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101.
Hideo Satsu Marie-Therese Schaeffer Miguel Guerrero Adrian Saldana Christina Eberhart Peter Hodder Charmagne Cayanan Stephan Schürer Barun Bhhatarai Ed Roberts Hugh Rosen Steven J. Brown 《Bioorganic & medicinal chemistry》2013,21(17):5373-5382
Molecular probe tool compounds for the Sphingosine 1-phosphate receptor 2 (S1PR2) are important for investigating the multiple biological processes in which the S1PR2 receptor has been implicated. Amongst these are NF-κB-mediated tumor cell survival and fibroblast chemotaxis to fibronectin. Here we report our efforts to identify selective chemical probes for S1PR2 and their characterization. We employed high throughput screening to identify two compounds which activate the S1PR2 receptor. SAR optimization led to compounds with high nanomolar potency. These compounds, XAX-162 and CYM-5520, are highly selective and do not activate other S1P receptors. Binding of CYM-5520 is not competitive with the antagonist JTE-013. Mutation of receptor residues responsible for binding to the zwitterionic headgroup of sphingosine 1-phosphate (S1P) abolishes S1P activation of the receptor, but not activation by CYM-5520. Competitive binding experiments with radiolabeled S1P demonstrate that CYM-5520 is an allosteric agonist and does not displace the native ligand. Computational modeling suggests that CYM-5520 binds lower in the orthosteric binding pocket, and that co-binding with S1P is energetically well tolerated. In summary, we have identified an allosteric S1PR2 selective agonist compound. 相似文献
102.
Alexandra D. Ogorodnikova Unab I. Khan Aileen P. McGinn Irfan Zeb Matthew J. Budoff S.M. Harman Virginia M. Miller Eliot A. Brinton JoAnn E. Manson Howard N. Hodis George R. Merriam Marcelle I. Cedars Hugh S. Taylor Frederick Naftolin Rogerio A. Lobo Nanette Santoro Rachel P. Wildman 《Obesity (Silver Spring, Md.)》2013,21(8):1726-1733
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Ecological genetics of Italian peach‐potato aphid (Myzus persicae) populations in relation to geography,dispersal and insecticide resistance as studied using microsatellite and resistance markers 下载免费PDF全文
Valentina Monti Hugh D. Loxdale Michele Cesari Milo Frattini Michela Panini Emanuele Mazzoni Gian Carlo Manicardi 《Agricultural and Forest Entomology》2016,18(4):376-389
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107.
Hugh F. Davies Willie Rioli Jos Puruntatameri Willie Roberts Colin Kerinaiua Vivian Kerinauia Kim Brooks Womatakimi Graeme R. Gillespie Brett P. Murphy 《Austral ecology》2019,44(5):868-879
Since European settlement, many granivorous birds of northern Australia's savanna landscapes have declined. One such example, the partridge pigeon (Geophaps smithii), has suffered a significant range contraction, disappearing from at least half of its pre‐European range. Multiple factors have been implicated in this decline, including the loss of traditional Aboriginal burning practices, grazing by large exotic herbivores and predation by feral cats (Felis catus). While populations of partridge pigeon on the Tiwi Islands may be particularly important for the long‐term persistence of this species, they too may be at risk of decline. However, as a reliable method to detect this species has not yet been developed and tested, we lack the ability to identify, at an early stage, the species' decline in a given location or region. This severely limits our capacity to make informed management decisions. Here, we demonstrate that the standard camera trapping approach for native mammal monitoring in northern Australia attained an overall probability of detecting partridge pigeon greater than 0.98. We thus provide a robust estimate of partridge pigeon site occupancy (0.30) on Melville Island, the larger of the two main Tiwi Islands. The information presented here for the partridge pigeon represents a critical first step towards the development of optimal monitoring programmes with which to gauge population trajectories, as well as the response to remedial management actions. In the face of ongoing biodiversity loss, such baseline information is vital for management agencies to make informed decisions and should therefore be sought for as many species as possible. 相似文献
108.
Capparicordis, genus novum is established for Capparicordis crotonoides, C. tweediana, and C. yunckeri, all new combinations here established for three former species of the New World Capparis, Sect. Colicodendron. The first two are xerophytic shrubs or small trees easily separated by flower color, and the last is a grapple-hook scrambler of which flowers are unknown. They have allopatric distributions: C. crotonoides is found in Peru and Ecuador west of the Andes, C. tweediana from Argentina to Bolivia and Paraguay east of the Andes, whereas C. yunckeri is a rare, local endemic from the arid woodlands near Coyoles in northern Honduras. All have stellate pubescence, broadly cordate to subrotund-reniform leaves with (sub)palmate venation at the leaf blade base; a valvate calyx with closed aestivation; baccate subspherical fruits dehiscent by 2–4 valves (indehiscent in C. yunckeri?); cochleate-reniform seeds surrounded by a pulp-derived sarcotesta densely infiltrated by unbranched, unicellular hairs from the testa; and snow-white embryos. Capparicordis crotonoides has n=8 chromosomes. 相似文献
109.
Gonzalez-Voyer A Székely T Drummond H 《Evolution; international journal of organic evolution》2007,61(8):1946-1955
In many parentally fed species, siblings compete for food not only by begging and scrambling, but also by violently attacking each other. This aggressive competition has mostly been studied in birds, where it is often combined with dominance subordination, aggressive intimidation, and siblicide. Previous experimental and theoretical studies proposed several life-history, morphological, and behavioral variables that may facilitate the evolution of broodmate aggression, and explain its taxonomic distribution. Here we apply phylogenetic comparative analyses for the first time to test the influence of five hypothesized facilitators of the evolution of broodmate aggression, analyzing 69 species in seven avian families using two quantitative measures of aggression: incidence and intensity. We show that incidence and intensity of aggression increase with long nestling periods and indirect feeding, and small brood size is associated with intense aggression. Large food parcels were not correlated with either the incidence or intensity of aggression. Our study suggests that indirect feeding, long nestling periods, and small broods, possibly in combination with other factors, have tended to favor the evolution of aggressive broodmate competition. 相似文献
110.
Sommer ME Farrens DL McDowell JH Weber LA Smith WC 《The Journal of biological chemistry》2007,282(35):25560-25568
In this study we investigate conformational changes in Loop V-VI of visual arrestin during binding to light-activated, phosphorylated rhodopsin (Rho*-P) using a combination of site-specific cysteine mutagenesis and intramolecular fluorescence quenching. Introduction of cysteines at positions in the N-domain at residues predicted to be in close proximity to Ile-72 in Loop V-VI of arrestin (i.e. Glu-148 and Lys-298) appear to form an intramolecular disulfide bond with I72C, significantly diminishing the binding of arrestin to Rho*-P. Using a fluorescence approach, we show that the steady-state emission from a monobromobimane fluorophore in Loop V-VI is quenched by tryptophan residues placed at 148 or 298. This quenching is relieved upon binding of arrestin to Rho*-P. These results suggest that arrestin Loop V-VI moves during binding to Rho*-P and that conformational flexibility of this loop is essential for arrestin to adopt a high affinity binding state. 相似文献