gebhart/patrepeval huggingface dataset:
Taxol: A Novel Investigational Antimicrotubule Agent (1990)

Microtubules are among the most strategic subcellular targets of anticancer chemotherapeutics. Despite this fact, new antimicrotubule agents that possess unique mechanisms of cytotoxic action and have broader antineoplastic spectra than the vinca alkaloids have not been introduced over the last several decades--until the recent development of taxol. Unlike classical antimicrotubule agents like colchicine and the vinca alkaloids, which induce depolymerization of microtubules, taxol induces tubulin polymerization and forms extremely stable and nonfunctional microtubules. Taxol has demonstrated broad activity in preclinical screening studies, and antineoplastic activity has been observed in several classically refractory tumors. These tumors include cisplatin-resistant ovarian carcinoma in phase II trials and malignant melanoma and non-small cell lung carcinoma in phase I studies. Taxol's structural complexity has hampered the development of feasible processes for synthesis, and its extreme scarcity has limited the use of a conventional, broad-scale screening approach for evaluation of clinical antitumor activity. However, taxol's unique mechanism of action, its spectrum of preclinical antitumor activity, and tumor responses in early clinical trials have generated renewed interest in pursuing its development.
Photo- and electro-functional self-assembled architectures of porphyrins (2012)

Recent developments in supramolecular strategies have enabled us to construct novel well-defined assemblies of dye molecules. These fundamental researches of such organic materials also entail the synthetic and photophysical processes of molecular aggregates at the nano- and micro-meter scale, since their optical properties significantly differ from those of monomeric species. One of the promising candidates for such functional molecules is a porphyrin dye, which acts as an electron donor as well as a sensitizer. In this perspective, the focus is on the recent advances in the construction of optically and electronically functionalized molecular architectures of porphyrins for light energy conversion and electronics. First, porphyrin aggregates with morphologies such as cube, rod and fiber, which are prepared by three different supramolecular techniques, are reported. Then, we discuss composite molecular nanoarchitectures of porphyrins and carbon nanotubes such as single-wall carbon nanotubes (SWCNTs), stacked-cup carbon nanotubes (SCCNTs) and carbon nanohorns (CNHs). Finally, the structural and photophysical properties of the composite assemblies of porphyrins and graphenes including polycyclic aromatic hydrocarbons (PAH) are presented.
Isoprene synthase activity and its relation to isoprene emission in Quercus robur L. leaves (1999)

Pedunculate oak ( Quercus robur L.) is known as a strong isoprene (2‐methyl‐1,3‐butadiene) emitter. Diurnal changes in isoprene emission were determined by branch enclosure measurements. In contrast to the diurnal cycle in emission rates, specific isoprene synthase activity in the leaves remained unchanged. Based on in vitro enzyme activity and its temperature dependency, an isoprene synthesis capacity at specific leaf temperatures was calculated. The comparison of these ‘leaf temperature‐dependent enzyme capacities’ and the measured emission rates revealed that the enzyme activity of isoprene synthase is comparable to the observed isoprene emission rates. In addition, variation in the isoprene synthase activity of the leaves due to changes in light intensity during leaf development was investigated. A 50% reduction of light intensity by shading of single branches reduced isoprene synthase activity by ≈ 60% compared with full sunlight. The calculation of isoprene synthesis capacities based on enzymatic data obtained under optimum reaction conditions, corrected for actual leaf temperature and related to leaf surface area, provides a sound basis for predicting the isoprene emission potential of plants.
Expression of the multidrug resistance gene product (P-glycoprotein) in human normal and tumor tissues. (1990)

We have characterized the normal human tissue distribution and tumor expression of the human multidrug resistance gene (MDR1) product P-glycoprotein (Pgp) by immunohistochemical staining of frozen tissue sections of human normal and tumor tissues, using three mouse monoclonal antibodies (MAb) which recognize at least two different epitopes of Pgp. Pgp expression on normal human tissues was detected in specialized epithelial cells with secretory/excretory functions, trophoblasts in the placenta, and on endothelial cells of capillary blood vessels at blood-tissue barrier sites. There were significant differences in the staining patterns of these MAb. Mouse MAb HYB-241 and HYB-612 each recognize an extracellular epitope of Pgp, whereas mouse MAb C219 detects a carboxy terminal intracellular epitope and has recently been reported to crossreact with the MDR3 gene product. HYB-241 and HYB-612 strongly stain endothelial cells and trophoblasts, whereas C219 is weakly positive or unreactive on these cells. Likewise, C219 strongly stains the biliary pole of hepatocytes, skeletal and heart muscle fibers, whereas HYB-241 and HYB-612 are unreactive on these cells. Immunopathological studies were performed on a wide variety of human tumors. Pgp expression on human tumors was most commonly detected in colon. renal, and adrenal carcinomas; rarely in lung and gastric carcinomas and certain germ cell tumors; and was undetectable in breast and endometrial carcinomas tested. Few sarcomas and none of the melanomas, neuroblastomas, gliomas, and pheochromocytomas had detectable Pgp expression. Intensity and pattern of staining varied among different cases of a given tumor type; although homogeneous immunoreactivity was observed, heterogeneity of expression in a single histological section was more common. The finding of Pgp expression in a variety of normal tissues with diverse physiological functions suggests that the role of Pgp may not be limited to excretion of xenobiotics. Pgp expression in capillaries of the brain and testis may explain the failure of drugs such as vincristine and actinomycin-D to penetrate into these tissues, allowing them to remain as pharmacological sanctuaries for malignant cells. Although Pgp expression can now be detected in a variety of human tumors, further studies are needed to establish the possible significance of this finding.
Boronic Esters in Asymmetric Synthesis (2013)

The author's work on (α-haloalkyl)boronic esters as reagents for asymmetric synthesis is reviewed. Diastereomeric ratios exceeding 1000 can be achieved with this chemistry, and ratios around 100 are commonplace. The method allows sequential installation of a series of stereocenters and tolerates a wide variety of suitably protected functional substituents. (α-Amidoalkyl)boronic acids include biochemically significant serine protease inhibitors, one of which is the clinically successful proteasome inhibitor bortezomib, used for treatment of multiple myeloma and mantle cell lymphoma.
Security and composability of randomness expansion from Bell inequalities (2013)

The nonlocal behavior of quantum mechanics can be used to generate guaranteed fresh randomness from an untrusted device that consists of two nonsignalling components; since the generation process requires some initial fresh randomness to act as a catalyst, one also speaks of randomness expansion. R. Colbeck and A. Kent [J. Phys. A 44, 095305 (2011)] proposed the first method for generating randomness from untrusted devices, but without providing a rigorous analysis. This was addressed subsequently by S. Pironio et al. [Nature (London) 464, 1021 (2010)], who aimed at deriving a lower bound on the min-entropy of the data extracted from an untrusted device based only on the observed nonlocal behavior of the device. Although that article succeeded in developing important tools for reaching the stated goal, the proof itself contained a bug, and the given formal claim on the guaranteed amount of min-entropy needs to be revisited. In this paper we build on the tools provided by Pironio et al. and obtain a meaningful lower bound on the min-entropy of the data produced by an untrusted device based on the observed nonlocal behavior of the device. Our main result confirms the essence of the (improperly formulated) claims of Pironio et al. and puts them on solid ground. We also address the question of composability and show that different untrusted devices can be composed in an alternating manner under the assumption that they are not entangled. This enables superpolynomial randomness expansion based on two untrusted yet unentangled devices.
Mechanisms of ferulic acid conversions to vanillic acid and guaiacol by Rhodotorula rubra. (1993)

Resting cells of Rhodotorula rubra converted transferulic acid (1) to vanillic acid (2), then to guaiacol (3) and protocatechuic acid (4), under aerobic conditions. In an argon atmosphere, R. rubra transformed ferulic acid to vanillic acid and 4-hydroxy-3-methoxystyrene (5). Metabolites were isolated by solid-phase extraction and characterized by mass spectrometry, 1H, and 13C-nuclear magnetic resonance spectroscopy (NMR). The biotransformation of ferulic acid to vanillic acid by R. rubra cell-free extracts required CoA, ATP, and NAD+. Mass spectrometry and 13C-NMR were used to demonstrate the incorporation of oxygen from H2(18)O during the conversion of ferulic acid to vanillic acid. The results suggest a parallel between this bioconversion reaction and the beta-oxidation of fatty acids. Proton-carbon correlation NMR spectroscopy was used to demonstrate the specific incorporation of deuterium from D2O into guaiacol obtained from vanillic acid. The incorporation of deuterium implicates the involvement of a quinoid vanillic acid tautomer as an intermediate in the decarboxylation reaction.
Phagocyte responses to endotoxin: intracellular signals and oxidative activity (1989)

Etude de l'activation de la proteine kinase C par deux agents, le phorbol myristoyl acetate (PMA) et l'endotoxine de Salmonella minnesota. L'utilisation d'antagonistes de ces deux produits revele qu'ils agissent par l'intermediaire de deux voies partiellement independantes. L'endotoxine genere un signal calcium dans un grand nombre de cellules phagocytiques
Biologically induced systemic acquired resistance in Arabidopsis thaliana (1994)

Summary Local infection with a necrotizing pathogen can render plants resistant to subsequent infection by normally virulent pathogens. A system for biological induction of such systemic acquired resistance (SAR) in Arabidopsis thaliana is reported. When plants were immunized by local inoculation of a single leaf with avirulent Pseudomonas syringae pv. tomato (Pst) carrying the avrRpt2 avirulence gene, after 2 days other leaves became resistant, as measured symptomatically and by in planta bacterial growth, to challenge with a virulent Pst strain lacking this avirulence gene. Resistance was systemic and protected the plants against infection by other virulent pathogens including P. syringae pv. maculicola. Low‐dose inoculation induced a strong SAR and double immunizations did not increase the level of protection indicating that the response of only a few cells to the immunizing bacteria is required. SAR was not induced by the virulent strain of Pst lacking avrRpt2. However, experiments with the Arabidopsis RPS2 disease resistance gene mutant rps2‐201 , which does not exhibit a local hypersensitive response to Pst carrying the corresponding avirulence gene avrRpt2 , indicate that a hypersensitive response contributes to, but is not essential for, the induction of SAR. Thus, avrRpt2 activates either a branching signal pathway or separate parallel pathways for induction of localized hypersensitive resistance and SAR, with downstream potentiation of the systemic response by the local response. Using this system for the biological induction of SAR in Arabidopsis , it should be possible to dissect the molecular genetics of SAR by the isolation of mutants affected in the production, transmission, perception and transduction of the systemic signal(s).
Characterization of regulatory T cells in patients with B-cell chronic lymphocytic leukemia (1994)

The status of the immune system of patients with B-cell chronic lymphocytic leukemia (B-CLL) is not yet sufficiently characterized. Clinically, B-CLL patients present immunodeficiency increasing along with disease progression and signs of autoimmunity. In the current study, we evaluated the expression of FOXP3 in CD4+CD25hi T regulatory lymphocytes (Treg) and their influence on immune response against tumor and viral antigens in the complex system of peripheral blood mononuclear cells. In 80 B-CLL patients, the frequency of Treg (CD4+CD25hi FOXP3+) cells was significantly higher in B-CLL patients when compared to healthy volunteers (HV) and increased with the progression of the disease (median: 8.24% in stage A, 11.24% in stage B and 12.57% in stage C according to the Binet classification). The frequency of Treg showed no correlation with prognostic markers such as ZAP-70, CD38 and HLA-G. Notably, Treg frequency correlated with serum levels of TNF (r(2)=0.45, p=0.001). T-cell immune responses against epitopes derived from the tumor-associated antigens survivin, fibromodulin and RHAMM as well as from the influenza matrix protein were evaluated. Functionally, higher frequencies of Treg correlated with decreased T-cell responses against viral and tumor antigens. In conclusion, we detected higher frequencies of Treg in B-CLL patients than in HV. Furthermore, Treg constitute the crucial mechanism of immunosuppression in B-CLL patients.
The Effect of Audio Visual Entrainment on Pre-Attentive Dysfunctional Processing to Stressful Events in Anxious Individuals (2014)

Experimental single case studies on automatic processing of emotion were carried on a sample of people with an anxiety disorder. Participants were required to take three Audio Visual Entrainment (AVE) sessions to test for anxiety reduction as proclaimed by some academic research. Explicit reports were measured as well as pre-attentive bias to stressing information by using affective priming studies before and after AVE intervention. Group analysis shows that indeed AVEs program applications do reduce anxiety producing significant changes over explicit reports on anxiety levels and automatic processing bias of emotion. However, case by case analysis of six anxious participants shows that even when all of the participants report emotional improvement after intervention, not all of them reduce or eliminate dysfunctional bias to stressing information. Rather, they show a variety of processing styles due to intervention and some of them show no change at all. Implications of this differential effect to clinical sets are discussed.
Expression and Porin Activity of P28 and OMP-1F during Intracellular Ehrlichia chaffeensis Development (2008)

Ehrlichia chaffeensis, an obligatory intracellular gram-negative bacterium, must take up various nutrients and metabolic compounds because it lacks many genes involved in metabolism. Nutrient uptake by a gram-negative bacterium occurs primarily through pores or channels in the bacterial outer membrane. Here we demonstrate that isolated E. chaffeensis outer membranes have porin activities, as determined by a proteoliposome swelling assay. The activity was partially blocked by an antibody that recognizes the two most abundant outer membrane proteins, P28/OMP-19 and OMP-1F/OMP-18. Both proteins were predicted to have structural features characteristic of porins, including 12 transmembrane segments comprised of amphipathic and antiparallel beta-strands. The sodium dodecyl sulfate stability of the two proteins was consistent with a beta-barrel structure. Isolated native P28 and OMP-1F exhibited porin activities, with pore sizes similar to and larger than, respectively, that of OprF, which is the porin with the largest pore size known to date. E. chaffeensis experiences temperature changes during transmission by ticks. During the intracellular development of E. chaffeensis, both P28 and OMP-1F were expressed mostly in the mid-exponential growth phase at 37 degrees C and the late-exponential growth phase at 28 degrees C. The porin activity of proteoliposomes reconstituted with proteins from the outer membrane fractions derived from bacteria in the mid- and late-exponential growth phases at 28 degrees C and 37 degrees C correlated with the expression levels of P28 and OMP-1F. These results imply that P28 and OMP-1F function as porins with large pore sizes, suggesting that the differential expression of these two proteins might regulate nutrient uptake during intracellular E. chaffeensis development at both temperatures.
Chemistry of MRI Contrast Agents: Current Challenges and New Frontiers (2018)

Tens of millions of contrast-enhanced magnetic resonance imaging (MRI) exams are performed annually around the world. The contrast agents, which improve diagnostic accuracy, are almost exclusively small, hydrophilic gadolinium(III) based chelates. In recent years concerns have arisen surrounding the long-term safety of these compounds, and this has spurred research into alternatives. There has also been a push to develop new molecularly targeted contrast agents or agents that can sense pathological changes in the local environment. This comprehensive review describes the state of the art of clinically approved contrast agents, their mechanism of action, and factors influencing their safety. From there we describe different mechanisms of generating MR image contrast such as relaxation, chemical exchange saturation transfer, and direct detection and the types of molecules that are effective for these purposes. Next we describe efforts to make safer contrast agents either by increasing relaxivity, increasing resistance to metal ion release, or by moving to gadolinium(III)-free alternatives. Finally we survey approaches to make contrast agents more specific for pathology either by direct biochemical targeting or by the design of responsive or activatable contrast agents.
In Vivo Evaluation of Ocular Demodicosis Using Laser Scanning Confocal Microscopy (2010)

Laser scanning confocal microscopy seems to be an efficient noninvasive tool in the diagnosis and follow-up of ocular demodicosis infestation.
Optimizing experimental protocols for quantitative behavioral imaging with 18F-FDG in rodents. (2007)

These studies support an experimental protocol in which animals can receive the 18F-FDG tracer injection intraperitoneally, away from the small-animal tomograph and with minimal impact on behavior. Further, animals can occupy the tomograph bed for a 10- to 30-min scan with a consequent increase in animal throughput.
Sequential directed ortho metalation-boronic acid cross-coupling reactions. A general regiospecific route to oxygenated dibenzo[b,d]pyran-6-ones related to ellagic acid (1991)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTSequential directed ortho metalation-boronic acid cross-coupling reactions. A general regiospecific route to oxygenated dibenzo[b,d]pyran-6-ones related to ellagic acidB. I. Alo, A. Kandil, P. A. Patil, M. J. Sharp, M. A. Siddiqui, Victor Snieckus, and P. D. JosephyCite this: J. Org. Chem. 1991, 56, 12, 3763–3768Publication Date (Print):June 1, 1991Publication History Published online1 May 2002Published inissue 1 June 1991https://pubs.acs.org/doi/10.1021/jo00012a004https://doi.org/10.1021/jo00012a004research-articleACS PublicationsRequest reuse permissionsArticle Views2154Altmetric-Citations159LEARN 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 Get e-Alerts
Barriers to drug delivery in solid tumors (2014)

Over the last decade, significant progress has been made in the field of drug delivery. The advent of engineered nanoparticles has allowed us to circumvent the initial limitations to drug delivery such as pharmacokinetics and solubility. However, in spite of significant advances to tumor targeting, an effective treatment strategy for malignant tumors still remains elusive. Tumors possess distinct physiological features which allow them to resist traditional treatment approaches. This combined with the complexity of the biological system presents significant hurdles to the site-specific delivery of therapeutic drugs. One of the key features of engineered nanoparticles is that these can be tailored to execute specific functions. With this review, we hope to provide the reader with a clear understanding and knowledge of biological barriers and the methods to exploit these characteristics to design multifunctional nanocarriers, effect useful dosing regimens and subsequently improve therapeutic outcomes in the clinic.
Laser based WDM multichannel video transmission system (1981)

The results of a WDM experiment involving the transmission of three video channels using AM-VSB modulation on each of three lasers in the 800–900 nm range are presented. A weighted video signal/noise ratio greater than 40 dB was achieved at each wavelength for a laser modulation index of 0.3 over a 1.1 km link.
Communication. Phase Equilibria and Telomerization Reaction (1964)

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTCommunication. Phase Equilibria and Telomerization ReactionL. M. Shorr, Manfred Rogozinski, Andre Varsanyi, and Avraham BanielCite this: Ind. Eng. Chem. Fundamen. 1964, 3, 1, 86–87Publication Date (Print):February 1, 1964Publication History Published online1 May 2002Published inissue 1 February 1964https://pubs.acs.org/doi/10.1021/i160009a016https://doi.org/10.1021/i160009a016research-articleACS PublicationsRequest reuse permissionsArticle Views23Altmetric-Citations1LEARN 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 options Get e-Alerts
Melanin concentrating hormone; molecular modelling and experimental analysis of conformation (1988)

Molecular dynamics analyses and associated energy minimizations for the peptide hormone MCH and the related cyclic decapeptide MCH(5–14) suggest that it may access two major families of conformations; experimental support comes from n.m.r. studies of MCH(5–14).