Table 1 Gating properties and toxin inhibition of Kv2.1 and Cav3.1/Kv2.1 chimaeric constructs.
From: Molecular Interactions between Tarantula Toxins and Low-Voltage-Activated Calcium Channels
Construct | V1/2 (mV) | z | Kd (μM) | |||
|---|---|---|---|---|---|---|
ProTx-II | PaTx-1 | GsAF-I | GsAF-II | |||
Kv2.1 | −5.8 ± 1 | 2.6 ± 0.3 | 7.4 ± 0.2 | 17 ± 0.3 | 36 ± 0.7 | 23 ± 0.5 |
DI | 4.4 ± 0.9 | 3.06 ± 0.4 | 2.2 ± 0.07 | 2.3 ± 0.2 | 6.6 ± 0.3 | 8.5 ± 0.3 |
E198A | 23 ± 2 | 2.8 ± 0.1 | 7.7 ± 0.2 | 5.4 ± 0.2 | 19 ± 0.6 | >50 |
DII | 25 ± 0.7 | 2.9 ± 0.1 | 9.2 ± 0.3 | 16 ± 0.5 | 11 ± 1 | >50 |
E855A | 8 ± 0.5 | 2.4 ± 0.1 | 30 ± 0.7 | >50 | >50 | >50 |
DIII | −1.3 ± 1 | 2.6 ± 0.1 | 1.2 ± 0.2 | 2.1 ± 0.01 | 2.7 ± 0.2 | 20 ± 0.2 |
V1370 | −4 ± 1 | 1.7 ± 0.1 | 1.3 ± 0.09 | 2 ± 0.1 | 2.4 ± 0.2 | 16 ± 0.6 |
I1371 | 21 ± 1 | 1.3 ± 0.1 | 1.6 ± 0.2 | 1.8 ± 0.3 | 1.6 ± 0.1 | 7.6 ± 0.1 |
D1372 | 11 ± 1 | 2.1 ± 0.2 | 9.1 ± 0.4 | 47 ± 1.1 | 7.2 ± 0.3 | 6.4 ± 0.7 |
I1373 | −12 ± 1 | 2.2 ± 0.1 | 1.07 ± 0.1 | 2.1 ± 0.1 | 2 ± 0.4 | 7.7 ± 1 |
L1374 | −9 ± 1 | 1.7 ± 0.1 | 0.9 ± 0.2 | 0.9 ± 0.07 | 2.3 ± 0.03 | 7.2 ± 0.5 |
V1375 | −14 ± 1 | 1.7 ± 0.1 | 1.1 ± 0.1 | 1.4 ± 0.2 | 2 ± 0.5 | 8.8 ± 0.5 |
S1376 | 13 ± 1 | 1.1 ± 0.1 | 1.1 ± 0.1 | 0.9 ± 0.06 | 1.2 ± 0.1 | 5.4 ± 0.5 |
M1377 | 28 ± 1 | 1.2 ± 0.1 | 2 ± 0.1 | ND | 2.8 ± 0.2 | 11 ± 0.4 |
V1378 | 8 ± 2 | 1.1 ± 0.1 | 1.3 ± 0.2 | 1.8 ± 0.1 | 1.7 ± 0.1 | 4.7 ± 0.4 |
S1379 | −4 ± 1 | 1.1 ± 0.1 | 1.2 ± 0.7 | 1.3 ± 0.1 | 2.4 ± 0.2 | 7.1 ± 0.4 |
D1380 | 13 ± 2 | 1.0 ± 0.1 | 1.9 ± 0.3 | 1.8 ± 0.2 | 2.8 ± 0.2 | 13 ± 0.5 |
S1381 | 25 ± 1 | 1.1 ± 0.1 | 1.8 ± 0.1 | 1.3 ± 0.1 | 1.3 ± 0.3 | 7.6 ± 0.2 |
G1392 | 26 ± 1 | 1.5 ± 0.1 | 1.5 ± 0.3 | 1.7 ± 0.08 | 2.2 ± 0.1 | 8.4 ± 0.4 |
T1383 | 7 ± 1 | 1.3 ± 0.1 | 1.2 ± 0.02 | 2.9 ± 0.1 | 1.9 ± 0.2 | 6.5 ± 0.4 |
K1384 | 5 ± 2 | 0.9 ± 0.05 | 1.2 ± 0.1 | 0.8 ± 0.07 | 1.3 ± .02 | 5 ± 0.07 |
I1385 | −7 ± 2 | 1.1 ± 0.1 | 1 ± 0.2 | 2.3 ± 0.1 | 2.2 ± 0.1 | 13 ± 0.3 |
L1386 | 4 ± 2 | 0.8 ± 0.05 | 1.2 ± 0.1 | 3 ± 0.2 | 2.4 ± 0.3 | 19 ± 0.7 |
G1387 | −9 ± 1 | 1.9 ± 0.1 | 1.1 ± 0.1 | 1.7 ± 0.1 | 2 ± 0.1 | 11 ± 0.1 |
M1388 | −4 ± 1 | 1.3 ± 0.1 | 2.3 ± 0.1 | 3.2 ± 0.1 | 2.1 ± 0.1 | 15 ± 0.5 |
L1389 | −28 ± 2 | 1.4 ± 0.1 | 1.8 ± 0.3 | 3.1 ± 0.07 | 3.5 ± 0.1 | 8.6 ± 0.4 |
DIV | −87 ± 1 | 3.4 ± 0.3 | >50 | 28 ± 1.2 | >50 | >50 |