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Shared determinants of receptor binding for subtype selective, and dual endothelin‐angiotensin antagonists on the AT 1 angiotensin II receptor
Author(s) -
Dascal David,
Nirula Vaneet,
Lawus Kimberly,
Yoo Sung-Eun,
Walsh Thomas F,
Sandberg Kathryn
Publication year - 1998
Publication title -
febs letters
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.593
H-Index - 257
eISSN - 1873-3468
pISSN - 0014-5793
DOI - 10.1016/s0014-5793(98)00040-4
Subject(s) - angiotensin ii , angiotensin receptor , angiotensin ii receptor type 1 , endothelin receptor , receptor , chemistry , renin–angiotensin system , pharmacology , angiotensin 1 , endocrinology , medicine , biology , biochemistry , blood pressure
Site‐directed interspecies amino acid exchange was used to compare the binding determinants of a novel dual endothelial‐angiotensin receptor ligand, L‐746,072, with type‐1 angiotensin receptor (AT 1 ) selective antagonists on AT receptors expressed in COS cells. These studies suggest that residues on AT receptors which are non‐conserved between amphibian and mammalian species play a greater role in subtype selective ligand recognition than for dual receptor ligands. These data also support the hypothesis that a common non‐peptide binding site exists within transmembrane domains on peptidergic receptors.