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71.
Cathy Poillot Kaouthar Dridi Hicham Bichraoui Julien Pêcher Sebastien Alphonse Badreddine Douzi Michel Ronjat Hervé Darbon Michel De Waard 《The Journal of biological chemistry》2010,285(44):34168-34180
Maurocalcine has been the first demonstrated animal toxin acting as a cell-penetrating peptide. Although it possesses competitive advantages, its use as a cell-penetrating peptide (CPP) requires that analogues be developed that lack its characteristic pharmacological activity on ryanodine-sensitive calcium channels without affecting its cell-penetrating and vector efficiencies. Here, we present the synthesis, three-dimensional 1H NMR structure, and activity of d-maurocalcine. We demonstrate that it possesses all of the desired features for an excellent CPP: preserved structure, lack of pharmacological action, conserved vector properties, and absence of cell toxicity. This is the first report of a folded/oxidized animal toxin in its d-diastereomer conformation for use as a CPP. The protease resistance of this new peptide analogue, combined with its efficient cell penetration at concentrations devoid of cell toxicity, suggests that d-maurocalcine should be an excellent vector for in vivo applications. 相似文献
72.
Jos H.M. Lange Martina A.W. van der Neut Henri C. Wals Gijs D. Kuil Alice J.M. Borst Arie Mulder Arnold P. den Hartog Hicham Zilaout Wouter Goutier Herman H. van Stuivenberg Bernard J. van Vliet 《Bioorganic & medicinal chemistry letters》2010,20(3):1084-1089
The synthesis and structure–activity relationship studies of imidazoles are described. The target compounds 6–20 represent a novel chemotype of potent and CB2/CB1 selective cannabinoid CB2 receptor antagonists/inverse agonists with very high binding efficiencies in combination with favourable log P and calculated polar surface area values. Compound 12 exhibited the highest CB2 receptor affinity (Ki = 1.03 nM) in this series, as well as the highest CB2/CB1 subtype selectivity (>9708-fold). 相似文献
73.
Jos H.M. Lange Amos Attali Martina A.W. van der Neut Henri C. Wals Arie Mulder Hicham Zilaout Ate Duursma Hans H.M. van Aken Bernard J. van Vliet 《Bioorganic & medicinal chemistry letters》2010,20(17):4992-4998
The synthesis and SAR of 3-alkyl-4-aryl-4,5-dihydropyrazole-1-carboxamides 1–23 and 1-alkyl-5-aryl-4,5-dihydropyrazole-3-carboxamides 24–27 as two novel cannabinoid CB1 receptor agonist classes were described. The target compounds elicited high affinities to the CB1 as well as the CB2 receptor and were found to act as CB1 receptor agonists. The key compound 19 elicited potent CB1 agonistic and CB2 inverse agonistic properties in vitro and showed in vivo activity in a rodent model for multiple sclerosis after oral administration. 相似文献
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Hicham El Miri Mohamed Rhajaoui Oumnia Himmi Souâd Ouahabi Abdelaziz Benhoussa Chafika Faraj 《法国昆虫学会纪事》2013,49(2):154-159
Résumé. La leishmaniose cutanée est un important problème de santé publique dans la province de Sidi Kacem au nord-ouest du Maroc. L'incidence de cette affetion, due aussi bien à Leishmania tropica qu'à L. infantum est en augmentation progressive depuis 1997. La présente étude a été menée dans le but d'étudier l'écologie et la dynamique des populations des vecteurs de cette maladie dans les principaux foyers de cette province. Un total de 4504 spécimens appartenant à deux genres et six espèces a été capturé à l'aide de pièges adhésifs et lumineux, dans cinq foyers. Les espèces dominantes sont Phlebotomus sergenti représentant 42,6% du total des phlébotomes capturés et P. longicuspis avec 27,2% des captures. Ces deux espèces sont présentes de mai à novembre et évoluent en deux générations avec deux pics de densité, le premier en juin et le second en septembre. En considérant la grande spécificité vecteur-parasite connue en épidémiologie des leishmanioses ainsi que l'abondance des espèces capturées pendant la saison favorable à la transmission, P. sergenti et P. longicuspis seraient respectivement les vecteurs les plus probables des leishmanioses à L. tropica et à L. infantum dans la région étudiée. Le risque de transmission de la maladie serait plus grand durant le deuxième pic de densité en fin été- début automne. 相似文献
76.
Khalid El Allali Hicham Farsi Mohammed Piro Mohamed Rachid Achaâban Mohammed Ouassat Etienne Challet 《Chronobiology international》2013,30(8):1047-1057
ABSTRACTDaily pattern of locomotor activity (LA), one of the most studied rhythms in humans and rodents, has not been widely investigated in large mammals. This is partly due to the high cost and breakability of used automatic devices. Since last decade, smartphones are becoming ubiquitous. Meanwhile, several applications detecting activity by using internal sensors were made available. In this study, we assumed that this device could be a cheaper and easier way to measure the LA rhythm in humans and large mammals, like camel and goat. A smartphone application (Nokia Mate Health), normally used to quantify physical activities in humans, was chosen for the study. To validate the rhythm data obtained from the smartphone, LA rhythm was simultaneously recorded using an automatic device, the Actiwatch-Mini®. Results showed that the smartphone provided a clear and significant daily rhythm of LA. The visual assessment of the superimposed LA rhythm’s curves in all three species showed that the smartphone application displayed similar rhythms as those recorded by the Actiwatch-Mini. Highly significant positive correlation (p≤ 0.0001) exists between the two recording rhythms. The daily periods were both the same at 24.0 h. Acrophases were also significantly similar and occurring around mid-day: 11:40 ± 0.35 h vs 11:41 ± 0.35 h for the camel, 11:25 ± 0.19 h vs 11:37 ± 0.25 h for the goat and 13:04 ± 0.11 h vs 13:51 ± 0.28 h for humans using smartphone and Actiwatch, respectively. The related mesor and amplitude were also close between the two recording devices. Results indicate clearly that using smartphones constitutes a reliable cheap tool to study LA rhythm for chronobiology studies, especially in laboratories facing lack of funding. 相似文献
77.
Haouane H El Bakkali A Moukhli A Tollon C Santoni S Oukabli A El Modafar C Khadari B 《Genetica》2011,139(9):1083-1094
The conservation of cultivated plants in ex-situ collections is essential for the optimal management and use of their genetic
resources. For the olive tree, two world germplasm banks (OWGB) are presently established, in Córdoba (Spain) and Marrakech
(Morocco). This latter was recently founded and includes 561 accessions from 14 Mediterranean countries. Using 12 nuclear
microsatellites (SSRs) and three chloroplast DNA markers, this collection was characterised to examine the structure of the
genetic diversity and propose a set of olive accessions encompassing the whole Mediterranean allelic diversity range. We identified
505 SSR profiles based on a total of 210 alleles. Based on these markers, the genetic diversity was similar to that of cultivars
and wild olives which were previously characterised in another study indicating that OWGB Marrakech is representative of Mediterranean
olive germplasm. Using a model-based Bayesian clustering method and principal components analysis, this OWGB was structured
into three main gene pools corresponding to eastern, central and western parts of the Mediterranean Basin. We proposed 10
cores of 67 accessions capturing all detected alleles and 10 cores of 58 accessions capturing the 186 alleles observed more
than once. In each of the 10 cores, a set of 40 accessions was identical, whereas the remaining accessions were different,
indicating the need to include complementary criteria such as phenotypic adaptive and agronomic traits. Our study generated
a molecular database for the entire OWGB Marrakech that may be used to optimise a strategy for the management of olive genetic
resources and their use for subsequent genetic and genomic olive breeding. 相似文献
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Validation of microsatellite multiplexes for parentage analysis and species discrimination in two hybridizing species of coral reef fish (Plectropomus spp., Serranidae)
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Hugo B. Harrison Kevin A. Feldheim Geoffrey P. Jones Kayan Ma Hicham Mansour Sadhasivam Perumal David H. Williamson Michael L. Berumen 《Ecology and evolution》2014,4(11):2046-2057
Microsatellites are often considered ideal markers to investigate ecological processes in animal populations. They are regularly used as genetic barcodes to identify species, individuals, and infer familial relationships. However, such applications are highly sensitive the number and diversity of microsatellite markers, which are also prone to error. Here, we propose a novel framework to assess the suitability of microsatellite datasets for parentage analysis and species discrimination in two closely related species of coral reef fish, Plectropomus leopardus and P. maculatus (Serranidae). Coral trout are important fisheries species throughout the Indo‐Pacific region and have been shown to hybridize in parts of the Great Barrier Reef, Australia. We first describe the development of 25 microsatellite loci and their integration to three multiplex PCRs that co‐amplify in both species. Using simulations, we demonstrate that the complete suite of markers provides appropriate power to discriminate between species, detect hybrid individuals, and resolve parent–offspring relationships in natural populations, with over 99.6% accuracy in parent–offspring assignments. The markers were also tested on seven additional species within the Plectropomus genus with polymorphism in 28–96% of loci. The multiplex PCRs developed here provide a reliable and cost‐effective strategy to investigate evolutionary and ecological dynamics and will be broadly applicable in studies of wild populations and aquaculture brood stocks for these closely related fish species. 相似文献
80.
Ultrasmall (mean diameter, 2.7 nm) gold nanoparticles conjugated to doxorubicin (Au-Dox) are up to 20-fold more cytotoxic to B16 melanoma cells than the equivalent concentration of doxorubicin alone, and act up to six times more quickly. Ultrasmall Au-Dox enters the cell endocytic vesicles and is also seen free in the cytoplasm and nuclei. This is in distinct contrast to larger particles reported in previous studies, which are excluded from the nucleus and which show no increased toxicity over Dox alone. Cell death with Au-Dox is confirmed to be apoptotic by TUNEL staining and ultrastructural examination using transmission electron microscopy. To further explore the mechanism of action, two other cell lines were examined: HeLa cells which are highly sensitive to Dox, and HeLa cells overexpressing Bcl-2 which show impaired apoptosis and Dox resistance. Interestingly, the Dox-sensitive cells show a slightly decreased sensitivity to Au-Dox relative to Dox alone, whereas the Dox-resistant cells are not resistant to Au-Dox. These results have implications for the design of chemotherapeutic nanoparticles, suggesting that it is possible to selectively target apoptosis-resistant cancer cells while at the same time reducing cytotoxicity to normal cells. 相似文献