Angiotensin converting enzyme (ACE) is a zinc metallopeptidase which plays a key role in the regulation of important vasoactive peptides through its proteolytic activity. Effective inhibitors of ACE were until recently designed in the absence of the solved 3D structure of this enzyme. About 15 ACE inhibitors are currently commercially available, all of which nonspecifically inhibit both active domains of ACE. Vasopeptidase inhibitors are mixed inhibitors of ACE and neutral endopeptidase (NEP). They contemporarily inhibit the catalytic function of two enzymes and currently are undergoing clinical trials exhibiting better efficacy in the treatment of hypertension and cardiovascular diseases, but in the same time higher risk of adverse side effects compared to ACE inhibitors.