Targeting phosphodiesterases in anti-platelet therapy.
Targeting phosphodiesterases in anti-platelet therapy.
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DOI：
10.1007/978-3-642-29423-5_9
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发表时间：
2012
影响因子：
--
通讯作者：
Weyrich, Andrew S
中科院分区：
文献类型：
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作者：
Rondina, Matthew T;Weyrich, Andrew S
血小板抑制主要有两种方式：阻断膜受体或中和细胞内通路。两种方法的抑制已被证明在预防和解决动脉粥样硬化血栓事件的好处。关于细胞内抑制，磷酸二酯酶（PDEs）是血小板功能的基础。血小板具有几种pde (PDE2， PDE3和PDE5)，它们催化环腺苷3 ' -5 ' -单磷酸（cAMP）和环鸟苷3 ' -5 ' -单磷酸（cGMP）的水解，从而限制细胞内核苷酸的水平。PDE抑制剂，如西洛他唑和双嘧达莫，通过增加cAMP和cGMP水平来抑制血小板功能。本文综述了PDE抑制剂在调节血小板功能中的作用，特别关注具有抗血小板临床适应症的药物。
There are two primary modes of platelet inhibition: blockade of membrane receptors or neutralization of intracellular pathways. Both means of inhibition have proven benefits in the prevention and resolution of atherothrombotic events. With regard to intracellular inhibition, phosphodiesterases (PDEs) are fundamental for platelet function. Platelets possess several PDEs (PDE2, PDE3 and PDE5) that catalyze the hydrolysis of cyclic adenosine 3′-5′-monophosphate (cAMP) and cyclic guanosine 3′-5′-monophosphate (cGMP), thereby limiting the levels of intracellular nucleotides. PDE inhibitors, such as cilostazol and dipyridamole, dampen platelet function by increasing cAMP and cGMP levels. This review focuses on the roles of PDE inhibitors in modulating platelet function, with particular attention paid to drugs that have anti-platelet clinical indications.