gebhart/patrepeval huggingface dataset:
New Bioactive Azaartemisinin Derivatives (2003)

Reaction of artemisinin (1) with ethanolamine, followed by acid treatment produced the lactam (4S,8S,9S,13S,1R,5R,12R)-11-aza-11-(2-hydroxyethyl)-1,5,9-trimethyl-14,15-dioxatetracyclo [10.2.1.0.0]pentadecan-10-one (4) and the diol (1S,2S,6S,7S,5R,8R)-4-aza-5,6-dihydroxy-4-(2-hydroxyethyl)-2,8-dimethyl-7-(3-oxobutyl) bicyclo[4.4.0]decan-3-one (7). When ethylenediamine was used instead of the ethanolamine, the dimeric lactam (1S,4S,8S,9S,13S,5R,12R)-11-[2-((1S,4S,8S,9S,13S,5R,12R)-11-aza-1,5,9-trimethyl-14,15-dioxa-10-oxotetracyclo[10.2.1.0.0] pentadec-11-yl)ethyl]-11-aza-1,5,9-tri-methyl-14,15-dioxatetracyclo-[10.2.1.0.0]-pentadecan-10-one (8) was obtained. All compounds are new azaartemisinin derivatives lacking the peroxide functionality. These compounds were evaluated for antimalarial and cytotoxic activities. Only the dimer 8 was found to possess antimalarial activity, while only the diol 7 exhibited cytotoxic activity against human breast ductal carcinoma.
A digital watermark (2002)

The paper discusses the feasibility of coding an "undetectable" digital water mark on a standard 512/spl times/512 intensity image with an 8 bit gray scale. The watermark is capable of carrying such information as authentication or authorisation codes, or a legend essential for image interpretation. This capability is envisaged to find application in image tagging, copyright enforcement, counterfeit protection, and controlled access. Two methods of implementation are discussed. The first is based on bit plane manipulation of the LSB, which offers easy and rapid decoding. The second method utilises linear addition of the water mark to the image data, and is more difficult to decode, offering inherent security. This linearity property also allows some image processing, such as averaging, to take place on the image, without corrupting the water mark beyond recovery. Either method is potentially compatible with JPEG and MPEG processing.< <ETX xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">&gt;</ETX>
A novel approach to the design of a transistorized inverter- converter operating at higher-than-audio frequencies (1972)

In this paper we describe some of the design and operating characteristics of an unusual 5-Kw 25kHz transistorized invertor- convertor, in which the high-power switch consists of a series arrangement of low-power transistors. The dc voltage is obtained from the three-phase line by voltage tripling rectification in each phase, thus avoiding a 60-Hz transformer. The resulting supply is exceptionally compact, light weight, and inexpensive. In contrast to most solid-state circuits, this supply is found to be extremely resistant to reactive voltage `spikes' attendant to the excitation of inductive loads. We also discuss the advantage in reliability resulting from the series arrangement of the transistors.
An acyclic 5-nitroindazole nucleoside analogue as ambiguous nucleoside (1995)

Acyclic nucleoside analogues with carboxamido- or nitro-substituted heterocyclic bases have been evaluated for their possible use as universal bases in oligodeoxynucleotides. The acyclic moiety endows the constructs with enough flexibility to allow good base stacking. The 5-nitroindazole analogue afforded the most stable duplexes among the acyclic derivatives with the least spread in Tm versus the four natural bases. In spite of the acyclic moiety, stabilities are comparable with those of duplexes incorporating the recently described 5-nitroindole nucleoside analogue, but considerably exceed those for the 3-nitropyrrole analogue.
Structural and Genetic Characterization of the Shigella boydii Type 13 O Antigen (2003)

Shigella is an important human pathogen. It is generally agreed that Shigella and Escherichia coli constitute a single species; the only exception is Shigella boydii type 13, which is more distantly related to E. coli and other Shigella forms and seems to represent another species. This gives S. boydii type 13 an important status in evolution. O antigen is the polysaccharide part of the lipopolysaccharide in the outer membrane of gram-negative bacteria and plays an important role in pathogenicity. The chemical structure and genetic organization of the S. boydii type 13 O antigen were investigated. The O polysaccharide was found to be acid labile owing to the presence of a glycosyl phosphate linkage in the main chain. The structure of the linear pentasaccharide phosphate repeating unit (O unit) was established by nuclear magnetic resonance spectroscopy, including two-dimensional COSY, TOCSY, ROESY, and H-detected 1H, 13C and 1H, 31P HMQC experiments, along with chemical methods. The O antigen gene cluster of S. boydii type 13 was located and sequenced. Genes for synthesis of UDP-2-acetamido-2,6-dideoxy-L-glucose and genes that encode putative sugar transferases, O unit flippase, and O antigen polymerase were identified. Seven genes were found to be specific to S. boydii type 13. The S. boydii type 13 O antigen gene cluster has higher levels of sequence similarity with Vibrio cholerae gene clusters and may be evolutionarily related to these gene clusters.
Twenty-Six Years of Anti-HIV Drug Discovery: Where Do We Stand and Where Do We Go? (2009)

status: Published
Combining battery-like and pseudocapacitive charge storage in 3D MnOx@carbon electrode architectures for zinc-ion cells (2017)

Nanoscale MnO<italic>x</italic> expressed in 3D carbon nanofoam electrodes exhibits both pseudocapacitive and battery-like charge-storage using a mixed Na<sup>+</sup> : Zn<sup>2+</sup> aqueous electrolyte.
Fabrication of a Covalently Attached Multilayer Film via In-Situ Reaction (2001)

A covalently linked ultrathin multilayer film was fabricated from 2-nitro-N-methyl-diphenylamine-4-diazonium-formaldehyde resin (NDR) and phenol-formaldehyde resin (PR) in methanol in-situ. The UV-vis, XRD, AFM and FTIR show that this multilayer is of high regularity, smoothness and stability.
DULO: an effective buffer cache management scheme to exploit both temporal and spatial locality (2005)

Sequentiality of requested blocks on disks, or their spatial locality, is critical to the performance of disks, where the throughput of accesses to sequentially placed disk blocks can be an order of magnitude higher than that of accesses to randomly placed blocks. Unfortunately, spatial locality of cached blocks is largely ignored and only temporal locality is considered in system buffer cache management. Thus, disk performance for workloads without dominant sequential accesses can be seriously degraded. To address this problem, we propose a scheme called DULO (DUal LOcality), which exploits both temporal and spatial locality in buffer cache management. Leveraging the filtering effect of the buffer cache, DULO can influence the I/O request stream by making the requests passed to disk more sequential, significantly increasing the effectiveness of I/O scheduling and prefetching for disk performance improvements.DULO has been extensively evaluated by both trace-driven simulations and a prototype implementation in Linux 2.6.11. In the simulations and system measurements, various application workloads have been tested, including Web Server, TPC benchmarks, and scientific programs. Our experiments show that DULO can significantly increase system throughput and reduce program execution times.
Sodium-channel turnover in rabbit cultured Schwann cells (1988)

Radiolabelled saxitoxin has been used as a chemical marker for the voltage-dependent sodium channels expressed in the plasmalemma of rabbit Schwann cells in culture. Proteolytic enzymes destroy this saxitoxin-binding capacity, which gradually reappears with an exponential time constant of about 3.1 days. Exposure of cultured Schwann cells to tunicamycin, an inhibitor of glycosylation, leads to a progressive exponential fall in saxitoxin-binding capacity, again with a time constant of about 3.1 days. The assumption that the steady-state density of Schwann cell sodium channels is maintained by a constant synthesis of channels in the face of a rate of loss from the membrane proportional to the amount of channel already present, leads to the conclusion that these channels have an average lifetime of about 3.1 days. The metabolic consequences of this rapid turnover of Schwann cell sodium channels is discussed.
Triangular CdS Nanocrystals: Structural and Optical Studies (2001)

CdS nanostructures with high crystallinityare widely investigated for their semiconductor properties. This work focuses on the preparation and properties of equilateral-triangular nanocrystals made by colloidal self-assembly. The picture shows the results of high-resolution transmission electron microscopy imaging of a CdS nanostructure prepared by this method.
Does phosphorylase kinase control glycogen biosynthesis in skeletal muscle? (1995)

Immunoblotting as well as enzyme assays demonstrate the presence of the self-glucosylating protein, glycogenin, in the protein-glycogen complex, in the sarcoplasmic reticulum and in phosphorylase kinase. In all three compartments glycogenin occurs in different, albeit, defined glucosylated forms, which upon deglucosylation are converted into a 42 kDa form. We suggest that phosphorylase kinase might have a dual function in glycogen biogenesis: firstly, control of glycogen degradation in the protein-glycogen complex via phosphorylation of glycogen phosphorylase b; secondly, regulation of glycogen biosynthesis on the sarcoplasmic reticular membranes via phosphorylation and thereby inhibition of glycogen synthase.
Quinazolin-4-one α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA) Receptor Antagonists:  Structure−Activity Relationship of the C-2 Side Chain Tether (2001)

A series of 6-fluoro-3-(2-chlorophenyl)quinazolin-4-ones has been prepared, which contains a 2-fluorophenyl ring attached to C-2 by a variety of two-atom tethers. These compounds were used to probe the structure-activity relationship (SAR) for AMPA receptor inhibition. The relative potencies of the new compounds ranged from 11 nM to greater than 10 microM. The differential activity of the compounds was rationalized on the basis of alterations of the 2-fluorophenyl positioning (planar and radial) relative to the quinazolin-4-one ring based on computational methods. From this effort, new AMPA receptor antagonists, containing the methylamino tether group, have been identified.
Liver tissue expression of CD80 and CD95 antigens in chronic hepatitis C: relationship with biological and histological disease activities. (1999)

The well known discrepancy between cytotoxic T lymphocyte (CTL) infiltration in the liver and disease biological activity, as assessed by alanine aminotransferase (ALT) levels, during the course of chronic hepatitis C virus (HCV) infection, suggests the possible failure of cytotoxic mechanisms devoted to virus clearance. To further investigate the biological events involved in CTL-mediated lysis, i.e. B7/CD28 costimulatory and Fas/Fas-ligand pathways, the CD80 and CD95 antigen expression in liver tissue specimens from chronically HCV-infected patients was evaluated. The results were analysed in relation to serum ALT values and the histological activity (HAI) of liver disease. The data provide evidence for a strong and comparable hepatocyte CD80 and C95 structure expression in chronically HCV-infected livers. CD80- and CD95-carrying liver cells were more frequently distributed at the periportal region of the hepatic lobule, above all near piecemeal necrosis areas, among infiltrating CTL. On the other hand, a negative correlation was found between liver tissue expression of both antigens and serum ALT activity. The relationship with HAI was not statistically significant. The results imply that HCV infection triggers CD80 and CD95 molecule expression on hepatocytes. Further studies are required to clarify the relevance of such a finding in the context of virus-host interactions.
Scramjet development and testing in the United States (2001)

Ramjet engines have been of interest in the United States since the 1940's. Subsonic burning ramjets were investigated/developed the 40's through the 60's. As higher speeds were desired for airbreathing propulsion systems, the supersonic combustion ramjet (scramjet) became the primary focus of research investigations in mid 1960's to the present. It is of interest therefore to review this past research with emphasis on the scramjet development. Historical and evolutionary reviews of the scramjet are presented. A tabulation of the scramjet engine concepts that were free-jet tested in the U.S. is included along with a tabulation of the facilities used for these scramjet tests, lessons learned during the many test programs, and an extended reference list. A combination of this information should be an aid for planning and conducting future airbreathing propulsion test programs. Nomenclature
Recruitment of host functions suggests a repair pathway for late steps in group II intron retrohoming (2005)

Retrohoming of group II introns occurs by a mechanism in which the intron RNA reverse splices directly into one strand of a DNA target site and is then reverse transcribed by the associated intron-encoded protein. Host repair enzymes are predicted to complete this process. Here, we screened a battery of Escherichia coli mutants defective in host functions that are potentially involved in retrohoming of the Lactococcus lactis Ll.LtrB intron. We found strong (greater than threefold) effects for several enzymes, including nucleases directed against RNA and DNA, replicative and repair polymerases, and DNA ligase. A model including the presumptive roles of these enzymes in resection of DNA, degradation of the intron RNA template, traversion of RNA-DNA junctions, and second-strand DNA synthesis is described. The completion of retrohoming is viewed as a DNA repair process, with features that may be shared by other non-LTR retroelements.
Combination and propagation of uncertainty with belief functions - a reexamination (1985)

The behavior of Dempster's rule of combination in typical situations is examined. Particularly, it is shown that assessing a zero value or a very small value may lead to very different results. Moreover a comparison with a possibility theory-based approach in case of conflicting information is provided. The general problem of representing uncertainty with one or several numbers is addressed. Lastly, the propagation of uncertainty from a fact and if...then... rule is discussed in the framework of belief functions.
Structural insight into selectivity and resistance profiles of ROS1 tyrosine kinase inhibitors (2015)

Oncogenic ROS1 fusion proteins are molecular drivers in multiple malignancies, including a subset of non-small cell lung cancer (NSCLC). The phylogenetic proximity of the ROS1 and anaplastic lymphoma kinase (ALK) catalytic domains led to the clinical repurposing of the Food and Drug Administration (FDA)-approved ALK inhibitor crizotinib as a ROS1 inhibitor. Despite the antitumor activity of crizotinib observed in both ROS1- and ALK-rearranged NSCLC patients, resistance due to acquisition of ROS1 or ALK kinase domain mutations has been observed clinically, spurring the development of second-generation inhibitors. Here, we profile the sensitivity and selectivity of seven ROS1 and/or ALK inhibitors at various levels of clinical development. In contrast to crizotinib's dual ROS1/ALK activity, cabozantinib (XL-184) and its structural analog foretinib (XL-880) demonstrate a striking selectivity for ROS1 over ALK. Molecular dynamics simulation studies reveal structural features that distinguish the ROS1 and ALK kinase domains and contribute to differences in binding site and kinase selectivity of the inhibitors tested. Cell-based resistance profiling studies demonstrate that the ROS1-selective inhibitors retain efficacy against the recently reported CD74-ROS1(G2032R) mutant whereas the dual ROS1/ALK inhibitors are ineffective. Taken together, inhibitor profiling and stringent characterization of the structure-function differences between the ROS1 and ALK kinase domains will facilitate future rational drug design for ROS1- and ALK-driven NSCLC and other malignancies.
Accuracy of circulating placental growth factor, vascular endothelial growth factor, soluble fms‐like tyrosine kinase 1 and soluble endoglin in the prediction of pre‐eclampsia: a systematic review and meta‐analysis (2012)

PlGF, sFLT1 and sENG showed modest but significantly different concentrations before 30 weeks of gestation in women who developed pre-eclampsia. Test accuracies of all four markers, however, are too poor for accurate prediction of pre-eclampsia in clinical practice.
Elution Conditions and Degradation Mechanisms in Long‐Term Immunoadsorbent Use (1991)

The limited life of immunoadsorbents used for the large-scale purification of biological macromolecules poses a significant limitation to the more widespread application of this technology. In this study, the binding activity of a monoclonal antibody (MAb) to bovine serum albumin (BSA) was measured as a function of pH, ionic strength, and varying concentrations of KSCN, ethylene glycol, or DMSO. Low pH (2.5) and 3 M KSCN each reduced the antibody binding constant below 6 x 10(5) L/mol, meeting criteria derived from a simple chromatographic model for identifying effective eluents. A panel of six MAb to BSA was exposed repeatedly to adsorption conditions and the two eluents. Four MAb lost less than 50% of their initial binding capacity over 100 cycles. The other two lost 75% of their initial capacity. One MAb was stable when exposed to low pH but lost binding capacity with KSCN. In all cases, the equilibrium constant was unchanged. The loss of capacity was also shown to be a strong function of antibody loading: at 14.5 mg/mL, 98% of the initial binding capacity of one MAb was lost within 40 cycles, versus 75% loss at 1 mg/mL. Antibody leakage and nonspecific adsorption of contaminants were not responsible for significant loss of antibody activity over time.
Chronic Cocaine Administration Increases CNS Tyrosine Hydroxylase Enzyme Activity and mRNA Levels and Tryptophan Hydroxylase Enzyme Activity Levels (1993)

Cocaine is an inhibitor of dopamine and serotonin reuptake by synaptic terminals and has potent reinforcing effects that lead to its abuse. Tyrosine hydroxylase (TH) and tryptophan hydroxylase (TPH) catalyze the rate-limiting steps in dopamine and serotonin biosynthesis, respectively, and are the subject of dynamic regulatory mechanisms that could be sensitive to the actions of cocaine. This study assessed the effects of chronic cocaine on brain TH and TPH activities. Cocaine was administered (0.33 mg/infusion, i.v.) to rats for 7 days every 8 min for 6 h per day. This administration schedule is similar to patterns of self-administration by rats when given ad libitum access to this dose. This chronic, response-independent administration increased TH enzyme activity in the substantia nigra (30%) and ventral tegmental area (43%). Moreover, TH mRNA levels were also increased (45 and 50%, respectively). In contrast to the enzymatic and molecular biological changes in the cell bodies, TH activity was unchanged in the terminal fields (corpus striatum and nucleus accumbens). Similarly, TPH activity was increased by 50% in the raphe nucleus (serotonergic cell bodies). In summary, the chronic response-independent administration of cocaine produces increases in the expression of TH mRNA and activity in both the cell bodies of motor (nigrostriatal) and reinforcement (mesolimbic) dopamine pathways. These increases are not manifested in the terminal fields of these pathways.
Low-dose amiodarone led to fewer cardiac deaths and serious arrhythmics in patients surviving myocardial infarction who had contraindications to β-blockers (1993)

Source Citation Ceremuzynski L, Kleczar E, Krzeminska-Pakula M, et al. Effect of amiodarone on mortality after myocardial infarction: a double-blind, placebo-controlled, pilot study. J Am Coll Cardiol. 1992 Nov 1;20:1056-62.
A new approach to time-resolved studies of ATP-requiring biological systems; laser flash photolysis of caged ATP. (1980)

2-Nitrobenzyl derivatives have been used for several years as photolabile protecting groups in synthetic organic chemistry. Recently, P3-1-(2-nitro phenylethyladenosine 5'-triphosphate "caged ATP" was synthesized and its photolysis was shown to generate ATP in situ. This and related reactions have great potential for structural and kinetic studies of both intact and soluble biological systems and it is thus important to define the kinetic characteristics of the photolytic reaction. Caged ATP (2.5 mM) was photolyzed at 347 nm by a single 30-nsec pulse from a frequency-doubled ruby laser of 25 mJ energy to generate 500 microM ATP. The kinetics of the overall reaction were determined by monitoring the kinetics of ATP-induced dissociation of actomyosin, a reaction of known kinetic characteristics. Release of 500 microM ATP was found to be controlled by a process having a rate constant of 2.2 X 10(9) [H+] sec-1 at 22 degrees C at pH 5.8-9.5, which corresponds to 220 sec-1 at pH 7. This process is believed to be the breakdown of an aci-nitro compound, which was identified on the basis of its spectral properties and the photochromicity of related 2-nitrobenzyl compounds.
Liposome encapsulation of retrovirus allows efficient superinfection of resistant cell lines (1984)

Cell lines which are infected with retrovirus are resistant to superinfection by a related retrovirus. Packaging of whole virions within synthetic lipid vesicles allows efficient infection of such resistant cell lines. This system is more efficient in introducing encapsulated virus into infected cells than into uninfected cells.
Polymer Pen Lithography (2008)

We report a low-cost, high-throughput scanning probe lithography method that uses a soft elastomeric tip array, rather than tips mounted on individual cantilevers, to deliver inks to a surface in a "direct write" manner. Polymer pen lithography merges the feature size control of dip-pen nanolithography with the large-area capability of contact printing. Because ink delivery is time and force dependent, features on the nanometer, micrometer, and macroscopic length scales can be formed with the same tip array. Arrays with as many as about 11 million pyramid-shaped pens can be brought into contact with substrates and readily leveled optically to ensure uniform pattern development.