| 正碳离子样的过渡态类似物研究进展 |
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| 引用本文： | 廖桂红,贺红武. 正碳离子样的过渡态类似物研究进展[J]. 化学进展, 2005, 17(6): 0-1053 |
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| 作者姓名： | 廖桂红 贺红武 |
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| 作者单位： | 华中师范大学化学学院有机合成研究所,教育部农药与化学生物学重点实验室,武汉,430079;华中师范大学化学学院有机合成研究所,教育部农药与化学生物学重点实验室,武汉,430079 |
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| 基金项目： | 国家自然科学基金资助项目(No.20072008,20372023)，国家973计划资助项目(No.2003CB114400) |
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| 摘 要： | 综述了应用酶催化过渡态理论设计的几类正碳离子样的过渡态类似物作为酶的抑制剂的研究进展。其中包括类异戊二烯的正离子过渡态类似物,唾液酸转移酶的过渡态类似物,3-脱氧-D-甘露糖-2-辛酮糖酸酯-8-磷酸酯(KDO8P) 合成酶的过渡态类似物,尿苷二磷酸酯葡糖醛酸基转移酶(UGT) 的过渡态类似物。
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| 关 键 词： | 酶 正碳离子 过渡态类似物 抑制剂 |
| 文章编号： | 1005-281X（2005）06-1048-06 |
| 收稿时间： | 2004-10-01 |
| 修稿时间： | 2005-01-01 |
The Development of the Carbenium Transition State Analogs |
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| Liao Guihong,He Hongwu. The Development of the Carbenium Transition State Analogs[J]. Progress in Chemistry, 2005, 17(6): 0-1053 |
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| Authors: | Liao Guihong He Hongwu |
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| Affiliation: | Key Laboratory of Pesticide &Chemical Biology , Ministry of Education,College of Chemistry,Central China Normal University,Wuhan 430079,China |
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| Abstract: | An important feature in the enzyme catalyzed reaction is that an enzyme recognizes and binds more tightly to the transition state than to the ground state of the substrate product interconversion.The transition state analog must be a potent inhibitor of the enzyme.The recent development of the carbenium transition state analogs as the enzymatic inhibitors which are designed by the transition state theory of enzyme catalyzed reactions is reviewed.Four types of enzymatic inhibitors including the transition state analogs of isoprenoid pyrophosphate,sialyltransferase,KDO8P and UGT are introduced. |
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| Keywords: | enzyme carbenium transition state analogs inhibitors |
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