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2.
Iman Azimi Jack U. Flanagan Ralph J. Stevenson Marco Inserra Irina Vetter Gregory R. Monteith William A. Denny 《Bioorganic & medicinal chemistry》2017,25(1):440-449
The Orai1 Ca2+ permeable ion channel is an important component of store operated Ca2+ entry (SOCE) in cells. It’s over-expression in basal molecular subtype breast cancers has been linked with poor prognosis, making it a potential target for drug development. We pharmacologically characterised a number of reported inhibitors of SOCE in MDA-MB-231 breast cancer cells using a convenient Fluorescence Imaging Plate Reader (FLIPR) assay, and show that the rank order of their potencies in this assay is the same as those reported in a wide range of published assays. The assay was also used in a screening project seeking novel inhibitors. Following a broad literature survey of classes of calcium channel inhibitors we used simplified ligand structures to query the ZINC on-line database, and following two iterations of refinement selected a novel Orai1-selective dichlorophenyltriazole hit compound. Analogues of this were synthesized and evaluated in the FLIPR assay to develop structure–activity relationships (SAR) for the three domains of the hit; triazole (head), dichlorophenyl (body) and substituted phenyl (tail). For this series, the results suggested the need for a lipophilic tail domain and an out-of-plane twist between the body and tail domains. 相似文献
3.
Susana Redondo-Gómez Manuel Cantos Enrique Mateos-Naranjo M. Enrique Figueroa Antonio Troncoso 《Soil & Sediment Contamination》2009,18(3):320-327
Soils from four estuaries of SW Iberian Peninsula, affected by anthropogenic influence (urban, industrial and agricultural activities), were analyzed for the occurrence of a variety of metals and trace elements including Al, As, B, Ba, Ca, Cd, Co, Cr, Cu, Fe, K, Mg, Mn, Na, Ni, P, Pb, S and Zn. The soils presented very high levels of salinity (high concentrations of Na, K and Mg), organic matter and, consequently, of C and N concentrations. In contrast, very low values of CaCO3, Ca and P were found. In addition, it should be highlighted that in certain localities (Piedras 1 and 2 and Guadiana in Huelva, Spain, and Ria Formosa, Faro, Portugal) the concentrations of Pb, S and Zn were extremely high, reaching levels of pollution. 相似文献
4.
Effects of facilitation on community stability and dynamics: synthesis and future directions 总被引:1,自引:1,他引:0
Bradley J. Butterfield† 《Journal of Ecology》2009,97(6):1192-1201
5.
Georg Steinhauser Johannes H. Sterba Karin Poljanc Max Bichler Karl Buchtela 《Journal of trace elements in medicine and biology》2006,20(3):119-153
In this study, 18 partly commercially available samples of rock salt from Austria, Germany, Pakistan, Poland, Switzerland, and Ukraine were investigated with respect to their content of trace elements using instrumental neutron activation analysis. Elements detected were Al, Ba, Br, Ca, Ce, Cl, Co, Cr, Cs, Eu, Fe, Hf, La, Mn, Na, Rb, Sb, Sc, Sm, Sr, Ta, Tb, Th, and Zn, some of them only in individual cases. An estimation of the bioavailability of these trace elements was performed by dissolving an equivalent of the sodium chloride samples in diluted hydrochloric acid (simulating stomach acid), filtering off the insoluble components, and analyzing the evaporated filtrate. It could be shown that in most cases bioactive trace elements like Fe can be found in rock salt in the form of almost insoluble compounds and are therefore not significantly bioavailable, whereas thorium, for example, was partly bioavailable in two cases. A significant contribution to the recommended daily intake of metal trace elements by using rock salt for nutrition can be excluded. 相似文献
6.
L. V. Natrus 《Neurophysiology》2006,38(1):34-38
We examined changes in the impulse activity (IA) generated by neurons of the anterior hypothalamus (including the preoptic
region) resulting from infusions of hyper-and hypotonic NaCl solutions (3.0 and 0.2%, respectively; hyper-and hypoosmotic
stimulations, respectively); the infused volumes did not exceed 200 μl. The effects of hyper-and hypoosmotic stimulations
were studied in detail in 83 and 88 neurons, respectively. In 31.2% (26 cells) and 29.6% (26 cells) of the neurons of the
above groups, these stimulations evoked changes in the IA frequency greater than +40 or −40% of the mean background IA frequency.
In approximately 50% of the responding neurons in each group, such shifts in the IA frequency were observed in the course
of infusions of test solutions (5 sec long) and within the subsequent 5 min after termination of the infusion. In another
50% of the neurons, changes in the IA frequency occurred within the afterperiod (30 sec long); these shifts could develop
exclusively within the latter interval, or these changes accompanied an initial early reaction. In general, activating responses
dominated (they were observed in 65% of the cases where test stimulations of both modalities were used). The possible aspects
of the involvement of neurons of the anterior hypothalamus in the control of the water/salt balance in the organism are discussed.
Neirofiziologiya/Neurophysiology, Vol. 38, No. 1, pp. 40–45, January–February, 2006. 相似文献
7.
In order to evaluate the effectiveness and selectivity of various reagents in the solubilization of bacterial membranes, membranes of Micrococcus lysodeikticus were treated with detergents and chaotropic agents. The composition of the extracts so obtained was analyzed by rocket and two-dimensional immunoelectrophoretic techniques. Recovery of succinate-, malate-, and reduced nicotinamide adenine dinucleotide- (NADH) dehydrogenases, ATPase, succinylated lipomannan and cytochromes in the extracts was measured. Treatment with a variety of non-denaturing detergents produced extracts that were generally qualitatively uniform although quantitative differences were observed. The degree of extraction of various components was correlated with the hydrophile-lipophile balance. Several chaotropic agents were also evaluated as reagents for membrane solubilization. These agents were less effective in extraction of bulk protein, but produced extracts enriched in some membrane components. 相似文献
8.
9.
CRAIG A. FAULHABER NOVA J. SILVY ROEL R. LOPEZ DAVID H. LAFEVER PHILIP A. FRANK MARKUS J. PETERSON 《The Journal of wildlife management》2008,72(5):1161-1167
Abstract: We used radiotelemetry to locate daytime forms of endangered Lower Keys marsh rabbits (LKMRs; Sylvilagus palustris hefneri) throughout their range so we could determine habitat characteristics of diurnal cover. We typically found forms (n = 1,298) of 36 rabbits in brackish wetlands in patches of saltmarsh or buttonwoods. In freshwater wetlands, forms (n = 54) were located most often in patches of freshwater hardwoods embedded in or adjacent to freshwater marshes. Forms (n = 942) in brackish wetlands were characterized by thick groundcover (>75%), whereas those (n = 42) in freshwater wetlands had both thick groundcover and canopy vegetation. The mean minimum convex polygon around forms of 15 rabbits was 1.4 ha (SD = 1.7), with smaller ranges characterized by thick bunchgrasses or clump-forming sedges. To increase the amount of annual space usable by LKMRs, managers should provide more saltmarsh habitat interspersed with buttonwoods and enhance ground cover in existing habitat. 相似文献
10.
Diego Sustaita Patty Finfrock Quickert Laura Patterson Laureen Barthman-Thompson Sarah Estrella 《The Journal of wildlife management》2011,75(6):1498-1507
We undertook a 2-year (2002–2004) mark–recapture study to investigate demographic performance and habitat use of salt marsh harvest mice (Reithrodontomys raviventris halicoetes) in the Suisun Marsh. We examined the effects of different wetland types and microhabitats on 3 demographic variables: density, reproductive potential, and persistence. Our results indicate that microhabitats dominated by mixed vegetation or pickleweed (Salicornia spp.) supported similar salt marsh harvest mouse densities, reproductive potential, and persistence throughout much of the year, whereas few salt marsh harvest mice inhabited upland grass-dominated microhabitats. We found that densities were higher in diked wetlands, whereas post-winter persistence was higher in tidal wetlands, and reproductive potential did not differ statistically between wetland types. Our results emphasize the importance of mixed vegetation for providing adequate salt marsh harvest mouse habitat and suggest that, despite their physiognomic and hydrological differences, both diked and tidal wetlands support salt marsh harvest mouse populations by promoting different demographic attributes. We recommend that habitat management, restoration, and enhancement efforts include areas containing mixed vegetation in addition to pickleweed in both diked and tidal wetlands. © 2011 The Wildlife Society. 相似文献