
Epac and the high affinity rolipram binding conformer of PDE4 …
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 …
解锁炎症治疗新纪元:PDE4靶点的创新药探索 - Pharmcube
Aug 20, 2024 · 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。
Epac and the high affinity rolipram binding conformer of PDE4 …
Jan 28, 2014 · 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.
PDE4抑制以Epac依赖性方式减少新内膜形成并抑制VCAM-1表达和 …
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。
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
PDE4 inhibitor, roflumilast protects cardiomyocytes against NO …
May 1, 2008 · 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 ...
PDE4 inhibition reduces neointima formation and inhibits VCAM-1 ...
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 ...
PDE4 regulates tissue plasminogen activator expression of
PDE4D siRNA reduced endothelial tPA mRNA to 40-55% of control (p<0.05). Use of Epac inducer mimicked, while use of Epac siRNA inhibited, these effects. Conclusions: Inhibition of PDE4 and PDE4D reduced expression of tPA by HBEC via Epac pathway.
磷酸二酯酶 4 抑制通过激活 PKA 和 EPAC/Akt 效应子并抑制 FoxO
We postulated that rolipram (selective PDE4 inhibitor) may activate cAMP downstream effectors, inhibiting proteolytic systems in skeletal muscles of diabetic rats. 越来越多的证据表明环磷酸腺苷 (cAMP) 信号和非选择性磷酸二酯酶 (PDE) 抑制剂能够缓解肌肉萎缩。 PDE4 是骨骼肌中主要的 cAMP 水解活性,因此有必要推进 PDE4 抑制剂治疗对萎缩肌肉蛋白质分解的影响。 我们假设咯利普兰 (选择性 PDE4 抑制剂) 可能激活 cAMP 下游效应子,抑制糖尿病大鼠骨骼肌中 …
PDE4抑制剂罗氟司特通过激活PKA和Epac双途径,保护心肌细胞免 …
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。