Target intelligence / Profile preview

Suppressor of tumorigenicity 14 protein (Matriptase) (ST14)

Target
ST14
Molecular classification
Enzyme, Serine protease, Type II transmembrane serine protease (TTSP), Peptidase family S1
01

Overview

Matriptase, also known as ST14 or MT-SP1, is a prominent type II transmembrane serine protease (TTSP) expressed on the surface of epithelial and various tumor cells. It plays a critical role in the pericellular activation of the plasminogen activator system by proteolytically converting the zymogen pro-urokinase plasminogen activator (pro-uPA) into its active form, uPA. Beyond its role in the uPA/plasmin cascade, matriptase is essential for the activation of hepatocyte growth factor (HGF) and protease-activated receptor 2 (PAR2), which are key drivers of cellular proliferation and migration. In oncology, the dysregulation or overexpression of matriptase is strongly associated with increased tumor invasion, metastasis, and poor prognosis in various epithelial-derived cancers, including breast, prostate, and ovarian carcinomas. Consequently, matriptase is a significant therapeutic target, with various small-molecule inhibitors and antibody-based therapies under investigation to disrupt its pro-tumorigenic proteolytic activity.

Other names
MatriptaseMT-SP1ST14MTSP1TADG-15SNC19Type II transmembrane serine protease 1Serine protease 14
02

Biological functions

ProteolysisZymogen activationCell surface signalingExtracellular matrix remodelingGrowth factor activationEpithelial barrier maintenance
03

Disease associations

CancerMetastasisTumor invasionInflammationIchthyosis (loss of function)
04

Safety considerations

Potential disruption of normal epithelial barrier functionRisk of skin disorders (e.g., ichthyosis-like symptoms)Off-target inhibition of related TTSPs (e.g., Hepsin, Prostasin)Impact on normal tissue repair and wound healing
05

Interacting drugs

CVS-3983

5 more in the full profile.

06

Biomarkers

Matriptase expression levels (mRNA/protein)uPA/uPAR expressionHAI-1/HAI-2 inhibitor levelsCleaved HGF levels

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