gebhart/patrepeval huggingface dataset:
5‐(<i>N</i>‐Arylnortropan‐3‐yl)‐ and 5‐(<i>N</i>‐Arylpiperidin‐4‐yl)‐2,4‐diaminopyrimidines. Novel Inhibitors of Dihydrofolate Reductase (1986)

Abstract Based on a computer‐assisted analysis of the three‐dimensional structure of the binary complex of E.coli dihydrofolate reductase (DHFR) with methotrexate, 5‐( N ‐arylnortropan‐3‐yl)‐ and 5‐( N ‐arylpiperidin‐4‐yl)‐2,4‐diaminopyrimidines 2 and 4 were designed as inhibitors of DHFR. Syntheses of the designed compounds have been carried out. The most potent compound 2a inhibited E. coli DHFR with K i = 0.49.10 −9 M. The activities within the series of compounds synthesized could be rationalized by molecular‐modelling experiments which served as the basis of this work. Several compounds within the presented series exhibit antimalarial activities in vitro and in vivo .
Choice and Application of Motion Compensation Systems (MCS) (1983)

Abstract DEFINITION OF AN MCS We will define the MCS in the following way: System allowing: – either to transfer a load – or to maintain a connection between a fixed-support (bottom-supported unit) and a floating support. This definition can also be extended to immobilisation into space (generally sea water) of a load suspended to a floating support. We will remind you also of the difference between active and passive systems, due to the fact that it is an essential difference for MCS. – a system is called passive when it is submitted to external actions and its reactions are only a function of its own characteristics. – an active system receives energy in order to counterbalance external actions. A data-acquisition system of the relative movements floating support/fixed support must be provided. CHOICE OF MCS Selection Chart We have designed a selection chart for MCS clients (see Fig. 1). To be effective, it is very important that the problem be well described and understood. Solutions for an MCS problem must be adapted since a universal solution does not exist. The selection chart is composed of different levels to be crossed step by step: – relative position of the handler and the handled – required function – different technical selection criteria allowing a first approach of the chosen active/passive system. (These criteria are information guide-lines only.) – handling system of the load on the handler – technical solution that we illustrate by a sketch or a reference to an existing leaflet, (see Fig. 2 – Design of solutions)
Adaptive Chromatic Dispersion Equalization for Non-Dispersion Managed Coherent Systems (2009)

Blind adaptive chromatic dispersion equalization for coherent polarization multiplexed (NRZ/RZ)-QPSK receivers is presented. A novel low complexity estimation algorithm precisely estimates arbitrarily large dispersion in a fixed adaptation length.
Airguns: Theory and operation of the marine seismic source (2010)

A detailed knowledge of the radiation field of seismic sources is essential to effective source design and source wavefield deconvolution. To understand the principles of airgun theory and operation it is necessary to follow the motion of the air bubble that is produced and released underwater by the airgun. An airgun is a mechanical device that releases a high pressure bubble of air underwater, the expansion of the air bubble generates seismic waves the water that are the source waves of the seismic waves used in reflection seismology.\n\nThis monograph is about the motion of the bubble of air in the water that creates the seismic pressure wave called the airgun signature. The relevant physical principles for a single bubble are discussed first, then the dynamic behavior of the bubble is derived from the basic equations of fluid mechanics for the ocean and thermodynamics for the air. \nThe surface ghost reflection part of the signature is derived and its behavior explained.\n\nOnce the dynamics of a single bubble is understood, the behavior of an array of airgun bubbles is easy to understand, the reasons for an array are explained and detailed. The discussion then moves on to practical performance specifications in the field.\n\nThe different types of airguns are discussed and their mechanical operation explained, this leads to the airgun system, a pneumatic-electrical computer controlled system on board the seismic vessel under the control of the GPS navigation system.
Multifractal Analysis of Soil Porosity Based on Mercury Injection and Nitrogen Adsorption (2010)

Pore‐size distributions (PSD) determined by different methods across various ranges of equivalent pore radius have shown multifractal characteristics. Here, the multifractal formalism was employed to describe both mercury injection porosimetry (MIP) and nitrogen adsorption isotherms (NAI) curves, measured in a Mollisol and in a Vertisol. Four different soil use intensities and three replicate samples per treatment were analyzed. Mercury injection and nitrogen adsorption were used to measure PSDs for equivalent pore radii 150 to 0.005 μm and 0.1 to 0.001 μm, respectively. The scaling properties of all the Hg injection curves and N 2 adsorption isotherms could be fitted reasonably well with multifractal models. A generalized dimension spectrum, D q , led to a better definition of multifractal scaling than a singularity spectrum, f (α). Parameters derived from these two functions showed highly significant differences between MIP and NAI in both soil types. Thus, mean values of entropy dimension, D 1, and correlation dimension, D 2 , were significantly higher for mercury injection than for nitrogen adsorption. On the contrary, Hölder exponents of order zero, α 0 , were on average significantly higher for nitrogen adsorption. Also, mean widths of the f (α) spectra were much larger for nitrogen adsorption. These results indicate heterogeneity due to the presence of different porous domains at the scale of primary soil aggregates. The multifractal approach was useful to characterize the heterogeneity of the soil pore system and to distinguish between different patterns of PSD corresponding to various degrees of clustering.
The dual-porosity model, A newly developed interpretation method for shaly sands (1984)

The dual-porosity model has recently been developed by Total-Compagnie Francaise des Petroles for the determination of water-saturation in hydrocarbons-bearing shaly reservoirs form wholly log-derived data. It is operated by use of an equation whereby the influence of the clay content of the reservoir rock onto the formation resistivity is interpreted through modern theories of cation-exchange conductance. By taking advantage of the concepts applied to the elaboration of the dual-water model, the equation relates the amount of clay-bound water in the reservoir to the total and effective porosities determined by interpretation of conventional logs. On the other hand the equation applies to the bound-water specific volume a geometrical factor which is different from that affecting the effective porosity. Hence the appelation of dual-porosity model.
Reduction of coke formation during naphtha pyrolysis using triethyl phosphite (1988)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTReduction of coke formation during naphtha pyrolysis using triethyl phosphiteKalyan K. Ghosh and Deepak KunzruCite this: Ind. Eng. Chem. Res. 1988, 27, 4, 559–565Publication Date (Print):April 1, 1988Publication History Published online1 May 2002Published inissue 1 April 1988https://pubs.acs.org/doi/10.1021/ie00076a005https://doi.org/10.1021/ie00076a005research-articleACS PublicationsRequest reuse permissionsArticle Views270Altmetric-Citations29LEARN 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
High-Throughput Mass Spectrometry Applied to Structural Genomics (2014)

Mass spectrometry (MS) remains under-utilized for the analysis of expressed proteins because it is inaccessible to the non-specialist, and sample-turnaround from service labs is slow. Here, we describe 3.5 min Liquid-Chromatography (LC)-MS and 16 min LC-MSMS methods which are tailored to validation and characterization of recombinant proteins in a high throughput structural biology pipeline. We illustrate the type and scope of MS data typically obtained from a 96-well expression and purification test for both soluble and integral membrane proteins (IMPs), and describe their utility in the selection of constructs for scale-up structural work, leading to cost and efficiency savings. We propose that value of MS data lies in how quickly it becomes available and that this can fundamentally change the way in which it is used.
Predictive Neural Networks for Learning the Time Course of Blood Glucose Levels from the Complex Interaction of Counterregulatory Hormones (1998)

Diabetes mellitus is a widespread disease associated with an impaired hormonal regulation of normal blood glucose levels. Patients with insulin-dependent diabetes mellitus (IDDM) who practice conventional insulin therapy are at risk of developing hypoglycemia (low levels of blood glucose), which can lead to severe dysfunction of the central nervous system. In large retrospective studies, up to approximately 4% of deaths of patients with IDDM have been attributed to hypoglycemia (Cryer, Fisher, & Shamoon, 1994; Tunbridge, 1981; Deckert, Poulson, & Larsen, 1978). Thus, a better understanding of the complex hormonal interaction preventing hypoglycemia is crucial for treatment. Experimental data from a study on insulin-induced hypoglycemia in healthy subjects are used to demonstrate that feedforward neural networks are capable of predicting the time course of blood glucose levels from the complex interaction of glucose counterregulatory (glucose-raising) hormones and insulin. By simulating the deficiency of single hormonal factors in this regulatory network, we found that the predictive impact of glucagon, epinephrine, and growth hormone secretion, but not of cortisol and norepinephrine, were dominant in restoring normal levels of blood glucose following hypoglycemia.
Interleukin 3- receptor targeted exosomes inhibit <i>in vitro</i> and <i>in vivo</i> Chronic Myelogenous Leukemia cell growth (2017)

Despite Imatinib (IM), a selective inhibitor of Bcr-Abl, having led to improved prognosis in Chronic Myeloid Leukemia (CML) patients, acquired resistance and long-term adverse effects is still being encountered. There is, therefore, urgent need to develop alternative strategies to overcome drug resistance. According to the molecules expressed on their surface, exosomes can target specific cells. Exosomes can also be loaded with a variety of molecules, thereby acting as a vehicle for the delivery of therapeutic agents. In this study, we engineered HEK293T cells to express the exosomal protein Lamp2b, fused to a fragment of Interleukin 3 (IL3). The IL3 receptor (IL3-R) is overexpressed in CML blasts compared to normal hematopoietic cells and thus is able to act as a receptor target in a cancer drug delivery system. Here we show that IL3L exosomes, loaded with Imatinib or with BCR-ABL siRNA, are able to target CML cells and inhibit <i>in vitro</i> and <i>in vivo</i> cancer cell growth.
Cyclooxygenase–2 Promotes Hepatocellular Carcinoma Cell Growth Through Akt Activation: Evidence for Akt Inhibition in Celecoxib–Induced Apoptosis (2003)

Cyclooxygenase-2 (COX-2)-controlled prostaglandin (PG) metabolism recently has been implicated in the pathogenesis of hepatocellular carcinoma (HCC). However, the biologic role and molecular mechanism of COX-2-mediated PGs in the control of liver cancer growth have not been established. This study was designed to examine the direct effect of COX-2 and its inhibitor celecoxib on the growth control of liver cancer cells. Human HCC cell lines Hep3B and HepG2 transfected with COX-2 expression vector showed increased cell growth and enhanced phosphorylation of serine/threonine protein kinase B (Akt). The level of COX-2 expression and Akt phosphorylation is correlated positively in cultured HCC cells and human liver cancer tissues. Inhibition of Akt activation by phosphatidylinositol 3-kinase (PI3-kinase) inhibitor LY294002 significantly decreased the viability of Hep3B and HepG2 cells (P <.01). These results reveal a novel role of Akt activation in COX-2-induced HCC cell survival. Furthermore, HCC cells treated with the COX-2 inhibitor celecoxib showed significant reduction of Akt phosphorylation and marked morphologic and biochemical characteristics of apoptosis. Overexpression of COX-2 or addition of exogenous PGE(2) partially prevented celecoxib-induced apoptosis (P <.01). In conclusion, our results suggest the involvement of COX-2-dependent and -independent mechanisms in celecoxib-mediated HCC cell apoptosis.
Stable N-bridged diiron (IV) phthalocyanine cation radical complexes: synthesis and properties (2009)

Oxidation of N-bridged diiron tetra-tert-butylphthalocyanine (FePc(t)Bu)(2)N with (t)BuOOH in halogenated solvents afforded mu-nitrido diiron (IV) phthalocyanine cation radical complexes, (X)PcFe(IV)-N-Fe(IV)Pc(+) (X) (X = Cl, Br), as evidenced by UV-vis, electron paramagnetic resonance (EPR), electrospray ionization mass spectrometry (ESI-MS), Mössbauer, X-ray absorption near edge structure (XANES) and extended X-ray absorption fine structure (EXAFS) data. Continuous introduction ESI-MS showed the initial formation of the t-butylperoxo diiron complex (t)BuOO-(FePc(t)Bu)(2)N followed by intermediate formation of a monohalogenated adduct which gave the dihalogenated complex as final stable product. Fe K-edge EXAFS analysis of (X)PcFe(IV)-N-Fe(IV)Pc(+) (X) showed bridging N atom at a distance of 1.69(1) A. The distance between two equivalent hexacoordinated in-plane iron (IV) centers is 3.39(1) A. Fe-X bond lengths are 2.33 and 2.54 A for X = Cl and Br, respectively. The use of (Cl)PcFe(IV)-N-Fe(IV)Pc(+) (Cl) for the catalytic oxidation of organic substrates has been shown for the first time.
Interrogation of wavelength multiplexed fiber bragg gratings using spectral filtering and amplitude-to-phase optical conversion (2003)

A technique for interrogating multiplexed FBG sensors using all-fiber low-cost devices is demonstrated. It is based on spectral filtering employing a fused biconical wavelength-division multiplexer and on amplitude-to-phase optical conversion to perform power referencing. Four FBG sensors are wavelength multiplexed in the network, and a 3-nm-wide tunable optical filter is employed at the detection block for sensor demultiplexing. With this technique an operation range of more than 2 nm is demonstrated for the sensors with achievable wavelength static resolution ranging from 1.9 to 13.4 pm/Hz <sup xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">1</sup> 2/ with no observable hysteresis. As for power referencing, the system is proven to be unaffected by power variations as high as 75% of the total power launched by the source. Finally, output-phase variations due to crosstalk are shown to be under 1% of the total output phase range, with more than 29-dB optical isolation between channels.
Susceptibility to inflammatory disease in HLA-B27 transgenic rat lines correlates with the level of B27 expression (1993)

To investigate the role of the class I MHC molecule HLA-B27 in the spondyloarthropathies, we produced rats transgenic for HLA-B27 and human beta 2-microglobulin. Of five lines bearing > 1 copy of each transgene and showing hemizygous expression of both transgenes, two (lines 21-4H and 33-3) developed spontaneous inflammatory disease that closely resembled B27-associated human disease. Two lines, 21-4L and 25-6, remained healthy even when homozygous for the transgene locus, whereas the 21-3 line, bearing the third highest transgene copy number, developed disease similar to that of the 21-4H and 33-3 lines only when homozygous for the transgene locus. The disease-prone lines showed higher expression of B27--thymic mRNA in utero, splenic mRNA by 5 days of age, and splenic cell surface protein by the time of disease onset--than the disease-resistant lines. Disease susceptibility thus appeared to correlate with gene copy number and the quantity of B27 in lymphoid cells. The increase in the amount of B27 protein did not appear to be simply a consequence of the inflammatory disease because 1) there was no similar change in endogenous RT1 class I expression; 2) no alteration of B27 expression occurred in 21-4H rats with adjuvant-induced arthritis; 3) in rats with inflammatory disease transgenic for HLA-A2 and the 21-4H transgene locus, A2 expression was the same as in healthy rats transgenic for A2 but not B27; and 4) the transgenes in disease-prone and disease-resistant lines were equally susceptible to induction by IFN-gamma. Immunocytochemistry of the distal colon, an early site of inflammation, showed that the B27 Ag is expressed at high levels in cells of the lamina propria, but not at all in colonic epithelial cells. Taken together, the data suggest that the B27 transgene is expressed in a copy number dependent, position-independent manner in lymphoid tissue and that disease results from the expression of B27 above a critical threshold level.
ChemInform Abstract: Electrochemical Potentials and Reactivity of Organo‐Metal Compounds (1991)

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.
Characterization of polyphenol oxidase from Chaetomium thermophile, a thermophilic fungus. (1988)

The polyphenol oxidase from Chaetomium thermophile Isolate O-453 was examined for its substrate specificity. The purified enzyme acted on polyphenols but not on monophenols. Among the polyphenols and phenol-like compounds tested, those oxidized were d-catechin (relative activity, 100%), l-epicatechin (95.3%), chlorogenic acid (80.0%), pyrocatechol (53.8%), DOPamine (47.8%), guaiacol (87.5%), and N, N-dimethyl-p-phenylenediamine (75.3%). Esculine (7.8%), resorcinol (0%), p-quinone (0%), o-phenylenediamine (1.3%), phenol (0%), and L-tyrosine (0%) werescarcely oxidized. The purified enzyme was inhibited by potassium xanthogenate, thiourea, cysteine, potassium cyanide, and sodium azide. Mercuric and ferrous ions inactivated the enzyme. Carbon monooxide did not inhibit the activity (residual activity, 92.0%). SDS-polyacrylamide gel electrophoresis showed that the purified enzyme (mw, 98, 000) is a trimer composed of three of the same kinds of monomers (mw, 36, 000). These data indicate that the polyphenol oxidase from C. thermophile Isolate O-453 is a copper-containing protein and is classified as laccase [benzenediol: oxygen oxidoreductase, EC 1.10.3.2].
A simple hypergraph min cut algorithm (1996)

We present an algorithm for finding the minimum cut of an edge-weighted hypergraph. It is simple in every respect. It has a short and compact description, is easy to implement and has a surprisingly simple proof of correctness. The runtime is O(jV j 2 log jV j+jV j \\Delta jjEjj) where jjEjj is the sum of the cardinalities of the hyperedges.
Low concentrations of indomethacin inhibit phospholipase A2 of rabbit polymorphonuclear leukocytes. (1978)

Inhibition of prostaglandin synthesis by indomethacin, a drug with anti-inflammatory properties, has been attributed to its action on fatty acid cyclooxygenase. However, prostaglandin synthesis would also be inhibited if precursor fatty acids were not supplied. We find that indomethacin inhibits phospholipase A2 (phosphatide 2-acylhydrolase, EC 3.1.1.4) of rabbit polymorphonuclear leukocytes in dose-dependent fashion. Inhibition is immediate and readily detected at 1 micrometer. The extent of inhibition is the same over a 10-fold range of substrate concentration and over a 500-fold range of enzyme purification. Inhibition is of the noncompetitive type, with an apparent Ki of 12 micrometer. Four other phospholipases A2--from venoms of Russell viper, Crotalus adamanteus, and bee, and from pig pancreas--are unaffected by 50 micrometer indomethacin, which inhibits leukocyte phospholipase A2 by 70%. This inhibition at low concentrations may well be important in the effects of the drug on protaglandin synthesis and inflammatory responses.
Liver Transplant Using Donors After Unexpected Cardiac Death: Novel Preservation Protocol and Acceptance Criteria (2007)

Donors after cardiac death (DCD) suffer irreversible cardiac arrest prior to donation. We describe our liver transplant experience with DCD whose cardiac arrest is unexpected, not following the removal of ventilatory support, whom we maintain with normothermic extracorporeal membrane oxygenation (NECMO). A potential donor goes into cardiac arrest outside the hospital and is brought to the hospital under continuous cardiopulmonary resuscitation (CPR). The donor is declared dead and placed on a cardiocompressor. Femoral vessels are cannulated and connected to cardiopulmonary bypass (CPB) to establish NECMO. Blood parameters and CPB pump flow are monitored throughout NECMO, which is continued until cold preservation. From April 2002 to May 2006, 10 of 40 potential DCD livers were transplanted. Only one graft was lost to primary nonfunction (PNF) and another to hepatic artery thrombosis. Posttransplant hepatic function was good. Certain parameters, such as CPR and NECMO times, hepatic transaminases during NECMO, and donor age, determined the viability of DCD liver grafts and were used to establish criteria for their acceptance. Though considered marginal, unexpected DCD can represent an important source of viable livers for transplant if strict acceptance criteria are employed and they are maintained with NECMO prior to recovery.
A Comparative Study of Facial Landmark Localization Methods for Face Recognition Using HOG descriptors (2010)

This paper compares several approaches to extract facial landmarks and studies their influence on face recognition problems. In order to obtain fair comparisons, we use the same number of facial landmarks and the same type of descriptors (HOG descriptors) for each approach. The comparative results are obtained using FERET and FRGC datasets and show that better recognition rates are obtained when landmarks are located at real facial fiducial points. However, if the automatic detection of these is compromised by the difficulty of the images, better results are obtained using fixed landmarks grids.