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磷酸二酯酶(PDEs)催化水解细胞内第二信使cAMP及cGMP,使细胞内cAMP和cGMP呈浓度梯度及区室化分布,在信号传导和调控生理学反应中起中心作用,包括心血管系统在内的所有类型细胞的新陈代谢、收缩性、运动性和转录等。PDE4是cAMP特异性的水解酶,其水解活性通常占细胞内水解cAMP活性的绝大部分。近来的研究表明,PDE4在心血管系统的各种细胞类型上都有表达,在调控心血管系统的运动中有重要的作用,其表达和活性的改变与心衰和心律失常的发展有关。这些研究为开发治疗心血管疾病的药物提供了新的靶点。
Phosphodiesterases (PDEs) catalyze the hydrolysis of cAMP and cGMP, the second messengers in cells, causing a concentration gradient and compartmentalization of cAMP and cGMP in cells, which play central roles in signal transduction and regulation of physiological responses, including cardiovascular system All types of cells within the metabolism, contractility, motility and transcription. PDE4 is a cAMP-specific hydrolase, whose hydrolytic activity usually accounts for most of the intracellular cAMP activity. Recent studies have shown that PDE4 is expressed in various cell types of the cardiovascular system and plays an important role in the regulation of cardiovascular system movement. Changes in its expression and activity are associated with the development of heart failure and arrhythmia. These studies provide a new target for the development of drugs for the treatment of cardiovascular disease.