Target intelligence / Profile preview

Cyclic nucleotide phosphodiesterase (None)

Target
None
Molecular classification
Enzyme
01

Overview

Cyclic nucleotide phosphodiesterases (PDEs) are a superfamily of enzymes that regulate cellular signaling by catalyzing the hydrolysis of cyclic nucleotides, primarily cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP), into their inactive 5′-monophosphate forms. By controlling the degradation rates of these second messengers, PDEs play a central role in modulating intracellular signaling pathways that govern numerous physiological processes. There are 11 distinct PDE families in mammals, named PDE1 through PDE11. Each family contains multiple isoforms and splice variants with unique structural, kinetic, regulatory, localization, expression, and inhibitor sensitivity profiles. Selective inhibitors for certain PDE families have been developed as drugs for various conditions, including erectile dysfunction, pulmonary hypertension, acute heart failure, and chronic obstructive pulmonary disease.

02

Mechanism of action

Inhibition of cyclic nucleotide phosphodiesterase activity, leading to increased intracellular levels of cAMP and/or cGMP.

03

Biological functions

Signal transductionRegulation of intracellular cAMP levelsRegulation of intracellular cGMP levelsHydrolysis of cyclic nucleotidesModulation of muscle contraction/relaxationModulation of neurotransmission/synaptic plasticityRegulation of metabolismRegulation of gene transcriptionRegulation of cell proliferationRegulation of cell differentiationRegulation of apoptosis
04

Disease associations

Heart failureErectile dysfunctionPulmonary hypertensionDepression/anxiety disordersChronic obstructive pulmonary disease
05

Safety considerations

Potential for drug interactions due to effects on cAMP/cGMP signaling pathways.Side effects associated with specific PDE inhibitors, such as visual disturbances (PDE5 inhibitors) or gastrointestinal issues (PDE4 inhibitors).
06

Interacting drugs

Sildenafil

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