Substituted dipiperidine alcohols as potent CCR2 antagonists

The synthesis and biological evaluation of a series of substituted dipiperidine alcohols are described. Structure-activity relationship studies led to the discovery of potent CCR2 antagonists displaying IC(50) values in the nanomolar or subnanomolar range. The cinnamoyl compounds had higher binding affinities than the corresponding urea analogs.     

Point pattern analysis of different age-classes of Larix principis-rupprechtii in Luya Mountain Reserve, Shanxi Province, China

Larix principis-rupprechtii forest is an important vegetation formation and has a large distribution area in Luya Mountain Reserve, China. Spatial pattern analysis on individual trees in different age-classes of Larix principis-rupprechtii was made in this paper. Here, we employed the technique of point pattern analysis, which could analyze patterns under all scales along a gradient. It was based on spatial mapped points of individual distribution. The results of this study showed that the densities of the five age-classes varied in the order: age-class 3 > age-class 4 > age-class 5 > age-class 2 > age-class 1. Although age-classes 1 and 2 have much fewer individuals than other three age-classes do, the population was stable at present. However, it would be necessary to take some measures for improving population regeneration for a long-time view. The individuals of all age-classes focused on clumping distribution in space; however, their distribution pattern varied with the change of scale. This mainly depended on biological features of Larix principis-rupprechtii and forest environments, but it also meant that the scale was an important factor in controlling spatial distribution pattern of tree individuals. The feature of clumping distribution became more significant with the increase of age. The relationships between individuals in different age-classes were almost all significantly correlated with each other. These associations became more significant within the older age-classes. This suggested that the individuals of different age-classes were interdistributed, by which the population could get benefits in resource utilization. The technique of point pattern analysis is effective and easy to be used in species pattern study. Its results are more closer to the reality, especially for community structure. Translated from Acta Ecologica Sinica, 2004, 24(1): 35–40 [译自: 生态学报]     

Biodegradation and detoxification of nicotine in tobacco solid waste by a Pseudomonas sp.

A Pseudomonas sp. grew with nicotine optimally 3 g l^–1 and at 30 °C and pH 7. Nicotine was fully degraded within 10 h. The resting cells degraded nicotine in tobacco solid waste completely within 6 h in 0.02 m sodium phosphate buffer (pH 7) at maximally 56 mg nicotine h^–1 g dry cell^–1.     

Donor substrate recognition in the raffinose-bound E342A mutant of fructosyltransferase <Emphasis Type="Italic">Bacillus subtilis</Emphasis> levansucrase

Background  

Fructans – β-D-fructofuranosyl polymers with a sucrose starter unit – constitute a carbohydrate reservoir synthesised by a considerable number of bacteria and plant species. Biosynthesis of levan (αGlc(1–2)βFru [(2–6)βFru]_n), an abundant form of bacterial fructan, is catalysed by levansucrase (sucrose:2,6-β-D-fructan-6-β-D-fructosyl transferase), utilizing sucrose as the sole substrate. Previously, we described the tertiary structure of Bacillus subtilis levansucrase in the ligand-free and sucrose-bound forms, establishing the mechanistic roles of three invariant carboxylate side chains, Asp86, Asp247 and Glu342, which are central to the double displacement reaction mechanism of fructosyl transfer. Still, the structural determinants of the fructosyl transfer reaction thus far have been only partially defined.     

AIDA Selectively Mediates Downregulation of Fat Synthesis Enzymes by ERAD to Retard Intestinal Fat Absorption and Prevent Obesity

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凝血瀑布机制的序结构分析方法

凝血系统的瀑布机制揭示了凝血因子间的酶促级联反应过程。在级联反应中,各个因子间明显地存在着序关系,而这种序关系的全体构成了系统的序结构。从系统论的观点看,系统的结构是系统性质与功能的基础,因此,通过模型化方法以及利用凝血因子序结构图建立的序结构分析方法,是分析凝血系统各因子相互作用的有用的工具。对蛋白Ｃ及ＴＦＰＩ进行序结构分析,进一步阐明了这两种抑制剂对外源途径凝血的作用特点。     

Cytotoxic,clonal fidelity,and antioxidant evaluation of in vitro propagated Vitex negundo var. cannabifolia

Plant Cell, Tissue and Organ Culture (PCTOC) - Vitex negundo L. var. cannabifolia (Sieb. et Zucc.) Hand.-Mazz. is an important medicinal plant rich in bioactive compounds. In vitro tissue culture...