Table 1.
Receptor binding affinity and potency | ||||||||||
---|---|---|---|---|---|---|---|---|---|---|
Residue mutation | hMC1R | hMC2R | hMC3R | hMC4R | hMC5R | |||||
TM2 (2.6) | E94 | ↓ | E80 | ↓ | E131 | ↓ | E100 | ↓ | E92 | ↓ |
TM3 (3.25) | D117 | ↓ | D103 | ↓ | D154 | ↓ | D122 | ↓ | D115 | ↓ |
TM3 (3.29) | D121 | ↓ | D107 | ↓ | D158 | ↓ | D126 | ↓ | D119 | ↓ |
TM6 (6.48) | W254 | ↓ | W232 | ↓ | W292 | ↓ | W258 | ↓ | W251 | ↓ |
TM6 (6.51) | F257 | ↓ | F235 | ↓ | F295 | ↓ | F261 | ↓ | F254 | ↓ |
TM6 (6.54) | H260 | ↓ | H238 | ↓ | H298 | ↓ | H264 | ↓ | H257 | ↓ |
binding affinity and potency decrease.