Target intelligence / Profile preview

Sigma Receptor 2 (S2R)

Target
S2R
Molecular classification
Receptor, Transmembrane protein
01

Overview

The sigma‑2 receptor/TMEM97 is an integral membrane protein involved broadly in cellular homeostasis—including lipid metabolism/cholesterol trafficking—and plays key roles both physiologically and pathologically across cancer biology and neurodegeneration research fields. It is a four-pass transmembrane protein primarily located in the endoplasmic reticulum. The receptor is highly expressed in several tissues, including the brain (notably cerebellum, motor cortex, hippocampus, substantia nigra), liver, kidney, and lungs. S2R forms a trimeric complex with Progesterone receptor membrane component 1 (PGRMC1) and Low-density lipoprotein receptor (LDLR). Ligands include small-molecule agonists and antagonists.

Other names
Sigma-2 ReceptorTMEM97
02

Mechanism of action

Sigma-2 receptor agonists show anticancer activity. Sigma-2 receptor antagonists provide neuroprotection/inhibit amyloid-beta oligomer toxicity.

03

Biological functions

Cholesterol homeostasisHormone signalingCalcium signalingNeuronal signalingCell proliferationCell survivalAutophagyNeuroprotectionLipid metabolismCholesterol trafficking
04

Disease associations

CancerNeurodegenerative diseaseAlzheimer's diseaseSchizophreniaTraumatic brain injury
05

Biomarkers

Tumor proliferative status (high expression in dividing cells)

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