Structure‐based design and in vivo anti‐arthritic activity evaluation of a potent cyclopropyl peptidyl nitrile inhibitor of cathepsin C
B Korkmaz, A Lesner, A Gieldon, C Lauritzen… - The FASEB …, 2019 - Wiley Online Library
Cathepsin C (CatC) is a dipeptidyl‐exopeptidase which activates neutrophil serine protease
precursors (elastase, proteinase 3, cathepsin G and NSP4) by removing their N‐terminal
propeptide in bone marrow cells at the promyelocytic stage of neutrophil differentiation. The
resulting active neutrophil serine proteases are implicated in chronic inflammatory and
autoimmune diseases. Hence, inhibition of CatC represents a therapeutic strategy to
suppress excessive neutrophil serine protease activities in various neutrophil mediated …
precursors (elastase, proteinase 3, cathepsin G and NSP4) by removing their N‐terminal
propeptide in bone marrow cells at the promyelocytic stage of neutrophil differentiation. The
resulting active neutrophil serine proteases are implicated in chronic inflammatory and
autoimmune diseases. Hence, inhibition of CatC represents a therapeutic strategy to
suppress excessive neutrophil serine protease activities in various neutrophil mediated …
Structure-based design and in vivo anti-arthritic activity evaluation of a potent dipeptidyl cyclopropyl nitrile inhibitor of cathepsin C
Cathepsin C (CatC) is a dipeptidyl-exopeptidase which activates neutrophil serine protease
precursors (elastase, proteinase 3, cathepsin G and NSP4) by removing their N-terminal
propeptide in bone marrow cells at the promyelocytic stage of neutrophil differentiation. The
resulting active proteases are implicated in chronic inflammatory and autoimmune diseases.
Hence, inhibition of CatC represents a therapeutic strategy to suppress excessive protease
activities in various neutrophil mediated diseases. We designed and synthesized a series of …
precursors (elastase, proteinase 3, cathepsin G and NSP4) by removing their N-terminal
propeptide in bone marrow cells at the promyelocytic stage of neutrophil differentiation. The
resulting active proteases are implicated in chronic inflammatory and autoimmune diseases.
Hence, inhibition of CatC represents a therapeutic strategy to suppress excessive protease
activities in various neutrophil mediated diseases. We designed and synthesized a series of …
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