. 2004 Apr;78(8):4134–4144. doi: 10.1128/JVI.78.8.4134-4144.2004

TABLE 2.

Effects of amino acid substitutions in hu-CCR5 and rh-CCR5 on HIV-1 Env pseudotype infectivity in a single-round assay

CCR5 construct	Result for the following Env-pseudotyped virus:
	HIV_JR-FL^a		HIV_ADA^b		HIV_YU2^c
	Relative IC₅₀^d	% Inhibition^e	Relative IC₅₀	% Inhibition	Relative IC₅₀	% Inhibition
hu-CCR5	1	95.3 ± 0.6	1	97.9 ± 0.7	1	98.7 ± 0.6
rh-CCR5^f	240 ± 15	57.3 ± 2.1	>490	51.5 ± 7.4	>390	61.8 ± 8.2
hu-CCR5(I9T)	0.6 ± 0.1	97.4 ± 1.4	0.2	99	2.3	98
hu-CCR5(N13D)	2.1 ± 0.1	95.9 ± 1.2	2.0	98	0.7	99
hu-CCR5(M49I)	1.0 ± 0.6	95.2 ± 0.3	0.9	99	1.5 ± 1.0	99.1 ± 0.7
hu-CCR5(I52V)	0.3 ± 0.1	97.1 ± 1.9	ND	ND	1.5	100
hu-CCR5(F78L)	0.6 ± 0.1	97.5 ± 1.2	0.1	100	0.6 ± 0.3	100
hu-CCR5(V130I)	3.7 ± 3.5	96.0 ± 2.5	0.5	98	1.8	97
hu-CCR5(K171R)	0.6 ± 0.4	96.4 ± 2.0	1.8	98	0.2	98
hu-CCR5(I198M)	>250	21.0 ± 16.6	>3,700	49	450	54
rh-CCR5(M198I)	0.8 ± 0.2	95.3 ± 3.1	ND	ND	2.1	93

n = 5 for hu-CCR5; n = 4 for rh-CCR5(M198I); n = 3 for rh-CCR5 and hu-CCR5(I198M); n = 2 for hu-CCR5(I9T), hu-CCR5(N13D), hu-CCR5(M49I), hu-CCR5(I52V), hu-CCR5(F78L), hu-CCR5(V130I), and hu-CCR5(K171R). Values are means ± standard errors of the means where n is >2 and means ± ranges where n is 2.

n = 5 for hu-CCR5 and n = 4 for rh-CCR5; values are means ± standard errors of the means. n = 1 for all other CCR5 constructs. ND, not done.

n = 5 for hu-CCR5 and n = 4 for rh-CCR5; values are means ± standard errors of the means. n = 2 for hu-CCR5(M49I) and hu-CCR5(F78L); values are means ± ranges. n = 1 for all other CCR5 constructs.

IC₅₀ were obtained from individual data sets fit to a sigmoidal dose-response curve by nonlinear regression using the Prism program (GraphPad Software) and were normalized to the IC₅₀ for hu-CCR5 in the same experiment.

Percent inhibition is the average percent reduction in luciferase activity at 1 μM SCH-C.

Boldfaced values indicate those CCR5 constructs for which inhibition by SCH-C was significantly reduced relative to that for hu-CCR5.