Renin – A therapeutic target for hypertension
The renin–angiotensin-aldosterone system (RAAS) plays a central role in the regulation of blood pressure and electrolyte homoeostasis.
Renin, a highly specific aspartyl protease, is produced from the pro-renin precursor by tryptic digestion. It cleaves angiotensinogen, produced in the liver, to yield angiotensin I, which is further converted into angiotensin II by ACE (Angiotensin Converting Enzyme).
Angiotensin II constricts blood vessels, leading to increased blood pressure. It also increases the secretion of ADH and aldosterone and stimulates the hypothalamus to activate the thirst reflex.
Since an overactive renin-angiotensin system is linked to hypertension, renin is proposed as a therapeutic target. Its activity can be easily measured in FRET-based enzymatic assays using specific peptide substrates.