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Algirdas Mikalkėnas Bazilė Ravoitytė Daiva Tauraitė Elena Servienė Rolandas Meškys 《Journal of enzyme inhibition and medicinal chemistry》2018,33(1):384-389
Small molecule inhibitors have a powerful blocking action on viral polymerases. The bioavailability of the inhibitor, nevertheless, often raise a significant selectivity constraint and may substantially limit the efficacy of therapy. Phosphonoacetic acid has long been known to possess a restricted potential to block DNA biosynthesis. In order to achieve a better affinity, this compound has been linked with natural nucleotide at different positions. The structural context of the resulted conjugates has been found to be crucial for the acquisition by DNA polymerases. We show that nucleobase-conjugated phosphonoacetic acid is being accepted, but this alters the processivity of DNA polymerases. The data presented here not only provide a mechanistic rationale for a switch in the mode of DNA synthesis, but also highlight the nucleobase-targeted nucleotide functionalization as a route for enhancing the specificity of small molecule inhibitors. 相似文献
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Haruki Yamada Shūichi Yanahira Hiroaki Kiyohara Jong-Chol Cyong Yasuo Otsuka 《Phytochemistry》1985,25(1):129-132
The water-soluble major polysaccharides from the seed of Coix lacryma-jobi var. ma-yuen eluted as a broad peak by gel filtration on Sepharose CL-2B. The mixture (CS-Glucan) was resolved into 7 glucans by HPLC on the column of Asahi-Pak GS-510 + GS-320. Similarities were observed between M, shown in the gel filtration profile and the elution volume in HPLC. Methylation analysis indicated that the ethanol-fractionated CS-glucan contained 4-O- and 4,6-di-O-substituted glucosyl residues. 1H and 13C NMR data accorded with the results of methylation analysis, and the glycosidic linkages were shown to have an α-configuration. Thus, CS-glucan contained (1 → 4) linked α-d-glucans to which are attached glucosyl side chains at O-6 of the main chain in a similar way to amylopectin. Each purified glucan was shown to have different absorption maxima ( > 550 nm or 530 nm) in the iodine reaction. The results of the methylation analysis and of the pullulanase digestion suggest that the 550 nm-glucan has a lower branching frequency and shorter side chains than the 530 nm-glucan. Although CS-glucan was found to have weak anti-complementary activity, HPLC-purified > 550 nm-glucan was found to be more potent than the 530 nm-glucan. Thus CS-glucan is highly heterogeneous, and the glucans which form a tight complex when tested with iodine, generally tend to have considerable anti-complementary activity. 相似文献
5.
Growth and fecundity of Daphnia after diapause and their impact on the development of a population 总被引:1,自引:1,他引:0
Laboratory and field investigations revealed that the life history traits of exephippial and parthenogenetic generations of Daphnia differ substantially. Daphniids hatching from resting eggs grow faster and their definitive body sizes are bigger than of hatchlings from subitaneous eggs. Size at maturity for exephippial animals is significantly larger. In spite of this, they mature a few days earlier than parthenogenetic females. In this study, the difference was 3–4 days for the laboratory experiments and 1–3 days for the field. Fecundity of the exephippial generation is markedly higher. Here, the clutch size for this generation was up to 3.5–4.0 times as large as for the parthenogenetic generation. Moreover, obtained results suggest that the relationship between clutch size and body length for both generations differ significantly.Estimates of the intrinsic rate of increase for field Daphnia populations demonstrated that life history traits of exephippial animals lead to a two or threefold higher rate of increase in the conditions of invertebrate predation pressure. Under moderate fish pressure, obtained r values for the daphniids hatching from resting eggs were larger than those from subitaneous. High growth rate of exephippial females is disadvantageous only under the conditions of severe pressure by fish. Obtained results suggest that hatchlings from diapausing eggs an acceleration of population increase by several times during the beginning of the development of a population with periodical re-establishment from resting eggs. 相似文献
6.
Martina Ferraguti Sergio Magallanes Jéssica Jiménez-Peñuela Josué Martínez-de la Puente Luz Garcia-Longoria Jordi Figuerola Jaime Muriel Tamer Albayrak Staffan Bensch Camille Bonneaud Rohan H. Clarke Gábor Á. Czirják Dimitar Dimitrov Kathya Espinoza John G. Ewen Farah Ishtiaq Wendy Flores-Saavedra László Zsolt Garamszegi Olof Hellgren Dita Horakova Kathryn P. Huyvaert Henrik Jensen Asta Križanauskienė Marcos R. Lima Charlene Lujan-Vega Eyðfinn Magnussen Lynn B. Martin Kevin D. Matson Anders Pape Møller Pavel Munclinger Vaidas Palinauskas Péter L. Pap Javier Pérez-Tris Swen C. Renner Robert Ricklefs Sergio Scebba Ravinder N. M. Sehgal Manuel Soler Eszter Szöllősi Gediminas Valkiūnas Helena Westerdahl Pavel Zehtindjiev Alfonso Marzal 《Global Ecology and Biogeography》2023,32(5):809-823
Aim
The increasing spread of vector-borne diseases has resulted in severe health concerns for humans, domestic animals and wildlife, with changes in land use and the introduction of invasive species being among the main possible causes for this increase. We explored several ecological drivers potentially affecting the local prevalence and richness of avian malaria parasite lineages in native and introduced house sparrows (Passer domesticus) populations.Location
Global.Time period
2002–2019.Major taxa studied
Avian Plasmodium parasites in house sparrows.Methods
We analysed data from 2,220 samples from 69 localities across all continents, except Antarctica. The influence of environment (urbanization index and human density), geography (altitude, latitude, hemisphere) and time (bird breeding season and years since introduction) were analysed using generalized additive mixed models (GAMMs) and random forests.Results
Overall, 670 sparrows (30.2%) were infected with 22 Plasmodium lineages. In native populations, parasite prevalence was positively related to urbanization index, with the highest prevalence values in areas with intermediate urbanization levels. Likewise, in introduced populations, prevalence was positively associated with urbanization index; however, higher infection occurred in areas with either extreme high or low levels of urbanization. In introduced populations, the number of parasite lineages increased with altitude and with the years elapsed since the establishment of sparrows in a new locality. Here, after a decline in the number of parasite lineages in the first 30 years, an increase from 40 years onwards was detected.Main conclusions
Urbanization was related to parasite prevalence in both native and introduced bird populations. In invaded areas, altitude and time since bird introduction were related to the number of Plasmodium lineages found to be infecting sparrows. 相似文献7.
8.
The effect of increasing doses of intravenously administered propranolol on electrophysiological features of heart was studied in 17 patients with untreated hyperthyroidism by using the transesophageal stimulation method. A positive and dose-dependent effect of propranolol on the studied parameters was found with the normalization of the majority of disturbances taking place after the administration of 6 mg of propranolol. This dose was safe and well tolerated by the patients. The sensitivity of the auriculo-ventricular junction to propranolol was less pronounced during the stimulated rhythm than during the sinus rhythm. 相似文献
9.
Šukienė Laura Šaulienė Ingrida Dubakienė Rūta Rudzevičienė Odilija Daunys Gintautas 《Aerobiologia》2021,37(4):843-860
Aerobiologia - Airborne allergenic pollen affects a significant part of the population and the information on pollen load is a valuable tool for public health prevention. The messages should be... 相似文献
10.
Feldmane Daina Druva-Lūsīte Ieva Pole Valentīna Butac Mădălina Maria Militaru Mădălina Missa Imants Meiere Diāna Rubauskis Edgars 《Journal of Plant Growth Regulation》2021,40(2):533-540
Journal of Plant Growth Regulation - Sour cherry ‘Latvijas Zemais’ (Prunus cerasus) is a promising dwarfing rootstock for sweet cherries in Latvia, but low growing rate of newly... 相似文献