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31.
32.
Klaus van Benthem Cecile S. Bonifacio Cristian I. Contescu Nidia C. Gallego Stephen J. Pennycook 《Carbon》2011,(12):4059-4063
Aberration corrected scanning transmission electron microscopy was used to demonstrate the feasibility of imaging individual Pd atoms that are highly dispersed throughout the volume of activated carbon fibers. Simultaneous acquisition of high-angle annular dark-field and bright-field images allows correlation of the location of single Pd atoms with microstructural features of the carbon host material. Sub-Ångström imaging conditions revealed that 18 wt% of the total Pd content is dispersed as single Pd atoms in three re-occurring local structural arrangements. The identified structural configurations may represent effective storage sites for molecular hydrogen through Kubas complex formation as discussed in detail in the preceding article. 相似文献
33.
Ana María Zrate Christian Espinosa-Bustos Simn Guerrero Anglica Fierro Felipe Oyarzún-Ampuero Andrew F. G. Quest Lucia Di Marcotullio Elena Loricchio Miriam Caimano Andrea Calcaterra Matías Gonzlez-Quiroz Adam Aguirre Jaime Melndez Cristian O. Salas 《International journal of molecular sciences》2021,22(16)
The Smoothened (SMO) receptor is the most druggable target in the Hedgehog (HH) pathway for anticancer compounds. However, SMO antagonists such as vismodegib rapidly develop drug resistance. In this study, new SMO antagonists having the versatile purine ring as a scaffold were designed, synthesised, and biologically tested to provide an insight to their mechanism of action. Compound 4s was the most active and the best inhibitor of cell growth and selectively cytotoxic to cancer cells. 4s induced cell cycle arrest, apoptosis, a reduction in colony formation and downregulation of PTCH and GLI1 expression. BODIPY-cyclopamine displacement assays confirmed 4s is a SMO antagonist. In vivo, 4s strongly inhibited tumour relapse and metastasis of melanoma cells in mice. In vitro, 4s was more efficient than vismodegib to induce apoptosis in human cancer cells and that might be attributed to its dual ability to function as a SMO antagonist and apoptosis inducer. 相似文献
34.
Camelia Ungureanu Cristian PirvuMihaela Mindroiu Ioana Demetrescu 《Progress in Organic Coatings》2012
In order to enhance properties of the polymer composite films, composite coatings based on polypyrrole (PPy) and polyethylene glycol (PEG), using various percentages of PEG (0.5%, 2%, 4%), were electrodeposited on a new titanium alloy electrode as insulating material. The structure of the coatings was investigated via infrared (FTIR) analysis, and the surface features were studied using contact angle determination, atomic force microscopy (AFM) and scanning electronic microscopy (SEM). When testing the antibacterial properties of the coatings, the best effect was found for the coating with 2% PEG concentration, which has hydrophilic character and small roughness. Such results are in concordance with mechanism of biomaterial–bacteria interaction which involves as factors affecting bacterial adhesion and growth an initial physicochemical interaction stage, where roughness and wettabilitty are factors promoting bacterial adhesion and biofilm deposition. 相似文献
35.
Insa Thale Sarah Maskri Lucie Grey Luca Matteo Todesca Prof. Dr. Thomas Budde Dr. Ivan Maisuls Prof. Dr. Cristian A. Strassert Prof. Dr. Oliver Koch Prof. Dr. Albrecht Schwab Prof. Dr. Bernhard Wünsch 《ChemMedChem》2023,18(2):e202200551
The Ca2+ activated K+ channel KCa3.1 is overexpressed in several human tumor cell lines, e. g. clear cell renal carcinoma, prostate cancer, non-small cell lung cancer. Highly aggressive cancer cells use this ion channel for key processes of the metastatic cascade such as migration, extravasation and invasion. Therefore, small molecules, which are able to image this KCa3.1 channel in vitro and in vivo represent valuable diagnostic and prognostic tool compounds. The [18F]fluoroethyltriazolyl substituted senicapoc was used as positron emission tomography (PET) tracer and showed promising properties for imaging of KCa3.1 channels in lung adenocarcinoma cells in mice. The novel senicapoc BODIPY conjugates with two F-atoms ( 9 a ) and with a F-atom and a methoxy moiety ( 9 b ) at the B-atom led to the characteristic punctate staining pattern resulting from labeling of single KCa3.1 channels in A549-3R cells. This punctate pattern was completely removed by preincubation with an excess of senicapoc confirming the high specificity of KCa3.1 labeling. Due to the methoxy moiety at the B-atom and the additional oxyethylene unit in the spacer, 9 b exhibits higher polarity, which improves solubility and handling without reduction of fluorescence quantum yield. Docking studies using a cryo-electron microscopy (EM) structure of the KCa3.1 channel confirmed the interaction of 9 a and 9 b with a binding pocket in the channel pore. 相似文献
36.
Cristian S. Campos-Fernández Bradley W. Smucker Rodolphe Clérac Kim R. Dunbar 《Israel journal of chemistry》2001,41(3):207-218
Reactions of 2,3,5,6-tetra(2-pyridyl) pyrazine (tppz) with [ML6][X]2 (L = CH3CN, H2O;X = [BF4]−, [ClO4]−, [NO3]− [BArF]−(BArF - B[3,5-C6H3(CF3)2]4) lead to the high-yield formation of mononuclear [M(tppz)2]2+, (M = MnII, FeII, CoII, and NiII) and dinuclear [Ni2(tppz)(CH3CN)6]4+ species. The new compounds were fully characterized by X-ray crystallographic, spectroscopic, and magnetic susceptibility measurements. Surprisingly, the 2:1 M:tppz reactions did not lead to isolation of the dinuclear species except in the case of Ni(II). It was further noted that even in the case of the Ni reactions, the nuclearity of the product depends on the choice of anions and the reaction conditions. Magnetic measurements of the mononuclear species [Co(tppz)2]2+ revealed thermally induced spin-crossover behavior from a high-spin S = 3/2 at higher temperatures to a low-spin S = 1/2 complex at lower temperatures. The dinuclear compound [Ni2(tppz)(CH3CN)6]4+ exhibits a weak anti-ferromagnetic interaction through the bridging tppz ligand. 相似文献
37.
Thioether Analogues of Disulfide‐Bridged Cyclic Peptides Targeting Death Receptor 5: Conformational Analysis,Dimerisation and Consequences for Receptor Activation 下载免费PDF全文
Dr. Karolina Pulka‐Ziach Dr. Valeria Pavet Neila Chekkat Dr. Karine Estieu‐Gionnet Roman Rohac Dr. Marie‐Charlotte Lechner Dr. Cristian R. Smulski Dr. Gabrielle Zeder‐Lutz Dr. Danièle Altschuh Dr. Hinrich Gronemeyer Prof. Dr. Sylvie Fournel Dr. Benoit Odaert Dr. Gilles Guichard 《Chembiochem : a European journal of chemical biology》2015,16(2):293-301
Cyclic peptides containing redox‐stable thioether bridges might provide a useful alternative to disulfide‐bridged bioactive peptides. We report the effect of replacing the disulfide bridge with a lanthionine linkage in a 16‐mer cyclic peptide that binds to death receptor 5 (DR5, TRAIL‐R2). Upon covalent oligomerisation, the disulfide‐bridged peptide has previously shown similar behaviour to that of TNF‐related apoptosis inducing ligand (TRAIL), by selectively triggering the DR5 cell death pathway. The structural and biological properties of the DR5‐binding peptide and its desulfurised analogue were compared. Surface plasmon resonance (SPR) data suggest that these peptides bind DR5 with comparable affinities. The same holds true for dimeric versions of these peptides: the thioether is able to induce DR5‐mediated apoptosis of BJAB lymphoma and tumorigenic BJELR cells, albeit to a slightly lower extent compared to its disulfide homologue. NMR analysis revealed subtle variation in the conformations of the two peptides and suggests that the thioether peptide is slightly less folded than its disulfide homologue. These observations could account for the different capability of the two dimers to cluster DR5 receptors on the cell surface and to trigger apoptosis. Nevertheless, our results suggest that the thioether peptide is a potential candidate for evaluation in animal models. 相似文献
38.
Degradation of poly(vinyl alcohol)‐graft‐lactic acid copolymers by Trichotecium roseum fungus 下载免费PDF全文
The biodegradation of poly(vinyl alcohol) and poly(vinyl alcohol)‐graft‐lactic acid copolymers was analyzed, using Trichotecium roseum fungus. The samples were examined during biodegradation at different periods of exposure. Structural modifications of the biodegraded samples were investigated by Fourier transform infrared‐attenuated total reflectance spectroscopy, and the surface morphology was investigated by scanning electron microscopy. The static light scattering results concluded that the weight average molecular mass (Mw) of the copolymers increased after biodegradation, because the fractions with low molecular weight of the copolymers were destroyed. The thermal behavior and stability of the samples before and after the biodegradation period were investigated by differential scanning calorimetry (DSC) and thermogravimetric analyses. The thermogravimetric analyses and their derivatives (TG‐DTG) showed that the thermal stability of the biodegraded samples was more raised comparatively to the unbiodegraded ones. The DSC results demonstrated that biodegradation took place in the amorphous domains of the investigated polymer samples and the crystallinity degree increased after 24 biodegradation days. © 2014 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2015 , 132, 41777. 相似文献
39.
Filippo Lococo Massimiliano Paci Cristian Rapicetta Teresa Rossi Valentina Sancisi Luca Braglia Silvio Cavuto Alessandra Bisagni Italia Bongarzone Douglas M. Noonan Adriana Albini Sally Maramotti 《International journal of molecular sciences》2015,16(8):19612-19630
Assessment of biological diagnostic factors providing clinically-relevant information to guide physician decision-making are still needed for diseases with poor outcomes, such as non-small cell lung cancer (NSCLC). Epidermal growth factor receptor (EGFR) is a promising molecule in the clinical management of NSCLC. While the EGFR transmembrane form has been extensively investigated in large clinical trials, the soluble, circulating EGFR isoform (sEGFR), which may have a potential clinical use, has rarely been considered. This study investigates the use of sEGFR as a potential diagnostic biomarker for NSCLC and also characterizes the biological function of sEGFR to clarify the molecular mechanisms involved in the course of action of this protein. Plasma sEGFR levels from a heterogeneous cohort of 37 non-advanced NSCLC patients and 54 healthy subjects were analyzed by using an enzyme-linked immunosorbent assay. The biological function of sEGFR was analyzed in vitro using NSCLC cell lines, investigating effects on cell proliferation and migration. We found that plasma sEGFR was significantly decreased in the NSCLC patient group as compared to the control group (median value: 48.6 vs. 55.6 ng/mL respectively; p = 0.0002). Moreover, we demonstrated that sEGFR inhibits growth and migration of NSCLC cells in vitro through molecular mechanisms that included perturbation of EGF/EGFR cell signaling and holoreceptor internalization. These data show that sEGFR is a potential circulating biomarker with a physiological protective role, providing a first approach to the functional role of the soluble isoform of EGFR. However, the impact of these data on daily clinical practice needs to be further investigated in larger prospective studies. 相似文献
40.
Andrei Mocan Dan Cristian Vodnar Laurian Vlase Ovidiu Cri?an Ana-Maria Gheldiu Gianina Cri?an 《International journal of molecular sciences》2015,16(9):21109-21127
Aerial parts of Veronica species are used in Romanian traditional medicine for the treatment of various conditions like kidney diseases, cough, and catarrh, and are known for their wound-healing properties. In the present study, the phenolic and sterolic content and the antioxidant and antimicrobial activities of three Veronica species (Plantaginaceae), V. officinalis L., V. teucrium L. and V. orchidea Crantz, were studied. The identification and quantification of several phenolic compounds and phytosterols were performed using LC/MS techniques and the main components were p-coumaric acid, ferulic acid, luteoline, hispidulin and β-sitosterol. More than that, hispidulin, eupatorin and eupatilin were detected for the first time in the Veronica genus. Nevertheless, representatives of the Veronica genus were never investigated in terms of their phytosterol content. The antioxidant potential investigated by Trolox equivelents antioxidant capacity (TEAC) and EPR spectroscopy revealed that V. officinalis and V. orchidea extracts presented similar antioxidant capacities, whilst the values registered for V. teucrium extract are lower. Regarding the antimicrobial activity of the investigated species, Staphylococcus aureus, Listeria monocytogenes and Listeria ivanovii were the most sensitive strains with MIC values between 3.9 and 15.62 mg/mL. The results obtained by this study may serve to promote better use of representatives from the genus Veronica as antioxidant and antimicrobial agents. 相似文献