PDE4 inhibitors targeted at the HARBS conformer or Epac agonists may provide promising novel targets for the treatment of SCI. Our study demonstrates the differential mechanisms of action of these compounds, as well as the benefit of a combined pharmacological approach and highlighting potential pro …

心肌细胞凋亡在心肌梗塞中起重要作用，而camp在调控心肌细胞凋亡中至关重要。磷酸二酯酶4（pde4）抑制剂可通过抑制pde4来阻断camp的水解，是新型抗炎药的有吸引力的候选药物。但是，其在心血管疾病和心肌细胞凋亡中的功能尚不清楚。

2008年5月1日 · Based on these results, we are reporting for the first time that PDE4 inhibitor roflumilast protects cardiomyocytes from NO-induced apoptosis via activation of PKA and Epac dual pathway. Our study provides a new insight into the mechanisms responsible for the pharmacological activity of roflumilast and suggests its possible application as a ...

总之，PDE4抑制通过一种新型的Epac依赖性机制调节VCAM-1，该机制涉及调节表观遗传成分并减少血管损伤后新内膜的形成。PDE4抑制和Epac激活可能代表了治疗血管疾病（包括动脉粥样硬化和支架内再狭窄）的新方法。

2024年8月20日 · pde4-camp 的下游信号通路主要包括 camp 依赖性蛋白激酶 (pka)和camp 激活的交换蛋白 (epac)。 这些下游级联反应在促炎性和抗炎性细胞因子释放过程中起到了重要作用。

2014年1月28日 · PDE4 inhibitors targeted at the HARBS conformer or Epac agonists may provide promising novel targets for the treatment of SCI. Our study demonstrates the differential mechanisms of action of these compounds, as well as the benefit of a combined pharmacological approach and highlighting potential promising targets for the treatment of SCI.

We demonstrated that the PDE4 inhibitor rolipram decreased endothelial tPA release in an in vitro ischemia model. Moreover, inhibition of PDE4D isoform reduced endothelial tPA expression. Furthermore, activating Epac mimicked the effect of rolipram, while inhibiting Epac attenuated effects of rolipram and PDE4D siRNA.

PDE4 inhibitors targeted at the HARBS conformer or Epac agonists may provide promising novel targets for the treatment of SCI. Our study demonstrates the differential mechanisms of action of these compounds, as well as the benefit of a combined

In summary, PDE4 inhibition regulates VCAM-1 through a novel Epac-dependent mechanism, which involves regulatory epigenetic components and reduces neointima formation following vascular injury. PDE4 inhibition and Epac activation might represent novel approaches for the treatment of vascular diseases, including atherosclerosis and in-stent ...

In summary, our data indicate that roflumilast protects NO-induced apoptosis via both cAMP-PKA/CREB and Epac/Akt-dependent pathway. Our study suggests a possibility of PDE4 inhibitor roflumilast as a potential therapeutic agent against myocardial ischemia/reperfusion (I/R) injury.