gebhart/patrepeval huggingface dataset:
A 20<i>S</i> Combined with a 22<i>R</i> Configuration Markedly Increases both in Vivo and in Vitro Biological Activity of 1α,25-Dihydroxy-22-methyl-2-methylene-19-norvitamin D<sub>3</sub> (2012)

Six new analogues of 1α,25-dihydroxy-19-norvitamin D(3) (3a-4b, 5, and 6) were prepared by a convergent synthesis applying the Wittig-Horner reaction as a key step. The influence of methyl groups at C-22 on their biological activity was examined. It was established that both in vitro and in vivo activity is strongly dependent on the configuration of the stereogenic centers at C-20 and C-22. Introduction of the second methyl group at C-22 (analogues 5 and 6) generates the compounds that are slightly more potent than 1α,25-(OH)(2)D(3) in the in vitro tests but much less potent in vivo. The greatest in vitro and in vivo biological activity was achieved when the C-20 is in the S configuration and the C-22 is in the R configuration. The building blocks for the synthesis, the respective (20R,22R)-, (20R,22S)-, (20S,22R)-, and (20S,22S)-diols, were obtained by fractional crystallization of mixtures of the corresponding diastereomers. Structures and absolute configurations of the diols 21a, 21b, and 22a as well as analogues 3a, 5, and 6 were confirmed by the X-ray crystallography.
Lentil-based diets attenuate hypertension and large-artery remodelling in spontaneously hypertensive rats (2013)

Hypertension is a major risk factor for CVD, the leading cause of mortality worldwide. The prevalence of hypertension is expected to continue increasing, and current pharmacological treatments cannot alleviate all the associated problems. Pulse crops have been touted as a general health food and are now being studied for their possible effects on several disease states including hypertension, obesity and diabetes. In the present study, 15-week-old spontaneously hypertensive rats (SHR) were fed diets containing 30% w/w beans, peas, lentils, chickpeas, or mixed pulses or a pulse-free control diet for 4 weeks. Normotensive Wistar-Kyoto (WKY) rats were placed on a control diet. Pulse wave velocity (PWV) was measured weekly, while blood pressure (BP) was measured at baseline and week 4. Fasting serum obtained in week 4 of the study was analysed for circulating lipids. A histological analysis was carried out on aortic sections to determine vascular geometry. Of all the pulse varieties studied, lentils were found to be able to attenuate the rise in BP in the SHR model (P< 0·05). Lentils were able to decrease the media:lumen ratio and media width of the aorta. The total cholesterol (TC), LDL-cholesterol (LDL-C) and HDL-cholesterol levels of rats fed the pulse-based diets were found to be lower when compared with those of the WKY rat and SHR controls (P< 0·05). Although all pulses reduced circulating TC and LDL-C levels in the SHR, only lentils significantly reduced the rise in BP and large-artery remodelling in the SHR, but had no effect on PWV. These results indicate that the effects of lentils on arterial remodelling and BP in the SHR are independent of circulating LDL-C levels.
Bis(Cyclic Alkyl Amino Carbene) Ruthenium Complexes: A Versatile, Highly Efficient Tool for Olefin Metathesis (2016)

Abstract The state‐of‐the‐art in olefin metathesis is application of N‐heterocyclic carbene (NHC)‐containing ruthenium alkylidenes for the formation of internal C=C bonds and of cyclic alkyl amino carbene (CAAC)‐containing ruthenium benzylidenes in the production of terminal olefins. A straightforward synthesis of bis(CAAC)Ru indenylidene complexes, which are highly effective in the formation of both terminal and internal C=C bonds at loadings as low as 1 ppm, is now reported.
Identification and Expression in <i>E. coli</i> of Novel Nitrile Hydratases from the Metagenome (2004)

Abstract A PCR‐based screening procedure using degenerate consensus primers was employed to identify nitrile hydratase (NHase) encoding genes in libraries of cloned environmental DNA. Screening of about 3 Gbp of metagenomic DNA led to the identification of twelve novel and highly diverse NHase α‐subunits, ten β‐subunits, and three NHase activator proteins. The disruption of the natural arrangement of the genes encoding the NHase subunits and a reduced temperature proved to be beneficial for the soluble expression in E. coli . Of nine NHases investigated, six were produced in an active conformation. The co‐expression of corresponding activator proteins resulted in the activation of a previously inactive enzyme and a marked increase in activity of another enzyme. Thus, the sequence‐homology based screening approach led to the identification and finally the production of novel and diverse NHase enzymes.
Diepitopic Construct of Functionally and Epitopically Complementary Peptides Enhances Immunogenicity, Reactivity with Glucosyltransferase, and Protection from Dental Caries (2001)

Coimmunization with peptide constructs from catalytic (CAT) and glucan-binding (GLU) domains of glucosyltransferase (GTF) of mutans streptococci has resulted in enhanced levels of antibody to the CAT construct and to GTF. We designed and synthesized a diepitopic construct (CAT-GLU) containing two copies of both CAT (B epitope only) and GLU (B and T epitope) peptides. The immunogenicity of this diepitopic construct was compared with that of individual CAT and GLU constructs by immunizing groups of Sprague-Dawley rats subcutaneously in the salivary gland vicinity with the CAT-GLU, CAT, or GLU construct or by treating rats by sham immunization. Levels of serum immunoglobulin G (IgG) antibody to GTF or CAT in the CAT-GLU group were significantly greater than in GLU- or CAT-immunized groups. Immunization with CAT-GLU was compared to coimmunization with a mixture of CAT and GLU in a second rodent experiment under a similar protocol. CAT-GLU immunization resulted in serum IgG and salivary IgA responses to GTF and CAT which were greater than after coimmunization. Immunization with the diepitopic construct and communization with CAT and GLU constructs showed proliferation of T lymphocytes to GTF. Immunization with either the CAT or GLU construct has been shown to elicit significant protection in a rodent dental caries model. Similarly in this study, the enhanced response to GTF after immunization with the CAT-GLU construct resulted in protective effects on dental caries. Therefore, the CAT-GLU diepitopic construct can be a potentially important antigen for a caries vaccine, giving rise to greater immune response than after immunization with CAT, GLU, or a mixture of the two.
Resistivity in Carbonates: New Insights (2002)

Abstract A detailed explanation of the non-Archie behavior of the resistivity index vs Sw curves in carbonates is proposed. The model is based on resistivity index (RI) curves measured at ambient and reservoir conditions, on double or triple porosity micritic and oolitic carbonates. We used the Fast Resistivity Index Measurement (FRIM) method to obtain accurate and continuous RI curves down to very low water saturation (5%). In general, the measured RI curves cannot be described by an Archie's law and the measurements at very low saturation are often a key observation to confirm a non-Archie behavior. A large variety of shapes is observed and the local saturation exponents can vary from 1 up to 3. These shapes can be explained qualitatively and quantitatively using two new models (DPC and TPC) in which the different porosity systems are connected together either in series or in parallel, or a combination of both. The second key feature of the models is the use of NMR and mercury injection curves to estimate the pore volume fraction of each population and the sequence of invasion of each population by oil during the primary drainage process. Hence, only two of three adjustable parameters are needed to model the experimental results. In particular, the saturation exponent of the dominant pore system can be extracted from the analysis. For field applications, we also propose a simple procedure to calibrate resistivity logs with variable saturation exponent. From the experimental results and the model, we conclude that the pore structure plays a key role. In particular, the microporosity can be responsible for the low resistivity contrast in carbonates, although it may represent less than 10% of the total pore volume. The water contained in the microporosity forms a continuous path for the current. When invaded by oil, the conductivity of the microporosity system is weakly modified.
Resource Allocation for Multihomed Scalable Video Streaming to Multiple Clients (2010)

We consider multihomed scalable video streaming, where videos are transmitted by a single server to multiple clients over heterogeneous access networks. The specific problem that we address is to determine which video packets to transmit over each network, in order to minimize a cost function of the expected video distortion at the clients. We present a network model and a video model that capture the network conditions and video characteristics, respectively. We develop an integer program for deterministic packet scheduling. We propose different cost functions in order to provide service differentiation and address fairness among users. We propose several suboptimal convex problems for randomized packet scheduling, and study their performance and complexity. We propose an algorithm that yields a good performance and is suitable for real-time applications. We conduct extensive trace-driven simulations to evaluate the proposed algorithms using real network conditions and scalable video streams. The simulation results show that the proposed algorithm: (i) outperforms the rate control algorithms defined in the Datagram Congestion Control Protocol (DCCP) by about 10 dB, (ii) results in video quality, of 4.33 dB and 1.84 dB higher than the two heuristics developed in [1], (iii) runs efficiently, up to six times faster than one of the heuristics, and (iv) indeed can provide service differentiation among users.
Nonlinear Joint Transform Processor (1990)

Abstract : A nonlinear joint transform image correlator is investigated. The Fourier transform interference intensity is threshold to provide higher correlation peak intensity and better defined correlation spot. Analytical expressions for the threshold joint power spectrum is provided. The effects of the nonlinearity at the Fourier plane on the correlation signals at the output plane is investigated. The correlation signals are determined in terms of the nonlinear characteristics of the spatial light modulator (SLM) at the Fourier plane. We show that thresholding the interference intensity results in a sum of infinite harmonic terms. Each harmonic term is envelope modulated due to the nonlinear characteristics of the device, and phase modulated by m times the phase modulation of the nonthresholded joint power spectrum. The correct phase information about the correlation signal is recovered for the first order harmonic of the threshold interference intensity. (RH)
A Novel Communication-Free Charge Controller for Electric Vehicles Using Support Vector Machines (2019)

As electric vehicles (EVs) are attaining significant attention in the auto market, efforts worldwide are being made for their cordial integration with the evolving distribution systems. While EVs are lucrative for the society, their uncontrolled charging may cause significant challenges to the power grid. Large-scale integration of EVs introduces voltage stresses in the systems causing anomaly to the customer appliances. In this paper, a novel EV charger based on nodal voltage and its sensitivity-to-load changes is proposed. The EV charging rate is adjusted using support vector machine (SVM) to avoid voltage violations to happen. Furthermore, a fair charging pattern is ensured in-between the EVs available at other charging points in the power system. The proposed controller is implemented in seven-node test secondary distribution system. Moreover, different loading conditions are used to verify the robustness of the proposed EV charge controller. Simulation results prove the efficacy of the proposed charge controller under both light and heavy loading conditions. In addition, fairness is achieved for all the EVs regardless of their charging points.
Characterization of Encapsulated Corrosion Inhibitors for Environmentally Friendly Smart Coatings (2015)

Research efforts are under way to replace current corrosion inhibitors with more environmentally friendly alternatives. However, problems with corrosion inhibition efficiency, coating compatibility and solubility have hindered the use of many of these materials as simple pigment additives.This paper will present technical details on how the Corrosion Technology Lab at NASAs Kennedy Space Center (KSC) has addressed these issues by encapsulating environmentally friendly inhibitors into organic and inorganic microparticles and microcapsules. The synthetic process for polymer particles was characterized and post-synthesis analysis was performed to determine the interactions between the inhibitors and the encapsulation material. The pH-controlled release of inhibitors from various particle formulations in aqueous base was monitored and compared to both electrochemical and salt immersion accelerated corrosion experiment. Furthermore, synergistic corrosion inhibition effects observed during the corrosion testing of several inhibitor combinations will be presented.
HPMA Copolymer–Drug Conjugates with Controlled Tumor‐Specific Drug Release (2017)

Over the past few decades, numerous polymer drug carrier systems are designed and synthesized, and their properties are evaluated. Many of these systems are based on water-soluble polymer carriers of low-molecular-weight drugs and compounds, e.g., cytostatic agents, anti-inflammatory drugs, or multidrug resistance inhibitors, all covalently bound to a carrier by a biodegradable spacer that enables controlled release of the active molecule to achieve the desired pharmacological effect. Among others, the synthetic polymer carriers based on N-(2-hydroxypropyl) methacrylamide (HPMA) copolymers are some of the most promising carriers for this purpose. This review focuses on advances in the development of HPMA copolymer carriers and their conjugates with anticancer drugs, with triggered drug activation in tumor tissue and especially in tumor cells. Specifically, this review highlights the improvements in polymer drug carrier design with respect to the structure of a spacer to influence controlled drug release and activation, and its impact on the drug pharmacokinetics, enhanced tumor uptake, cellular trafficking, and in vivo antitumor activity.
Reduced-complexity decoding for concatenated codes based on rectangular parity-check codes and turbo codes (2002)

We compare the performance of several different decoding strategies for concatenated codes based on a serial concatenation of a rectangular parity-check code (RPCC) with a turbo code. These concatenated codes are referred to as RPCC+turbo codes. RPCC+turbo codes have been shown to outperform turbo codes significantly in several scenarios (see Shea, J.M., Proc. 2001 IEEE Int. Symp. Information Theory, p.144, 2001; Shea and Wong, T.F., Proc. 2001 IEEE Military Commun. Conf., 2001). One particularly useful application is to replace a turbo code with an RPCC+turbo code based on constituent codes of smaller memory. This combination can provide comparable or better performance while also achieving a lower decoder complexity (see Shea and Wong, 2001). However, the complexity of the iterative MAP decoder for such a code is still relatively high. We compare several different decoding strategies for the RPCC+turbo code that offer various trade-offs between performance and complexity.
360 PPI Flip-Chip Mounted Active Matrix Addressable Light Emitting Diode on Silicon (LEDoS) Micro-Displays (2013)

In this paper, we describe the design and fabrication of 360 PPI flip-chip mounted active matrix (AM) addressable light emitting diode on silicon (LEDoS) micro-displays. The LEDoS micro-displays are self-emitting devices which have higher light efficiency than liquid crystal based displays (LCDs) and longer lifetime than organic light emitting diodes (OLEDs) based displays . The LEDoS micro-displays were realized by integrating monolithic LED micro-arrays and silicon-based integrated circuit using a flip-chip bonding technique. The active matrix driving scheme was designed on the silicon to provide sufficient driving current and individual controllability of each LED pixel. Red, green, blue and Ultraviolet (UV) LEDoS micro-displays with a pixel size of 50 μm and pixel pitch of 70 μm were demonstrated. With a peripheral driving board, the LEDoS micro-display panels were programmed to show representative images and animations.
PAPD5/7 Are Host Factors That Are Required for Hepatitis B Virus RNA Stabilization (2018)

RG7834 is a potent, orally bioavailable small-molecule inhibitor of hepatitis B virus (HBV) gene expression that belongs to the dihydroquinolizinone (DHQ) chemical class and uniquely blocks production of both viral DNA and antigens. In this study, we used DHQ compounds as tools in a compound-based adaptation version of the yeast three-hybrid screen to identify the cognate cellular protein targets, the non-canonical poly(A) RNA polymerase associated domain containing proteins 5 and 7 (PAPD5 and PAPD7). Interaction with RG7834 was mapped to the catalytic domains of the two cellular enzymes. The role of PAPD5 and PAPD7 in HBV replication was confirmed by oligonucleotide-mediated knockdown studies that phenocopied the result seen with RG7834-treated HBV-infected hepatocytes. The greatest effect on HBV gene expression was seen when PAPD5 and PAPD7 mRNAs were simultaneously knocked down, suggesting that the two cellular proteins play a redundant role in maintaining HBV mRNA levels. In addition, as seen previously with RG7834 treatment, PAPD5 and PAPD7 knockdown led to destabilization and degradation of HBV mRNA without impacting production of viral RNA transcripts. Conclusion: We identify PAPD5 and PAPD7 as cellular host factors required for HBV RNA stabilization and as therapeutic targets for the HBV cure.
Single-Step Deposition of Cerium-Substituted Yttrium Iron Garnet for Monolithic On-Chip Optical Isolation (2015)

Photonic integrated circuits require magneto-optical (MO) materials for making nonreciprocal devices such as isolators and circulators. The most successful MO materials are rare-earth-substituted iron garnets, but these can be challenging to grow on silicon without a seed layer, which introduces spacing loss between the waveguide and the MO cladding. A pulsed-laser deposition (PLD) method is used for making MO Ce:YIG (Ce[superscript 1]Y[superscript 2]Fe[superscript 5]O[superscript 12])/YIG (Y[superscript 3]Fe[superscript 5]O[superscript 12]) bilayer or trilayer films on different substrates, including silicon, quartz, and Gd[superscript 3]Ga[superscript 5]O[superscript 12] (GGG), in which a multilayer film is deposited in one run and then annealed. A YIG seed layer grown above the MO Ce:YIG facilitates recrystallization during ex situ rapid thermal annealing, which results in a reduced thermal budget and simplified deposition process. A monolithically integrated optical isolator was demonstrated by direct deposition of a bilayer Ce:YIG/YIG capping layer onto a silicon-on-insulator resonator. The device exhibited an insertion loss of 7.4 ± 1.8 dB and an isolation ratio of 13.0 ± 2.2 dB within the telecommunication window (λ = 1564.4 nm), which outperforms previously reported monolithic isolators.
Lipid Phase Control of DNA Delivery (2005)

Cationic lipids form nanoscale complexes (lipoplexes) with polyanionic DNA and can be utilized to deliver DNA to cells for transfection. Here we report the correlation between delivery efficiency of these DNA carriers and the mesomorphic phases they form when interacting with anionic membrane lipids. Specifically, formulations that are particularly effective DNA carriers form phases of highest negative interfacial curvature when mixed with anionic lipids, whereas less effective formulations form phases of lower curvature. Structural evolution of the carrier lipid/DNA complexes upon interaction with cellular lipids is hence suggested as a controlling factor in lipid-mediated DNA delivery. A strategy for optimizing lipofection is deduced. The behavior of a highly effective lipoplex formulation, DOTAP/DOPE, is found to conform to this "efficiency formula".
Coal dissolving process. [400-425/sup 0/C; 2000-5000 psig] (1975)

A process for dissolving subbituminous coal by heating coal in the presence of a hydrogen-donor oil, gaseous carbon monoxide, water, hydrogen, and an ammonium or alkali metal molybdate at a temperature of from about 400 to about 425/sup 0/C and at a total pressure of from about 2000 to about 5000 psig is described. (auth)
Synthesis of Novel <i>trans</i>-4-(Substituted-benzamido)-3,4-dihydro-2<i>H</i>-benzo[<i>b</i>]pyran-3-ol Derivatives as Potential Anticonvulsant Agents with a Distinctive Binding Profile (1996)

ADVERTISEMENT RETURN TO ISSUEPREVLetterNEXTSynthesis of Novel trans-4-(Substituted-benzamido)-3,4-dihydro-2H-benzo[b]pyran-3-ol Derivatives as Potential Anticonvulsant Agents with a Distinctive Binding Profile†Wai N. Chan, John M. Evans, Michael S. Hadley, Hugh J. Herdon, Jeffrey C. Jerman, Helen K. A. Morgan, Tania O. Stean, Mervyn Thompson, Neil Upton, and Antonio K. VongView Author Information SmithKline Beecham Pharmaceuticals, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, U.K. Cite this: J. Med. Chem. 1996, 39, 23, 4537–4539Publication Date (Web):November 8, 1996Publication History Received25 July 1996Published online8 November 1996Published inissue 1 January 1996https://pubs.acs.org/doi/10.1021/jm960535whttps://doi.org/10.1021/jm960535wrapid-communicationACS PublicationsCopyright © 1996 American Chemical SocietyRequest reuse permissionsArticle Views372Altmetric-Citations27LEARN 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-AlertscloseSupporting Info (1)»Supporting Information Supporting Information SUBJECTS:Molecular structure,Potassium,Rodent models,Screening assays,Stereochemistry Get e-Alerts