features of KIC InnoEnergy education and gives examples of the application of new pedagogical methods.
Preparation of amphiphilic polyisobutylenes‐b‐polyethylenamines by mannich reaction. II. Study of mannich reaction on model systems (1993)

Abstract The study of the reactions which take place when α‐methyl‐ω‐phenolpolyisobutylene is polycondensed with triethylenetetramine (TETA) and para ‐formaldehyde (Mannich condensation) is carried out on model systems including monofunctional [2,4‐di‐ tert ‐butylphenol ( A ), dibutylamine ( B ), and dodecylamine ( B ′)] and difunctional reactants [4‐ tert ‐butylphenol ( A ′) and 1,6‐hexamethylenediamine ( B ″)]. With the exception of the A + B system which gives only Mannich condensation, all the systems including at least one difunctional reactant are characterized by side reactions which accompany the Mannich condensation. However, when one of the compounds is monofunctional ( A + B ;′ A ′ + B ′) only nonpolymeric molecules are formed; their structures were determined by 1 H‐ and 13 C‐NMR spectroscopy. On the other hand, when both reactants are bifunctional ( A ′ + B ; A ′ + TETA) polymers are formed whose monomer units were identified by comparison of their spectra with those of the nonpolymeric molecules. © 1993 John Wiley & Sons, Inc.
Identification of Lipid Aggregate Structures on TiO<sub>2</sub> Surface Using Headgroup IR Bands (2005)

Attenuated total reflection-Fourier transform infrared (ATR-FTIR) spectroscopy was used to study the nature of the dipalmitoylphosphatidylcholine (DPPC) aggregated structures adsorbed on TiO(2). DPPC molecules were assembled on TiO(2) using Langmuir-Blodgett (LB) deposition methods or by directly flowing the DPPC liposome solution across the TiO(2)-coated ATR crystal. We found that there is a direct correlation between the intensity and frequency position of the zwitterionic headgroup IR bands and the nature of LB films. Specifically, we have shown that the bands due to PO(2)(-) modes are sensitive to changes in the degree of hydration of the LB films and that the symmetric deformation vibrational mode (delta(s) (+)N-CH(3)) is sensitive to interaction with oppositely charged surface sites. Using this information, we found that the liposomes adsorbed on TiO(2) remain intact as vesicles and that the vesicles are stable and not removed in flowing water. We have also shown that the antisymmetric deformation vibrational (delta(as) (+)N-CH(3)) modes are sensitive to changes in lateral-lateral DPPC interactions. This information was used to show that there is a lateral interaction between each positively charged (+)N(CH(3))(3) headgroup and negatively charged PO(2)(-) headgroup of the adjacent DPPC molecule in the adsorbed vesicles and LB films. This study provides a framework for the use of this IR technique in studies of adsorption and transport of molecules across membrane interfaces.
Teaching the nations how to play: sport and society in the British empire and commonwealth (1989)

(1989). Teaching the nations how to play: sport and society in the British empire and commonwealth. The International Journal of the History of Sport: Vol. 6, No. 2, pp. 145-155.
Recent developments in molecular beam epitaxy (MBE) (1979)

Semiconductor material research is motivated by the need for new devices which may improve the performance of a system. In turn, a new material technology may generate new devices and new technology. Molecular beam epitaxy (MBE) is a high-vacuum technique for the growth of epitaxial layers, usually semiconductors, that utilizes thermal beams of source atoms or molecules impinging on a single-crystal substrate. The ultrahigh vacuum nature of the process permits in situ metallization and growth of insulating materials on freshly grown semiconducting surfaces resulting in contamination-free interfaces. In situ Schottky barriers, nonalloyed ohmic contacts, and high-quality MIS structures have been grown with MBE. In addition, shadow masking techniques have been used to produce three-dimensional epitaxial structures on the substrate for possible monolithically integrated optical devices and patterned amorphous coatings have permitted the growth of isolated conducting islands of GaAs within a semi-insulating ’’sea’’. Ultrathin layered structures and superlattice structures have been grown and recently modulated doping of superlattice structures has yielded increased mobility anisotropic semiconductor material. This review is limited to recent developments in MBE of III–V compound and an extensive reference list is also included.
Positioning with punctured GPS (2008)

We examine reasons for interrupting the data stream from a GPS receiver integrated into a mobile phone, and the effects such interruptions have on the pseudorange and pseudorange rate determined by the receiver in tracking mode. We present measurements of the multi-path environment inside an office at the Cavendish Laboratory, UK, and find that interruptions of several tens of seconds can be tolerated without serious impact on the positioning performance. This conclusion, if supported by measurements made in other environments typical of mobile-phone use, bodes well for the integration of GNSS receivers within mobile phones suitable for the mass market.
Using simulated annealing to design good codes (1987)

Simulated annealing is a computational heuristic for obtaining approximate solutions to combinatorial optimization problems. It is used to construct good source codes, error-correcting codes, and spherical codes. For certain sets of parameters codes that are better than any other known in the literature are found.
Cybersecurity Strategies: The QuERIES Methodology (2008)

QuERIES offers a novel multidisciplinary approach to quantifying risk associated with security technologies resulting in investment-efficient cybersecurity strategies. R esearchers can use the QuERIES methodology to rigorously determine, for the first time, appropriate investment levels and strategies for the protection of intellectual property in complex systems. As a result, it can have a significant and immediate impact on the protection of critical IP, including weapons systems and chip designs, complex computer software, and databases containing personal and financial information. In this paper, initial testing of QuERIES in small-scale, realistic scenarios, were performed with results that suggest the methodology can significantly improve risk assessments in complex systems under attack by rational and capable adversaries. Such systems include software, hardware, and data critical to national security and industrial competitiveness. Consequently, it is believed that QuERIES has wide applicability within both the DoD and private sectors.
Modeling Pressure-Transient Behavior of Sectionally Homogeneous Reservoirs by the Boundary-Element Method (1993)

Summary Pressure-transient solution in a piecewise homogeneous reservoir with arbitrary geometry of each region is proposed by the Laplace domain boundary-element method (BEM). Any number of such regions with different rock and fluid properties can be included in the solution procedure. This formulation can solve for impermeable barriers of any shape, size, and orientation, including large pressure-support sources (aquifers) and fluid-injection problems that show composite behavior. Any number of line-source wells can be included. Example solutions are verified against known analytical solutions. Injection-fluid-front velocity is calculated as part of the solution; thus, the fluid fronts can be tracked in a quasistationary sense. The analytical aspects of this procedure are discussed. BEM solutions are accurate because the method retains the free-space Green's function of the governing differential operator as a global weighting function in the integral equation.
Two-mode Squeezed Gaussons (1993)

Abstract Two-mode squeezed Gaussons are non-classical states of light which are intermediate between single-mode and two-mode squeezed states. They may be prepared by coherently mixing two single-mode squeezed states at a beam-splitter or via a frequency converter. When equally squeezed single-mode squeezed states are incident on a 50/50 beam-splitter the output will range between a two-mode squeezed state and two single-mode squeezed states as the phase of the input squeezed light is varied. This behaviour is reflected when the properties of such states are investigated.
Preparation of Ultraviolet Stabilizing Polymers. I. Copolymerization of 2-Hydroxy-4-acryloyloxybenzophenone and Its Ultraviolet Stability (1967)

Abstract To obtain ultraviolet stabilizing polymers, 2-hydroxy-4-acryloyloxybenzophenone was prepared from 2,4-dihydroxybenzophenone and copolymerized with styrene. Copolymers containing three different amounts of ultraviolet absorber were prepared. These copolymers, unstabilized pure polystyrene and a series of stabilized polystyrene, were exposed to ultraviolet, and the ultraviolet stability of these polymers was compared by the relative amount of infrared absorption around 1700 cm−1 due to the carbonyl group. Ultraviolet stability of the copolymers is very similar to that of blend polymers and is higher than that of unstabilized pure polystyrene.