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Phosphodiesterase 1 (PDE1)
- Target
- PDE1
- Molecular classification
- Enzyme, Phosphodiesterase
01
Overview
Phosphodiesterase 1 (PDE1) is an enzyme that hydrolyzes both cAMP and cGMP, thereby modulating various physiological processes. It is activated by Ca²⁺/calmodulin and has three main isoforms: PDE1A, PDE1B, and PDE1C. Dysregulation is implicated in several diseases, making it a potential therapeutic target.
02
Mechanism of action
Phosphodiesterase 1 hydrolyzes cAMP and cGMP, reducing their intracellular concentrations. Inhibitors of PDE1 would increase cAMP and cGMP levels.
03
Biological functions
Signal transductionRegulation of cAMP levelsRegulation of cGMP levelsNeurotransmitter releaseModulation of muscle contractionRegulation of cell proliferation
04
Disease associations
Cardiovascular diseasesPulmonary arterial hypertensionNeurodegenerative disordersAlzheimer's diseaseMetabolic syndromeRenal diseaseCertain cancers
05
Safety considerations
Lack of highly selective inhibitors for individual isoforms.
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