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61.
Identification of amino acid residues involved in the binding of Huperzine A to cholinesterases. 总被引:2,自引:0,他引:2 下载免费PDF全文
A. Saxena N. Qian I. M. Kovach A. P. Kozikowski Y. P. Pang D. C. Vellom Z. Radi D. Quinn P. Taylor B. P. Doctor 《Protein science : a publication of the Protein Society》1994,3(10):1770-1778
Huperzine A, a potential agent for therapy in Alzheimer's disease and for prophylaxis of organophosphate toxicity, has recently been characterized as a reversible inhibitor of cholinesterases. To examine the specificity of this novel compound in more detail, we have examined the interaction of the 2 stereoisomers of Huperzine A with cholinesterases and site-specific mutants that detail the involvement of specific amino acid residues. Inhibition of fetal bovine serum acetylcholinesterase by (-)-Huperzine A was 35-fold more potent than (+)-Huperzine A, with KI values of 6.2 nM and 210 nM, respectively. In addition, (-)-Huperzine A was 88-fold more potent in inhibiting Torpedo acetylcholinesterase than (+)-Huperzine A, with KI values of 0.25 microM and 22 microM, respectively. Far larger KI values that did not differ between the 2 stereoisomers were observed with horse and human serum butyrylcholinesterases. Mammalian acetylcholinesterase, Torpedo acetylcholinesterase, and mammalian butyrylcholinesterase can be distinguished by the amino acid Tyr, Phe, or Ala in the 330 position, respectively. Studies with mouse acetylcholinesterase mutants, Tyr 337 (330) Phe and Tyr 337 (330) Ala yielded a difference in reactivity that closely mimicked the native enzymes. In contrast, mutation of the conserved Glu 199 residue to Gln in Torpedo acetylcholinesterase produced only a 3-fold increase in KI value for the binding of Huperzine A.(ABSTRACT TRUNCATED AT 250 WORDS) 相似文献
62.
河南叶县下寒武统辛集组单板类和腹足类化石的研究 总被引:8,自引:3,他引:5
本文描述和讨论了河南叶县杨寺庄下寒武统辛集组单板类13种,腹足类2种,未定类1种。其中包括2新属6新种:Repenoconus xinjiensis gen.nov.,Scenella pycna sp.nov.,Securiconus vulgaris sp.nov.,Obtusocnus grossicostus sp.nov.,Igorellina proboscis sp.nov.,Gal 相似文献
63.
薏苡胚发育及贮藏营养物质积累的研究 总被引:4,自引:0,他引:4
薏苡(Coix lacrym a-jobi)胚发育分下列各期:棒形胚前的原胚期、棒形胚期、胚芽鞘期、1叶期、2 叶期、3叶期、4 叶期、5 叶期及6叶期成熟胚。3 叶期胚具1 条不定根(种子根),4 叶期具2 条,5 叶期及成熟胚期具3 条。不定根与胚根排成1 纵行。营养物质最先在盾片细胞中积累。开花后9 天的1 叶期胚,在盾片、胚芽鞘及胚轴细胞中积累了淀粉,以后遍及成熟胚的各部分。淀粉粒含量与器官发生及生长顺序成正相关,但发育后期,盾片细胞内的淀粉粒含量下降。开花后10 天,盾片细胞中形成含晶体的蛋白质体,晶体含蛋白质及植酸钙镁。以后,这种蛋白质体增多、增大。同时,又形成不含晶体的蛋白质体。一定时期,含晶体的蛋白质体消失,不含晶体的蛋白质体增多,直到胚成熟。开花后13 天,胚芽鞘上部细胞形成蛋白质体。以后遍及成熟胚的各部分,器官发生越早,所含蛋白质体越多、越大。开花后10 天,盾片细胞中产生了脂体,成熟胚的盾片细胞,含有大量的脂体。还观察了胚发育各期与颖果及盾片长度的对应关系 相似文献
64.
Gary L. Johnson Anne M. Gardner Carol Lange-Carter Nan-Xin Qian Marijane Russell Sim Winitz 《Journal of cellular biochemistry》1994,54(4):415-422
Serpentine receptors coupled to the heterotrimeric G protein, Gi2, are capable of stimulating DNA synthesis in a variety of cell types. A common feature of the Gi2-coupled stimulation of DNA synthesis is the activation of the mitogen-activated protein kinases (MAPKs). The regulation of MAPK activation by the Gi2-coupled thrombin and acetylcholine muscarinic M2 receptors occurs by a sequential activation of a network of protein kinases. The MAPK kinase (MEK) which phosphorylates and activates MAPK is also activated by phosphorylation. MEK is phosphorylated and activated by either Raf or MEK kinase (MEKK). Thus, Raf and MEKK converge at MEK to regulate MAPK. Gi2-coupled receptors are capable of activating MEK and MAPK by Raf-dependent and Raf-independent mechanisms. Pertussis toxin catalyzed ADP-ribosylation of αi2 inhibits both the Raf-dependent and-independent pathways activated by Gi2-coupled receptors. The Raf-dependent pathway involves Ras activation, while the Raf-independent activation of MEK and MAPK does not involve Ras. The Raf-independent activation of MEK and MAPK most likely involves the activation of MEKK. The vertebrate MEKK is homologous to the Ste11 and Byr2 protein kinases in the yeast Saccharomyces cerevisiae and Schizosaccharomyces pombe, respectively. The yeast Ste11 and Byr2 protein kinases are involved in signal transduction cascades initiated by pheromone receptors having a 7 membrane spanning serpentine structure coupled to G proteins. MEKK appears to be conserved in the regulation of G protein-coupled signal pathways in yeast and vertebrates. Raf represents a divergence in vertebrates from the yeast pheromone-responsive protein kinase system. Defining MEKK and Raf as a divergence in the MAPK regulatory network provides a mechanism for differential regulation of this system by Gi2-coupled receptors as well as other receptor systems, including the tyrosine kinases. 相似文献
65.
玉米胚性愈伤组织的长期继代及其染色体分析 总被引:23,自引:1,他引:22
对5种基因型幼胚诱导的愈伤组织继代培养表明,玉米胚性愈伤组织的长期继代受基因型,培养基成分,激素,培养条件的影响。适时继代,逐代筛选对胚性保持起重要作用。适当降低培养温度(12±2℃)有利于愈伤组织的保存和胚性保持,可以减少愈伤组织长期继代所需的物质和工作量。长期继代培养的胚性愈伤组织,胚状体发生能力和植株再生率无显著变化,但正常苗的再生频率显著下降。观察愈伤组织细胞染色体发现:(1)基因型对不同倍性细胞的比例有明显影响。(2)随着继代时间的延长,二倍体细胞下降,四倍体和非二倍体细胞增多。(3)愈伤组织中出现多种染色体结构变异,这些结构变异有可能导致非整倍体细胞的形成。 相似文献
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