Phosphodiesterases (PDEs) are a class of enzymes that hydrolyze cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP) which is involved in many physiological processes including visual transduction, cell proliferation and differentiation, cell-cycle regulation, gene expression, inflammation, apoptosis, and metabolic function. PDEs are composed of 11 different families and each family contains different subtypes. The distribution, expression, regulation mode and sensitivity to inhibitors of each subtype are different, and they are involved in cancer, inflammation, asthma, depression, erectile dysfunction and other pathological processes of development. A large number of studies have shown that PDEs play an important role in the development of tumors by affecting the intracellular level of cAMP and/or cGMP and PDEs could become diagnostic markers or therapeutic targets. This review will give a brief overview of the expression and regulation of PDE families in the process of tumorigenesis and their anti-tumor inhibitors, which may guide the design of novel therapeutic drugs targeting PDEs for anticancer agent.

磷酸二酯酶（PDEs）是一类酶，它水解环状腺苷单磷酸（cAMP）和环状鸟苷单磷酸（cGMP），这涉及许多生理过程，包括视觉转导，细胞增殖和分化，细胞周期调控，基因表达，炎症，细胞凋亡和代谢功能。PDE由11个不同的家族组成，每个家族包含不同的亚型。每种亚型的分布，表达，调控方式和对抑制剂的敏感性不同，它们涉及癌症，炎症，哮喘，抑郁，勃起功能障碍和其他病理发展过程。大量研究表明，PDE通过影响细胞内cAMP和/或cGMP的水平在肿瘤的发展中起重要作用，PDE可能成为诊断标记或治疗靶标。本文将简要概述PDE家族在肿瘤发生过程中的表达和调控及其抗肿瘤抑制剂，这可能指导设计针对PDEs的新型抗癌药物。