gebhart/patrepeval huggingface dataset:
Photochemical Internalization of Tamoxifens Transported by a “Trojan‐Horse” Nanoconjugate into Breast‐Cancer Cell Lines (2015)

Photochemical internalization (PCI) has shown great promise as a therapeutic alternative for targeted drug delivery by light-harnessed activation. However, it has only been applicable to therapeutic macromolecules or medium-sized molecules. Herein we describe the use of an amphiphilic, water-soluble porphyrin-β-cyclodextrin conjugate (mTHPP-βCD) as a "Trojan horse" to facilitate the endocytosis of CD-guest tamoxifens into breast-cancer cells. Upon irradiation, the porphyrin core of mTHPP-βCD expedited endosomal membrane rupture and tamoxifen release into the cytosol, as documented by confocal microscopy. The sustained complexation of mTHPP-βCD with tamoxifen was corroborated by 2D NMR spectroscopy and FRET studies. Following the application of PCI protocols with 4-hydroxytamoxifen (4-OHT), estrogen-receptor β-positive (Erβ+, but not ERβ-) cell groups exhibited extensive cytotoxicity and/or growth suspension even at 72 h after irradiation.
Selective Inhibition of HIV-1 Reverse Transcriptase by an Antiviral Inhibitor, (R)-9-(2-Phosphonylmethoxypropyl)adenine (1998)

(R)-9-(2-Phosphonylmethoxypropyl)adenine (PMPA) is an acyclic nucleoside phosphonate that has been shown to be effective in the treatment of AIDS although it has a shorter separation between the adenine and phosphorus than dideoxy-AMP and dAMP. By using pre-steady state kinetic methods, we examined the incorporation of the diphosphate of PMPA, 2',3'-dideoxyadenosine 5'-triphosphate (ddATP), and dATP catalyzed by wild-type human immunodeficiency virus type 1 (HIV-1) reverse transcriptase, an exonuclease-deficient T7 DNA polymerase (T7 exo-), and wild-type rat DNA polymerase beta in order to evaluate the selectivity of PMPA as an antiviral inhibitor. With a DNA/DNA or DNA/RNA 22/43-mer duplex, the diphosphate of PMPA (PMPApp) is as effective as ddATP in reactions catalyzed by HIV-1 reverse transcriptase in that both analogs have similar substrate specificity constants (kp/Kd) which are only 5-fold lower than dATP. In contrast, PMPApp is a much weaker inhibitor of the reaction catalyzed by T7 exo- (with the DNA/DNA 22/43-mer duplex) in that PMPApp has a 5 x 10(-4)-fold lower kp/Kd than ddATP and dATP. The lower kp/Kd of PMPApp is due to a 1000-2000-fold lower incorporation rate (kp) and a 35-45-fold lower binding constant (Kd). Similarly, PMPApp is 800-fold less inhibitory toward polymerase beta with the DNA/DNA 22/43-mer duplex, whereas in studies with a single nucleotide gapped DNA (22-20/43-mer) PMPApp is 13-fold less inhibitory than ddATP. Although parallel studies will need to be performed using appropriate human polymerases, these results begin to define the mechanistic basis for the reported lower toxicity of PMPA in the treatment of AIDS.
Inulin and Oligofructose Are Part of the Dietary Fiber Complex (1999)

Dietary fiber has been defined as the remnants of plant cells resistant to hydrolysis by human alimentary enzymes. Its main chemical constituents are hemicelluloses, celluloses, lignin, pectins, gums, and waxes. The U.S. Food and Drug Administration and the U.S. Department of Agriculture determine compliance with nutritional labeling regulations for dietary fiber by use of the existing AOAC INTERNATIONAL methods for total dietary fiber. The above compounds are readily detected by these methods. However, some oligo- and polysaccharides are resistant to human alimentary enzymes and do not precipitate in 78% ethanol, the usual reagent for precipitating dietary fiber in analytical procedures. Some of these saccharides, termed fructans, are inulin and oligofructose. They possess many physiological attributes normally associated with dietary fiber. Inulin is a mixture of oligo- and polysaccharides composed of fructose moieties joined by beta(2-->1) linkages in linear chains. Almost each chain ends with a glucose moiety. Oligofructose is a synonym for fructo-oligosaccharides, with fructose moieties joined by beta(2-->1) linkages, as in inulin. Not all molecules have a glucose unit, and the chain length is less than 10 units. A method for inulin and oligofructose was developed and approved official first action by AOAC INTERNATIONAL in early 1997. It involves extraction of sample and treatment of the extract with amyloglucosidase followed by fructozyme (Fructozyme Enzyme Process Division, Novo Nordisk, Novo Industry, Copenhagen, Denmark). The sugars released in each of the 3 steps are measured by anion-exchange chromatography. The concentration of fructans is calculated as the difference of sugars, glucose and fructose, after the enzymatic treatments and the initial sample. The repeatability standard deviations for inulin and oligofructose ranged from 2.9 to 5.8% and the reproducibility standard deviations ranged from 4.7 to 11.1%. The method was accepted by AOAC INTERNATIONAL.
Longitudinal bias method using a long distance exchange coupling field in tunnel magnetoresistance junctions (2001)

A longitudinal bias method using a long distance exchange coupling field, which was observed between an IrMn layer and a NiFe/CoFe bilayer across a Cu interlayer, has been investigated for magnetic read heads. The exchange coupling field could be changed in the layered film consisting of Ta/NiFe/Cu(0, 1.0, 1.5, 2.0 nm)/IrMn. In order to align the easy axes of the free and pinned ferromagnetic layers perpendicular to each other, a two-step annealing process was carried out to rotate the easy axis of the free layer in the tunnel magnetoresistive read heads. The angle between the two easy axes was 72° in the junction after an optimized two-step annealing. The tunnel magnetoresistive readers, which have a resistance×area product of about 2000 Ω μm2 and a tunnel magnetoresistance ratio of about 15%, showed an output voltage of 9080 μVp−p and 2270 μVp−p/μm, which was comparable to that of a typical giant magnetoresistive reader for a 7.5 Gbits/in.2 hard disk drive.
Cannabinoids in Autism and Fragile X Syndrome: Value-Based Treatment Revolution Ahead? (2017)

Journal of Intellectual & Developmental Disabilities in the field of intellectual and developmental disability. GJIDD journal is an open access peer reviewed scientific journal focused towards publishing a complete and reliable source of information origin
(P(C<sub>6</sub>H<sub>5</sub>)<sub>3</sub>)CpRu<sup>+</sup>‐Catalyzed Deprotection of Allyl Carboxylic Esters. (2002)

Abstract For Abstract see ChemInform Abstract in Full Text.
[The structure of the skin of the ear in domesticated pigs, with special reference to their use for human dermatological research. 2. Specific histology of the integument]. (2001)

Based on light microscopy, the study describes the specific histology of the ear integument of the white domesticated pig. After careful tissue fixation and embedding, routine histological staining, collagen fibre staining, fat demonstration based on frozen sections, and ink injection of the integumental blood vessel system were applied. A detailed description is presented of the structure of the skin layers (epidermis, dermis, hypodermis), the ear cartilage envelopes (fascia, perichondrium), the plica scaphae, the blood vessel distribution, the architecture of the collagen fibre bundles, as well as the hair follicles and the skin glands (sebaceous glands, apocrine tubular glands). The results are discussed with regard to a direct comparison with the histological structure of the human integument, and the advantages and disadvantages of the use of the porcine ear skin as model system in human dermatological research are emphasized.
<title>Migration to zero-offset in variable velocity media</title> (1994)

As a condition for further generalization of the migration to zero-offset in variable velocity media, I develop the theory for 2D migration to zero offset (MZO) in constant velocity media, starting from prestack migration in midpoint-offset coordinates. In arrive at an integral formulation for the MZO operator, analytically derived from the double square root (DSR) prestack migration equation. The integral formulation for the MZO is similar in form to the DSR equation, suggesting a generalization to variable velocity media using a phase-shift algorithm.
Parameter Identification of PM Motor System at Standstill (2003)

This paper proposes the on-line parameter identification method of PM motor system including inverter. The d and q-axis inductances, phase resistance and voltage drop of inverter can be identified from the detected currents and voltage references at standstill. The validity of the proposed method is confirmed by experimental results.
N-acetyl muramyl dipeptide stimulation of bone resorption in tissue culture (1982)

N-Acetyl-muramyl-L-alanyl-D-isoglutamine (MDP), a structurally defined fragment of bacterial peptidoglycan, stimulated significant release of previously incorporated 45Ca from fetal rat bones in tissue culture over the concentration range of 0.1 to 10.0 micrograms/ml. MDP-Stimulated bone resorption was not inhibited by the addition of the prostaglandin synthetase inhibitor indomethacin to the culture medium. MDP was neither mitogenic for nor stimulated the release of osteoclast-activating factor from cultured human peripheral blood mononuclear cells. Thus, MDP-stimulated bone resorption in vitro is mediated by a mechanism which is not dependent upon prostaglandins or osteoclast-activating factor. 6-O-Stearoyl-N-acetyl-muramyl-L-alanyl-D-isoglutamine, a lipophilic analog of MDP, was slightly more potent than MDP. Two diastereomers of MDP, N-acetyl-muramyl-L-alanyl-L-isoglutamine and N-acetyl-muramyl-D-alanyl-D-isoglutamine, which are inactive as adjuvants, were at least 1,000 times less active than MDP in stimulating bone resorption. The stereochemical specificity for bone-resorptive activity paralleled that required for adjuvant activity, macrophage activation, and activation of the reticuloendothelial system.
Single Intranasal Immunization with Recombinant Adenovirus-Based Vaccine Induces Protective Immunity against Respiratory Syncytial Virus Infection (2007)

Respiratory syncytial virus (RSV) is a major cause of severe lower respiratory tract disease in infancy and early childhood. Despite its importance as a pathogen, there is no licensed vaccine against RSV. The G glycoprotein of RSV, a major attachment protein, is a potentially important target for protective antiviral immune responses. Here, a recombinant replication-deficient adenovirus-based vaccine, rAd/3xG, expressing the soluble core domain of G glycoprotein (amino acids 130 to 230) engineered by codon optimization and tandem repetition for higher-level expression, was constructed and evaluated for its potential as an RSV vaccine in a murine model. A single intranasal immunization with rAd/3xG provided potent protection against RSV challenge which lasted for more than 10 weeks. Strong mucosal immunoglobulin A responses were also induced by a single intranasal immunization but not by intramuscular or oral administration of rAd/3xG. Interestingly, neither gamma interferon- nor interleukin-4-producing CD4 T cells directed to I-E(d)-restricted epitope were detected in the lungs of rAd/3xG-immune mice upon challenge, whereas priming with vaccinia virus expressing RSV G (vvG) elicited strong Th1/Th2 mixed CD4 T-cell responses. Lung eosinophilia and vaccine-induced weight loss were significantly lower in the rAd/3xG-immune group than in the vvG-primed group. Together, our data demonstrate that a single intranasal administration of rAd/3xG elicits beneficial protective immunity and represents a promising vaccine regimen against RSV infection.
Rifampicin Inhibition of Ribonucleic Acid and Protein Synthesis in Normal and Ethylenediaminetetraacetic Acid-Treated <i>Escherichia coli</i> (1970)

The kinetics of ribonucleic acid (RNA) and protein synthesis in rifampicin-inhibited normal and ethylenediaminetetraacetic acid (EDTA)-treated Escherichia coli was measured. Approximately 200-fold higher external concentrations of rifampicin were needed to produce a level of inhibition in normal cells comparable to that observed in EDTA-treated cells. The rates of RNA and protein synthesis in both kinds of cells decreased exponentially, after an initial lag phase, at all rifampicin concentrations tested. The lag phase was longer and the final exponential slope less for protein synthesis than for RNA synthesis at a given rifampicin concentration. Below certain rifampicin concentrations, both the lag phase and the subsequent exponential decrease in the rates of RNA and protein synthesis were found to be rifampicin concentration dependent. At greater concentrations only the time of the lag phase was decreased by higher rifampicin concentrations, whereas the slope of the exponential decrease in the rates of RNA and protein synthesis was unaffected. In all cases, the exponential decrease continued to at least a 99.8% inhibition of the original rate of synthesis. These in vivo results are consistent with the mode of rifampicin action determined from in vitro studies; rifampicin prevents initiations of RNA polymerase on deoxyribonucleic acid, but not its propagation, by binding the enzyme essentially irreversibly. The results also indicate the size distribution of messenger RNA molecules in E. coli under our conditions.
<title>Processing of transparent inorganic/organic hybrids using metal alkoxides and polydimethylsiloxane</title> (1997)

Transparent inorganic/organic hybrids containing various inorganic components have been synthesized from modified metal alkoxides and silanol-terminated polydimetylsiloxane (PDMS). The chemical modification of metal alkoxides with chelating ligands was carried out in order to prevent the precipitation during hydrolysis and condensation. The chemical modification and hydrolysis reaction were investigated by IR and NMR spectroscopic methods. The formation of transparent hybrids was found to be influenced by the inorganic source and M(OR)<SUB>n</SUB>/PDMS ratio. The transparent hybrids were flexible, indicating the storage modulus from 10<SUP>6</SUP> to 10<SUP>8</SUP> Pa at room temperatures. It increased with the increase in valence number of the inorganic components. The hybrids were transparent in the visible wavelength region, especially long- wavelength region. The refractive index of the hybrids linearly increased with increasing the inorganic content. The refractive index was also dependent on the inorganic component derived from metal alkoxides. It increased with valence of metallic elements in the inorganic components, in the order Al < Zr <EQ Ti < Ta <EQ Nb.
Meeting performance goals with the HP-UX workload manager (2000)

The HP-UX Workload Manager helps workloads meet user-specified performance goals by dynamically adjusting their access to resources such as CPU. We implemented this workload manager as a part of a feedback control system, using existing resource control and performance instrumentation infrastructure.
Controlling the Catalytic Aerobic Oxidation of Phenols (2014)

The oxidation of phenols is the subject of extensive investigation, but there are few catalytic aerobic examples that are chemo- and regioselective. Here we describe conditions for the ortho-oxygenation or oxidative coupling of phenols under copper (Cu)-catalyzed aerobic conditions that give rise to ortho-quinones, biphenols or benzoxepines. We demonstrate that each product class can be accessed selectively by the appropriate choice of Cu(I) salt, amine ligand, desiccant and reaction temperature. In addition, we evaluate the effects of substituents on the phenol and demonstrate their influence on selectivity between ortho-oxygenation and oxidative coupling pathways. These results create an important precedent of catalyst control in the catalytic aerobic oxidation of phenols and set the stage for future development of catalytic systems and mechanistic investigations.
Acoustic wave propagation along a fluid-filled cylinder (1974)

Phenomena of elastic wave propagation from a point source located in a fluid-filled cylinder are investigated. Detailed consideration is given to the natural mode wave propagation for either fluid or elastic solid surroundings of infinite extent. Phase and group velocity dispersion curves are presented and the relative modal sensitivity, interference pattern, and decay rates are determined for typical sources having various dominant wavelengths. Curves showing actual waveforms including both axial and radial dependence are also presented for this coupled system.
Transmissible encephalopathies and biopharmaceutical production. (1996)

The use of post-mortem tissues as sources for the production of biologicals, vaccines and feedstuffs has led to the transmission or generation of transmissible encephalopathies in some recipients. For example, the use of pituitary-derived human growth hormone and gonadotropins has resulted in the transmission of Creutzfeldt-Jakob disease to other humans [1], the use of formalin-inactivated sheep brain as a source for louping ill vaccine led to the transmission of scrapie to over 1,000 sheep from one vaccine lot [2], and the use of rendered products from ruminant carcasses in the domestic animal food chain led to the emergence and epizootic of bovine spongifrom encephalopathy in the United Kingdom [3]. Infection with transmissible encephalopathies by iatrogenic or other mechanisms is difficult to predict or control. The characteristics of these pathogens do not permit easy detection, clearance, or inactivation in routine biopharmaceutical production environments.
A clinical study of 22.5 mg. La-2550: A new subcutaneous depot delivery system for leuprolide acetate for the treatment of prostate cancer. (2002)

LA-2550 (22.5 mg. depot) produced and maintained safe and effective suppression of serum testosterone to well below the medical castrate level of 50 ng./dl. or less.
Transition‐state regulators: sentinels of <i>Bacillus subtilis</i> post‐exponential gene expression (1993)

When Bacillus subtilis encounters a nutrient-depleted environment, it expresses a wide variety of genes that encode functions in alternative pathways of metabolism and energy production. Expression of these genes first occurs during the transition from active growth into stationary phase and is controlled by a class of proteins termed transition-state regulators. In several instances, a given gene is redundantly controlled by two or more of these regulators and many of these regulators control genes in numerous different pathways. The AbrB, Hpr and Sin proteins are the best-studied examples of these regulatory molecules. Their role is to prevent inappropriate and possibly detrimental functions from being expressed during exponential growth when they are not needed. They serve as elements integrating sporulation with ancillary stationary-phase phenomena and appear to participate in the timing of early sporulation events and in fine-tuning the magnitude of gene expression in response to specific environmental conditions.
NH2-terminal Inactivation Peptide Binding to C-type–inactivated Kv Channels (2004)

In many voltage-gated K(+) channels, N-type inactivation significantly accelerates the onset of C-type inactivation, but effects on recovery from inactivation are small or absent. We have exploited the Na(+) permeability of C-type-inactivated K(+) channels to characterize a strong interaction between the inactivation peptide of Kv1.4 and the C-type-inactivated state of Kv1.4 and Kv1.5. The presence of the Kv1.4 inactivation peptide results in a slower decay of the Na(+) tail currents normally observed through C-type-inactivated channels, an effective blockade of the peak Na(+) tail current, and also a delay of the peak tail current. These effects are mimicked by addition of quaternary ammonium ions to the pipette-filling solution. These observations support a common mechanism of action of the inactivation peptide and intracellular quaternary ammonium ions, and also demonstrate that the Kv channel inner vestibule is cytosolically exposed before and after the onset of C-type inactivation. We have also examined the process of N-type inactivation under conditions where C-type inactivation is removed, to compare the interaction of the inactivation peptide with open and C-type-inactivated channels. In C-type-deficient forms of Kv1.4 or Kv1.5 channels, the Kv1.4 inactivation ball behaves like an open channel blocker, and the resultant slowing of deactivation tail currents is considerably weaker than observed in C-type-inactivated channels. We present a kinetic model that duplicates the effects of the inactivation peptide on the slow Na(+) tail of C-type-inactivated channels. Stable binding between the inactivation peptide and the C-type-inactivated state results in slower current decay, and a reduction of the Na(+) tail current magnitude, due to slower transition of channels through the Na(+)-permeable states traversed during recovery from inactivation.
Orbital Contributions to the Electron <mml:math xmlns:mml="http://www.w3.org/1998/Math/MathML" display="inline"><mml:mrow><mml:mi>g</mml:mi></mml:mrow></mml:math> Factor in Semiconductor Nanowires (2017)

Recent experiments on Majorana fermions in semiconductor nanowires [S. M. Albrecht, A. P. Higginbotham, M. Madsen, F. Kuemmeth, T. S. Jespersen, J. Nygård, P. Krogstrup, and C. M. Marcus, Nature (London) 531, 206 (2016)NATUAS0028-083610.1038/nature17162] revealed a surprisingly large electronic Landé g factor, several times larger than the bulk value-contrary to the expectation that confinement reduces the g factor. Here we assess the role of orbital contributions to the electron g factor in nanowires and quantum dots. We show that an L·S coupling in higher subbands leads to an enhancement of the g factor of an order of magnitude or more for small effective mass semiconductors. We validate our theoretical finding with simulations of InAs and InSb, showing that the effect persists even if cylindrical symmetry is broken. A huge anisotropy of the enhanced g factors under magnetic field rotation allows for a straightforward experimental test of this theory.
Evaluation of knee ligament surgery results with special emphasis on use of a scoring scale (1982)

We have designed a scoring scale for knee ligament surgery follow-up emphasizing evaluation of symptoms of instability. Instability is defined as "giving way" during activity. Our scoring scale was compared to a slightly modified Larson scale in patients with anteromedial and/or anterolateral instability, posterolateral and straight posterior instability, chondromalacia patellae, and meniscus lesion. The two scales gave basically the same results in patients with meniscus rupture. In patients with unstable knees, the new scale gave a significantly lower total score. Thus, the new scale evaluates functional impairment due to clinical instability better than the modified Larson scale. The total score, with the new scoring scale, corresponded to the patients' own opinion of function and to the presence or absence of signs of instability.