Target intelligence / Profile preview

Prostate-specific antigen (PSA) (PSA)

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

Overview

Prostate-specific antigen (PSA), also known as Kallikrein-3 (KLK3), is a serine protease produced primarily by the epithelial cells of the prostate gland. Its primary physiological function is the liquefaction of the seminal coagulum through the cleavage of proteins such as semenogelin, which facilitates sperm motility. In clinical practice, PSA is the most widely utilized serum biomarker for the screening, diagnosis, and monitoring of prostate cancer, as its levels often rise significantly in the presence of malignant cells. While PSA is predominantly used as a diagnostic tool, it is also considered a therapeutic target for cancer vaccines, such as PROSTVAC, which are designed to stimulate the immune system to recognize and destroy PSA-expressing tumor cells. However, its utility as a direct drug target is complicated by its secretion into the systemic circulation, which can neutralize targeted agents before they reach the tumor site. The term "Prostate cancer antigen" is considered imprecise as it is frequently used as a generic descriptor for PSA, Prostate-specific membrane antigen (PSMA), or Prostate cancer antigen 3 (PCA3).

Other names
Kallikrein-3KLK3Gamma-seminoproteinSemininP-30 antigen
02

Mechanism of action

Antigen for immunotherapy (vaccines); Proteolytic activity (enzyme)

03

Biological functions

ProteolysisLiquefaction of seminal coagulumCell proliferation
04

Disease associations

CancerProstate cancerBenign prostatic hyperplasia
05

Safety considerations

Low specificity for cancer (elevated in BPH and prostatitis)Risk of overdiagnosis and overtreatmentSerum 'sink' effect limiting therapeutic targeting
06

Interacting drugs

PROSTVAC

3 more in the full profile.

07

Biomarkers

Serum PSA levelFree PSAPSA velocityPSA density

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