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Angiotensin II is a peptide hormone known best as a vasoconstrictor with central roles in chronic hypertension, heart failure, and stroke.1 It is an octapeptide typically generated by the removal of two residues from angiotensin I by angiotensin-converting enzyme (ACE).2 Angiotensin II is a ligand for at least two distinct receptors, AT1 and AT2, each evoking distinct signaling pathways and physiological responses.1,3 The development of antagonists for specific angiotensin II receptor subtypes represents a valuable alternative to ACE inhibitors.4
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1. Angiotensin II type 1 receptor blockers. Circulation 103(6), 904-912 (2001).
2. Development of domain-
3. Relative affinity of angiotensin peptides and novel ligands at AT1 and AT2 receptors. Clin. Sci. (Lond.) 121(7), 297-303 (2011).
4. Nonpeptide angiotensin II receptor antagonists: The next generation in antihypertensive therapy. J. Med. Chem. 39(3), 625-656 (2014).