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191.
Summary Structure-activity relationships of cyclic substance P (SP) analogs were extensively studied in our laboratories utilizing the new concept of backbone cyclization. Employing the C-terminal hexapeptide SP6–11, we examined the influence of chemical changes in peptides containing backbone-to-amino-end cyclization. These changes in the ring have significant influence on activity, and should be carefully designed in order to optimize pharmacological feature.  相似文献   
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Shlesinger  Tom  Loya  Yossi 《Coral reefs (Online)》2016,35(4):1357-1368

Events of mass coral bleaching and mortality have increased in recent decades worldwide, making coral recruitment more important than ever in sustaining coral-reef ecosystems and ensuring their resilience. During the last four decades, the coral reefs of Eilat have undergone severe deterioration due to both anthropogenic and natural causes. Recruitment failure has been frequently suggested as one of the main mechanisms underlying this deterioration. Here we assess the demographic replenishment and resilience potential of the local reefs, i.e., the potential for new sexually derived corals to recruit and exceed the community’s mortality rate. We present a detailed analysis of coral community demography, obtained by means of high-resolution photographic monitoring of permanently marked plots. Coral spats as small as 1 mm were documented and the detailed dynamics of coral recruitment and mortality were recorded, in addition to other common ecological measurements. The cumulative quantity of recruited individuals was twofold to fivefold higher than total mortality. The most significant predictor variable for coral recruitment among all ecological parameters measured was the available substrate for settlement, and the survival of recruited corals was correlated with reef structural complexity. Two consecutive annual reproductive seasons (June–September of each year) with high recruitment rates were monitored. Combined with the high survival of recruits and the increase in coral live cover and abundance, the findings from this study indicate an encouraging potential for recovery of these reefs.

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Sulfur amino acids [cysteine (Cys) and methionine (Met)] play two major roles during animal development: protein synthesis for growth and glutathione synthesis for defense. For caterpillars, the levels of sulfur amino acids found in foliar protein can be especially low relative to their nutritional needs. Previous work has measured concentrations of glutathione (GSH; containing Cys) in specific animal tissues, but has not examined whole‐body levels to ascertain the costliness of this defense in terms of Cys allocation. This study examined whether the production of GSH varies between species and within individuals in accordance with an insect's need for antioxidant defense. Secondly, we quantified the allocation of total Cys (peptide‐bound plus free Cys) to GSH in caterpillars as an estimate of its cost. Two contrasting species were compared: Lymantria dispar (Lymantriidae), a species that is highly defended, and Malacosoma disstria (Lasiocampidae), a species that is less defended. As expected, GSH levels were significantly higher in L. dispar than in M. disstria. Consistent with the function of the midgut as a first line of defense against ingested toxins, GSH levels were significantly higher in these tissues than in the whole bodies of both species. A major finding in this study was that a large fraction of total Cys is used to produce GSH: GSH in the midguts of L. dispar and M. disstria contained 23 and 21%, respectively, of the total Cys in these tissues, and the GSH in their remaining body tissues contained 19 and 17% of the total Cys in these tissues. Levels of total Cys in caterpillar tissues followed the same pattern of distribution as did GSH, producing a strong association between GSH and total Cys (R2 = 0.794). We conclude that GSH is a costly defense, especially in generalist tree‐feeding species such as L. dispar. These results further suggest that the large allocation of Cys to GSH in highly defended species might produce a tradeoff by limiting the amount of Cys available for rapid growth.  相似文献   
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Rhizopus delemar and associated species attack a wide range of fruit and vegetables after harvest. Host nutrients and acidic pH are required for optimal germination of R. delemar, and we studied how this process is triggered. Glucose induced spore swelling in an acidic environment, expressed by an up to 3-fold increase in spore diameter, whereas spore diameter was smaller in a neutral environment. When suspended in an acidic environment, the spores started to float, indicating a change in their density. Treatment of the spores with HgCl2, an aquaporin blocker, prevented floating and inhibited spore swelling and germ-tube emergence, indicating the importance of water uptake at the early stages of germination. Two putative candidate aquaporin-encoding genes—RdAQP1 and RdAQP2—were identified in the R. delemar genome. Both presented the conserved NPA motif and six-transmembrane domain topology. Expressing RdAQP1 and RdAQP2 in Arabidopsis protoplasts increased the cells'' osmotic water permeability coefficient (Pf) compared to controls, indicating their role as water channels. A decrease in R. delemar aquaporin activity with increasing external pH suggested pH regulation of these proteins. Substitution of two histidine (His) residues, positioned on two loops facing the outer side of the cell, with alanine eliminated the pH sensing resulting in similar Pf values under acidic and basic conditions. Since hydration is critical for spore switching from the resting to activate state, we suggest that pH regulation of the aquaporins can regulate the initial phase of R. delemar spore germination, followed by germ-tube elongation and host-tissue infection.  相似文献   
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Gene-activating lipophilic compounds are carried into the nucleus when loaded on fatty-acid-binding proteins (FABP). Some of these proteins are recognized by the α-Karyopherin (Kapα) through its nuclear localization signal (NLS) consisting of three positive residues that are not in a continuous sequence. The Importin system can distinguish between FABP loaded with activating and non-activating compounds. In the present study, we introduced molecular dynamics as a tool for clarifying the mechanism by which FABP4, loaded with activating ligand (linoleate) is recognized by Kapα. In the first phase, we simulated the complex between KapαΔIBB (termed “Armadillo”) that was crystallized with two NLS hepta-peptides. The trajectory revealed that the crystal-structure orientation of the peptides is rapidly lost and new interactions dominate. Though, the NLS sequence of FABP4 is cryptic, since the functional residues are not in direct sequence, implicating more than one possible conformation. Therefore, four possible docked conformations were generated, in which the NLS of FABP4 is interacting with either the major or the minor sites of Kapα, and the N → C vectors are parallel or anti-parallel. Out of these four basic starting positions, only the FABP4-minor site complex exhibited a large number of contact points. In this complex, the FABP interacts with the minor and the major sites, suppressing the self-inhibitory interaction of the Kapα, rendering it free to react with Kapβ. Finally, we propose that the transportable conformation generated an extended hydrophobic domain which expanded out of the boundary of the FABP4, allowing the loaded linoleate to partially migrate out of the FABP into a joint complex in which the Kapα contributes part of a combined binding pocket.  相似文献   
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Investigating the alimentary tract in several species of lizardfishes (Synodontidae, Teleostei) of the genera Saurida, Synodus and Trachinocephalus, from various sites of their distribution, revealed melanization of the tract wall. This phenomenon was observed in several species of the genus Saurida, but not in the other two genera. This melanization is caused by layers of melanosomes rich in melanin granules and deposited within the connective tissue of the submucosa, between the muscular wall and the muscularis submucosa. From this site this black submucosa extends into the folds of the mucosa. In S. tumbil and S. filamentosa, the entire alimentary tract is black, whereas in S. macrolepis only the stomach is partially or entirely black. This phenomenon and its possible importance are discussed.  相似文献   
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