Shared determinants of receptor binding for subtype selective, and dual endothelin‐angiotensin antagonists on the AT 1 angiotensin II receptor
1998; Wiley; Volume: 423; Issue: 1 Linguagem: Inglês
10.1016/s0014-5793(98)00040-4
ISSN1873-3468
AutoresDavid Dascal, Vaneet Nirula, Kimberly Lawus, Sung‐Eun Yoo, Thomas F. Walsh, Kathryn Sandberg,
Tópico(s)Nitric Oxide and Endothelin Effects
ResumoSite‐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.
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