Target intelligence / Profile preview

Cyclic GMP phosphodiesterase 5 (PDE5)

Target
PDE5
Molecular classification
Enzyme, Phosphodiesterase
01

Overview

Cyclic GMP phosphodiesterase 5 (PDE5) is an enzyme that hydrolyzes cyclic guanosine monophosphate (cGMP), a key intracellular second messenger. It is highly expressed in the corpus cavernosum, retina, and vascular smooth muscle cells. PDE5 regulates vasodilation and smooth muscle relaxation by controlling cGMP levels. Inhibition of PDE5 is the mechanism of action for drugs used to treat erectile dysfunction and pulmonary arterial hypertension.

Other names
cGMP phosphodiesterase 5PDE VPDE5A
02

Mechanism of action

Selective inhibition of PDE5, leading to increased intracellular cGMP levels.

03

Biological functions

Hydrolysis of cGMPRegulation of cGMP levelsVasodilation regulationSmooth muscle relaxation regulationSignal transduction
04

Disease associations

Erectile dysfunctionPulmonary arterial hypertensionBenign prostatic hyperplasiaCardiovascular disease
05

Safety considerations

HypotensionVisual disturbancesPriapismDrug interactions (nitrates)
06

Interacting drugs

Sildenafil

3 more in the full profile.

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