1,721,794 research outputs found
Development of a novel approach to overcome biofilm formation by natural product derivatives
No full textWith the aim to prevent biofilm formation, and based on our previous studies, 1, 2 we explored new strategies
involving inorganic nanoparticles for surface covering. In detail, we investigated the functionalization of silica
nanoparticles with natural derivatives showing anti-biofilm properties, using linkers of different nature and
length. After their analytical characterization, the new derivatives were used to obtain glass coverslips by spin-coating technology for the biological testing (Figure 1). The promising results towards E. coli and P.
aeruginosa will be presented.
1 C. Cattò; S. Dell'Orto; F. Villa; S. Villa; A. Gelain; A. Vitali; V. Marzano; S. Baroni S; F. Forlani; F. Cappitelli. PLoS ONE 2015, 10(7), e0131519.
2 C. Cattò; G. Grazioso; S. Dell’Orto; A. Gelain; S. Villa, V. Marzano; A. Vitali; F. Villa; F. Cappitelli; F. Forlani. Biofouling 2017, 33, 235-25
Going Beyond Counting First Authors in Author Co-citation Analysis
Full text linkThe present study examines one of the fundamental aspects of author co-citation analysis (ACA) - the way co-citation
counts are defined. Co-citation counting provides the data on which all subsequent statistical analyses and mappings
are based, and we compare ACA results based on two different types of co-citation counting - the traditional type that
only counts the first one among a cited work's authors on the one hand and a non-traditional type that takes into
account the first 5 authors of a cited work on the other hand. Results indicate that the picture produced through this non-traditional author co-citation counting contains more coherent author groups and is therefore considerably clearer. However, this picture represents fewer specialties in the research field being studied than that produced through the traditional first-author co-citation counting when the same number of top-ranked authors is selected and analyzed. Reasons for these effects are discussed
STAT3 direct inhibitors: from MD77 to AC33
No full textSTAT3 (Signal Transducer and Activator of Transcription 3) is a latent cytosolic protein overexpressed in various cancer cell lines which was found to participate in oncogenesis by stimulating cell proliferation and preventing apoptosis [1]. Furthermore, previous studies have shown that blocking constitutively activated STAT3 signaling leads to tumor cell apoptosis, with minimal effect on normal cells [2,3]. This work aims at the synthesis, the structural analysis and the biological evaluation of novel potential antitumor agents, able to inhibit STAT3 protein-protein interaction, starting from MD77 previously identified by our research group [4,5]. Among them, AC33 was selected for further investigations since the AlphaScreen-based assay highlighted its ability to disrupt the STAT3 dimerization, with high selectivity over STAT1 and Grb2. These data induced us to modulate its pharmacokinetic and pharmacodynamic properties. The interesting results obtained will be presented.
This work was supported by a PRIN2010 Grant from MIUR, Italy.
References:
[1] H. Yu, R. Jove, Nat Rev Cancer, 2004, 4, 97-105.
[2] R. Buettner, L.B. Mora, R. Jove, Clin Cancer Res, 2002, 8(4), 945-954.
[3] T. Bowman, R. Garcia, J. Turkson, R. Jove, Oncogene, 2000, 19, 2474-2488.
[4] D-S. Shin, D. Masciocchi, A. Gelain, S. Villa, D. Barlocco, F. Meneghetti, A. Pedretti, Y-M Han, D. C. Han, B.M. Kwon, L. Legnani, L. Toma, Med. Chem. Comm., 2010, 1, 156-164.
[5] D. Masciocchi, S. Villa, F. Meneghetti, A. Pedretti, D. Barlocco, L. Legnani, L. Toma, B. M. Kwon, S. Nakano, A. Asai, A. Gelain, Med. Chem. Comm., 2012, 3, 592-599
Variations on the Author
Full text link“Variations on the Author” discusses two of Eduardo Coutinho’s recent films (Um Dia na Vida, from 2010, and Últimas Conversas, posthumously released in 2015) and their contribution to the general question of documentary authorship. The director’s filmography is characterized by a consistent yet self-effacing form of authorial self-inscription: Coutinho often features as an interviewer that rather than express opinions propels discourses; an interviewer that is good at listening. This mode of self-inscription characterizes him as an author who is not expressive but who is nonetheless markedly present on the screen. In Um Dia na Vida, however, Coutinho is completely absent form the image, while Últimas Conversas, on the contrary, includes a confessional prologue that moves the director from the margins to the center of his films. This article examines the ways in which these works stand out in the filmography of a director who offers new insights into the notion of cinematic authorship
Appropriate Similarity Measures for Author Cocitation Analysis
Full text linkWe provide a number of new insights into the methodological discussion about author cocitation analysis. We first argue that the use of the Pearson correlation for measuring the similarity between authors’ cocitation profiles is not very satisfactory. We then discuss what kind of similarity measures may be used as an alternative to the Pearson correlation. We consider three similarity measures in particular. One is the well-known cosine. The other two similarity measures have not been used before in the bibliometric literature. Finally, we show by means of an example that our findings have a high practical relevance.information science;Pearson correlation;cosine;similarity measure;author cocitation analysis
Chemical behaviour and crystallographic characterization of ureido 1,2,5-oxadiazole derivatives, related to Stat3 inhibitors
No full textSTAT3 (Signal Transducer and Activator for Transcription 3) is a latent cytosolic protein that directly relates extracellular signals(e.g. growth factors, poly-peptide, cytokines etc.) from the membrane to the nucleus [1]. STAT3 is constitutively
activated by aberrant upstream tyrosine kinase activities in a broad spectrum of human solid and blood tumours. Since STAT3
inhibition leads to apoptosis in tumour cells but not in normal cells, it represents a promising target for cancer therapy [2].
In our research we focused on the discovery of new ureido oxadiazole derivatives related to AVS-2088 (lead compound), as
potential STAT3 inhibitors, with the aim to identify the essential structure-activity requirements for the development of novel
active compounds.
Our previous results [3] indicated that the presence of a phenyl moiety in position 4 of the oxadiazole ring was critical for the
interaction with the biological target, so we planned the synthesis of the styryl derivatives.
On these basis, we analyzed the X-Ray structures of the compounds having the general formula reported in Figure 2 and
structure-activity relationships were derived. The drop in activity of the derivatives with respect to the lead could be due to the
presence of the common flexible benzyl chain linked to the urea that disrupted the flat conformation of the entire molecule,
influencing its orientation and interaction at the receptor site.
The synthetic procedures applied for the preparation of the new derivatives as well as the results of the crystallographic studies
and their biological evaluation will be presented.[1] Yu, H.; Jove, R. The STATs of cancer-new molecular targets come of age. Nat. Rev. Cancer 2004, 4, 97-105.
[2] D. Masciocchi, A. Gelain, S. Villa, F. Meneghetti, D. Barlocco. Signal Transducer and Activator of Transcription 3 (STAT3): a
promising target for anticancer therapy. Future Med. Chem. 2011, 3, 567-597.
[3] Shin, D.-S.; Masciocchi, D.; Gelain, A.; Villa, S.; Barlocco, D.; Meneghetti, F.; Pedretti, A.; Han, Y.-M.; Han, D. C.; Han, M.
Y.; Kwon, B.-M.; Legnani, L.; Toma L. Synthesis, modeling, and crystallographic study of 3,4-disubstituted-1,2,5-oxadiazoles
and evaluation of their ability to decrease STAT3 activity. Med. Chem. Comm. 2010, 1, 156-164
Dispelling the Myths Behind First-author Citation Counts
Full text linkWe conducted a full-scale evaluative citation analysis study of scholars in the XML research field to explore just how different from each other author rankings resulting from different citation counting methods actually are, and to demonstrate the capability of emerging data and tools on the Web in supporting more realistic citation counting methods. Our results contest some common arguments for the continued
use of first-author citation counts in the evaluation of scholars, such as high correlations between author rankings by first-author citation counts and other citation
counting methods, and high costs of using more realistic citation counting methods that are not well-supported by the ISI databases. It is argued that increasingly available digital full text research papers make it possible for citation analysis studies to go beyond what the ISI databases have directly supported and to employ more
sophisticated methods
koamabayili/VECTRON-author-checklist: VECTRON author checklist
No full textWe have done our best to complete the author checklist relating to the use of animals in the hut study. Note that the objective for the hut study was to evaluate the IRS treatment applications for residual efficacy against Anopheles mosquitoes, including the local An. coluzzii mosquito population. Cows were only used to attract mosquitoes into the huts and no tests were carried out directly on the cows. The author checklist is intended for use with studies where experiments are carried out on animals, which is why we have had such difficulty in completing this for the hut study, as many of the questions do not relate to how the cows were used
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