gebhart/patrepeval huggingface dataset:
Competition between trichodermin and several other sesquiterpene antibiotics for binding to their receptor site(s) on eukaryotic ribosomes (1976)

1. Of the five sesquiterpene antibiotics tested and found to inhibit protein synthesis in yeast spheroplasts, trichothecin, trichodermol or trichodermin stabilized polyribosomes whereas, in contrast, verrucarin A or T-2 toxin induced 'run off' of polyribosomes with a corresponding increase in 80S monoribosomes. The effect of fusarenon X on the system could not be determined as the drug failed to enter the cells. 2. [acetyl-14C]Trichodermin bound to yeast polyribosomes with a dissociation constant of 2.10 muM and to yeast 'run off' ribosomes with a dissociation constant of 0.72 muM. 3. Trichothecin, trichodermol, fusarenon X, T-2 toxin and verrucarin A competed with [acetyl-14C]trichodermin for binding to its receptor site on 'run off' ribosomes. The observed competition was quantitatively similar for all drugs tested. In contrast, the five drugs competed to different extents with trichodermin for binding to its receptor site on polyribosomes. Thus trichothecin competed with relative efficiency, whereas verrucarin A competed poorly, and the other drugs occupied intermediate positions between these two extremes. 4. Studies were also carried out with yeast 'run off' ribosomes prepared from both a wild-type strain and a strain resistant to trichodermin. Competition experiments between verrucarin A and [3H]anisomycin indicated that verrucarin A bound to 'run off' ribosomes from the mutant strain less efficiently than to those from the wild-type.
rf-SQUID-Mediated Coherent Tunable Coupling between a Superconducting Phase Qubit and a Lumped-Element Resonator (2010)

We demonstrate coherent tunable coupling between a superconducting phase qubit and a lumped-element resonator. The coupling strength is mediated by a flux-biased rf SQUID operated in the nonhysteretic regime. By tuning the applied flux bias to the rf SQUID we change the effective mutual inductance, and thus the coupling energy, between the phase qubit and resonator. We verify the modulation of coupling strength from 0 to 100 MHz by observing modulation in the size of the splitting in the phase qubit's spectroscopy, as well as coherently by observing modulation in the vacuum Rabi oscillation frequency when on resonance. The measured spectroscopic splittings and vacuum Rabi oscillations agree well with theoretical predictions.
Quantitative structure‐activity analysis of larvicidal 1‐(substituted benzoyl)‐2‐benzoyl‐1‐tert‐butylhydrazines against Chilo suppressalis (1994)

Abstract The larvicidal activity of a number of 1‐(substituted benzoyl)‐2‐benzoyl–1 ‐ten ‐butylhydrazines against the rice stem borer ( Chilo suppressalis Walk.) was measured. Variations in the activity were examined quantitatively using physico‐chemical substituent and molecular parameters and regression analysis. The results indicated that the molecular hydrophobicity and the electron‐withdrawing inductive/ field effect of ontho substituents are favourable to larvicidal activity. The bulkiness of substituents at the meta and para positions was unfavourable to activity, substitution at the para position being more unfavourable than that at the meta position in terms of van der Waals' volume. The 2,3–, 2,5‐ and 2,6‐disubstitution patterns were also unfavourable to activity. Reductions in larvicidal activity caused by the 2,6‐,‐ 2,3,5‐ and 2,3,4,5‐substitutions were greater than those induced by the 2,3‐ and 2,5‐disubstitutions. When the sum of contributions from favourable effects is greater than that from unfavourable effects, the larvicidal activity is expected to be superior to that of the unsubstituted compound.
Cessation of neutrophil influx in C5a-induced acute experimental arthritis is associated with loss of chemoattractant activity from the joint space. (1989)

Neutrophil emigration is a critical component of the inflammatory process and is generally thought to play a role in host defense as well as in the tissue injury that often accompanies inflammation. Most inflammatory reactions exhibit a sequence of emigrating cell types, thus clearly demonstrating that the neutrophil influx eventually ceases and that the neutrophils are then removed from the lesion. It has been our premise that in order to understand the processes that lead to the progressive inflammatory reactions that underly so many disease processes, it is important to determine the mechanism by which the "normal" inflammatory response resolves. The purpose of this study was to identify the time of cessation of neutrophil influx in experimental arthritis induced by the injection of C5 fragments (C5f) and to investigate mechanisms underlying the cessation process. The migration of i.v. delivery pulses to inflamed joints was assessed by lavage of the joint space and by external scintigraphy. We found no evidence for the development of inhibitory systems against chemotactic factors or "desensitization" of the inflamed site, because a second injection of C5f into joints which had been injected previously with C5f resulted in enhancement rather than inhibition of migration. Neither was evidence found for altered tissue barriers to migration or for desensitization of neutrophils as possible explanations for cessation of influx. The major mechanism appeared to be a loss of chemoattractant activity in the joint space between 2 h and 6 h after C5f injection which was detected by transfer into a fresh joint. Radiolabeled C5a des-Arg had a t1/2 of disappearance from the joint of less than 1 h, which suggested that the transferred chemoattractant must, in part, have been due to the generation of new chemotaxins by C5f injection. These observations suggest that continued generation of chemoattractants or failure of their subsequent removal may be mechanisms leading to persistent neutrophil influx in chronic inflammation.
Bibliografías especializadas en la biblioteca histórica de la Universidad Complutense (2009)

A partir de un trabajo de investigacion iniciado hace unos anos se da cuenta del fin propuesto consistente en la elaboracion de un catalogo en el que se reunieran los repertorios bibliograficos (bibliografias y catalogos de todo tipo) publicados entre 1501 y 1801 y que estuvieran conservados en la Biblioteca Historica de la Universidad Complutense, las fases del trabajo y la descripcion de cada uo de los repertorios.
Dynamic epidermal cooling in conjunction with laser‐induced photothermolysis of port wine stain blood vessels (1996)

When a cryogen spurt is applied to the skin surface for an appropriately short period of time (on the order of tens of milliseconds), the spatial distribution of cooling remains localized in the normal overlying epidermis, while leaving the temperature of the deeper port wine stain (PWS) blood vessels unchanged. Furthermore, cooling continues after pulsed laser exposure as cryogen remaining on the surface evaporates and removes heat deposited by light absorption in epidermal melanin. An additional advantage of dynamic cooling is a reduction in the level of pain and discomfort associated with flashlamp-pumped pulsed dye laser therapy of PWS. Preliminary clinical studies and supporting theoretical calculations demonstrate the feasibility of selective epidermal cooling while achieving photothermolysis of blood vessels during pulsed laser treatment of PWS. © 1996 Wiley-Liss, Inc.
Auto-WEKA : combined selection and hyperparameter optimization of supervised machine learning algorithms (2014)

Many different machine learning algorithms exist; taking into account each algorithm's set of hyperparameters, there is a staggeringly large number of possible choices. This project considers the problem of simultaneously selecting a learning algorithm and setting its hyperparameters. Previous works attack these issues separately, but this problem can be addressed by a fully automated approach, in particular by leveraging recent innovations in Bayesian optimization. The WEKA software package provides an implementation for a number of feature selection and supervised machine learning algorithms, which we use inside our automated tool, Auto-WEKA. Specifically, we examined the 3 search and 8 evaluator methods for feature selection, as well as all of the classification and regression methods, spanning 2 ensemble methods, 10 meta-methods, 27 base algorithms, and their associated hyperparameters. On 34 popular datasets from the UCI repository, the Delve repository, the KDD Cup 09, variants of the MNIST dataset and CIFAR-10, our method produces classification and regression performance often much better than obtained using state-of-the-art algorithm selection and hyperparameter optimization methods from the literature. Using this integrated approach, users can more effectively identify not only the best machine learning algorithm, but also the corresponding hyperparameter settings and feature selection methods appropriate for that algorithm, and hence achieve improved performance for their specific classification or regression task.
Opsonic properties of C-reactive protein. Stimulation by phorbol myristate acetate enables human neutrophils to phagocytize C-reactive protein-coated cells. (1985)

We examined phagocytosis of sheep erythrocytes passively sensitized with pneumococcal C-polysaccharide (E-PnC) and of E-PnC coated with C-reactive protein (E-PnC-CRP) by human polymorphonuclear leukocytes (PMN). PMN isolated from blood of normal individuals failed to ingest either E-PnC or E-PnC-CRP; however, after stimulation with 12-O-tetradecanoylphorbol-13-acetate (PMA; 2 ng/ml), PMN ingested E-PnC-CRP efficiently with a mean phagocytic index (PI) of 99.5 +/- 4.8 (mean +/- SD, n = 11), and E-PnC to a lesser extent with a mean PI of 33.2 +/- 11.7 (mean +/- SD, n = 11). PMN that had adhered to PnC-coated glass and that were stimulated with PMA attached but did not ingest E-PnC-CRP. In contrast, PMN plated on E-PnC-CRP-coated glass and stimulated with PMA did not attach or ingest E-PnC-CRP. These data indicate that PMN can be induced to phagocytize PnC-CRP and that both PnC and CRP are required for ingestion. They also suggest that specific receptors for these ligands are expressed by stimulated PMN. Neither attachment nor phagocytosis of E coated with rabbit anti-E IgG (E-IgG) was affected by plating PMN on PnC or PnC-CRP. On the other hand, both phagocytosis and ingestion of E-PnC-CRP as well as E-IgG was blocked by plating PMA-stimulated PMN on immune complexes containing rabbit IgG. Inhibition experiments with the use of 3G8, a monoclonal antibody to the Fc gamma receptor of PMN, and human monomeric IgG1 demonstrated that attachment of E-PnC-CRP is mediated by receptors other than the Fc gamma receptors. These combined results indicated a nonreciprocal association between the putative CRP receptors and the Fc gamma receptors of stimulated PMN, resulting in the clearance of both types of receptors from the apical surface of PMN by antigen-immobilized rabbit IgG.
<p>Potential New Cancer Immunotherapy: Anti-CD47-SIRPα Antibodies</p> (2020)

CD47 belongs to immunoglobulin superfamily and is widely expressed on the surface of cell membrane, while another transmembrane protein SIRPα is restricted to the surface of macrophages, dendritic cells, and nerve cells. As a cell surface receptor and ligand, respectively, CD47 and SIRPα interact to regulate cell migration and phagocytic activity, and maintain immune homeostasis. In recent years, studies have found that immunoglobulin superfamily CD47 is overexpressed widely across tumor types, and CD47 plays an important role in suppressing phagocytes activity through binding to the transmembrane protein SIRPα in phagocytic cells. Therefore, targeting CD47 may be a novel strategy for cancer immunotherapy, and a variety of anti-CD47 antibodies have appeared, such as humanized 5F9 antibody, B6H12 antibody, ZF1 antibody, and so on. This review mainly describes the research history of CD47-SIRPα and focuses on macrophage-mediated CD47-SIRPα immunotherapy of tumors.
Matrix metalloproteinases and angiogenesis (2005)

Matrix metalloproteinases (MMPs) are a family of enzymes that proteolytically degrade various components of the extracellular matrix (ECM). Angiogenesis is the process of forming new blood vessels from existing ones and requires degradation of the vascular basement membrane and remodeling of the ECM in order to allow endothelial cells to migrate and invade into the surrounding tissue. MMPs participate in this remodeling of basement membranes and ECM. However, it has become clear that MMPs contribute more to angiogenesis than just degrading ECM components. Specific MMPs have been shown to enhance angiogenesis by helping to detach pericytes from vessels undergoing angiogenesis, by releasing ECM-bound angiogenic growth factors, by exposing cryptic proangiogenic integrin binding sites in the ECM, by generating promigratory ECM component fragments, and by cleaving endothelial cell-cell adhesions. MMPs can also contribute negatively to angiogenesis through the generation of endogenous angiogenesis inhibitors by proteolytic cleavage of certain collagen chains and plasminogen and by modulating cell receptor signaling by cleaving off their ligand-binding domains. A number of inhibitors of MMPs that show antiangiogenic activity are already in early stages of clinical trials, primarily to treat cancer and cancer-associated angiogenesis. However, because of the multiple effects of MMPs on angiogenesis, careful testing of these MMP inhibitors is necessary to show that these compounds do not actually enhance angiogenesis.
A simple method for the determination of individual rate constants for substrate hydrolysis by serine proteases (2000)

A simple method is presented for the determination of individual rate constants for substrate hydrolysis by serine proteases and other enzymes with similar catalytic mechanism. The method does not require solvent perturbation like viscosity changes, or solvent isotope effects, that often compromise nonspecifically the activity of substrate and enzyme. The rates of substrate diffusion into the active site (k1), substrate dissociation (k-1), acylation (k2), and deacylation (k3) in the accepted mechanism of substrate hydrolysis by serine proteases are derived from the temperature dependence of the Michaelis-Menten parameters kcat/Km and kcat. The method also yields the activation energies for these molecular events. Application to wild-type and mutant thrombins reveals how the various steps of the catalytic mechanism are affected by Na+-binding and site-directed mutations of the important residues Y225 in the Na+ binding environment and L99 in the S2 specificity site. Extension of this method to other proteases should enable the derivation of detailed information on the kinetic and energetic determinants of protease function.
New Triterpenes of Lantana camara . A Comparative Study of the Constituents of Several Taxa (1976)

The triterpenes of Lantana camara vary widely between taxa. In taxa toxic to livestock 22ß-angeloyloxy-3-oxoolean-12-en-28-oic acid (lantadene A) and 22ß-dimethylacryloyloxy-3-oxoolean-12-en-28- oic acid (lantadene B) are present, usually as major constituents, although 3-oxolup-20(29)-en-28-oic acid (betulonic acid) predominates in the taxon Helidon White. 22ß-Angeloyloxy-3ß-hydroxyolean- 12-en-28-oic acid, 22ß -dimethylacryloyloxy-3ß -hydroxyolean-12-en-28-oic acid and 22ß-hydroxy-3-oxoolean-12-en-28-oic acid, not previously known to occur in L. camara , have been isolated as well as a number of other well-known triterpenes. The non-toxic Townsville Prickly Orange contains small amounts of lantadenes A and B, and is the only taxon found to contain 228-angeloyloxy-23- hydroxy-3-oxoo1ean-12-en-28-oic acid (icterogenin). Another constituent is the new triterpene 24-hydroxy-3-oxoolean-12-en-28-oic acid. Common Pink, which is non-toxic and does not contain lantadenes A and B, is characterized by triterpene acids which have a C3, C25 oxide-bridge. It contains lantanolic acid, lantic acid, and a new acid, lantabetulic acid, considered to be 3,25-epoxy- 3a-hydroxylup-20(29)-en-28-oic acid. A mixture of the 22ß-angeloyloxy and 22ß-dimethylacryloyloxy derivatives of lantanolic acid from Common Pink has been converted into 22P-hydroxylantanolic acid. Wolff-Kishner reduction of 22~-hydroxy-3-oxoolean-12-en-28-oic acid gives a low yield of 22ß-hydroxyolean-12-en-28-oic acid, and the major product is the C22-epimer, 22a-hydroxyolean- 12-en-28-oic acid. Corresponding products are obtained from Wolff-Kishner reduction of 22ß- hydroxylantanolic acid.
Improving the Binding Characteristics of Tripodal Compounds on Single Layer Graphene (2013)

Graphene is an atomically thin, transparent, and conductive electrode material of interest for sensors and energy conversion and storage devices, among others. Fully realizing its potential will require robust and general methods to anchor active functionality onto its pristine basal plane. Such strategies should not utilize covalent bond formation, which disrupts the graphene’s π-electron system, from which most of its desirable properties arise. We recently introduced a tripodal binding motif, which forms robust monolayers on graphene capable of immobilizing active proteins and preventing their denaturation. Here we describe structure–property relationships for a series of tripod binding groups with “feet” of different sizes. Each derivative adsorbs strongly (ΔGads ≈ −39 kJ mol–1) to graphene’s basal plane, yet the resulting monolayers exhibit kinetic stabilities that vary over 2 orders of magnitude and molecular densities that vary by a factor of 2. This study identifies phenanthrene as a superior anchor relative to pyrene on the basis of its increased monolayer density and similar kinetic stability. We also demonstrate that varying the length of the methylene linkers between the feet and tripodal core does not affect binding substantially. These results represent the first demonstration of structure–property relationships in the assembly of molecular adsorbates on graphene and provide a paradigm for designing effective graphene binding motifs.
Persistence of an [E1-, Polymerase-] Adenovirus Vector Despite Transduction of a Neoantigen into Immune-Competent Mice (1999)

The ability of a uniquely modified [E1-, polymerase-] adenovirus (Ad) vector to persist after the transduction of the bacterial beta-galactosidase gene into the livers of nontolerant, immune-competent adult mice was compared with an identical gene transfer attempt with an [E1-] Ad vector. After transduction, the E1-deleted vector was rapidly eliminated, but the modified vector persisted for at least 2 months (experiment duration). Modified vector persistence was also accompanied by prolonged transgene expression and decreased hepatotoxicity profiles. This result was in contrast to several reports suggesting that the transgene expressed by an Ad vector is the primary determinant of Ad vector elimination in vivo. Our results implied that the rapid immune clearance of Ad-transduced cells in vivo is codependent on the presence of two stimuli, or "hits." Hit 1 is due to Ad vector-derived gene expression while hit 2 is due to transgene immunogenicity. Attenuation of the first hit by the use of a significantly modified vector (such as the [E1-, polymerase-] Ad vector) allowed for extended persistence, despite the continued presence of the transgene-derived stimulus (hit 2). We discuss how the two-hit hypothesis is in fact congruent with a number of other reports that have analyzed Ad vector persistence in immune-competent animals. On the basis of our results, [E1-, polymerase-] Ad vectors should have broad benefits for use in human gene therapy situations in which the encoded transgene may be perceived as a neoantigen by the intact human immune system.
Schwingungsisolierung für Bauwerke durch Verwendung naturgegebener Materialien. (1992)

Abstract Über die Entwicklung eines Isolators aus wassergesättigtem Boden zur Schwingungsdämpfung von Gebäuden gegen Erdbebenerschütterung
Collagen production and replication by cardiac fibroblasts is enhanced in response to diverse classes of growth factors. (1995)

The tissue distribution and cellular effects of platelet-derived growth factor (PDGF), basic fibroblast growth factor (bFGF), transforming growth factor beta-1 (TGF beta 1) and insulin-like growth factor 1 (IGF-1) suggest a potential role for these factors in cardiovascular matrix deposition. The objective of this study was to assess the capacity of these growth factors to promote cardiac fibroblast collagen production and replication in vitro which will lead to studies identifying their role in vivo during cardiac development and disease. Fibroblasts were isolated from fetal rat hearts by explant culture, and their response to growth factors was assessed with respect to fibroblast replication and collagen synthesis. Fibroblast replication was stimulated by PDGF and by bFGF.IGF-1 and TGF beta 1 had no effect on fibroblast replication. Collagen production was stimulated by all of the growth factors tested in order of potency TGF beta 1 > PDGF, IGF > bFGF. None of the growth factors affected the proportion of newly synthesized collagen rapidly degraded. We have shown that TGF beta 1, PDGF, bFGF and IGF-1 are all capable of increasing collagen deposition by cardiac fibroblasts by either stimulating fibroblast replication or collagen synthesis or both. The sensitivity of cardiac fibroblasts to these factors is consistent with their playing a role in the rapid changes in cardiac collagen deposition seen during development and disease.
Characterization of the CCR2 chemokine receptor: functional CCR2 receptor expression in B cells (1997)

We have derived anti-human CCR2-specific mAbs by immunization with synthetic peptides corresponding to CCR2 sequences presumably involved in the interaction with its ligand(s). The characterization of these mAbs includes the ability to recognize the CCR2 receptor specifically, as well as the function based on their ability to promote Ca2+ influx or to block MCP-1-induced Ca2+ influx and chemotaxis. One mAb (MCP-1 R02) that is directed to the NH2 terminal domain of the CCR2 receptor has MCP-1 agonist activity, and two that recognize the third extracellular domain (MCP-1R04 and MCP-1 R05) have MCP-1 antagonist activity. We analyzed the presence of CCR2 in several PBL and tonsil-derived leukocyte populations and found expression of this receptor in monocytes, activated T cells, and, surprisingly, in B cells. CCR2 receptor expression in B cells was further corroborated in Southern blot using CCR2-specific probes. Moreover, both MCP-1 and the agonist mAb trigger specific B cell migration via a PTX-sensitive mechanism, indicating the presence of a functional CCR2 receptor in these cells.
Analysis of essential oils of Origanum vulgare from six production areas of China and Pakistan (2014)

Origanum vulgare L., Lamiaceae, from six different production areas of China and Pakistan were analyzed via gas chromatography equipped with a flame ionization detector (GC-FID) and examined for their volatile constituents by gas chromatography-mass spectroscopy (GC-MS). This procedure allowed the identification of 11 to 46 components among six production areas, representing 98.5% to 99.9% of the total oil extracted. The yields of the essential oil of the six production areas of O. vulgare ranged from 0.1 to 0.7%. The class of oxygenated monoterpenes was predominant in all the essential oils. However, samples S5 and S6 have high content of sesquiterpene hydrocarbons (33.7 and 43.7%); while sample S6 is high on oxygenated sesquiterpene (32.9%). The principal component analysis of O. vulgare was employed to provide a comprehensive evaluation of essential oil components. The cluster analysis of O. vulgare was classified into three subsets, characterized according to the major essential oil components. The current study investigated the composition differences of essential oil among six production areas offering foundation for quality control, resource optimization, and clinical treatments.