2005年11月15日 · In this review we will discuss the cellular and molecular biology of PDE4 isoforms (of which ∼20 have been characterized) and, in particular, the pivotal role that PDE4 isoforms play in achieving compartmentalized signaling in …

2021年1月7日 · The PDE4 family comprises four genes, PDE4A–D, each expressed as multiple variants. The selective modulation of individual PDE4 subtypes revealed that individual subtypes exert unique and non...

The PDE4 family comprises four genes, PDE4A to D, which together are expressed as more than 25 splicing variants that each exert unique and non-redundant physiological functions. PAN-PDE4 inhibitors exert memory- and cognition-enhancing as well as neuroprotective, neuroregenerative and anti-inflammatory effects in preclinical models.

This review elaborately shows that safer and more effective PDE4 targeting is possible by characterizing 1) which PDE4 subtypes and isoforms exist, 2) how PDE4 isoforms can adopt specific conformations upon post-translational modifications and protein-protein interactions, and 3) which PDE4 inhibitors can selectively bind specific PDE4 subtypes ...

2023年1月1日 · PDE4, abundantly expressed in CNS, hydrolyzes cAMP involved in cognitive functions. Inhibition of PDE4 is beneficial to counteract cognitive deficits. Development of PDE4 inhibitors is hindered by dose-limiting adverse effects. Targeting specific PDE4 subtypes may be feasible for cognitive improvement.

Phosphodiesterase 4 (PDE4) enzymes catalyze cyclic adenosine monophosphate (cAMP) hydrolysis and are involved in a variety of physiological processes, including brain function, monocyte and macrophage activation, and neutrophil infiltration.

2023年3月1日 · Using in vitro, ex vivo, and in vivo models, we demonstrate that selective inhibition of phosphodiesterase 4 (PDE4), a family of enzymes that hydrolyzes and inactivates cyclic adenosine monophosphate (cAMP), reduces inflammation and promotes myelin repair.

Phosphodiesterase-4 (PDE4), one of eleven PDE enzyme families, specifically catalyzes hydrolysis of cyclic AMP (cAMP); it has four subtypes (PDE4A-D) with at least 25 splice variants. PDE4 plays a critical role in the control of intracellular cAMP concentrations. PDE4 inhibitors produce antidepressa …

PDE4 exists as four subtypes (A, B, C, and D) each with a capacity to degrade cAMP, a second messenger involved in inflammatory responses. PDE4 inhibitors inhibit PDE4 activity, consequently increasing cAMP levels. This results in an …

2020年3月20日 · In this review, we compare the evidence examining the functional role of each PDE4 subtype across malignancies, looking for common signaling themes, signaling pathways, and establishing the case...