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Endothelin-converting enzyme inhibitors: current status and perspectives.
1F. Hoffmann-La Roche Ltd, Pharma Division, Preclinical Research, Basel, Switzerland. bernd-m.loeffler@roche.com
Journal of Cardiovascular Pharmacology
|September 8, 2000
Summary
New inhibitors targeting cardiovascular systems like endothelin (ET) and renin-angiotensin are available. Future research will determine if combined inhibition of multiple systems is more effective than selective inhibition.
Area of Science:
- Pharmacology
- Cardiovascular Research
- Biochemistry
Background:
- Emerging evidence indicates interconnected functions between endothelin (ET), renin-angiotensin, and neutral endopeptidase (NEP) systems in regulating cardiovascular homeostasis.
- A complex regulatory network governs these systems.
Purpose of the Study:
- To explore the potential of newly developed selective and mixed endothelin-converting enzyme (ECE) inhibitors.
- To investigate whether combined inhibition of multiple cardiovascular systems offers advantages over selective inhibition.
Main Methods:
- Discovery of potent selective or mixed inhibitors for endothelin-converting enzyme (ECE).
- Development of inhibitors targeting ECE/neutral endopeptidase 24.11 (NEP) and ECE/NEP24.11/angiotensin-converting enzyme (ACE).
Main Results:
- Potent selective and mixed inhibitors for ECE, ECE/NEP, and ECE/NEP/ACE have been identified.
- Growing evidence supports a complex regulatory network linking ET, renin-angiotensin, and NEP systems.
Conclusions:
- Newly available selective and mixed ECE-1 inhibitors present opportunities for future research.
- Determining the superiority of combined versus selective cardiovascular system inhibition is a key future challenge.