Target intelligence / Profile preview

Prostate-specific Membrane Antigen (PSMA)

Target
PSMA
Molecular classification
Enzyme, Type II transmembrane glycoprotein, Carboxypeptidase
01

Overview

Prostate-specific membrane antigen (PSMA) is a type II transmembrane glycoprotein highly overexpressed in prostate carcinoma and expressed in all types of prostatic tissue, including benign, dysplastic, and malignant cells. PSMA is also found on the neovasculature of most solid tumors but has minimal expression in normal tissues outside the prostate. It acts as a glutamate-preferring carboxypeptidase and is a target for diagnostic imaging and therapeutic interventions in prostate cancer.

Other names
Glutamate carboxypeptidase IIGCPIIFolylpoly-gamma-glutamate carboxypeptidaseFGCPN-acetylated alpha-linked acidic dipeptidase INAALADase IProstate-specific membrane antigen
02

Mechanism of action

PSMA inhibitors bind to the active site of PSMA, inhibiting its enzymatic activity. Antibody-drug conjugates bind to PSMA and are internalized, delivering a cytotoxic payload to the tumor cell.

03

Biological functions

Hydrolyzes small molecule substratesGlutamate carboxypeptidase activityNeuropeptide hydrolysisFolate derivative hydrolysisMethotrexate hydrolysis
04

Disease associations

Prostate cancerSolid tumorsAngiogenesis
05

Safety considerations

Off-target effects due to PSMA expression in non-prostate tissues (minimal)Potential immunogenicity of antibody-based therapies
06

Interacting drugs

ProstaScint® (mAb 7E11)

3 more in the full profile.

07

Biomarkers

PSMA expression levelPSMA internalization

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