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. Author manuscript; available in PMC: 2011 Nov 15.

Published in final edited form as: Biochemistry. 2007 Sep 18;46(40):11389–11397. doi: 10.1021/bi700125e

Table 2.

Effect of the substitutions of the conserved amino acid residues of hMC2R on ¹²⁵I ACTH binding and cAMP production

	Receptor expression (% of WT)	¹²⁵I- ACTH binding Ki (nM)	cAMP production EC₅₀ (nM)

hMC2RWT	100	5.6 ± 1.0	0.8 ± 0.2
D70A	No	NB	NR
K77A	73 ± 9.5	25.2 ± 4.1^*	6.2 ± 0.9^*
E80A	75 ± 12.3	65.2 ± 7.1^*	7.8 ± 1.1^*
D103N	68 ± 14	15.7 ± 0.7^*	5.8 ± 1.2^*
D107N	66 ± 11	>10³^*	>10³^*
F178A	67 ± 8.7	>10³^*	>10³^*
F235A	84 ± 6.8	98 ± 6.9^*	216 ± 18^*
H238A	69 ± 11.7	>10³^*	>10³^*
F258A	78 ± 12.7	78 ± 4.4^*	187 ± 10^*
D272A	No	NB	NR

^*

P<0.05 compared with WT receptor.