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1.
Amides from indole-3-glyoxylic acid and 4-benzoyl-2-methylpiperazine, which are related to entry inhibitors developed by Bristol-Myers Squibb (BMS), have been synthesized with aliphatic chains located at the C7 position of the indole ring. These spacers contain an azido group suitable for the well-known Cu(I)-catalyzed (3+2)-cycloaddition or an activated triple bond for the nucleophilic addition of thiols under physiological conditions. Reaction with polyols (β-cyclodextrin and hyperbranched polyglycerol) decorated with complementary click partners has afforded polyol-BMS-like conjugates that are not cytotoxic (TZM.bl cells) and retain the activity against R5-HIV-1NLAD8 isolates. Thus, potential vaginal microbicides based on entry inhibitors, which can be called of 4th generation, are reported here for the first time.  相似文献   
2.
Journal of Chemical Ecology - Biocontrol agents such as parasitic wasps use long-range volatiles and host-associated cues from lower trophic levels to find their hosts. However, this chemical...  相似文献   
3.
Analog Integrated Circuits and Signal Processing - In this paper a four mode 130 nm RF CMOS power amplifier (PA) in a single propagation path topology is presented and evaluated with IEEE...  相似文献   
4.
This study assessed the performance of modeling approaches to estimate personal exposure in Kenyan homes where cooking fuel combustion contributes substantially to household air pollution (HAP). We measured emissions (PM2.5, black carbon, CO); household air pollution (PM2.5, CO); personal exposure (PM2.5, CO); stove use; and behavioral, socioeconomic, and household environmental characteristics (eg, ventilation and kitchen volume). We then applied various modeling approaches: a single-zone model; indirect exposure models, which combine person-location and area-level measurements; and predictive statistical models, including standard linear regression and ensemble machine learning approaches based on a set of predictors such as fuel type, room volume, and others. The single-zone model was reasonably well-correlated with measured kitchen concentrations of PM2.5 (R2 = 0.45) and CO (R2 = 0.45), but lacked precision. The best performing regression model used a combination of survey-based data and physical measurements (R2 = 0.76) and a root mean-squared error of 85 µg/m3, and the survey-only-based regression model was able to predict PM2.5 exposures with an R2 of 0.51. Of the machine learning algorithms evaluated, extreme gradient boosting performed best, with an R2 of 0.57 and RMSE of 98 µg/m3.  相似文献   
5.
Characteristics of sheep milk are of great interest for the dairy industry, as almost the totality of production is intended for cheesemaking. However, the existing relationships between these variables are complex. This study assessed composition, hygienic quality, coagulation properties, and curd yield of 1,200 individual Manchega sheep milk samples. The aim was to compare the effect of composition and hygienic quality on coagulation and curdling, and to evaluate the relationship between curd yields and the coagulation process and the effect of other features by using path analysis methodologies. Outcomes proved path analysis to be a useful and effective tool to assess these relationships through direct and indirect paths within the same model. Results showed that the factors that had a direct influence on milk coagulation were lactose concentration, casein content, and initial pH of milk. Contrastingly, somatic cells did not seem to have any effect (direct or indirect) on the coagulation process. Factors that directly affected curd yield were fat content, lactose concentration, casein content, and curd moisture. However, technological parameters showed little effect over curd yield.  相似文献   
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Water Resources Management - This paper aims to evaluate the possibility of using non-utilized hydraulic energy in urban water distribution systems. For this purpose, the viability and possible...  相似文献   
9.
The objective of this study was to characterise the nutritional potential of leaves and identify a diversity centre with low cyanide and high nutrient content among 178 Latin American cassava genotypes. This field-based collection represents the seven diversity centres, held at The International Center for Tropical Agriculture (CIAT Palmira, Colombia) by the Cassava Program. The cyanide, all-trans-β-carotene and lutein concentrations in cassava leaves ranged from 346 to 7484 ppm dry basis (db), from 174–547 μg g−1 db and 15–181 μg g−1 db, respectively. Cassava leaves also showed significant levels of essential amino acids leucine, lysine, phenylalanine, valine and threonine, and average total protein content of 26.24 g 100 g−1 db. Among seven diversity centres, South American rainforest group showed low cyanide and high carotene content in leaves. In addition, VEN77 and PAN51 genotypes stood out for having low cyanide in leaves and roots and high carotene in leaves. This genetic diversity can be used to select high potential progenitors for breeding purposes.  相似文献   
10.
Spontaneous mutations in the EEF1A2 gene cause epilepsy and severe neurological disabilities in children. The crystal structure of eEF1A2 protein purified from rabbit skeletal muscle reveals a post-translationally modified dimer that provides information about the sites of interaction with numerous binding partners, including itself, and maps these mutations onto the dimer and tetramer interfaces. The spatial locations of the side chain carboxylates of Glu301 and Glu374, to which phosphatidylethanolamine is uniquely attached via an amide bond, define the anchoring points of eEF1A2 to cellular membranes and interorganellar membrane contact sites. Additional bioinformatic and molecular modeling results provide novel structural insight into the demonstrated binding of eEF1A2 to SH3 domains, the common MAPK docking groove, filamentous actin, and phosphatidylinositol-4 kinase IIIβ. In this new light, the role of eEF1A2 as an ancient, multifaceted, and articulated G protein at the crossroads of autophagy, oncogenesis and viral replication appears very distant from the “canonical” one of delivering aminoacyl-tRNAs to the ribosome that has dominated the scene and much of the thinking for many decades.  相似文献   
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