Pharmacological properties of swelling-activated anion currents
| Construct | IC50 (μM) | Hill coefficient | ||
|---|---|---|---|---|
| +100 mV | −100 mV | +100 mV | −100 mV | |
| Chimera | ||||
| 8C-8A(IL125) | 2.1 | 2.3 | 2.15 | 2.26 |
| 8C-8A(IL125) E6A | 0.28 | 0.33 | 1.18 | 1.28 |
| P < 0.0001 | P < 0.0001 | P < 0.005 | P < 0.01 | |
| 8C-8A(IL125) M48D | 412.9 | 109.1 | 0.37 | 0.48 |
| P < 0.0001 | P < 0.0001 | P < 0.0001 | P < 0.0001 | |
| 8C-8A(IL125) M48K | 36.9 | 21.7 | 0.65 | 1.53 |
| P < 0.0001 | P < 0.0001 | P < 0.0001 | | |
| 8C-8A(IL125) M48R | 10.2 | 19.4 | 0.75 | 1.33 |
| P < 0.0001 | P < 0.0001 | P < 0.0001 | | |
| 8C-8A(IL125) L105F | 2.1 | 2.4 | 1.91 | 1.87 |
| 8C-8A(IL125) L105R | 0.8 | 0.8 | 1.87 | 2.11 |
| P < 0.0001 | P < 0.0001 | | | |
| 8C-8A(IL125) Q106A | 3.1 | 3.5 | 2.28 | 2.48 |
| P < 0.0005 | P < 0.0001 | | | |
| 8C-8A(IL125) Y108A | 1.2 | 1.2 | 1.28 | 1.17 |
| P < 0.005 | P < 0.0005 | P < 0.05 | P < 0.01 | |
| 8C-8A(IL125) N112A | 5.0 | 5.9 | 2.03 | 2.47 |
| P < 0.0001 | P < 0.0001 | | | |
| 8C-8A(IL125) Y126F | 0.40 | 0.47 | 1.26 | 1.30 |
| P < 0.0001 | P < 0.0001 | P < 0.05 | P < 0.05 | |
| 8C-8A(IL125) L136E | N.D. | N.D. | N.D. | N.D. |
| 8C-8A(IL125) L136K | 0.40 | 0.53 | 1.08 | 1.28 |
| P < 0.0001 | P < 0.0001 | P < 0.001 | P < 0.005 | |
| Heteromer | ||||
| 8A + 8C | 4.5 | 4.1 | 1.71 | 1.69 |
| 8A E6A + 8C E6A | 0.53 | 0.65 | 1.26 | 1.25 |
| P < 0.0001 | P < 0.0001 | | | |
| 8A T48D + 8C M48D | 301.3 | 124.9 | 0.68 | 0.59 |
| P < 0.0001 | P < 0.0001 | | P < 0.05 | |
| 8A + 8C L105R | 3.3 | 2.59 | 1.58 | 1.49 |
| | P < 0.005 | | | |
| 8A Y124F + 8C Y126F | 3.4 | 3.1 | 1.75 | 1.73 |
| | P < 0.05 | | | |
| 8A L134E + 8C L136E | 1.9 | 2.2 | 1.24 | 1.34 |
| P < 0.0001 | P < 0.0001 | | | |
| 8A L134K + 8C L136K | 1.3 | 1.4 | 1.17 | 1.21 |
| P < 0.0001 | P < 0.0001 | | | |
| Construct | IC50 (μM) | Hill coefficient | ||
|---|---|---|---|---|
| +100 mV | −100 mV | +100 mV | −100 mV | |
| 8C-8A(IL125) | 2.1 | 2.3 | 2.15 | 2.26 |
| 8C-8A(IL125) E6A | 0.28 | 0.33 | 1.18 | 1.28 |
| P < 0.0001 | P < 0.0001 | P < 0.005 | P < 0.01 | |
| 8C-8A(IL125) M48D | 412.9 | 109.1 | 0.37 | 0.48 |
| P < 0.0001 | P < 0.0001 | P < 0.0001 | P < 0.0001 | |
| 8C-8A(IL125) M48K | 36.9 | 21.7 | 0.65 | 1.53 |
| P < 0.0001 | P < 0.0001 | P < 0.0001 | | |
| 8C-8A(IL125) M48R | 10.2 | 19.4 | 0.75 | 1.33 |
| P < 0.0001 | P < 0.0001 | P < 0.0001 | | |
| 8C-8A(IL125) L105F | 2.1 | 2.4 | 1.91 | 1.87 |
| 8C-8A(IL125) L105R | 0.8 | 0.8 | 1.87 | 2.11 |
| P < 0.0001 | P < 0.0001 | | | |
| 8C-8A(IL125) Q106A | 3.1 | 3.5 | 2.28 | 2.48 |
| P < 0.0005 | P < 0.0001 | | | |
| 8C-8A(IL125) Y108A | 1.2 | 1.2 | 1.28 | 1.17 |
| P < 0.005 | P < 0.0005 | P < 0.05 | P < 0.01 | |
| 8C-8A(IL125) N112A | 5.0 | 5.9 | 2.03 | 2.47 |
| P < 0.0001 | P < 0.0001 | | | |
| 8C-8A(IL125) Y126F | 0.40 | 0.47 | 1.26 | 1.30 |
| P < 0.0001 | P < 0.0001 | P < 0.05 | P < 0.05 | |
| 8C-8A(IL125) L136E | N.D. | N.D. | N.D. | N.D. |
| 8C-8A(IL125) L136K | 0.40 | 0.53 | 1.08 | 1.28 |
| P < 0.0001 | P < 0.0001 | P < 0.001 | P < 0.005 | |
| 8A + 8C | 4.5 | 4.1 | 1.71 | 1.69 |
| 8A E6A + 8C E6A | 0.53 | 0.65 | 1.26 | 1.25 |
| P < 0.0001 | P < 0.0001 | | | |
| 8A T48D + 8C M48D | 301.3 | 124.9 | 0.68 | 0.59 |
| P < 0.0001 | P < 0.0001 | | P < 0.05 | |
| 8A + 8C L105R | 3.3 | 2.59 | 1.58 | 1.49 |
| | P < 0.005 | | | |
| 8A Y124F + 8C Y126F | 3.4 | 3.1 | 1.75 | 1.73 |
| | P < 0.05 | | | |
| 8A L134E + 8C L136E | 1.9 | 2.2 | 1.24 | 1.34 |
| P < 0.0001 | P < 0.0001 | | | |
| 8A L134K + 8C L136K | 1.3 | 1.4 | 1.17 | 1.21 |
| P < 0.0001 | P < 0.0001 | | | |
P values reflect comparisons of WT 8C-8A(IL125) or 8A + 8C with mutants.
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