Target intelligence / Profile preview

cGMP-specific phosphodiesterase type 5 (PDE5)

Target
PDE5
Molecular classification
Enzyme, Phosphodiesterase
01

Overview

cGMP-specific phosphodiesterase type 5 (PDE5) is an enzyme that hydrolyzes cyclic guanosine monophosphate (cGMP) to its inactive form, 5’-GMP, thereby regulating intracellular levels of cGMP. It plays a central role in the control of smooth muscle contraction and relaxation by modulating the cGMP signaling pathway. PDE5 is a major drug target due to its tissue distribution and physiological importance, with inhibitors like sildenafil and tadalafil being used to treat erectile dysfunction and pulmonary arterial hypertension.

Other names
Cyclic guanosine monophosphate-specific phosphodiesterase type 5PDE 5A
02

Mechanism of action

Competitive inhibition of PDE5 catalytic site.

03

Biological functions

Regulation of smooth muscle contractionRegulation of vascular tonePlatelet aggregationCardiac function modulationNeurotransmissionCalcium homeostasisRetinal phototransduction
04

Disease associations

Erectile dysfunction (ED)Pulmonary arterial hypertension (PAH)Cardiac hypertrophyHeart failureCancer
05

Interacting drugs

Sildenafil

3 more in the full profile.

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