Target intelligence / Profile preview

Prostate-specific antigen (Kallikrein-3) (PSA)

Target
PSA
Molecular classification
Enzyme, Serine protease, Kallikrein-related peptidase family
01

Overview

Prostate-specific antigen (PSA), also known as Kallikrein-3 (KLK3), is a 34-kDa serine protease primarily produced by the epithelial cells of the prostate gland (UniProt P07288). Its primary biological function is the liquefaction of the seminal coagulum through the hydrolysis of semenogelin proteins, which facilitates sperm motility (PubMed: 12670375). While PSA is most widely recognized as a gold-standard clinical biomarker for the detection and monitoring of prostate cancer, it also serves as a therapeutic target (NCBI: Gene ID 354). Various molecular isoforms, such as proPSA and BPSA, provide higher diagnostic specificity to differentiate between prostate cancer and benign conditions like hyperplasia (PubMed: 25230330). In drug development, PSA's enzymatic activity is exploited to activate prodrugs specifically within the prostate, and its status as a tissue-specific antigen makes it a candidate for cancer vaccines and T-cell engaging therapies (PubMed: 21813910).

Other names
Kallikrein-3KLK3Gamma-seminoproteinSemininP-30 antigenhK3Prostate-specific antigen isoforms
02

Mechanism of action

PSA is targeted via immunotherapy to induce T-cell responses against PSA-producing cells or utilized as an enzymatic trigger for the site-specific activation of cytotoxic prodrugs (PubMed: 21813910).

03

Biological functions

ProteolysisLiquefaction of seminal coagulumSemenogelin hydrolysisRegulation of sperm motility
04

Disease associations

Prostate cancerBenign prostatic hyperplasiaProstatitis
05

Safety considerations

Low specificity for malignancy leading to overdiagnosisRisk of overtreatment of indolent diseasePotential for off-target activation of prodrugs in non-cancerous prostatic tissue
06

Interacting drugs

PROSTVAC-VF

2 more in the full profile.

07

Biomarkers

Total PSAFree PSAproPSA[-2]proPSAProstate Health Index (PHI)Benign PSA (BPSA)Complexed PSA (cPSA)

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