In this review, we illustrate that PDE4 inhibitors retain their therapeutic potential in myriad diseases, but target identification should be more precise to establish selective inhibition of disease-affected PDE4 isoforms while avoiding isoforms involved in adverse effects.

Apr 9, 2013 · In the present study, we identified PDE4B as a key negative regulator for CYLD via selective activation of c-jun N-terminal kinase 2 (JNK2), but not JNK1, and inhibition of PDE4B significantly...

Aug 19, 2022 · PDE4 (phosphodiesterase-4) hydrolyzes intracellular cyclic adenosine monophosphate and it has 4 subtypes A-D. This study aimed to delineate the role of PDE4B (phosphodiesterase-4 subtype B) in MI/R injury.

Oct 6, 2016 · Phosphodiesterase 4 (PDE4) has four subtypes: PDE4A, PDE4B, PDE4C and PDE4D. The expression of PDE4 subtypes in microglial cells and the specific contribution of each subtype to inflammation remain unclear. In this study, the expression of PDE4 subtypes in primary microglial cells was assayed.

This review describes a new generation of oral PDE4B/D selective inhibitors under development and compares their PDE4 subtype profile with the approved PDE4 inhibitors currently used for treatment of psoriasis and atopic dermatitis.

Apr 8, 2020 · Our results suggest that a moderate increase in cardiac PDE4B is beneficial to counteract the detrimental effect of excessive sympathetic system activation in heart failure.

May 15, 2022 · In this multicenter, randomized, double-blind, phase 2 trial, we investigated the efficacy and safety of BI 1015550, an oral preferential inhibitor of PDE4B, 17 in patients with IPF according to...

Mar 21, 2016 · Phosphodiesterase-4 (PDE4) hydrolyses cyclic adenosine monophosphate (cAMP), a crucial secondary messenger for cellular adaptation to diverse external stimuli. The activity of PDE4 is tightly controlled by post-translational regulation, structure-based auto-regulation and locus specific ‘compartmentalization’ of PDE4 with its interactive ...

PDE4 subtype inhibition to treat demyelinating central and peripheral nervous system neuropathies: PDE4B and PDE4D have recently been described as novel therapeutic targets for managing distinct pathological processes of MS including neuroinflammation and myelin regeneration respectively.

Dec 19, 2024 · In this review, we provide a comprehensive overview of the molecular functions and properties of human PDE4s. The study presents detailed sequence information for the PDE4 isoforms and the structural properties of the catalytic domain in members of the PDE4 family.