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Chen Chen Raymond Dagnino Jr. Charles Q. Huang James R. McCarthy Dimitri E. Grigoriadis 《Bioorganic & medicinal chemistry letters》2001,11(24):3165-3168
Cyclizations of alkylhydrazines with N-acyl-S-methylisothioureas, readily synthesized from acyl chlorides, sodium thioisocyanate, dialkylamines then methyl iodide in a one-pot reaction, gave 1-alkyl-3-dialkylamino-5-phenyltriazoles 7 as major products. The regioisomers were assigned through the use of NOE NMR experiments. While bearing a N-bis(cyclopropyl)methyl-N-propylamino group, this series of compounds shows very good binding affinity on the human CRF1 receptor. Among them, 1-methyl-3-[N-bis(cyclopropyl)methyl-N-propylamino]-5-(2,4-dichlorophenyl)-1H-[1,2,4]triazole 7a had the best binding affinity for the CRF1 receptor (Ki=9 nM). 相似文献
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The light organ symbiont Vibrio fischeri possesses two distinct secreted ADP-ribosyltransferases. 下载免费PDF全文
We have previously described the purification, cloning, and initial characterization of a secreted ADP-ribosyltransferase, halovibrin (gene designation hvn), from the luminescent light organ symbiont Vibrio fischeri. This report describes a strategy for overexpression of halovibrin, the production and refinement of antihalo-vibrin antisera, and the molecular biological construction of a V. fischeri halovibrin null strain. Biochemical analysis of this mutant revealed that V. fischeri hvn null still possessed ADP-ribosyltransferase activity and that this activity is immunologically, genetically, and structurally distinct from the previously described enzyme. This unusual finding, of two ADP-ribosyltransferase enzymes produced by a microorganism, is complemented by the details of the purification to apparent homogeneity and in vitro regulation of this new protein, halovibrin-beta. 相似文献
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Escherichia coli strain CAN is unable to support the growth of bacteriophage T4 strains requiring the suppressor function of T4 tRNASer. Biochemical analysis of the mutant strain revealed that it is deficient in a RNase which acts on the artificial tRNA precursor tRNA-C-U. 相似文献
219.
The physical mechanism of calcium pump regulation in the heart. 总被引:4,自引:3,他引:1
The Ca-ATPase in the cardiac sarcoplasmic reticulum membrane is regulated by an amphipathic transmembrane protein, phospholamban. We have used time-resolved phosphorescence anisotropy to detect the microsecond rotational dynamics, and thereby the self-association, of the Ca-ATPase as a function of phospholamban phosphorylation and physiologically relevant calcium levels. The phosphorylation of phospholamban increases the rotational mobility of the Ca-ATPase in the sarcoplasmic reticulum bilayer, due to a decrease in large-scale protein association, with a [Ca2+] dependence parallel to that of enzyme activation. These results support a model in which phospholamban phosphorylation or calcium free the enzyme from a kinetically unfavorable associated state. 相似文献
220.
Chromosomal location and cloning of the gene (trmD) responsible for the synthesis of tRNA (m1G) methyltransferase in Escherichia coli K-12 总被引:5,自引:0,他引:5
Summary The trmD gene, which governs the formation of 1-methyl-guanosine (m1G) in transfer ribonucleic acid (tRNA), has been located by phage P1 transduction at 56 min on the chromosomal map of Escherichia coli. Cotransduction to tyrA at 56 min is 80%. From the Clarke and Carbon collection a ColE1-tyrA
+ hybrid plasmid was isolated, which carried the trmD
+ gene and was shown to over-produce the tRNA (m1G)methyltransferase. By subcloning restriction enzyme fragments in vitro, the trmD
+ gene was located to a 3.4 kb DNA fragment 6.5 kb clockwise from the tyrA
+ gene. The mutation trmD1, which renders the tRNA (m1G) methyltransferase temperaturesensitive both in vivo and in vitro could be complemented by trmD
+ plasmids. These results suggest that the gene trmD
+ is the structural gene for the tRNA (m1G)methyltransferase (EC 2.1.1.3.1). 相似文献