Target intelligence / Profile preview

Phosphodiesterase 3A (PDE3A)

Target
PDE3A
Molecular classification
Enzyme, Phosphodiesterase
01

Overview

Phosphodiesterase 3A (PDE3A) is an enzyme that hydrolyzes cAMP and cGMP, thereby regulating their intracellular concentrations and modulating various signaling pathways. It plays a critical role in cardiovascular tissues, cancer biology, and gastrointestinal physiology. Mutations in PDE3A are linked to hypertension with brachydactyly syndrome, while overexpression is implicated in breast cancer progression. Selective inhibitors like cilostazol are used as antiplatelet agents and show promise in cancer therapy.

Other names
cGMP-inhibited cGMP phosphodiesteraseCGI-PDEPDE3
02

Mechanism of action

Selective inhibition of PDE3A, leading to increased intracellular cAMP and cGMP levels in target cells.

03

Biological functions

cAMP hydrolysiscGMP hydrolysisRegulation of cardiac contractilityRegulation of vascular toneRegulation of platelet aggregationRegulation of cell proliferationCalcium reuptake regulation in cardiac myocytes
04

Disease associations

Hypertension with brachydactyly syndrome (HTNB)Breast cancerGastrointestinal motility disorders
05

Safety considerations

Potential for cardiovascular effects due to vasodilatory and inotropic actions
06

Interacting drugs

Cilostazol
07

Biomarkers

PDE3A expression levels in breast cancer tissueICC density in gastrointestinal tissue

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