Skip to main content

View full-text article in PMC

. Author manuscript; available in PMC: 2016 Aug 1.

Published in final edited form as: J Mol Endocrinol. 2015 Jul 28;55(2):107–117. doi: 10.1530/JME-15-0116

Table 2.

The ligand binding and signaling properties of WT and mutant hMC3Rs.

hMC3R	NDP-MSH binding	NDP-MSH-stimulated cAMP
hMC3R	IC₅₀ (nM)	EC₅₀ (nM)	R_max (100%)
WT	2.63 ± 0.27	0.47 ± 0.05	100
D332A	1.59 ± 0.27	0.43 ± 0.04	98.50 ± 18.45
P333A	N/A^d	N/A^d	N/A^d
L334A	1.09 ± 0.07^b	0.39 ± 0.10	79.50 ± 12.12
Y336A	0.79 ± 0.10^b	N/A	N/A
A337G	2.32 ± 0.42	0.57 ± 0.17	98.25 ± 11.27
F338A	3.17 ± 0.79	0.90 ± 0.24^a	94.75 ± 15.58
R339A	2.38 ± 0.28	2.34 ± 0.37^c	48.33 ± 20.00^a
S340A	0.84 ± 0.12^b	0.77 ± 0.22	52.29 ± 13.18^a
L341A	4.81 ± 1.13^a	0.50 ± 0.07	102.50 ±19.31
E342A	0.58 ±0.02^c	N/A^d	N/A^d
L343A	N/A^d	N/A^d	N/A^d
R344A	N/A^d	N/A^d	N/A^d
N345A	1.89 ± 0.17	0.36 ± 0.08	107.00 ± 12.13
T346A	2.08 ± 0.18	0.48 ± 0.16	91.80 ± 8.89
F347A	1.09 ± 0.19^b	0.25 ± 0.06^a	67.25 ± 8.38^a
R348A	0.91 ± 0.04^b	0.42 ± 0.11	53.40 ± 5.62^b
E349A	1.21 ± 0.18^a	0.47 ± 0.16	103.00 ± 23.34
I350A	0.61 ± 0.07^b	0.33 ± 0.07	15.75 ± 1.55^c
L351A	0.64 ± 0.03^b	0.32 ± 0.10	17.50 ± 2.02^c

Values are expressed as the mean ± SEM of at least four independent experiments.

The R_max of WT hMC3R was 2386.00 ± 239.95 pmol/10⁶ cells upon NDP-MSH stimulation.

^a

Significantly different from WT hMC3R, p<0.05.

^b

Significantly different from WT hMC3R, p<0.01.

^c

Significantly different from WT hMC3R, p<0.001.

^d

Not detectable.