FEBS Letters | |
Shared determinants of receptor binding for subtype selective, and dual endothelin‐angiotensin antagonists on the AT1 angiotensin II receptor | |
Yoo, Sung-Eun1  Walsh, Thomas F2  Sandberg, Kathryn3  Nirula, Vaneet3  Lawus, Kimberly3  Dascal, David3  | |
[1] Korean Research Institute of Chemical Technology, Taejon 305-343, South Korea;Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 19486, USA;Department of Medicine, Georgetown University Medical Center, Building D, Room 394, 4000 Reservoir Road, NW, Washington, DC 20007, USA | |
关键词: Angiotensin; Endothelin; AT1 receptor; Non-peptide; Biphenylimidazole; Dual receptor antagonist; RAS; renin angiotensin system; Ang II; angiotensin II; AT receptor; angiotensin receptor; rAT1b; rat (Sprague-Dawley) angiotensin receptor type 1b; xATa; frog (Xenopus laevis) angiotensin receptor type a; xCM46; xATa combinatorial mutant receptor defined in Table 1; COS-7; monkey kidney epithelial cells; TM; transmembrane; | |
DOI : 10.1016/S0014-5793(98)00040-4 | |
学科分类:生物化学/生物物理 | |
来源: John Wiley & Sons Ltd. | |
【 摘 要 】
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 (AT1) 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.
【 授权许可】
Unknown
【 预 览 】
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