gebhart/patrepeval huggingface dataset:
Polo-Like Kinases: A Team in Control of the Division (2006)

Polo, the founding member of the family of polo-like kinases (Plks) was identified in a Drosophila screen for mutants affecting spindle pole behavior.(1) Several mutants showed defects at their spindle poles and were hence named after the magnetic poles of the earth or geo-magnetic phenomena associated with them, like Polo and Aurora. Currently, the conserved family of Plks consists of many members throughout various species. Multiple Plks are present in mammalian cells (Plk1, Plk2/Snk, Plk3/Fnk/Prk, and Plk4/Sak) and Xenopus (Plx1-3), whereas in other species only one member has been identified, like Polo in Drosophila, Cdc5 in budding yeast and Plo1 in fission yeast. Plks are now viewed as important regulators of multiple functions before and during the mitotic cell division. In this review, we will focus our attention on human Plk1 and its family members Plk2-4 and the many roles they play during mitosis. Furthermore, we will describe the currently knowledge of the regulation of these functions.
DNA hydration studied by pressure perturbation scanning microcalorimetry (2008)

Pressure perturbation differential scanning calorimetry was used to determine thermal expansion coefficients and thus temperature-induced volume changes of DNA duplexes differing in their GC/AT content. It was shown that the temperature-induced unfolding of the DNA duplexes proceeds with a significant increase of the thermal expansion coefficient and the partial volume of the DNA. Unusually, large temperature-induced changes in the partial volume were observed for an AT-rich dodecamer, a finding consistent with previous crystallographic studies showing the presence of highly ordered water molecules hydrating the minor groove of such duplexes. The data show that the density of this ordered water is substantially higher than that of the bulk water. This ordered water cannot, therefore, be equated to ice at normal pressures but it thermodynamically resembles ice formed at high pressures.
Effects of antacid formulation on postprandial oesophageal acidity in patients with a history of episodic heartburn (2002)

The meal model used in this study dependably produced acidic gastro-oesophageal reflux. Antacids increased oesophageal pH independent of gastric pH, demonstrating that chewing antacids controls oesophageal acidity more effectively than swallowing antacid tablets.
Influence of Rigid Contact Lens Overall and Optic Zone Diameters on Tear Pump Efficiency (1990)

To determine the effects of contact lens overall diameter on tear pump efficiency, oxygen uptake rates were measured for the open-eye condition and following steady-state periods of static (without blinking) and dynamic (with blinking once every 5 s) contact lens wear of oxygen-impermeable (polymethylmethacrylate) lenses of 5 overall diameters (8.2, 8.5, 8.8, 9.1, and 9.4 mm). The optic zone diameters were 1.4 mm smaller than the overall diameters in each case, while all other parameters remained constant. Differences in corneal oxygen demand following the static and dynamic conditions are a quantitative index of the tear pump efficiency for each lens size on the same cornea, and the differences were found to increase with reduction in lens overall diameter. This indicated that a more efficient tear pump was associated with small diameter designs. In addition, subjects with large palpebral aperture size, relative to lens overall diameter, were found to demonstrate better tear exchange.
Ginkgolide and bilobalide biosynthesis in Ginkgo biloba. II : Identification of a possible intermediate compound by using inhibitors of cytochrome P-450-dependent oxygenases (1997)

The presence of diterpene hydrocarbons as biosynthetic intermediates in the formation of ginkgolides and bilobalide has been investigated in Ginkgo biloba seedlings. Diterpene hydrocarbons are present only in roots. as trace amounts (1-3 μg g -1 FW). Dehydroabietane is the main hydrocarbon compound. Two inhibitors of cytochrome P-450-dependent oxygenases, teteyclacis and clotrimazole, were supplied to the seedlings via the roots in order to deregulate the terpene pathway. As a consequence of the treatment with inhibitors, the ginkgolide and bilobalide content was lowered, both in roots and leave. A treatment with 10 mM tetcyclacis was more effective than a 100 mM clotrimazole treatment and resulted in a strong increase (up to 41 times of diterpene hydrocarbons in roots This increase concerned primarily dehydroabietane. 14 CO 2 feeding experiments. following 10 μM tetcyclacis treatment, showed that only dehydroabietane was highly labelled. The absence of labelling in both ginkgolides and bilobalide indicates that the oxygenation reactions leading to the end-products are fully inhibited. All together, these results support the existence of a precursor-product relationship between dehydroabietane and ginkgolides plus bilobalides. The biosynthesis of oxygenated terpenes in G. biloba proceeds via a hydrocarbon intermediate.
Endocardial Unipolar Voltage Mapping to Detect Epicardial Ventricular Tachycardia Substrate in Patients With Nonischemic Left Ventricular Cardiomyopathy (2010)

EPI arrhythmia substrate can be reliably identified in most patients with LVCM using ENDO UNI voltage mapping in the absence of ENDO BIP abnormalities.
Light scattering from nonionic surfactants of the sugar-lipid hybrid type in aqueous solution (1989)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTLight scattering from nonionic surfactants of the sugar-lipid hybrid type in aqueous solutionPeter Denkinger, Walther Burchard, and Martin KunzCite this: J. Phys. Chem. 1989, 93, 4, 1428–1434Publication Date (Print):February 1, 1989Publication History Published online1 May 2002Published inissue 1 February 1989https://doi.org/10.1021/j100341a050Request reuse permissionsArticle Views122Altmetric-Citations26LEARN 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 InReddit PDF (1 MB) Get e-Alerts
Arylomycins A and B, New Biaryl-bridged Lipopeptide Antibiotics Produced by Streptomyces sp. Tue 6075. II. Structure Elucidation. (2002)

The structures of new lipopeptide antibiotics, arylomycins A and B, were elucidated by a combination of ESI-FTICR-mass spectrometry, NMR spectroscopy, Edman sequencing, and fatty acid and chiral amino acid analyses. The colourless arylomycins A share the peptide sequence of D-N-methylseryl2(D-MeSer2)-D-alanyl3-glycyl4-N-methyl- 4-hydroxyphenylglycyl5(MeHpg5)-L-alanyl6-tyrosine7 cyclised by a [3,3]biaryl bond between MeHpg5 and Tyr7. The yellow arylomycins B differ from arylomycins A by nitro substitution of Tyr7. The N-termini of arylomycins A and B are acylated with saturated C11-C15 fatty acids (fa1) comprising n, iso, and anteiso isomers. Arylomycins A and B represent the first examples of biaryl-bridged lipopeptides.
Molecular Mechanisms of Ligand Recognition by Parathyroid Hormone 1 (PTH1) and PTH2 Receptors. (2001)

The mammalian parathyroid hormone (PTH) PTH receptor family includes PTH1 and PTH2 receptors and three related ligands (PTH, PTH-related protein (PTHrP) and tuberoinfundibular peptide of 39 residues (TIP39)). Here we comparatively and systematically review the pharmacological properties of PTH receptors and ligands, structure of the ligands, and molecular mechanisms of receptor-ligand interaction. The PTH1 receptor is activated by PTH and PTHrP but not by TIP39. The PTH2 receptor is activated by TIP39 but not by PTHrP. PTH strongly activates the human PTH2 receptor but is a weak partial agonist for rat and zebrafish PTH2 receptors. Receptor-G-protein interaction increases the receptor binding selectivity of PTHrP and TIP39. Despite different primary structures, the secondary structures of PTH, PTHrP and TIP39 are quite similar. Each ligand contains an N-terminal and a C-terminal a-helix in secondary structure-inducing conditions. Receptor-bound ligand structure is less well-characterized. The orientation of receptor-ligand interaction is highly similar for PTH and PTHrP binding to the PTH1 receptor and TIP39 interaction with the PTH2 receptor. Ligands bind according to a two-site mechanism, in which the C-terminal portion of the ligand binds the extracellular N-terminal domain of the receptor (N-interaction), and the N-terminal ligand portion binds to the juxtamembrane receptor domain (J-interaction). The N-interaction provides most of the PTH1-receptor binding energy for PTH and PTHrP but provides less energy for PTH2 receptor-TIP39 interaction. The J-interaction stimulates G-protein activation. For the PTH-PTH1 receptor interaction, the efficacy-generating component of the J-interaction is independent of the N-domain of the receptor and C-terminal portion of the ligand. This finding suggests that it might be possible to design low molecular-weight PTH1 receptor agonists, which could be bone anabolic agents and used for the treatment of osteoporosis.
Crossed Nanotube Junctions (2000)

Junctions consisting of two crossed single-walled carbon nanotubes were fabricated with electrical contacts at each end of each nanotube. The individual nanotubes were identified as metallic (M) or semiconducting (S), based on their two-terminal conductances; MM, MS, and SS four-terminal devices were studied. The MM and SS junctions had high conductances, on the order of 0.1 e(2)/h (where e is the electron charge and h is Planck's constant). For an MS junction, the semiconducting nanotube was depleted at the junction by the metallic nanotube, forming a rectifying Schottky barrier. We used two- and three-terminal experiments to fully characterize this junction.
The genetics of bipolar affective disorder (2006)

Molecular genetic research in bipolar affective disorder may lead to the development of new diagnostic paradigms for classifying the psychoses and affective states. In addition, determining the functional significance of the susceptibility genes will pave the way for enhanced diagnostic accuracy and improved treatments.
Mechanisms influencing the immunodominance of T cell determinants. (1988)

The preferential recognition of certain amino acid sequences from foreign protein antigens by T cells is referred to as T cell epitope immunodominance. To determine the mechanisms underlying this phenomenon, we have studied the correlation between the interaction of a series of synthetic peptides encompassing the entire hen egg-white lysozyme (HEL) sequence with class II molecules of the H-2k haplotype, and T cell responsiveness to these peptides. After HEL priming, three immunodominant T cell epitopes were found: two, included in the HEL sequences 51-61 and 112-129, were recognized in association with I-Ak molecules, and one, included in sequence 1-18, in association with I-Ek molecules. Accordingly, these peptides bound to the appropriate class II molecule, as demonstrated by competition for antigen presentation. Several other HEL peptides, although capable of associating with class II molecules, were not immunodominant. The absence of immunodominance has been shown to arise by three different mechanisms: (a) competition by an immunodominant peptide for presentation in vivo, (b) failure to generate the peptide during antigen processing, and (c) an inherently poor capacity of the T cell repertoire to respond to a particular peptide-MHC complex.
Bronchial circulation in pulmonary artery occlusion and reperfusion (1990)

Obstruction of pulmonary arterial blood flow results in minimal biochemical and/or morphological changes in the involved lung. If the lung is reperfused, a syndrome of leukopenia and lung edema occurs. We used the radiolabeled microsphere technique to measure the response of the bronchial circulation in rabbits to acute pulmonary artery occlusion (PAO) and to pulmonary artery reperfusion. We found that the bronchial blood flow (Qbr) decreased from a base line of 0.37 +/- 0.10 to 0.09 +/- 0.04 (SE) ml.min-1.g dry lung-1 (P less than or equal to 0.05) after 4 h of PAO. In a separate group of animals, Qbr 24 h after PAO remained low (0.20 +/- 0.07 ml.min-1.g dry lung-1, P = 0.06). Qbr during PAO was inversely correlated with the wet-to-dry ratio after reperfusion (r = -0.68, P = 0.06). Qbr did not change during 4 h of reperfusion. We speculate that a critical level of Qbr may be necessary during PAO to prevent ischemia/reperfusion injury from occurring.
Concise Total Synthesis of (+)-Asperazine, (+)-Pestalazine A, and (+)-iso-Pestalazine A. Structure Revision of (+)-Pestalazine A (2016)

The concise, enantioselective total syntheses of (+)-asperazine (1), (+)-iso-pestalazine A (2), and (+)-pestalazine A (3) have been achieved by the development of a late-stage C3-C8' Friedel-Crafts union of polycyclic diketopiperazines. Our modular strategy enables the union of complex polycyclic diketopiperazines in virtually their final forms, thus providing rapid and highly convergent assembly at the challenging quaternary stereocenter of these dimeric alkaloids. The significance of this carbon-carbon bond formation can be gauged by the manifold constraints that were efficiently overcome, namely the substantial steric crowding at both reactive sites, the nucleophilic addition of C8' over N1' to the C3 carbocation, and the multitude of reactivity posed by the use of complex diketopiperazine fragments in the coupling event. The success of the indoline π-nucleophile that evolved through our studies is notable given the paucity of competing reaction pathways observed in the presence of the highly reactive C3 carbocation generated. This first total synthesis of (+)-pestalazine A also allowed us to revise the molecular structure for this natural alkaloid.
Post noise smoother to improve low bit rate speech-coding performance (2003)

A new post-process called a post noise smoother (PNS) for the CELP decoder is proposed in order to improve low bit rate speech-coding performance under various background noise conditions. In the PNS, spectral amplitude smoothing and phase randomizing are performed on the decoded speech in order to obtain smoothed background noise. The decoded speech, the smoothed signal, and an automatically generated imitative noise signal are multiplied by adaptive gains and are summed up in the final output speech. These gains are computed from each frame's estimated ratio of background noise to signal. Evaluation test results show that the PNS significantly improves the subjective quality of a 4-kbps speech coder under various conditions of background noise.
Fetal and Maternal Effects of Phenylephrine and Ephedrine during Spinal Anesthesia for Cesarean Delivery (2002)

Giving phenylephrine alone by infusion at cesarean delivery was associated with a lower incidence of fetal acidosis and maternal nausea and vomiting than giving ephedrine alone. There was no advantage to combining phenylephrine and ephedrine because it increased nausea and vomiting, and it did not further improve fetal blood gas values, compared with giving phenylephrine alone.
The Emergence of Extensively Drug‐Resistant Tuberculosis: A Global Health Crisis Requiring New Interventions: Part II: Scientific Advances that May Provide Solutions (2009)

The need for new tuberculosis (TB) diagnostics has never been greater as TB in the HIV-infected is often sputum smear negative or extrapulmonary and may progress rapidly unless diagnosed and treated appropriately. In addition, the empirical treatment of patients with drug-resistant TB leads to the acquisition of additional resistance. Fortunately there is a robust and adequately funded developments pipeline including investigational rapid diagnostics that may replace smear, culture, and drug susceptibility testing. The dogma that drug resistance usually develops as a consequence of patient nonadherence has never been entirely plausible. Recent observations indicate that certain mutations in drug resistance genes promote the acquisition of additional resistance. Further, Mycobacterium tuberculosis (MTB) may demonstrate tolerant phenotypes due to induction of a multidrug-resistant like pump. It will be difficult to "treat our way" out of the problem of extensively drug-resistant (XDR)-TB without access to new interventions. Vaccines in development offer a distant hope. Promising new therapeutics in clinical trials may shorten the duration of treatment of TB, which will lessen the development of drug resistance or provide potent new and MTB specific agents that should be effective in treatment of XDR-TB.
Neural Interface Devices: Spinal Cord Stimulation Technology (2008)

This review of spinal cord stimulation (SCS) and its technology begins with an overview of the history and background of electroanalgesia, from the use of electric fish in ancient times through the development of the first SCS devices. Discussion of the clinical goals of SCS as a treatment for neuropathic and ischemic pain includes accepted and emerging indications and focuses on various aspects of the technical goal of appropriate paresthesia coverage. While acknowledging that much remains to be discovered about the mechanisms of action of SCS, the review describes what is known about its neurochemical effects and summarizes the results of experimental and clinical studies that seek to illuminate why SCS is effective. After noting the importance and development of computer modeling studies that indicate ways to improve delivery of the electrical pulses, the review covers the advantages of various types of SCS electrodes and power generators and the use of computerized methods to optimize SCS therapy in individual patients and to provide information about the clinical performance of various types of equipment. Finally, this paper identifies important design issues and options as well as the challenges posed by various failure modes, by environmental and medical precautions, and by cost effectiveness and patient access issues.
[The effect of gamma radiation on the enzyme activity of collalitin during storage]. (1990)

A study was made of the effect of gamma-irradiation of collalitin samples with doses of 25 and 50 kGy on proteolytic and enzyme activity with respect to denaturated collagen. The enzyme properties were found to change upon storage for periods of 6 and 12 months at 15 degrees C under unsterile conditions. No significant changes in the molecular mass of the collalitin samples were revealed by the method of gell-chromatography after irradiation and storage.
Variability in surface antigen expression of human breast epithelial cells cultured from normal breast, normal tissue peripheral to breast carcinomas, and breast carcinomas. (1984)

Single-cell heterogeneity and variability in expression of several surface antigens on human mammary epithelial cells in short-term culture were studied with immunofluorescence techniques, using polyclonal and monoclonal antibodies. The cultures, derived from normal breast, a fibroadenoma, a gynecomastia, normal breast tissue peripheral to breast carcinomas, and breast carcinomas and their metastases, were studied after one passage in vitro. The percentage of positive cells varied considerably from one tissue sample to another in all categories from normal to malignant, although there was an overall trend toward a decreasing percentage of positive cells of malignant tissues. The relative antigen content varied 3- to 8-fold among individual samples of cells from normal, peripheral, and carcinoma tissue, while the mean values in the three categories were similar. The single-cell variability in relative antigen content was considerable in all individual samples of normal, peripheral, and carcinoma tissues, as reflected in the high coefficients of variation. However, the coefficients of variation were significantly higher for cells from carcinoma and peripheral tissues [69 +/- 10% (S.E.) and 75 +/- 9%, respectively] than for cells from normal breast (48 +/- 5%). By analyzing in clonal colonies the appearance of quantitative variants in expression of a specific surface antigen, detected with a monoclonal antibody, the carcinoma cells were found to have a 10-fold higher rate of phenotypic variability (mean, 1.21 X 10(-2)/cell/generation) than did cells from normal breast (mean, 0.119 X 10(-2)) and one gynecomastia (0.045 X 10(-2)). Mammary epithelial cells from apparently "normal" tissue peripheral to a carcinoma had an intermediate rate of phenotypic variability (mean, 0.310 X 10(-2)) that was significantly higher than that of the normal tissue.
Structure-Guided Evolution of Potent and Selective CHK1 Inhibitors through Scaffold Morphing (2011)

Pyrazolopyridine inhibitors with low micromolar potency for CHK1 and good selectivity against CHK2 were previously identified by fragment-based screening. The optimization of the pyrazolopyridines to a series of potent and CHK1-selective isoquinolines demonstrates how fragment-growing and scaffold morphing strategies arising from a structure-based understanding of CHK1 inhibitor binding can be combined to successfully progress fragment-derived hit matter to compounds with activity in vivo. The challenges of improving CHK1 potency and selectivity, addressing synthetic tractability, and achieving novelty in the crowded kinase inhibitor chemical space were tackled by multiple scaffold morphing steps, which progressed through tricyclic pyrimido[2,3-b]azaindoles to N-(pyrazin-2-yl)pyrimidin-4-amines and ultimately to imidazo[4,5-c]pyridines and isoquinolines. A potent and highly selective isoquinoline CHK1 inhibitor (SAR-020106) was identified, which potentiated the efficacies of irinotecan and gemcitabine in SW620 human colon carcinoma xenografts in nude mice.