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Related Experiment Videos

Chymase: its pathophysiological roles and inhibitors.

H Fukami1, H Okunishi, M Miyazaki

  • 1Institute for Biomedical Research, Santory, Ltd., Osaka, Japan.

Current Pharmaceutical Design
|April 10, 1999
PubMed
Summary

Chymase, a protease in mast cells, generates angiotensin II and remodels tissues. Inhibitors targeting chymase may prevent inflammatory diseases, though in vivo functions require further study.

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Area of Science:

  • Biochemistry
  • Enzymology
  • Pharmacology

Background:

  • Chymase is a mast cell-localized serine protease.
  • Different species exhibit distinct chymase functions regarding Angiotensin II (Ang II) metabolism.
  • Chymase contributes to cardiovascular tissue remodeling and extracellular matrix degradation.

Purpose of the Study:

  • To review the pathophysiological roles of chymase.
  • To discuss the potential of chymase inhibitors in treating inflammatory diseases.
  • To explore structure-activity relationships of novel chymase inhibitors.

Main Methods:

  • Literature review of chymase functions and inhibitors.
  • Analysis of existing data on chymase's role in disease.
  • Discussion of structure-activity relationships for specific inhibitor classes.

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Main Results:

  • Chymase generates Ang II, potentially impacting the renin-angiotensin system.
  • Chymase's proteolytic activities contribute to tissue remodeling in inflammatory conditions.
  • Various chymase inhibitors, including non-peptide small molecules, have been developed.

Conclusions:

  • Chymase plays a significant role in inflammatory tissue remodeling.
  • Chymase inhibitors hold therapeutic potential for inflammatory diseases.
  • Further in vivo validation of chymase inhibitors is necessary.