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51.
Paul Eastwood Jacob Gonzalez Sergio Paredes Silvia Fonquerna Arantxa Cardús Juan Antonio Alonso Arsenio Nueda Teresa Domenech Raquel F. Reinoso Bernat Vidal 《Bioorganic & medicinal chemistry letters》2010,20(5):1634-1637
Several new potent and selective A2B adenosine receptor antagonists have been prepared in which the aryl–amide moiety of the lead series, exemplified by 1a, has been replaced by bioisosteric bicyclic moieties. Although the majority of compounds had generally improved microsomal stability as compared to 1a, this was not translated into overall improvements in the pharmacokinetic profiles of a representative set of compounds. 相似文献
52.
The fight against epizootics is today better organized. The tools, methods and strategies used work well and are constantly being improved, which is necessary since disease epidemiology is evolving extremely fast, dominated by a growing complexity associated to global changes and the emergence of new pathologies. The foundation of the strategy is still based on a permanent epidemiological surveillance and the immediate use of appropriate measures. Among the essential prerequisites there is the existence of effective veterinary services, for which support programmes have been developed, notably by the OIE, which is also responsible for the definition of the norms applicable in animal health. Three examples of control programmes against major epidemics are discussed here: Rinderpest (declared eradicated worldwide in 2011), Highly Pathogenic Avian Influenza (H5N1), and Foot and Mouth Disease. 相似文献
53.
The anterior ligament of the human malleus. 总被引:2,自引:0,他引:2
The authors have studied the anterior ligament of the malleus (ALM) from a morphological and embryological point of view. Classical textbooks of anatomy stress the correlation between the ALM and the anterior pin of the sphenoid and define the ligament as a residual of Meckel's cartilage. This study demonstrates the y-shaped form of the ligament, one arm of which reaches the capsule of the temporomandibular joint and the other the pin of the sphenoid bone. Meckel's cartilage pilots the fibres of the ligament itself. Several clinical implications may be hypothesised on the basis of this study. 相似文献
54.
Phosphorylcholine phosphatase (PchP) of Pseudomonas aeruginosa, a product of the PA5292 gene, catalyzes the hydrolysis of phosphocholine to choline and inorganic phosphate (Pi). Phosphocholine is produced after hemolytic phospholipase C (PlcH) acts upon phosphatidylcholine or sphingomyelin. Therefore, PlcH and PchP are involved in the pathogenesis of P. aeruginosa. PchP belongs to the HAD superfamily as it contains three conserved sequences motifs. In mature PchP, the motifs I, II, and III are (31)DMDNT(35), (166)S, and (261)GDTPDSD(267), respectively. Kinetic characterization of wild-type and mutated proteins, obtained by site-directed mutagenesis, in addition to a molecular model of PchP helped us to understand the contribution of key residues in the conserved motifs I, II and III that are involved in the catalysis of p-nitrophenylphosphate processing after the addition of Mg(2+), Zn(2+) or Cu(2+) (these are activators of PchP activity). Our results are explained by invoking the concept of chemical hardness and softness introduced by Pearson in 1963 and its extension that "hard acids prefer to coordinate to hard bases and soft acids to soft bases" [Parr and Pearson, J. Am. Chem. Soc., 105, 7512-7516 (1983)]. 相似文献
55.
Liffourrena AS López FG Salvano MA Domenech CE Lucchesi GI 《Journal of applied microbiology》2008,104(2):396-402
Aims: To establish if tetradecyltrimethylammonium (TDTMA) might be degraded by pure culture of Pseudomonas strains, and how the presence of a Lewis’ acid in the medium influences its biodegradability. Methods and Results: From different strains of Pseudomonas screened, only Pseudomonas putida A ATCC 12633 grows with 50 mg l?1 of TDTMA as the sole carbon and nitrogen source. A monooxygenase activity catalyzed the initial step of the biodegradation. The trimethylamine (TMA) produced was used as nitrogen source or accumulated inside the cell. To decrease the intracellular TMA, the culture was divided, and 0·1 mmol l?1 AlCl3 added. In this way, the growth and TDTMA consumption increased. The internal concentration of TMA, determined using the fluorochrome Morin, decreased by the formation of Al3+ : TMA complex. Conclusions: Pseudomonas putida utilized TDTMA as its sole carbon and nitrogen source. The TMA produced in the initial step of the biodegradation by a monooxygenase activity was used as nitrogen source or accumulated inside the cell, affecting the bacterial growth. This effect was alleviated by the addition of AlCl3. Significance and Impact of the Study: The use of Lewis’ acids to sequester intracellular amines offers an alternative to achieve an efficient utilization of TDTMA by Ps. putida. 相似文献
56.
Macho P Solis E Sánchez G Schwarze H Domenech R 《Molecular and cellular biochemistry》2001,216(1-2):129-136
Brief episodes of tachycardia without myocardial ischemia prior to a coronary occlusion decrease myocardial infarct size in dogs. This non-ischemic preconditioning is mediated by adenosine. Because ischemic preconditioning is mediated through ATP dependent potassium channels, particularly the mitochondrial ones, we studied whether non-ischemic preconditioning is also mediated through these channels. In anesthetized dogs heart rate was kept constant at 120 cycles/min and aortic pressure changes were damped. Myocardial infarction was induced by occlusion of the anterior descending coronary artery for 60 min and reperfusion for 270 min. In a control group the infarct size (necrotic volume/risk region volume × 100) was 15.8 ± 1.5%. Preconditioning with five periods of tachycardia, 5 min in duration each at 213 cycles/min with intervening periods of 5 min of basal heart rate at 120 cycles/min, reduced the infarct size by 45.6% (p < 0.05) with respect to the control group. This effect was completely reverted by the blockade of ATP dependent potassium channels with glibenclamide or 5 hydroxydecanoate (a specific blocker of mitochondrial ATP dependent potassium channels) prior to preconditioning. These effects were not due to differences in collateral flow, risk region size or hemodynamic variables between the groups. These results show that mitochondrial ATP dependent potassium channels mediate non-ischemic preconditioning by tachycardia in dogs. 相似文献
57.
Domenech J Palacios O Villarreal L González-Duarte P Capdevila M Atrian S 《FEBS letters》2003,533(1-3):72-78
Drosophila MTO metal binding features were analyzed for comparison with MTN, the paralogous Drosophila metallothionein, and to classify MTO as either zinc- or copper-thionein. This was achieved by a combination of in vivo, in vitro and in silico methodologies. All the results unambiguously classified MTO as a second Drosophila copper-thionein, putting Drosophila forward as the only metazoan in which any zinc-thionein has still to be reported. Interestingly, experimental data only showed minor differences in the coordinative behavior of both MTs, but provided a characteristic spectroscopic fingerprint, revealing the possible binding of chloride anions in certain metal-MTO aggregates. 相似文献
58.
Sterols and gibberellins are the main terpenoids in the Ascomycete Fusarium fujikuroi. Their respective precursors squalene and ent-kaur-16-ene (henceforth called kaurene) were the main terpenoids synthesised from radioactive mevalonate by extracts of F. fujikuroi in vitro. Kaurene predominated when the extracts were obtained from mycelia engaged in gibberellin production. Squalene predominated in all other cases, and particularly when the extracts were obtained from mutants with various defects in gibberellin synthesis or nitrogen-fed wild-type cultures. New protein synthesis was required to maintain the production of gibberellins in vivo and of kaurene in vitro, but not to maintain the capacity to produce squalene in vitro. Addition of a nitrogen source to cultures engaged in gibberellin production caused a large, transient increase in the mycelial concentration of L-glutamine and abolished the accumulation of gibberellins immediately and the capacity to produce kaurene later. 相似文献
59.
J. Domenech S. B. Ramos A. Probanza G. J. A. Lucas M. F. J. Gutierrez 《Plant and Soil》2007,290(1-2):43-50
The ability of six putative plant growth promoting rhizobacteria, isolated from the rhizosphere of Nicotiana glauca L., to stimulate growth and induce systemic resistance against Xanthomonas campestris CECT 95 in Arabidopsis thaliana L. Col-0 was evaluated. The six bacterial strains significantly reduced the disease symptoms caused by the pathogen compared
to the controls, with the best results obtained with the Bacillus strain N11.37 and the Stenotrophomonas strain N6.8. These two strains were tested on A. thaliana NahG plants and jar1-1 and etr1-1 mutants, to elucidate whether the salicylic acid (SA)-dependent or SA-independent pathway was involved in the induction of
systemic resistance. The results indicate that N6.8 induces the SA-dependent pathway. For N11.37 it is as yet not clear as
in the etr1-1 mutants and NahG plants ISR is not expressed, while in jar1-1 it is. In addition, levels of SA were measured in Col-0 plants treated with N6.8 and N11.37 to confirm whether or not the
two strains produced an increased level of SA. N6.8- and N11.37-induced plants showed higher levels of SA than the controls.
It is concluded that N6.8 induces a SA-dependent pathway while N11.37 induces a pathway that is both ethylene (ET)- and SA-dependent. 相似文献
60.
Mirian Domenech Diana Damián Carmen Ardanuy Josefina Li?ares Asunción Fenoll Ernesto García 《PloS one》2015,10(4)