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Table 2 Inhibitory properties of AAR029b and KR13 against HIV-1 pseudotyped with wild type and resistance Env variants

From: Altered Env conformational dynamics as a mechanism of resistance to peptide-triazole HIV-1 inactivators

 

AAR029b IC50 (nM) (fold-change relative to WT)

KR13 IC50 (nM) (fold-change relative to WT)

NL4-3

HxBc2

NL4-3

HxBc2

Wild type

250 ± 90 (1)

230 ± 130 (1)

2.0 ± 0.56 (1)

1.2 ± 0.17 (1)

S143N

380 ± 20 (1.5)

540 ± 50 (2.3)

3.5 ± 1.5 (1.8)

1.4 ± 0.24 (1.2)

V255I

7.6 × 104 ± 1.6 × 104 (300)

1.4 × 104 ± 810 (50)

120 ± 18 (62)

91 ± 23 (77)

V255T

9.1 × 104 ± 3.9 × 104 (370)

1.5 × 104 ± 1.5 × 104 (62)

360 ± 35 (180)

330 ± 70 (280)

V255I/S143N

2.0 × 105 ± 2.6 × 104 (790)

3.4 × 104 ± 2.9 × 104 (150)

3700 ± 560 (1900)

4600 ± 510 (3900)

V255T/S143N

2.4 × 105 ± 2.7 × 104 (980)

3.7 × 104 ± 1.8 × 104 (160)

6200 ± 320 (3100)

7100 ± 1100 (6000)