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Quantitative Stucture-Activity Relationship Studies onCalmodulin Antagonists of Alkylamino 1,2-Diphenylethvl-ene Compounds
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作者 雷小平 李重华 钟海振 《Journal of Chinese Pharmaceutical Sciences》 CAS 1996年第4期169-173,共5页
从新的先导化合物6-氨基1,2-二苯乙烯-1出发,研究了15个烷氨基1,2-二苯乙烯类钙调素拮抗剂的结构与活性之间的关系。发现:顺式构型的活性一般比反式构型强,而双键还原的化合物活性更低。从芳香亲脂中心到碱性中心之间... 从新的先导化合物6-氨基1,2-二苯乙烯-1出发,研究了15个烷氨基1,2-二苯乙烯类钙调素拮抗剂的结构与活性之间的关系。发现:顺式构型的活性一般比反式构型强,而双键还原的化合物活性更低。从芳香亲脂中心到碱性中心之间的烷基链长度增加时,拮抗活性随之增强。QSAR分析显示:苯环上具较大脂水分配系数及给电子的取代基时拮抗活性可提高。 展开更多
关键词 calmodulin antagonists QSAR Hansch analysis
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Studies on Plant Calmodulin and Its Interaction with Antagonist W_7 by Ln^(3+) Luminescence Probes
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作者 刘德龙 杨燕生 +2 位作者 王淑彬 张宏杰 龚孟濂 《Journal of Rare Earths》 SCIE EI CAS CSCD 1998年第2期55-59,共5页
Plant calmodulin(CaM) has been extracted from cauliflower, and the purified CaM has been identified with the activation of NAD kinase(NADK) and the inhibition effect of CaM antagonist W 7. CaM′s intrinsic fluorescen... Plant calmodulin(CaM) has been extracted from cauliflower, and the purified CaM has been identified with the activation of NAD kinase(NADK) and the inhibition effect of CaM antagonist W 7. CaM′s intrinsic fluorescence and Tb 3+ fluorescence showed that there was one tyrosine residue and four metal binding sites in cauliflower CaM. Based on Frster type nonradiative energy theory, the distances of Tyr→site Ⅲ, Ⅳ have been determined , and these are 1 23 nm(Tyr→site Ⅲ) and 1 18 nm(Tyr→site Ⅳ). The Eu 3+ and Tb 3+ fluorescence probes showed that the combination of CaM with W 7 resulted in significant change on CaM′s conformation, but did not affect coordination environment of metal binding sites. 展开更多
关键词 Rare earths calmodulin Luminescence probe calmodulin antagonist
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