Highly potent, selective, and bioavailable inhibitors of human, mouse, or rat cathepsin S are described. The key structural features combine a sulfonyl moiety attached to a large group in P2 and a small substituent in P3. 相似文献
The Na(+)/H(+) exchanger regulatory factor 2 (NHERF2/TKA-1/E3KARP) contains two PSD-95/Dlg/ZO-1 (PDZ) domains which interact with the PDZ docking motif (X-(S/T)-X-(V/L)) of proteins to mediate the assembly of transmembrane and cytosolic proteins into functional signal transduction complexes. One of the PDZ domains of NHERF2 interacts specifically with the DSLL, DSFL, and DTRL motifs present at the carboxy-termini of the 2-adrenergic receptor, the platelet-derived growth factor receptor, and the cystic fibrosis transmembrane conductance regulator, respectively. Serum- and glucocorticoid-induced protein kinase 1 (SGK1) also carries a putative PDZ-binding motif (D-S-F-L) at its carboxy tail, implicated in the specific interaction with NHERF2. There is a 3-phosphoinositide-dependent protein kinase 1 (PDK1) interacting fragment (PIF) in the tail of NHERF2. Using pull-down assays and co-transfection experiments, we demonstrated that the DSFL tail of SGK1 interacts with the first PDZ domain of NHERF2 and the PIF of NHERF2 binds to the PIF-binding pocket of PDK1 to form an SGK1-NHERF2-PDK1 complex. Formation of the protein complex promoted the phosphorylation and activation of SGK1 by PDK1. Thus, it was suggested that NHERF2 mediates the activation and phosphorylation of SGK1 by PDK1 through its first PDZ domain and PIF motif, as a novel SGK1 activation mechanism. 相似文献
Recycled paper mills produce large quantities of fibrous rejects and fines which are usually sent to landfills as solid waste. These cellulosic materials can be enzymatically hydrolyzed into sugars for the production of biofuels and biomaterials. Paper mill wastes also contain large amounts of calcium carbonate which inhibits cellulase activity. The calcium carbonate (30%, w/w) decreased 40–60% of sugar yield of unbleached softwood kraft pulp. The prime mechanisms for this are by pH variation, competitive and non-productive binding, and aggregation effect. Addition of acetic acid (pH adjustment) increased the sugar production from 19 to 22 g/L of paper mill waste fibers. Strong affinity of enzyme—calcium carbonate decreased free enzyme in solution and hindered sugar production. Electrostatic and hydrogen bond interactions are mainly possible mechanism of enzyme—calcium carbonate adsorption. The application of the nonionic surfactant Tween 80 alleviated the non-productive binding of enzyme with the higher affinity on calcium carbonate. Dissociated calcium ion also inhibited the hydrolysis by aggregation of enzyme.
To investigate the relationship between crown width of a parent plant and seedling distribution, seedling ages and sizes, and their distances from the maternal tree were surveyed under a maple (Acer palmatum) crown at Chungdam Park, Chungdam-dong, Kangnam-gu, Seoul, in 1998. Maple crown width increased 33.0 cm per year during the eight-year study. Seedlings ranged from 1 to 10 years old; their density was highest the third year, and decreased with age. Seedling-distribution ranges from the parent plant were 43 cm to 487 cm, and seedling density was highest at the border of the parent plant canopy. One-year-old seedlings were distributed broadly, but the main distribution areas became more distant from the maternal plant with seedling age. Seedling heights increased with age; differences between two consecutive ages were significant at the 0.1% level for ages less than 5 years, but not for over 6 years. For seedlings of the same age, heights were similar, but short under the tree crown, but were varied and taller outside the crown. The variation in seedling height increased with age and distance from the parent plant In particular, seedlings older than 5 years that were distributed outside the crown showed conspicuous variations among distance classes. Therefore, maple seedlings were distributed to an appropriate distance at which their growth could be supported by the understory-light environment. This study demonstrated that newA. palmatum trees are not recruited from the seedlings growing beneath the crown but from those that grow vigorously outside the crown. 相似文献
Mitochondrial fatty acid -oxidation is an important energy resource for many mammal tissues. Acyl-CoA dehydrogenases (ACADs) are a family of flavoproteins that are involved in the -oxidation of the fatty acyl-CoA derivatives. Deficiency of these ACADs can cause metabolic disorders including muscle fatigue, hypoglycaemia, hepatic lipidosis and so on. By large scale sequencing, we identified a cDNA sequence of 3960 base pairs with a typical acyl-CoA dehydrogenase function domain. RT-PCR result shows that it is widely expressed in human tissues, especially high in liver, kidney, pancreas and spleen. It is hypothesized that this is a novel member of ACADs family.
Abbreviations: ACADs – acyl-CoA dehydrogenases, FAD – flavinadenine dinucleotide, SCAD – short-chain acyl-CoA dehydrogenase,MCAD – medium-chain acyl-CoA dehydrogenase, LCAD – long-chain acyl-CoAdehydrogenase, VLCAD – very long- chain acyl-CoA dehydrogenase, IVD –isocalery-CoA dehydrogenase, SBCAD – short/branched chain acyl-CoAdehydrogenase, GCD – glutaryl- CoA dehydrogenase, ETF – electron transferflavoprotein, ACAD8 – acyl-CoA dehydrogenase 8, ACAD9 – acyl-CoAdehydrogenase 9, ACAD10 – acyl-CoA dehydrogenase 10. 相似文献
Heloniopsis orientalis (Liliaceae) is an important horticultural crop native to Korea. Under natural conditions, germination is poor and plant growth
is delayed. Therefore, we have developed a vegetative propagation method to produce plants with vigorous growth characteristics
via tissue culture. Leaf tissues were cultured on MS basal media supplemented with growth regulators 2,4-D, TDZ, BA, or zeatin.
The regenerated shoots were then initiated directly from leaf expiants on an MS medium containing either 0.1 to 1.0 mg/L 2,4-D
or 0.1 to 3.0 mg/L BA. Healthy plantlets with adventitious roots were formed on the medium supplemented with 0.1 mg/L BA.
TDZ triggered callus initiation without caulogenesis or rhizogenesis, and callus formation was better on the half-strength
MS medium than on the full-strength medium. After the plants were acclimatized for one month at 4°C, they were successfully
transferred to soil. In addition, we used LM and SEM to investigate shoot morphogenesis at various stages of differentiation. 相似文献
正Dear Editor,Dispute between agriculture and initial population expansion in Neolithic Time has been in suspense for a long time.Agriculture first appeared in the Fertile Crescent of West Asia about 11–12 thousand years ago(kya),with domesticating few wild plant and animal species.There is also evidence of the cultivation of rice and millet in Yangtze and Yellow River Basins of China approximately 9 kya.During the subsequent times between 9 and 4 kya,agriculture arose 相似文献