Table 3. Mutations at Tyr102, Tyr198, Tyr241, and Tyr247a.
| Y102 |
Y198 |
Y241 |
Y247 |
|||||
|---|---|---|---|---|---|---|---|---|
| residues | EC50 (μM) | nH | EC50 (μM) | nH | EC50 (μM) | nH | EC50 (μM) | nH |
| Y(wild type) | 1.4 ± 0.2 | 1.6 ± 0.3 | 1.4 ± 0.2 | 1.6 ± 0.3 | 1.4 ± 0.2 | 1.6 ± 0.3 | 1.4 ± 0.2 | 1.6 ± 0.3 |
| F | 1.9 ± 0.6 | 1.1 ± 0.3 | 12 ± 1b | 1.6 ± 0.1 | 21 ± 1b | 1.3 ± 0.1 | 42 ± 4b | 1.5 ± 0.2 |
| A | 110 ± 20b | 1.2 ± 0.2 | 2000 ± 200b | 1.1 ± 0.1 | 4900 ± 480b | 1.1 ± 0.1 | NR | |
| S | 135 ± 25b | 1.3 ± 0.3 | 5600 ± 600b | 1.6 ± 0.2 | 1500 ± 96b | 1.2 ± 0.1 | NR | |
| W | 860 ± 60b | 1.4 ± 0.1 | 250 ± 30b | 1.1 ± 0.1 | 8.2 ± 1.4b | 1.3 ± 0.3 | 99 ± 8b | 1.3 ± 0.1 |
| 4-F-Phe | 3.1 ± 0.3 | 1.5 ± 0.2 | 34 ± 7c | 1.9 ± 0.3 | 1100 ± 370b | 0.6 ± 0.1b | 90 ± 3b | 1.9 ± 0.1 |
| 3,5-F2–Phe | 6.1 ± 0.9b | 1.6 ± 0.3 | 1700 ± 400c | 1.4 ± 0.2 | 490 ± 190b | 1.5 ± 0.3 | NR | |
| 3,4,5-F3-Phe | 3.4 ± 0.5 | 1.3 ± 0.2 | 8400 ± 1000c | 1.5 ± 0.1 | 950 ± 140b | 1.3 ± 0.3 | NR | |
| 4-Br-Phe | 1.6 ± 0.8 | 1.3 ± 0.4 | 620 ± 30b | 1.8 ± 0.2 | 2900 ± 170b | 1.1 ± 0.1 | ||
| 4-Me-Phe | 4.6 ± 2.1 | 1.4 ± 0.3 | 140 ± 100b | 1.4 ± 0.4 | NR | |||
| 4-MeO-Phe | 180 ± 20b | 1.4 ± 0.2 | 6.6 ± 2c | 1.6 ± 0.2 | 530 ± 50b | 1.7 ± 0.2 | NR | |
| 3-OH-Phe | 66 ± 9b | 1.7 ± 0.3 | 350 ± 70b | 1.5 ± 0.4 | NR | |||
Data = mean ± SEM, n ≥ 3.
Significantly different to wild type, p < 0.05.
Previously published (ref (11)).