Effective Predictor of Human Mast Cell Tryptase Inhibitors
نویسندگان
چکیده
SORIN AVRAM1, STEFANA AVRAM2*, CRISTINA DEHELEAN3 1 Romanian Academy, Institute of Chemistry Timisoara, 24 Mihai Viteazul Blvd., 300223, Timisoara, Romania 2 University of Medicine and Pharmacy Victor Babes Timisoara, Faculty of Pharmacy, Discipline of Pharmacognosy, 2 Eftimie Murgu Sq., 300041, Timisoara, Romania 3 University of Medicine and Pharmacy Victor Babes Timisoara, Faculty of Pharmacy, Discipline of Toxicology, 2 Eftimie Murgu Sq., 300041, Timisoara, Romania
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Inhibitors of tryptase as mast cell-stabilizing agents in the human airways: effects of tryptase and other agonists of proteinase-activated receptor 2 on histamine release.
Tryptase, the major secretory product of human mast cells, is emerging as a new target for therapeutic intervention in allergic airways disease. We have investigated the ability of tryptase and inhibitors of tryptase to modulate histamine release from human lung mast cells and have examined the potential contribution of proteinase-activated receptor 2 (PAR2). The tryptase inhibitor APC366 [N-(1...
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AIM To examine the influence of protease inhibitors on tryptase release, and as a comparison the influence of the inhibitors on histamine secretion was assessed. METHODS Enzymatically dispersed cells from human tonsil were challenged with anti-IgE or calcium ionophore A23187 (CI) in the absence or presence of the tryptase and chymase inhibitors, and tryptase and histamine release was determin...
متن کاملProcessing of human protryptase in mast cells involves cathepsins L, B, and C.
Human β-tryptase is stored in secretory granules of human mast cells as a heparin-stabilized tetramer. β-Protryptase in solution can be directly processed to the mature enzyme by cathepsin (CTS) L and CTSB, and sequentially processed by autocatalysis at R(-3), followed by CTSC proteolysis. However, it is uncertain which CTS is involved in protryptase processing inside human mast cells, because ...
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BACKGROUND If mast cells are stimulated they release multiple mediators that delineate markers for immunologic and nonimmunologic reactions; histamine and tryptase are the two best known. Although histamine can be assayed in plasma, it is a nonspecific marker with a very short half-life. Tryptase has a longer half-life, but its release has not been proven to be specific for anaphylaxis. The aut...
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