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Target intelligence / Profile preview
Phosphodiesterase type 5A (PDE5A)
- Target
- PDE5A
- Molecular classification
- Enzyme, Cyclic nucleotide phosphodiesterase
01
Overview
Phosphodiesterase type 5A (PDE5A) is an enzyme that selectively hydrolyzes cyclic guanosine monophosphate (cGMP), converting it into inactive 5’ GMP. This action regulates intracellular levels of cGMP, which plays a central role in various physiological processes including vasodilation, smooth muscle relaxation, neurotransmission, calcium homeostasis, and retinal phototransduction. Selective inhibitors of PDE5A are widely used drugs for erectile dysfunction and pulmonary arterial hypertension.
02
Mechanism of action
Selective inhibitors of PDE5A prolong penile erection via increased local blood flow and decrease pulmonary vascular resistance/pressure by preventing the breakdown of cGMP.
03
Biological functions
Hydrolyzes cGMPRegulates vasodilationRegulates smooth muscle toneRegulation of growthRegulation of viabilityRegulation of secretionRegulation of ion transportRegulation of endothelial permeabilityRegulation of gene transcription
04
Disease associations
Erectile dysfunctionPulmonary hypertensionCardiovascular disordersHeart failureNeurodegenerative diseases
05
Interacting drugs
Sildenafil
3 more in the full profile.
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