Table 3.
Effect of mutation in D137, N138, and previously reported residues of H+,K+-ATPase.
| TM | mutation | K i[SCH28080] | K i[SCH-Me−] | K i[SCH-CN−] | K i[BYK99] | K i[BYK73] | |||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| nM | -folda | μM | -fold | μM | -fold | nM | -fold | μM | -fold | ||
| WT | WT | 150 ± 10 | 1.0 | 11 ± 0.1 | 1.0 | 3.2 ± 0.3 | 1.0 | 5.8 ± 0.6 | 1.0 | 4.9 ± 0.4 | 1.0 |
| M2 | D137E* | 170 ± 100 | 1.1 | n.d. | — | 4.4 ± 0.4 | 1.4 | 57 ± 16 | 9.8 | n.d. | — |
| D137N | > 10000 | > 67 | n.d. | — | 120 ± 30 | 38 | 450 ± 100 | 78 | n.d. | — | |
| N138D | 200 ± 20 | 1.3 | n.d. | — | 2.6 ± 0.2 | 0.8 | 7.7 ± 0.7 | 1.3 | n.d. | — | |
| D137N/N138D | 1800 ± 200 | 12 | n.d. | — | 23 ± 20 | 7.2 | 110 ± 10 | 19 | n.d. | — | |
| M4 | A335G | 60 ± 5 | 0.4 | 1.6 ± 0.2 | 0.15 | 1.0 ± 0.1 | 0.3 | 1.2 ± 0.1 | 0.2 | 0.078 ± 0.006 | 0.016 |
| A335V | > 10000 | > 67 | n.d. | — | n.d. | — | > 1000 | > 170 | n.d. | — | |
| A335C/C813A | > 10000 | >67 | 4200 ± 2300 | 382 | 71 ± 10 | 22 | > 1000 | > 170 | n.d. | — | |
| M5 | Y799A | > 10000 | > 67 | 740 ± 170 | 67 | 81 ± 15 | 25 | > 1000 | > 170 | > 200 | > 40 |
| Y799F | 880 ± 60 | 5.9 | 31 ± 3 | 2.8 | 18 ± 2 | 5.6 | 110 ± 10 | 19 | 21 ± 2.7 | 4.3 | |
| M6 | L809F | 4400 ± 800 | 29 | 110 ± 20 | 10 | 98 ± 12 | 31 | 850 ± 130 | 150 | n.d. | — |