Target intelligence / Profile preview

Kallikrein-3 (PSA) (PSA)

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

Overview

Kallikrein-3, widely known as Prostate-Specific Antigen (PSA), is a serine protease primarily synthesized by the secretory epithelial cells of the prostate gland. Its primary biological function is the liquefaction of the seminal coagulum by cleaving semenogelins, thereby facilitating sperm motility. PSA is a critical biomarker in clinical oncology, where elevated serum levels are used to screen for, diagnose, and monitor the progression of prostate cancer and benign prostatic hyperplasia. In therapeutic development, PSA serves as a tumor-associated antigen for various immunotherapies, including mRNA-based vaccines like CV9103 and viral-vector vaccines like PROSTVAC, which aim to stimulate a cytotoxic T-cell response against malignant cells. Furthermore, the specific proteolytic activity of PSA is utilized in prodrug strategies, where inactive toxins are engineered to be selectively activated by the enzyme within the tumor microenvironment. Despite its utility, targeting PSA or using it for screening presents challenges such as overdiagnosis and the potential for treatment-related side effects like urinary incontinence.

Other names
Prostate-specific antigenKLK3P-30 antigenGamma-seminoproteinSemininhK3Kallikrein-related peptidase 3
02

Mechanism of action

Induction of antigen-specific T-cell immune response; Enzymatic activation of prodrugs; Protease inhibition

03

Biological functions

ProteolysisLiquefaction of seminal coagulumSperm motility regulationNegative regulation of angiogenesis
04

Disease associations

Prostate cancerBenign prostatic hyperplasiaProstatitis
05

Safety considerations

Overdiagnosis and overtreatment of indolent tumorsBiopsy-related complications (e.g., sepsis, pain, bleeding)Potential for autoimmune prostatitisTreatment-related side effects (e.g., urinary incontinence, erectile dysfunction)
06

Interacting drugs

PROSTVAC (PROSTVAC-VF)

4 more in the full profile.

07

Biomarkers

Serum total PSA levelFree-to-total PSA ratioPSA densityPSA velocityKLK3 mRNA expression

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