Jun 17, 2021 · Inhibition of phosphodiesterase 4 (PDE4), which is poorly expressed in the human heart, activates AMPK in other tissues. In a screen to identify novel PDE4 inhibitors, we discovered compound CBU91, which is 5-10 fold more potent than rolipram, the best characterized PDE4 inhibitor.

Rolipram is a selective phosphodiesterase 4 (PDE4) inhibitor that exerts a variety of effects, including anti-inflammatory, immunosuppressive, and anti-tumor effects. The aim of this study was to investigate the effect of rolipram on metabolic disorder and its underlying mechanisms.

Thus, we proposed that PDEs and in particular PDE4 participate in the metabolic syndrome by regulating the AMP-activated protein kinase (AMPK) [85]. In this way, it is noteworthy that the effect of roflumilast depended on the activation of the metabolic regulator AMPKα.

Here we investigated the roles of PDE3B, PDE4, protein kinase B (PKB) and the exchange protein activated by cAMP 1 (Epac1), as well as lipolysis, in the regulation of AMPK in primary rat adipocytes.

Jul 31, 2024 · AMPK phosphorylates β-arrestin-1 Ser330, which inhibits cAMP/PKA (protein kinase A) pathway activation by increasing PDE4 (phosphodiesterase 4) expression and activity. β-arrestin-1 Ser330 phosphorylation can inhibit the isoproterenol (ISO)-induced cardiac inflammation and fibrosis.

May 1, 2019 · Taken together, these results suggest that FCPR16 is effective in protecting SH-SY5Y cells and neurons against oxidative stress via AMPK-dependent autophagy. Our findings indicate the potential application of FCPR16 in PD treatment.

Jun 17, 2021 · Inhibition of phosphodiesterase 4 (PDE4), which is poorly expressed in the human heart, activates AMPK in other tissues. In a screen to identify novel PDE4 inhibitors, we discovered compound...

Jan 1, 2021 · PDE4 mediates inflammation through hydrolyzing cyclic adenosine monophosphate (cAMP), which is an endogenous second messenger that involved in the regulation of multiple physiological and pathological processes, including cellular metabolism [2], autophagy [3], apoptosis and inflammation [4].

Jun 17, 2021 · Inhibition of phosphodiesterase 4 (PDE4), which is poorly expressed in the human heart, activates AMPK in other tissues. In a screen to identify novel PDE4 inhibitors, we discovered compound CBU91, which is 5–10 fold more potent than rolipram, the best characterized PDE4 inhibitor.

Nov 6, 2015 · Objective: Recent evidence suggests an important role for cAMP-dependent pathways in modulation of innate immune function. Phosphodiesterase 4 (PDE4) is widely expressed in innate immune cells such as macrophages/dendritic cells with potent anti-inflammatory effects on pharmacologic inhibition of the enzyme.