Target intelligence / Profile preview

Human mast cell tryptase (TPSAB1) (TPSAB1)

Target
TPSAB1
Molecular classification
Enzyme, Serine protease
01

Overview

Human mast cell tryptases are a family of trypsin-like serine proteases, primarily alpha and beta isoforms, that are stored in the secretory granules of mast cells and released upon degranulation (UniProt P23946, P20648). They are the most abundant proteins in mast cells and serve as key mediators of allergic and inflammatory responses (StatPearls: Tryptase). Beta-tryptase, in particular, is a tetrameric enzyme that activates protease-activated receptor 2 (PAR-2), leading to bronchoconstriction, mucus production, and recruitment of other inflammatory cells (PubMed: 17291286). Elevated levels of tryptase are found in the serum of patients during anaphylaxis and in the airways of individuals with asthma, making it a significant biomarker and therapeutic target (PubMed: 29107133). Pharmacological inhibition of tryptase aims to reduce airway hyperresponsiveness and tissue remodeling in chronic inflammatory conditions. Recent clinical efforts have focused on monoclonal antibodies like MTPS9579 and small-molecule inhibitors like BMS-986235 to selectively target these enzymes (ClinicalTrials.gov: NCT03756311).

Other names
Mast cell protease IISkin tryptaseLung tryptasePituitary tryptaseTPSB2TPSAB1Tryptase-1Tryptase-2Tryptase alpha/beta-1
02

Mechanism of action

Serine protease inhibition; Allosteric inhibition of tetramer formation

03

Biological functions

Immune responseInflammationTissue remodelingProteolysisCoagulation regulation
04

Disease associations

AsthmaAnaphylaxisMastocytosisHereditary alpha-tryptasemiaChronic obstructive pulmonary disease (COPD)Allergic rhinitis
05

Safety considerations

Potential for bleeding due to fibrinogen degradationRisk of off-target inhibition of other serine proteasesPotential for impaired host defense against certain parasites
06

Interacting drugs

MTPS9579

5 more in the full profile.

07

Biomarkers

Serum total tryptaseSerum mature beta-tryptase

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