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Review

Inhibitors of human mast cell serine proteases and potential therapeutic applications

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Pages 1537-1555 | Published online: 25 Feb 2005
 

Abstract

The mast cell (MC) is a multifunctional effector cell in the human immune system that serves to modulate the inflammatory response as well as wound healing and tissue growth processes. MC stimulation leads to the secretion of several preformed mediators including pro-inflammatory and growth mediating cytokines and proteolytic enzymes, most notably the serine proteases tryptase and chymase. Recent immunological and biological studies have demonstrated an association of MCs as well as tryptase and chymase activity with a broad range of allergic and inflammatory conditions affecting nearly all the major systems of the human body. Tryptase is implicated as a critical mediator of asthma and other inflammatory and allergic disease pathologies. While the evidence for chymase is less convincing at present, probable roles in inflammatory and cardiovascular disease are being investigated. Recent advances in the design of potent and selective inhibitors of the MC serine proteases tryptase and chymase are discussed.

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