Angiotensin-converting enzyme

Angiotensin-converting enzyme (ACE) is a zinc-containing metallopeptidase, best known for its role in the conversion of Ang I in the active peptide Ang II, which plays a pivotal role in the blood pressure (BP) regulation trough the renin-angiotensin system (RAS). In the past decades, RAS has been deeply studied in all its aspects and implications. It has been seen that ACE and its substrates are involved in many other physiological and pathological processes in addition to pressure control, such as hematopoiesis, reproduction, renal development, and immune response. Its homologous protein ACE2, critical enzyme in counter-regulatory response to RAS, was studied, and its pharmacological modulation has been evaluated. According to ACE in vivo roles and its implication in a great number of physiological pathways, several studies focused on the potential role of classic ACE inhibitors (ACEIs) and new domain-selective compounds for the treatments of several diseases. This chapter seeks to review the evolution of the physio/pathological roles of ACEs and their pharmacological modulation, for the treatment of a wide range of pathologies.