TABLE 4.

Activities of various PIs against GRL-216-, GRL-246-, GRL-286-, and GRL-396-selected HIV-1 isolates^a

Virus	EC50 (μM)
	APV	NFV	LPV	AZV	TPV	DRV	GRL-216	GRL-246	GRL-286	GRL-396
HIV-1NL4-3	0.032 ± 0.001	0.040 ± 0.007	0.035 ± 0.004	0.0032 ± 0.0001	0.29 ± 0.05	0.003 ± 0.001	0.004 ± 0.001	0.033 ± 0.003	0.006 ± 0.005	0.017 ± 0.005
HIV-1216-P50	0.26 ± 0.03 (8)	0.13 ± 0.04 (4)	0.19 ± 0.06 (5)	0.014 ± 0.003 (4)	0.029 ± 0.0004 (0.1)	0.009 ± 0.006 (3)	0.094 ± 0.075 (24)	0.26 ± 0.05 (8)	0.19 ± 0.06 (32)	0.24 ± 0.06 (14)
HIV-1246-1 μM	0.34 ± 0.015 (11)	0.29 ± 0.006 (7)	0.33 ± 0.04 (8)	0.032 ± 0.003 (10)	0.095 ± 0.089 (0.3)	0.029 ± 0.001 (10)	0.30 ± 0.01 (75)	0.42 ± 0.09 (12)	0.33 ± 0.03 (55)	0.37 ± 0.013 (22)
HIV-1286-1 μM	>1 (>31)	0.37 ± 0.003 (9)	>1 (>23)	0.021 ± 0.012 (7)	0.037 ± 0.001 (0.1)	0.20 ± 0.05 (67)	>1 (>250)	>1 (>30)	>1 (>167)	>1 (>59)
HIV-1396-1 μM	0.35 ± 0.0002 (11)	0.22 ± 0.02 (6)	0.28 ± 0.05 (6)	0.024 ± 0.002 (8)	0.042 ± 0.002 (0.1)	0.016 ± 0.001 (5)	0.073 ± 0.011 (18)	0.37 ± 0.002 (11)	0.25 ± 0.05 (42)	0.52 ± 0.07 (31)

^aThe amino acid substitutions identified in the protease-encoding region of HIV-1_216-P50, HIV-1_{246-1 μM}, HIV-1_{286-1 μM}, and HIV-1_{396-1 μM} compared to the consensus type B sequence cited from the Los Alamos database include L10I/L24I/M46I/V82I/I84V; L10F/M46I/T91S; L10F/M46L/I50V/A71V; and L10F/M46M, I/Q61Q, or K/V82I/I84V, respectively. MT-4 cells (10⁴) were exposed to 100 TCID₅₀s of each HIV-1 isolate, and inhibition of p24 Gag protein production by each drug was used as the end point. Numbers in parentheses represent the n-fold changes in EC₅₀s for each isolate compared to the EC₅₀s for wild-type isolate HIV-1_NL4-3. All assays were conducted in duplicate or triplicate, and the data shown represent the mean values (±1 standard deviation) derived from the results of three independent experiments.