1 <h5>Introduction</h5> Like other leukocytes, mast cells are derived from hematopoietic progenitor cells of the bone marrow. In contrast to basophiles that circulate as mature cells in the blood, mast cells reside in virtually all peripheral tissues of the human body, in particular the dermis, the lung, and the mucosa and submucosa of the intestine. It is well accepted that mast cells play a pivotal role in the pathogenesis of a variety of allergic and inflammatory diseases, most prominent among them allergic asthma, psoriasis, and rheumatoid arthritis. 1–3 Beside by other mechanisms, mast cells are activated upon crosslinking of F c&z.epsiv; RI-bound IgE with multivalent allergens on the cells’ surface. The signaling cascade elicited eventually results in downstream events that trigger the release of a set of preformed mediators, which are stored in cytoplasmic granules, into the surrounding tissue by degranulation. 4 </P>The mediators released by degranulation include, for example, histamine and heparin proteoglycan as well as β-tryptase, a trypsin-like serine protease that is abundantly and virtually exclusively expressed in mast cells. 1 The amount of catalytically active β-tryptase accounts for up to 20% of the entire protein of a mast cell and thus is higher than those
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The arginine mimicking β-amino acid β 3 hPhe(3-H 2 N-CH 2 ) as S1 ligand in cyclotheonamide-based β-tryptase inhibitors
Janke, Dennis; Sommerhoff, Christian P.; Schaschke, Norbert
Follow Bioorganic & Medicinal Chemistry
, Volume 19 (23)
Elsevier – Dec 1, 2011
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