Target intelligence / Profile preview

Amine oxidase (AO)

Target
AO
Molecular classification
Enzyme, Oxidoreductase, Flavin-dependent amine oxidase, Copper-containing amine oxidase
01

Overview

Amine oxidases are a diverse family of enzymes that catalyze the oxidative deamination of biogenic and xenobiotic amines, producing aldehydes, ammonia, and hydrogen peroxide [4, 11]. They are broadly classified into two groups based on their cofactors: flavin-dependent amine oxidases (such as monoamine oxidase A and B) and copper-containing amine oxidases (such as diamine oxidase and vascular adhesion protein-1) [1, 2]. These enzymes play critical roles in regulating neurotransmitter levels in the central nervous system, metabolizing dietary amines in the periphery, and mediating leukocyte trafficking during inflammatory responses [3, 16]. Due to their central role in neurochemistry and vascular biology, amine oxidases are major therapeutic targets for treating depression, Parkinson's disease, and chronic inflammatory conditions [9, 12]. Drugs targeting these enzymes include monoamine oxidase inhibitors (MAOIs) for neuropsychiatric disorders and emerging VAP-1 inhibitors for inflammatory and fibrotic diseases like non-alcoholic steatohepatitis (NASH) [5, 16].

Other names
Amine:oxygen oxidoreductase (deaminating)Monoamine oxidaseDiamine oxidaseSemicarbazide-sensitive amine oxidaseCopper amine oxidaseFlavin amine oxidaseHistaminaseVascular adhesion protein-1
02

Mechanism of action

Inhibition of the oxidative deamination of amines, leading to increased synaptic neurotransmitter concentrations or reduced production of pro-inflammatory mediators and reactive oxygen species.

03

Biological functions

Oxidative deamination of biogenic and xenobiotic aminesRegulation of neurotransmitter levels (serotonin, dopamine, norepinephrine)Metabolism of dietary amines (histamine, tyramine)Mediation of leukocyte trafficking and cell adhesion (VAP-1)Polyamine catabolismSignal transduction through hydrogen peroxide production
04

Disease associations

DepressionParkinson's diseaseAlzheimer's diseaseChronic inflammationFibrosis (e.g., NASH)Cancer progression and metastasisHistamine intoleranceCardiovascular disease
05

Safety considerations

Hypertensive crisis (cheese effect) due to tyramine interactionSerotonin syndrome when combined with other serotonergic agentsDrug-drug interactions with sympathomimeticsPotential hepatotoxicityOff-target inhibition of diamine oxidase leading to histamine sensitivity
06

Interacting drugs

Phenelzine

9 more in the full profile.

07

Biomarkers

Soluble Vascular Adhesion Protein-1 (sVAP-1) levels in serumPlatelet Monoamine Oxidase B (MAO-B) activityUrinary 5-hydroxyindoleacetic acid (5-HIAA)Plasma histamine levelsPlasma methylamine and benzylamine levels

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