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有机化学
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有机化学 ›› 2009, Vol. 29 ›› Issue (02): 159-165. 上一篇    下一篇

综述与进展

磷酸二酯酶2 (PDE2)结构及其选择性抑制剂的研究进展

赵新筠; 陈 喜; 湛昌国*   

  1. (a华中师范大学化学学院 农药与化学生物学教育部重点实验室 武汉 430079)
    (b Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky,
    725 Rose Street, Lexington, KY 40536, USA)
  • 收稿日期:2007-12-16 修回日期:2008-06-15 发布日期:2009-02-20
  • 通讯作者: 湛昌国

Advances in the Structure of Phosphodiesterase 2 and Selective Inhibitors

Zhao, Xinyun; Chen, Xi ; Zhan, Changguo*   

  1. (a Key Laboratory of Pesticide & Chemical Biology of Ministry of Education, College of Chemistry,
    Central China Normal University, Wuhan, 430079 China)
    (b Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, 725 Rose Street,
    Lexington, KY 40536, USA)
  • Received:2007-12-16 Revised:2008-06-15 Published:2009-02-20
  • Contact: Zhan, Changguo

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磷酸二酯酶2 (PDE2)主要分布在大脑、心脏细胞中, 作为潜在的药物靶标, 通过水解细胞内第二信使cAMP和cGMP, 对维持cAMP和cGMP的水平起着重要的作用, 其选择性抑制剂有望在内皮渗透性和改善记忆力等方面发挥作用. 综述了PDE2的组织分布、生理功能、催化区域和调节区域晶体结构的特点以及选择性的抑制剂. 最后, 根据药物设计发展的趋势对未来PDE2抑制剂的设计进行了展望.

关键词: 调节区域, 选择性抑制剂, 催化区域, 磷酸二酯酶2 (PDE2), 酶功能, 酶分布

Phosphodiesterase 2 (PDE2) is mainly distributed in brain and heart cells. PDE2 is a potential drug target that plays an important role to maintain the level of intracellular second messengers cAMP and cGMP through PDE2-catalyzed hydrolysis of cAMP and cGMP. Selective inhibitors of PDE2 are expected to be valuable in improving permeability of endothelial cells and memory. In this article, the physiological function, distribution, and characteristics of the regulatory and catalytic domains, as well as some selective inhibitors against PDE2 are reviewed. Finally, based on the trend of the drug design, future design of PDE2 inhibitors is also prospected.