Hypertension is a major risk factor for cardiovascular diseases, with high prevalence in low- and high-income countries. Among the various antihypertensive therapeutic strategies, synthetic Angiotensin I-converting enzyme inhibitors (ACEI) are one of the most used pharmacological agents. However, their use in hypertension therapy has been linked to various side effects. In recent years considerable research has been performed on the use of food-derived ACEI peptides (ACEIp) as antihypertensive agents. Although promising, the industrial production of these ACEIp through conventional methods, such as chemical synthesis and enzymatic hydrolysis of food proteins, has been proven troublesome and expensive. Limitations to the large-scale production of ACEIp for functional foods and supplements can be overcome by producing the precursors of these peptides in heterologous hosts. Bacterial hosts have been the privileged choice, particularly to test the success of the genetic engineering strategies, but new platforms based on plants and microalgae have also been emerging. This work provides an overview of the state of antihypertensive therapy, focusing on ACEI, illustrates the latest advances on ACEIp research, and describes current genetic engineer-based approaches for the heterologous production of ACEIp for antihypertensive therapy.