Table 3.
hMC3R | α-MSH | ||
---|---|---|---|
cAMP | pERK1/2 | Bias | |
WT | ↑ | ↑ | No |
S17T | ↑ | ↑ | No |
S69C | ↑ | ↑ | No |
A70T | ↑ | ↑ | No |
F82S | — | ↑ | Yes |
I87T | ↑ | — | Yes |
N128S | ↑ | — | Yes |
M134I | ↑ | — | Yes |
D158Y | — | — | No |
V177I | ↑ | ↑ | No |
I183N | — | ↑ | Yes |
L249F | ↑ | ↑ | No |
L249V | ↑ | ↑ | No |
R257S | ↑ | ↑ | No |
A260V | ↑ | ↑ | No |
M275T | ↑ | ↑ | No |
T280S | — | — | No |
L285V | ↑ | ↑ | No |
A293T | ↑ | ↑ | No |
L297V | ↑ | — | Yes |
L299V | ↑ | ↑ | No |
I335S | — | ↑ | Yes |
X361S | ↑ | ↑ | No |
“↑”: Denotes increased activity compared to the basal level. “−”: denotes no significant changes between basal and maximal signaling levels. “Bias” column is designed to demonstrate whether α-MSH-stimulated cAMP and pERK1/2 signaling pathways were divergent. “Yes” denotes biased activation of either signaling pathway; “No” denotes balanced cAMP and pERK1/2 signaling.