Structure--activity relations of antagonists of the renin--angiotensin system

In this review, inhibitors of the renin-angiotensin system, both naturally occurring and synthetic, are considered. Inhibition of renin itself, of converting enzyme (dipeptidyl carboxypeptidase), and of interaction with the receptor is characterized from the point of view of mechanism, structure-activity relations, and future developments. The concept of transition state analog and its relevance to the inhibition of renin by pepstatin is discussed. Questions concerning selectivity, increased affinity, and longer duration of action are raised with regard to future design of inhibitors of the renin-angiotensin system.