gebhart/patrepeval huggingface dataset:
Tumor targeting using liposomal antineoplastic drugs. (2008)

During the last years, liposomes (microparticulate phospholipid vesicles) have been used with growing success as pharmaceutical carriers for antineoplastic drugs. Fields of application include lipid-based formulations to enhance the solubility of poorly soluble antitumor drugs, the use of pegylated liposomes for passive targeting of solid tumors as well as vector-conjugated liposomal carriers for active targeting of tumor tissue. Such formulation and drug targeting strategies enhance the effectiveness of anticancer chemotherapy and reduce at the same time the risk of toxic side-effects. The present article reviews the principles of different liposomal technologies and discusses current trends in this field of research.
Human Endogenous Retroviral Element K10 (HERV-K10) Encodes a Full-Length Gag Homologous 73-kDa Protein and a Functional Protease (1993)

The gag-homologous region of the human endogenous retrovirus K10 (HERV-K10) was amplified by PCR from human genomic DNA and was analyzed by DNA cloning, sequencing, and expression of open reading frames in the prokaryotic pATH expression system. The analysis of genomic DNA of three donors provided evidence that HERV-K10 genes contain an open reading frame of 1966 bp spanning the entire gag-homologous region. In the prokaryotic system the entire reading frame of the HERV-K10 gag gene could be expressed as a fusion protein exhibiting a molecular weight of about 110,000. In addition, when the gag-homologous region and the adjacent HERV-K10 protease gene were prokaryotically expressed, we observed a Gag-protease fusion protein that exhibited specific autoproteolytic activities and processing of HERV-K10 Gag protein. By introducing deletions on the right end of the putative protease gene an autocatalytic site could be localized within 300 bp of the putative HERV-K10 protease gene. For the first time, these results provide evidence that the HERV-K10 encodes a full-length Gag protein and a functional protease.
Sketch-to-photo matching: a feature-based approach (2010)

This paper presents a local feature-based method for matching facial sketch images to face photographs, which is the first known feature-based method for performing such matching. Starting with a training set of sketch to photo correspondences (i.e. a set of sketch and photo images of the same subjects), we demonstrate the ability to match sketches to photos: (1) directly using SIFT feature descriptors, (2) in a "common representation" that measures the similarity between a sketch and photo by their distance from the training set of sketch/photo pairs, and (3) by fusing the previous two methods. For both matching methods, the first step is to sample SIFT feature descriptors uniformly across all the sketch and photo images. In direct matching, we simply measure the distance of the SIFT descriptors between sketches and photos. In common representation matching, the distance between the descriptor vectors of the probe sketches and gallery photos at each local sample point is measured. This results in a vector of distances across the sketch or photo image to each member of the training basis. Further recognition improvements are shown by score level fusion of the two sketch matchers. Compared with published sketch to photo matching algorithms, experimental results demonstrate improved matching performances using the presented feature-based methods.
Nonlinear Periodization Maximizes Strength Gains in Split Resistance Training Routines (2009)

The purpose of our study was to compare strength gains after 12 weeks of nonperiodized (NP), linear periodized (LP), and nonlinear periodized (NLP) resistance training models using split training routines. Twenty-seven strength-trained men were recruited and randomly assigned to one of 3 balanced groups: NP, LP, and NLP. Strength gains in the leg press and in the bench press exercises were assessed. There were no differences between the training groups in the exercise pre-tests (p > 0.05) (i.e., bench press and leg press). The NLP group was the only group to significantly increase maximum strength in the bench press throughout the 12-week training period. In this group, upper-body strength increased significantly from pre-training to 4 weeks (p < 0.0001), from 4 to 8 weeks (p = 0.004), and from 8 weeks to the post-training (p < 0.02). The NLP group also exhibited an increase in leg press 1 repetition maximum at each time point (pre-training to 4 weeks, 4-8 week, and 8 weeks to post-training, p < 0.0001). The LP group demonstrated strength increases only after the eight training week (p = 0.02). There were no further strength increases from the 8-week to the post-training test. The NP group showed no strength increments after the 12-week training period. No differences were observed in the anthropometric profiles among the training models. In summary, our data suggest that NLP was more effective in increasing both upper- and lower-body strength for trained subjects using split routines.
Calf spleen purine nucleoside phosphorylase: purification, sequence and crystal structure of its complex with an N(7)‐acycloguanosine inhibitor (1995)

Calf spleen purine nucleoside phosphorylase was purified to homogeneity and its amino acid sequence was determined. The complex of the enzyme with an N(7)-acycloguanosine inhibitor crystallized in the cubic space group P2(1)3, with unit cell dimension a = 94.02 A and one monomer in the asymmetric crystal unit. The biologically active trimer is formed by the crystallographic three-fold axis. The structure was solved by molecular replacement methods, using the model of the human erythrocyte enzyme, and refined at a resolution of 2.9 A to an R-factor of 0.21. The orientation of the inhibitor at the active site is examined in relation to the catalytic activity of the enzyme in the phosphorolysis of N(7)-beta-D-purine nucleosides.
Lytic action of cloned pneumococcal phage lysis genes in Streptococcus pneumoniae (1993)

The genes hbl3, cpl1 and cpl7 coding for the pneumococcal phage lytic enzymes HBL3, CPL1 and CPL7, respectively, have been cloned into shuttle plasmids that can replicate in Streptococcus pneumoniae and Escherichia coli. All these genes were expressed in E. coli under the control of either the lytP promoter of the lytA gene, which codes for the major pneumococcal autolysin, or the promoter of the tetracycline-resistance gene (tetP). In contrast, cpl1 and cpl7 genes that code for lysozymes were expressed in pneumococcus only under the control of tetP, whereas the hbl3 gene that codes for an amidase can be expressed using either promoter. The phage lysozymes or amidase expressed in S. pneumoniae M31, a mutant deleted in the lyA gene coding for short chains, were placed under physiological control since these transformed bacteria grew as normal ‘diplo’ cells during the exponential phase and underwent autolysis only after long incubation at 37°C. The lysis genes appear to be expressed constitutively in the transformed pneumococci, since sharply defined lysis of these cultures could be induced prematurely during the exponential phase of growth by addition of sodium deoxycholate.
Lactate shuttles at a glance: from physiological paradigms to anti-cancer treatments (2011)

Hypoxia and oncogene expression both stimulate glycolytic metabolism in tumors, thereby leading to lactate production. However, lactate is more than merely a by-product of glycolysis: it can be used as a metabolic fuel by oxidative cancer cells. This phenomenon resembles processes that have been described for skeletal muscle and brain that involve what are known as cell-cell and intracellular lactate shuttles. Two control points regulate lactate shuttles: the lactate dehydrogenase (LDH)-dependent conversion of lactate into pyruvate (and back), and the transport of lactate into and out of cells through specific monocarboxylate transporters (MCTs). In tumors, MCT4 is largely involved in hypoxia-driven lactate release, whereas the uptake of lactate into both tumor cells and tumor endothelial cells occurs via MCT1. Translating knowledge of lactate shuttles to the cancer field offers new perspectives to therapeutically target the hypoxic tumor microenvironment and to tackle tumor angiogenesis.
Efficient side lobe suppression of laser diode arrays (1987)

An optical technique is described which converts multilobed far-field patterns from in-phase laser arrays into a single-lobed pattern. The technique redistributes the output light from the laser array to produce a uniformly illuminated aperture. This filled aperture produces negligible side lobes, and efficiently channels the array power into the main lobe. Experiments performed on a ten-element Y-guide laser array show an increase in main lobe power from 51 to 90% of the total array power.
Epithelial Expression and Chromosomal Location of HumanTLEGenes: Implications for Notch Signaling and Neoplasia (1996)

The TLE genes are the human homologues of Drosophila groucho, a member of the Notch signaling pathway. This pathway controls a number of different cell-fate choices in invertebrates and vertebrates. We are interested in investigating the functions of the TLE gene family during epithelial determination and carcinogenesis. We show that expression of individual TLE genes correlates with immature epithelial cells that are progressing toward their terminally differentiated state, suggesting a role during epithelial differentiation. In both normal tissues and conditions resulting from incorrect or incomplete maturation events, such as metaplastic and neoplastic transformations, TLE expression is elevated and coincides with Notch expression, implicating these molecules in the maintenance of the undifferentiated state in epithelial cells. We also show that TLE1 and TLE2 are organized in a tandem array at chromosomal location 19p13.3, while TLE3 maps to 15q22.
Magnetic self-assembly of three-dimensional surfaces from planar sheets (2005)

This report describes the spontaneous folding of flat elastomeric sheets, patterned with magnetic dipoles, into free-standing, 3D objects that are the topological equivalents of spherical shells. The path of the self-assembly is determined by a competition between mechanical and magnetic interactions. The potential of this strategy for the fabrication of 3D electronic devices is demonstrated by generating a simple electrical circuit surrounding a spherical cavity.
Biochemical Characterisation of Ornithine Carbamoyltransferase from Pyrococcus Furiosus (1997)

Ornithine carbamoyltransferase (OTCase) was purified to homogeneity from the hyperthermophilic archaeon Pyrococcus furiosus. The enzyme is a 400 +/- 20-kDa polymer of a 35-kDa subunit, in keeping with the corresponding gene sequence [Roovers, M., Hethke, C., Legrain, C., Thomm, M. & Glansdorff, N. (1997) Isolation of the gene encoding Pyrococcus furiosus ornithine cabamoyltransferase and study of its expression profile in vivo and in vitro, Eur. J. Biochem. 247, 1038-1045]. In contrast with the dodecameric catabolic OTCase of Pseudomonas aeruginosa, P. furiosus OTCase exhibits no substrate cooperativity. In keeping with other data discussed in the text, this suggests that the enzyme serves an anabolic function. Half-life estimates for the purified enzyme ranged over 21-65 min at 100 degrees C according to the experimental conditions and reached several hours in the presence of ornithine and phosphate. The stability was not markedly influenced by the protein concentration. Whereas comparative examination of OTCase sequences did not point to any outstanding feature possibly related to thermophily, modelling the enzyme on the X-ray structure of P. aeruginosa OTCase (constituted by four trimers assembled in a tetrahedral manner) suggests that the molecule is stabilized, at least in part, by a set of hydrophobic interactions at the interfaces between the trimers. The comparison between P. aeruginosa and P. furiosus OTCases suggests that two different properties, allostery and thermostability, have been engineered starting from a similar quaternary structure of high internal symmetry. Recombinant P. furiosus OTCase synthesised by Escherichia coli proved less stable than the native enzyme. In Saccharomyces cerevisiae, however, an enzyme apparently identical to the native one could be obtained.
A New Method for the Synthesis of Tri-tert-butyl Diethylenetriaminepentaacetic Acid and Its Derivatives (2000)

ADVERTISEMENT RETURN TO ISSUEPREVNoteNEXTA New Method for the Synthesis of Tri-tert-butyl Diethylenetriaminepentaacetic Acid and Its DerivativesSamuel Achilefu, R. Randy Wilhelm, Hermo N. Jimenez, Michelle A. Schmidt, and Ananth SrinivasanView Author Information Discovery Research, Mallinckrodt, Inc., St. Louis, Missouri 63042 Cite this: J. Org. Chem. 2000, 65, 5, 1562–1565Publication Date (Web):February 12, 2000Publication History Received14 September 1999Published online12 February 2000Published inissue 1 March 2000https://pubs.acs.org/doi/10.1021/jo991453thttps://doi.org/10.1021/jo991453tbrief-reportACS PublicationsCopyright © 2000 American Chemical SocietyRequest reuse permissionsArticle Views806Altmetric-Citations30LEARN 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:Conjugate acid-base pairs,Metals,Peptides and proteins,Reaction products,Redox reactions Get e-Alerts
Desaggregation of Human Red Blood Cells by Various Surface-Active Agents as Related to Changes of Cell Shape and Hemolysis (1975)

The effect of several surface-active substances (Na-oleate, Na-desoxycholate, Triton X 100, Pluronic F 38, Pluronic F 68, Pluronic F 108) on dextran-induced red cell aggregation (RCA) and red cell shape was investigated. Sedimentation measurements and photometric determinations of RCA indicated a desaggregating effect of oleate, Triton, F 38 and F 68. Shape changes were found in the presence of oleate and desoxycholate (crenation) and Triton (cup formation); in addition, these substances induced pronounced hemolysis. No hemolysis and no shape changes were found with any of the Pluronic polyols.
Wide-aperture microwave catheter-based cardiac ablation (2003)

This study investigates a novel means of treating cardiac arrhythmias using microwave heating. A catheter-based spiral antenna, approximately one wavelength in circumference, produces wide, deep ablation in in vivo cardiac tissue. The spiral antenna is designed to be inserted transluminally, in a straightened state, and then released to re-form when in position within the heart. A balloon inflated with electrically non-conducting fluid surrounds the spiral to direct power forward into the cardiac tissue, and to prevent surface overheating.
Bacterial phenylalanine and phenylacetate catabolic pathway revealed (2010)

Aromatic compounds constitute the second most abundant class of organic substrates and environmental pollutants, a substantial part of which (e.g., phenylalanine or styrene) is metabolized by bacteria via phenylacetate. Surprisingly, the bacterial catabolism of phenylalanine and phenylacetate remained an unsolved problem. Although a phenylacetate metabolic gene cluster had been identified, the underlying biochemistry remained largely unknown. Here we elucidate the catabolic pathway functioning in 16% of all bacteria whose genome has been sequenced, including Escherichia coli and Pseudomonas putida. This strategy is exceptional in several aspects. Intermediates are processed as CoA thioesters, and the aromatic ring of phenylacetyl-CoA becomes activated to a ring 1,2-epoxide by a distinct multicomponent oxygenase. The reactive nonaromatic epoxide is isomerized to a seven-member O-heterocyclic enol ether, an oxepin. This isomerization is followed by hydrolytic ring cleavage and beta-oxidation steps, leading to acetyl-CoA and succinyl-CoA. This widespread paradigm differs significantly from the established chemistry of aerobic aromatic catabolism, thus widening our view of how organisms exploit such inert substrates. It provides insight into the natural remediation of man-made environmental contaminants such as styrene. Furthermore, this pathway occurs in various pathogens, where its reactive early intermediates may contribute to virulence.
Transcript from 2017 Mitchell Hamline Trade Secret Conference, Cybaris scholar symposium (2017)

Transcript of a panel discussion on trade secret law held April 21, 2017 at Mitchell Hamline School of Law in St. Paul, Minnesota. Panelists: Rochelle Dreyfuss, Christoph Rademacher, Susy Frankel, and Nari Lee.Moderator: Sharon Sandeen.
Semipermeable membranes of cellulose acetate for desalination in the process of reverse osmosis. II. Parameters affecting membrane gel structure (1965)

A quantitative study has been made of the effects on the membrane gel structure of parameters whose significance with respect to desalination performance had previously been empirically established. The composition of the polymer solutions, the fabrication temperatures, and the pressure employed during desalination are shown to be related, in that they all influence the swelling behavior of the gel structure. The relationship which has been found between the water content and the rate of water transport across semipermeable membranes of cellulose acetate is explained on the basis of a solution transport mechanism.
Systolic time intervals: a review of the method in the non-invasive investigation of cardiac function in health, disease and clinical pharmacology (1983)

Measurement of systolic time intervals is a valuable, non-invasive procedure to assess left ventricular performance, particularly when influenced by drugs. In this review, we discuss various factors affecting systolic time intervals, the therapeutic implications of the technique and its place among other non-invasive tests of cardiac function.
Rates of HIV‐1 Transmission per Coital Act, by Stage of HIV‐1 Infection, in Rakai, Uganda (2005)

The rate of HIV transmission per coital act was highest during early-stage infection. This has implications for HIV prevention and for projecting the effects of antiretroviral treatment on HIV transmission.
Purification, sequence, and model structure of charybdotoxin, a potent selective inhibitor of calcium-activated potassium channels. (1988)

Charybdotoxin (ChTX), a protein present in the venom of the scorpion Leiurus quinquestriatus var. hebraeus, has been purified to homogeneity by a combination of ion-exchange and reversed-phase chromatography. Polyacrylamide gel electrophoresis, amino acid analysis, and complete amino acid sequence determination of the pure protein reveal that it consists of a single polypeptide chain of 4.3 kDa. Purified ChTX is a potent and selective inhibitor of the approximately 220-pS Ca2+-activated K+ channel present in GH3 anterior pituitary cells and primary bovine aortic smooth muscle cells. The toxin reversibly blocks channel activity by interacting at the external pore of the channel protein with an apparent Kd of 2.1 nM. The primary structure of ChTX is similar to a number of neurotoxins of diverse origin, which suggests that ChTX is a member of a superfamily of proteins that modify ion-channel activities. On the basis of this similarity, the three-dimensional structure of ChTX has been modeled from the known crystal structure of alpha-bungarotoxin. These studies indicate that ChTX is useful as a probe of Ca2+-activated K+-channel function and suggest that the proposed tertiary structure of ChTX may provide insight into the mechanism of channel block.
Seliciclib (CYC202, R-Roscovitine) Induces Cell Death in Multiple Myeloma Cells by Inhibition of RNA Polymerase II–Dependent Transcription and Down-regulation of Mcl-1 (2005)

Seliciclib (CYC202, R-roscovitine) is a cyclin-dependent kinase (CDK) inhibitor that competes for the ATP binding site on the kinase. It has greatest activity against CDK2/cyclin E, CDK7/cyclin H, and CDK9/cyclin T. Seliciclib induces apoptosis from all phases of the cell cycle in tumor cell lines, reduces tumor growth in xenografts in nude mice and is currently in phase II clinical trials. This study investigated the mechanism of cell death in multiple myeloma cells treated with seliciclib. In myeloma cells treated in vitro, seliciclib induced rapid dephosphorylation of the carboxyl-terminal domain of the large subunit of RNA polymerase II. Phosphorylation at these sites is crucial for RNA polymerase II-dependent transcription. Inhibition of transcription would be predicted to exert its greatest effect on gene products where both mRNA and protein have short half-lives, resulting in rapid decline of the protein levels. One such gene product is the antiapoptotic factor Mcl-1, crucial for the survival of a range of cell types including multiple myeloma. As hypothesized, following the inhibition of RNA polymerase II phosphorylation, seliciclib caused rapid Mcl-1 down-regulation, which preceded the induction of apoptosis. The importance of Mcl-1 was confirmed by short interfering RNA, demonstrating that reducing Mcl-1 levels alone was sufficient to induce apoptosis. These results suggest that seliciclib causes myeloma cell death by disrupting the balance between cell survival and apoptosis through the inhibition of transcription and down-regulation of Mcl-1. This study provides the scientific rationale for the clinical development of seliciclib for the treatment of multiple myeloma.
Predictors of Atrasentan-Associated Fluid Retention and Change in Albuminuria in Patients with Diabetic Nephropathy (2015)

In the Reducing Residual Albuminuria in Subjects With Diabetes and Nephropathy With Atrasentan/JAPAN trials, atrasentan-associated fluid retention was more likely in patients with diabetes and nephropathy who had lower eGFR or received a higher dose of atrasentan. Finding that albuminuria reduction was not associated with changes in body weight and Hb suggests that the albuminuria-reducing efficacy of atrasentan is not impaired by fluid retention.