Why the study?
Angiotensin peptides also bind to receptors distinct from AT 1 R, particularly AT 2 R, producing different and sometimes antagonistic effects that may serve as therapeutic targets.
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Design
Perspective review
AT2R modulation may offer distinct RAS effects; leaves open therapeutic translation pending targeted trials.
The active hormone of the renin–angiotensin system (RAS), angiotensin II (Ang II), is involved in several human diseases, driving the development and clinical use of several therapeutic drugs, mostly angiotensin I converting enzyme (ACE) inhibitors and angiotensin receptor type I (AT 1 R) antagonists. However, angiotensin peptides can also bind to receptors different from AT 1 R, in particular, angiotensin receptor type II (AT 2 R), resulting in biological and physiological effects different, and sometimes antagonistic, of their binding to AT 1 R. In the present Perspective, the components of the RAS and the therapeutic tools developed to control it will be reviewed. In particular, the characteristics of AT 2 R and tools to modulate its functions will be discussed. Agonists or antagonists to AT 2 R are potential therapeutics in cardiovascular diseases, for agonists, and in the control of pain, for antagonists, respectively. However, controlling their binding properties and their targeting to the target tissues must be optimized.
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Lucienne Juillerat‐Jeanneret (2020) studied this question.
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