Table 1 Activity data for RXFP2 mutants compared to wild-type RXFP2.
Construct | Eu-INSL3 binding | Eu-H2 relaxin binding | INSL3 activation | H2 Relaxin activation | ||||
|---|---|---|---|---|---|---|---|---|
B max | K d | B max | K d | E max | pEC50 | E max†| pEC50 | |
RXFP2 | 23675 ± 5961 (3) | 1.07 ± 0.22 (3) | 19543 ± 3673 (3) | 9.96 ± 0.62 (3) | 100 (6) | 9.99 ± 0.40 (6) | 100 (6) | 8.45 ± 0.15 (6) |
G42A | 35678 ± 7441 (3) | 1.93 ± 0.69 (3) | ND | ND | 39.47 ± 12.90 (3)* | 8.98 ± 0.45 (3) | 75.21 ± 12.02 (3) | 7.98 ± 0.55 (3) |
D43A | 25734 ± 10412 (3) | 1.18 ± 0.15 (3) | No binding (3) | No activity (3) | No activity (3) | |||
T44A | 32817 ± 4006 (3) | 2.11 ± 0.63 (3) | ND | ND | 98.66 ± 29.83 (4) | 10.50 ± 0.44 (4) | 53.02 ± 5.55 (3)* | 8.63 ± 0.40 (3) |
S45A | 26897 ± 5303 (3) | 1.05 ± 0.20 (3) | ND | ND | 92.15 ± 21.82 (3) | 10.14 ± 0.20 (3) | 100 ± 7.23 (4) | 9.03 ± 0.13 (4) |
G46A | 34363 ± 2825 (3) | 1.51 ± 0.43 (3) | No binding (3) | No activity (3) | No activity (3) | |||
W47A | 40744 ± 10281 (3) | 1.50 ± 0.41(3) | No binding (3) | No activity (3) | No activity (3) | |||
F51A | 39612 ± 5290 (3) | 1.55 ± 0.13 (3) | No binding (3) | 39.76 ± 3.69 (3)* | 9.36 ± 0.09 (3) | 18.78 ± 5.0 (3)** |  < 6 (3) | |
