Table 1 Binding affinities (Kd) of Ang II and ARBs to AT1 WT and mutants receptors
Receptor | [Sar 1 , Ile 8 ]Ang II | Candesartan | Azilsartan | Azilsartan-7H |
|---|---|---|---|---|
WT | 0.7±0.1 (1.0) | 2.6±0.5 (1.0) | 3.1±0.2 (1.0) | 49±9 (1.0) |
S105A | 0.5±0.3 (0.7) | 5.4±2.0 (2.1) | 12±3 (3.9) | 33±5 (0.7) |
S109A | 1.4±0.1 (2.0) | 5.6±0.7 (2.2) | 11±3 (3.5) | 29±9 (0.6) |
N111G | 0.8±0.5 (1.0) | 15±5 (5.8) | 48±6 (15) | 2362±756 (48) |
N111G/ | 1.3±0.9 (1.9) | 241±41 (93) | 754±54 (243) | 13654±667 (279) |
K199Q | Â | Â | Â | Â |
N111G/ | 1.0±0.2 (1.4) | 64±18 (25) | 71±27 (15) | 4477±437 (91) |
Q257A | Â | Â | Â | Â |
Y113A | 1.0±0.4 (1.4) | 173±45 (67) | 232±96 (75) | 14794±482 (302) |
Y113F | 1.8±1.0 (2.6) | 7.9±3.6 (3.0) | 14±0.3 (4.5) | 523±128 (11) |
V116A | 1.0±0.4 (1.4) | 7.4±2.7 (2.8) | 9.6±0.8 (3.1) | 76±23 (1.6) |
F182A | 0.6±0.2 (0.9) | 3.2±0.5 (1.2) | 7.1±0.9 (2.3) | 23±5 (0.5) |
Y184A | 1.0±0.4 (1.4) | 2.0±0.7 (1.2) | 4.8±1.3 (2.3) | 24±9 (0.5) |
K199A | 3.3±0.5 (4.7) | 53±5 (20) | 103±7 (33) | 2059±344 (42) |
F208A | 0.7±0.3 (1.0) | 3.6±1.2 (1.4) | 7.5±1.9 (2.4) | 30±12 (0.6) |
W253A | 2.2±0.8 (3.1) | 13±2 (5.0) | 25±4 (8.1) | 40±7 (0.8) |
H256A | 0.8±0.3 (1.1) | 4.3±1.6 (1.7) | 5.6±2.4 (1.8) | 54±11 (1.1) |
Q257A | 2.5±0.2 (3.6) | 37±8 (14) | 309±22 (100) | 5028±1216 (103) |
T287A | 1.3±0.2 (1.9) | 15±5 (5.8) | 30±7 (9.7) | 741±35 (15) |
Y292A | 1.7±0.8 (2.4) | 4.6±1.4 (1.8) | 18±5 (5.8) | 22±4 (0.4) |
N295A | 6.4±2.1 (9.3) | 99±16 (38) | 212±97 (68) | 2291±861 (47) |
