Target intelligence / Profile preview

Trypsin-1 (PRSS1) (PRSS1)

Target
PRSS1
Molecular classification
Enzyme, Serine protease, S1 family peptidase
01

Overview

Trypsin-1, encoded by the PRSS1 gene and also known as cationic trypsinogen, is a major digestive enzyme synthesized by the pancreatic acinar cells. It is secreted into the small intestine as an inactive zymogen, where it is activated by enteropeptidase to initiate the digestion of dietary proteins and the activation of other pancreatic proenzymes. Mutations in the PRSS1 gene, particularly gain-of-function variants like R122H, are the primary cause of hereditary pancreatitis, as they lead to premature intrapancreatic trypsin activation and resistance to inactivation, resulting in organ autodigestion. Because of its central role in pancreatic inflammation, Trypsin-1 is a key therapeutic target for serine protease inhibitors such as camostat and nafamostat, which are used to treat acute and chronic pancreatitis. Furthermore, PRSS1 serves as a critical biomarker in clinical diagnostics, including neonatal screening for cystic fibrosis and the genetic assessment of chronic pancreatic diseases.

Other names
Protease, serine 1Cationic trypsinogenSerine protease 1TRP1TRY1TRY4TRYP1Trypsinogen A
02

Mechanism of action

Serine protease inhibition

03

Biological functions

ProteolysisDigestionZymogen activationSignal transductionApoptosisImmune response
04

Disease associations

Hereditary pancreatitisChronic pancreatitisPancreatic cancerCystic fibrosis (screening)Inflammation
05

Safety considerations

Systemic inhibition of coagulation and fibrinolysis cascadesRisk of bleeding or thrombosis due to non-selective inhibitionHypersensitivity and anaphylaxis (notably with aprotinin)Potential for malabsorption with long-term high-dose inhibition
06

Interacting drugs

Camostat mesylate

4 more in the full profile.

07

Biomarkers

Serum immunoreactive trypsinogen (IRT)PRSS1 mutation status (e.g., R122H, N29I, A16V)Fecal elastase-1 (as a proxy for exocrine function)

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