期刊论文详细信息
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.
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【 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   

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