2018年1月31日 · The ability of cAMP to elicit cell surface receptor-specific responses relies on its compartmentalisation by cAMP hydrolysing enzymes known as phosphodiesterases. One family of these enzymes, PDE4, is particularly important in the cardiovascular system, where it has been extensively studied and shown to orchestrate complex, localised signalling ...

pdes具有不同的底物专一性：pde 4、7、8专一作用于camp，而pde 5、6、9则选择性地作用于cgmp。pde3以相似的亲和力与camp和cgmp结合，但相对较少地水解cgmp，因而在功能上被视作对camp专一，cgmp通过与酶作用部位的竞争性结合而起 负调控 因子作用。

2024年5月31日 · pde是唯一降解细胞内环状腺苷单磷酸（camp）和环状鸟苷单磷酸（cgmp）等第二信使的酶，包含11个家族成员（pde1~pde11）。其中，pde4专一性水解camp。pde4包含4种亚型（pde4a、pde4b、pde4c和pde4d），20多种同工型。

The phosphodiesterase 4 (PDE4) enzyme family plays a pivotal role in regulating levels of the second messenger cAMP. Consequently, PDE4 inhibitors have been investigated as a therapeutic strategy to enhance cAMP signaling in a broad range of diseases, including several types of cancers, as well as i …

Although cardiac myocytes have taken centre stage in terms of PDE4 research, this group of enzymes also has major roles in the wider cardiovascular system, regulating many characteristics of the vasculature. cAMP signalling is particularly important in the signalling systems of vascular endothelial cells (VECs) where increases in cAMP ...

2003年2月15日 · PDE4 cAMP-specific phosphodiesterases appear to have specific functions with selective inhibitors serving as potent anti-inflammatory agents. The recent elucidation of the structure of the PDE4 catalytic unit allows for molecular insight into the mode of catalysis as well as substrate and inhibitor selectivity.

6 天之前 · Phosphodiesterase 4 (PDE4) is a key regulator of cyclic adenosine monophosphate (cAMP) signalling in cardiomyocytes, controlling contractility, calcium handling, and hypertrophic responses. PDE4 provides spatial and temporal precision to cAMP signalling, particularly under β-adrenergic stimulation, through its compartmentalised activity in subcellular nanodomains, including the sarcoplasmic ...

2023年5月10日 · 磷酸二酯酶4(phosphodiesterase4, PDE4)是磷酸二酯酶家族中重要成员之一，可特异性水解环磷酸腺苷(cyclic adenosine monophosphate, cAMP)，通过改变cAMP浓度引发下游磷酸化级联反应，与多种疾病密切相关。

Inhibition of PDE4 is predicted to have diverse effects via the elevation of the level of cyclic adenosine monophosphate (cAMP) and the subsequent regulation of a wide array of genes and proteins. It has been identified that PDE4 is a promising therapeutic target for the treatment of diverse pulmonary, dermatological, and severe neurological ...

2022年9月13日 · The PDE4 family, which exclusively hydrolyses the cAMP (K m = 2–4 µM), is the most extensive family, coded by four genes, namely PDE4A to PDE4D. Each gene encodes multiple protein products generated by alternative splicing and/or …