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Review

Inhibitors of human mast cell serine proteases and potential therapeutic applications

&
Pages 1537-1555 | Published online: 25 Feb 2005

Bibliography

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  • •A research article that reports on mechanistic studies related to tryptase induced fibrinogenolysis and implications for tryptase as an anticoagulant and modulator of cellular interactions.
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  • •A research article that reports on the ability of tryptase to induce histamine release from MCs in vitro. The authors note that histamine release could be attenuated by treatment with APC366 and suggest a therapeutic role for tryptase inhibitors as MC stabilisers that block amplification of the inflammatory response.
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  • •A condensed review article that broadly covers the biochemistry of tryptase, implications for tryptase activity in asthma pathology and early small molecule inhibitors of tryptase.
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  • •A research article that reports on the ability of tryptase to function as a pro-inflammatory mediator through endothe-lial cell activation. The authors suggest that activation might be PAR-2 mediated and could represent a critical pathway for leukocyte recruitment to inflammation sites.
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  • •A research article that implicates tryptase and possibly cathepsin G in the activation of MMP activity in vivo supported by immunological studies involving patients with BE. Importantly, the authors note that the plasmin-plasminogen activator cascade was down regulated.
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  • •A research article that reports on the ability of tryptase to stimulate fibroblasts and ECM production. The article provides some overview discussion on fibrotic disease and the authors suggest a possible therapeutic role for tryptase inhibitors in the treatment of chronic conditions associated with MC activity.
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  • •A research article that similarly reports on the ability of tryptase to stimulate fibroblasts and also provides evidence for the induction of fibroblast chemotaxis.
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  • •A research article that summarises recent immunological studies in diseased liver tissue. The authors suggest that MC activity may play a role in the pathology of certain biliary diseases where fibrosis is involved.
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  • •A research article that provides evidence for tryptase and chymase mediated MMP activation and atherosclerotic plaque destabilisation in vitro. A brief overview of athero-sclerosis is also provided.
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  • ••A research article that provides a detailed SAR as a functionof extended scaffold length in a series of dibasic tryptase inhibitors.
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  • ••A detailed research article that provides a discussion oncrystallographic structures of the protease-zinc-ligand complexes, thermodynamics of complex formation as well as some first generation structure-activity relationships.
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  • ••A recent review on chymase inhibitors and their potentialtherapeutic applications.
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