2013年8月1日 · PDE4 is the main selective cAMP-metabolizing enzyme in inflammatory and immune cells. Because PDE4 is highly expressed in leukocytes and other inflammatory cells involved in the pathogenesis of inflammatory lung diseases, such as asthma and chronic obstructive pulmonary disease (COPD), inhibition of PDE4 has been predicted to have an ...

In this study, we elucidated expression and the role of individual subtypes of PDE4 in primary normal human lung fibroblast (NHLF) in controlling cytokines-induced proliferation and conversion to myofibroblasts by short-interfering RNAs (siRNAs) induced knockdown.

Phosphodiesterase-4 (PDE4) inhibitors have been reported as an effective therapeutic strategy for inflammatory conditions, such as asthma and COPD, but their use is limited because of class-related side effects.

Inhaled administration of PDE4 inhibitors for the treatment of respiratory diseases applies the drug directly to the site of action, the lungs, and minimizes the systemic exposure. This is an important advantage that can greatly increase the therapeutic index of a drug.

2023年1月1日 · In an attempt to improve the therapeutic window of xanthines, a number of selective PDE inhibitors have been developed for the treatment of respiratory diseases with only the selective PDE 4 inhibitor, roflumilast, being approved for the treatment of severe COPD.

2024年12月23日 · The PDE4B subtype is highly expressed in the brain, lungs, heart, skeletal muscle and immune cells. As such, inhibition of PDE4B may be a novel approach for fibrosing ILDs such as idiopathic pulmonary fibrosis (IPF) and SARD-ILD.

2012年4月23日 · Our findings suggest that PDE4 is expressed in lung cancer, crosstalks with HIF signaling and promotes lung cancer progression. Thus, PDE4 may represent a therapeutic target for lung...

Phase I and II trials of a novel PDE4B inhibitor in patients with idiopathic pulmonary fibrosis have shown promising results, stabilising pulmonary function measured by change in forced vital capacity from baseline, while maintaining an acceptable safety profile.

Altogether, the new PDE4 inhibitor, NCS 613, might be promising as a therapeutic compound in lung inflammation. In that way, NCS 613, inhibits in vivo lupus progression in MRL/lpr mice and inhibits ex vivo basal and LPS-induced TNF- α secretion by peripheral blood lymphocytes from MRL/lpr mice as well as from SLE patients, attesting the in ...

2019年5月1日 · Reports have shown that expression levels of PDE4 isoforms vary between the lung tissue derived from patients with COPD or asthma as compared to those of healthy donors, thereby pointing to PDE4 as an interesting and potential drug target in the treatment of chronic pulmonary diseases.