Angiotensin-converting enzyme 2 (ACE2) or human homologue of ACE was first described in 2000. Although ACE2 is related to angiotensin-converting enzyme (ACE), it is not inhibited by ACE inhibitors. The major function of ACE2 is to degrade angiotensin II, resulting in the production of angiotensin 1–7 (Ang 1–7), which counteracts the activities of Ang II. This has altered our entire perspective on the part of renin-angiotensin system in the regulation of blood pressure, cardiac and renal function. ACE2 has important role in variety of conditions where its expression is reduced, such as in hypertension, CKD and cardiovascular pathologies. In these disorders, current therapy methods involving ACE2 include utilizing ACE2 adenoviruses, recombinant ACE2, or chemicals that increase its expression, hence providing some organ protection.