Table 1.

Summary of the IC₅₀ (nM) values for different integrase inhibitors with wt and mutant INs^*.

Inhibitor	Products with wt IN			Products with N155H IN			Products with Q148H IN
	FS	DD	CHS	FS	DD	CHS	FS	CHS
EVG	8.5 ± 1.3	8.6 ± 1.2	145 ± 5	87 ± 7.5	62 ± 24	250 ± 24	173 ± 50	230 ± 29
RAL	21 ± 4	14 ± 2.5	246 ± 81	68 ± 15	58 ± 15	160 ± 71	341 ± 69	222 ± 45
MK-2048	42 ± 5	21 ± 3	365 ± 45	42 ± 3	26 ± 8	171 ± 27	97 ± 29	122 ± 31
RDS 1997	90 ± 24	66 ± 18	352 ± 49	150 ± 32	87 ± 12	245 ± 60	500 ± 58	363 ± 95
RDS 2197	495 ± 76	347 ± 42	1757 ± 362	395 ± 48	260 ± 91	622 ± 164	1021 ± 186	822 ± 180

^*The IN-DNA complexes were assembled with IN (20 nM) and 5′-³²P end-labeled 1.6 kb U5 substrate (0.5 nM) at 14°C for 15 min. Increasing concentrations of inhibitor along with the supercoiled DNA (1.5 nM) were added and strand transfer was carried out for 2 h at 37°C. In the reactions with N155H and Q148H IN, 30 nM of protein was added and strand transfer was carried out for 3 h at 37°C. The samples were deproteinized and subjected to 0.7% agarose gel electrophoresis. The quantity of each type of product (FS, D-D and CHS) was determined by Image-Quant 5.2 and the inhibition of each product was calculated. The IC₅₀ (nM) for each DNA product with each inhibitor was determined from at least three independent experiments.