Target intelligence / Profile preview

Phosphodiesterase III (PDE3)

Target
PDE3
Molecular classification
Enzyme, Phosphodiesterases (PDEs), PDE3 subfamily
01

Overview

Phosphodiesterase III (PDE3) is a member of the phosphodiesterase enzyme family that hydrolyzes cyclic nucleotides such as cAMP and cGMP, playing a critical role in cellular signaling. It regulates cardiac muscle contractility, vascular smooth muscle tone, and platelet aggregation. There are two main genes encoding PDE3 isoforms: PDE3A and PDE3B. PDE3 inhibitors are used for acute heart failure management, peripheral arterial disease, and prevention/treatment of thrombocytosis-related conditions, but long-term use is associated with increased risk of arrhythmias and mortality.

02

Mechanism of action

Blockade of PDE3 leads to increased cellular concentrations of cAMP/cGMP, resulting in enhanced cardiac contractility, faster myocardial relaxation, vasodilation, and reduced platelet aggregation through PKA activation.

03

Biological functions

Hydrolyzes cAMP and cGMPRegulation of cardiac muscle contractilityRegulation of vascular smooth muscle toneRegulation of platelet aggregationLipolysis regulation
04

Disease associations

Cardiovascular diseasePeripheral arterial diseaseThrombocytosis-related conditionsHeart failure
05

Safety considerations

Long-term use associated with increased risk for arrhythmias and higher mortality rates among chronic heart failure patients.
06

Interacting drugs

Milrinone

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