Target intelligence / Profile preview

Translocator Protein (None)

Target
None
Molecular classification
Transmembrane protein, Mitochondrial protein, Receptor
01

Overview

Translocator protein (TSPO), an 18 kDa transmembrane protein primarily localized to the outer mitochondrial membrane, plays a critical role in cholesterol transport into mitochondria for steroid hormone synthesis, as well as in apoptosis regulation, mitochondrial respiration, and other cellular processes. It is widely expressed throughout the body and is implicated in various diseases, including neuroinflammation, cancer, endocrine disorders, and psychiatric conditions. Its accessibility to small-molecule ligands makes it a potential biomarker for disease imaging and a therapeutic target.

Other names
Peripheral-type benzodiazepine receptor (PBR)
02

Mechanism of action

Ligand binding modulates cholesterol transport into mitochondria and affects steroid hormone synthesis; influences apoptosis via mitochondrial permeability transition pore opening; interacts with other proteins to modulate diverse cellular processes.

03

Biological functions

Cholesterol transportSteroidogenesisApoptosis regulationMitochondrial respirationIon transportMetabolite exchangeOxidative stress responseInflammation modulationEnergy metabolismCell proliferation
04

Disease associations

NeuroinflammationCancerEndocrine disordersPsychiatric diseasesNeurodegenerationBrain injury
05

Safety considerations

Altered ligand affinity due to polymorphisms can impact drug efficacyPotential for off-target effects due to widespread tissue expression
06

Interacting drugs

PK11195

3 more in the full profile.

07

Biomarkers

TSPO expression levels in neuroinflammationTSPO polymorphisms affecting ligand affinity in psychiatric diseases

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