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1.
Dr. Elena Petit Dr. Lluís Bosch Prof. Anna M. Costa Ignacio Rodríguez-Izquierdo Dr. Daniel Sepúlveda-Crespo Prof. M. Angeles Muñoz-Fernández Prof. Jaume Vilarrasa 《ChemMedChem》2021,16(14):2217-2222
Amides from indole-3-glyoxylic acid and 4-benzoyl-2-methylpiperazine, which are related to entry inhibitors developed by Bristol-Myers Squibb (BMS), have been synthesized with aliphatic chains located at the C7 position of the indole ring. These spacers contain an azido group suitable for the well-known Cu(I)-catalyzed (3+2)-cycloaddition or an activated triple bond for the nucleophilic addition of thiols under physiological conditions. Reaction with polyols (β-cyclodextrin and hyperbranched polyglycerol) decorated with complementary click partners has afforded polyol-BMS-like conjugates that are not cytotoxic (TZM.bl cells) and retain the activity against R5-HIV-1NLAD8 isolates. Thus, potential vaginal microbicides based on entry inhibitors, which can be called of 4th generation, are reported here for the first time. 相似文献
2.
María Fuentes-Baile Pilar García-Morales Elizabeth Prez-Valenciano María P. Ventero Jesús M. Sanz Camino de Juan Romero Víctor M. Barber Cristina Alenda Miguel Saceda 《International journal of molecular sciences》2020,21(22)
The combination of the choline binding domain of the amidase N-acetylmuramoyl-L-alanine (CLytA)-D-amino acid oxidase (DAAO) (CLytA-DAAO) and D-Alanine induces cell death in several pancreatic and colorectal carcinoma and glioblastoma cell lines. In glioblastoma cell lines, CLytA-DAAO-induced cell death was inhibited by a pan-caspase inhibitor, suggesting a classical apoptotic cell death. Meanwhile, the cell death induced in pancreatic and colon carcinoma cell lines is some type of programmed necrosis. In this article, we studied the mechanisms that trigger CLytA-DAAO-induced cell death in pancreatic and colorectal carcinoma and glioblastoma cell lines and we acquire a further insight into the necrotic cell death induced in pancreatic and colorectal carcinoma cell lines. We have analyzed the intracellular calcium mobilization, mitochondrial membrane potential, PARP-1 participation and AIF translocation. Although the mitochondrial membrane depolarization plays a crucial role, our results suggest that CLytA-DAAO-induced cell death is context dependent. We have previously detected pancreatic and colorectal carcinoma cell lines (Hs766T and HT-29, respectively) that were resistant to CLytA-DAAO-induced cell death. In this study, we have examined the putative mechanism underlying the resistance in these cell lines, evaluating both detoxification mechanisms and the inflammatory and survival responses. Overall, our results provide a better understanding on the cell death mechanism induced by CLytA-DAAO, a promising therapy against cancer. 相似文献
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The combined effect of resistance spot welding and precipitation hardening on the localised corrosion of A286 superalloy is studied. The specimens tested by double loop electrochemical potentiokinetic reactivation were welded in the solution treated condition, and then subjected to different precipitation hardening treatments. For both base metal and weld nugget, the maximum localised corrosion is reached when η phase is clearly observable. The fact that the localised corrosion resistance of weld nugget is different from that shown by base metal may be explained by the segregation of Ni and Ti towards the interdendritic region of weld nugget (studied by using scanning electron microscope/energy dispersive X-ray analysis). 相似文献
5.
Valderrama Pilar Escabias Manuel Jiménez-Contreras Evaristo Valderrama Mariano J. Baca Pilar 《Scientometrics》2018,116(2):1203-1212
Scientometrics - In order to estimate the impact factor value for a journal in Dentistry, two sets of variables were considered in this study: the first takes in the longitudinal behavior of the... 相似文献
6.
Gastón Gutiérrez-Gamboa Eva P. Pérez-Álvarez Pilar Rubio-Bretón Teresa Garde-Cerdán 《International Journal of Food Science & Technology》2019,54(4):1160-1168
Edible mushrooms production presents a potential problem for the environment, due to the large amount of waste generated. These wastes contain nitrogenous matter, which could be used as biostimulant in plants. The aim of this work was to study the effect of waste waters, from the mushroom production process, applied at veraison and 1 week later to grapevine leaves, on grape volatile compounds over two vintages. The results evidenced that mushroom water treatment decreased the grape content of certain terpenoids, C13 norisoprenoids, benzenoid compounds and esters, increasing C6 compounds content during the first season. Treated mushroom water application slightly affected grape volatile composition. This was the treatment that least affected the content of grape volatile composition. Few differences were found after the biostimulation during the second vintage. The season was the dominant factor of grape volatile content variation compared to the treatment and their interaction. 相似文献
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Ruth Blanco-Rojo Laura Toxqui Ana M. López-Parra Carlos Baeza-Richer Ana M. Pérez-Granados Eduardo Arroyo-Pardo M. Pilar Vaquero 《International journal of molecular sciences》2014,15(3):4077-4087
The aim of this study was to investigate the combined influence of diet, menstruation and genetic factors on iron status in Spanish menstruating women (n = 142). Dietary intake was assessed by a 72-h detailed dietary report and menstrual blood loss by a questionnaire, to determine a Menstrual Blood Loss Coefficient (MBLC). Five selected SNPs were genotyped: rs3811647, rs1799852 (Tf gene); rs1375515 (CACNA2D3 gene); and rs1800562 and rs1799945 (HFE gene, mutations C282Y and H63D, respectively). Iron biomarkers were determined and cluster analysis was performed. Differences among clusters in dietary intake, menstrual blood loss parameters and genotype frequencies distribution were studied. A categorical regression was performed to identify factors associated with cluster belonging. Three clusters were identified: women with poor iron status close to developing iron deficiency anemia (Cluster 1, n = 26); women with mild iron deficiency (Cluster 2, n = 59) and women with normal iron status (Cluster 3, n = 57). Three independent factors, red meat consumption, MBLC and mutation C282Y, were included in the model that better explained cluster belonging (R2 = 0.142, p < 0.001). In conclusion, the combination of high red meat consumption, low menstrual blood loss and the HFE C282Y mutation may protect from iron deficiency in women of childbearing age. These findings could be useful to implement adequate strategies to prevent iron deficiency anemia. 相似文献
9.
ABSTRACTThrough a literature review, this paper proposes an assessment framework to evaluate environmental open data in urban platforms under the data life cycle approach. For this purpose, a set of quantitative and qualitative indicators has been defined for each of the stages of the data life cycle: acquisition, access, analysis, and application. As confirmation of the capabilities of this approach, we illustrate the results of its application in six data portals along with analyses, comparisons, and conclusions regarding the results. The cases reveal that an interest exists in providing environmental information, but the capability to transform the data information into knowledge relevant for cities is rather low. 相似文献
10.
Wong Ademar Materón Elsa María Freitas Tayane A. Faria Ronaldo C. Gonçalves Débora Del Pilar Taboada Sotomayor Maria 《Journal of Applied Electrochemistry》2022,52(8):1249-1257
Journal of Applied Electrochemistry - The present work reports the development of screen-printed electrode (SPE) using flexible polyester sheets modified with nanodiamond (ND), Au nanoparticles... 相似文献