Target intelligence / Profile preview

Phosphodiesterase type IV (PDE4)

Target
PDE4
Molecular classification
Enzyme, Phosphodiesterase
01

Overview

Phosphodiesterase type IV (PDE4) is an enzyme that catalyzes the hydrolysis of cyclic adenosine monophosphate (cAMP) to its inactive form. It plays a central role in regulating intracellular signaling pathways that depend on cAMP as a second messenger. PDE4 consists of four subtypes: PDE4A, PDE4B, PDE4C, and PDE4D. It is highly expressed in immune cells and the central nervous system. Inhibition of PDE4 leads to increased intracellular levels of cAMP, resulting in anti-inflammatory and neuroprotective effects, but may cause gastrointestinal side effects.

02

Mechanism of action

Inhibition of PDE4 leads to increased intracellular levels of cAMP, activating downstream effectors like protein kinase A (PKA), exchange proteins directly activated by cAMP (Epac1/2), and cyclic nucleotide-gated ion channels, modulating inflammation and immune balance.

03

Biological functions

Signal transductionRegulation of cAMP levelsRegulation of immune responsesRegulation of inflammationCell proliferationCell differentiation
04

Disease associations

Chronic obstructive pulmonary disease (COPD)AsthmaPsoriasisRheumatoid arthritisMajor depressive disorderSchizophreniaBipolar disorderParkinson’s diseaseAlzheimer’s diseaseMultiple sclerosisHuntington's diseaseStrokeAutism
05

Safety considerations

NauseaEmesisGastrointestinal side effects
06

Interacting drugs

Roflumilast

1 more in the full profile.

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