Target intelligence / Profile preview

Monoamine oxidase A (MAO-A)

Target
MAO-A
Molecular classification
Enzyme, Flavoprotein oxidase, Mitochondrial outer membrane protein
01

Overview

Monoamine oxidase A is a mitochondrial outer membrane-bound enzyme that catalyzes the oxidative deamination of biogenic and dietary amines, including key neurotransmitters such as serotonin, norepinephrine, and dopamine. It uses flavin adenine dinucleotide (FAD) as a cofactor to facilitate the oxidation process. The enzyme plays a central role in regulating neurotransmitter levels in both the central nervous system and peripheral tissues. Beyond its classical neurological functions, recent research has identified roles for monoamine oxidase A in modulating immune responses within the tumor microenvironment—acting as an immune checkpoint that can suppress antitumor T cell immunity—making it a promising target for cancer immunotherapy strategies. Clinically, selective inhibition of this enzyme is used primarily in the treatment of depressive disorders but also has implications for neurodegenerative diseases and cancer therapy. Safety concerns include potential hypertensive crises from dietary amines during treatment with non-selective or irreversible inhibitors.[1][2][3][8][10]

Other names
MAOAMonoamine oxidase type AAmine oxidase (flavin-containing) A
02

Mechanism of action

Inhibition of enzymatic activity to increase synaptic levels of monoamines for antidepressant effect[6] Reversible or irreversible inhibition depending on drug class (RIMAs vs. classic MAOIs)[6]

03

Biological functions

Oxidative deamination of monoamines (e.g., serotonin, norepinephrine, dopamine)Regulation of neurotransmitter metabolismModulation of cellular growth and differentiation[1][2]Immune modulation (acts as an immune checkpoint)[8][10]
04

Disease associations

Neuropsychiatric disorders (e.g., depression, anxiety)Cancer (immune checkpoint function in tumor microenvironment)[8][10]Cardiovascular disease[2]Neurodegenerative disease[5]
05

Safety considerations

Risk of hypertensive crisis with dietary tyramine ("cheese effect") due to impaired breakdown when inhibited by non-selective or irreversible inhibitorsDrug-drug interactions leading to serotonin syndrome when combined with serotonergic agents or certain other drugs
06

Interacting drugs

Phenelzine[10]

2 more in the full profile.

07

Biomarkers

Intratumoral MAOA expression as a marker for T cell dysfunction and poor prognosis in cancer patients[10]

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