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Table 2 Inhibitory activity of SC29EK and MT-SC29EK against T20-resistant HIV-1 variants a

From: Two M-T hook residues greatly improve the antiviral activity and resistance profile of the HIV-1 fusion inhibitor SC29EK

 

T20

SC29EK

MT-SC29EK

HIV-1NL4–3

IC50

n-foldb

IC50

n-fold

IC50

n-fold

WT

52.1 ± 8.5

1

1.8 ± 0.2

1

0.6 ± 0.1

1

I37T

552.2 ± 123.4

10.6

15.0 ± 0.3

8.3

0.8 ± 0.2

1.3

V38A

1842.6 ± 56.1

35.4

16.2 ± 1.9

9

0.6 ± 0.1

1

V38M

378.3 ± 41.7

7.3

15.1 ± 1.8

8.4

1.7 ± 0.0

2.8

Q40H

1321.5 ± 92.3

25.4

83.8 ± 10.8

46.6

0.8 ± 0.1

1.3

N43K

366.8 ± 47.4

7

>250

>138.9

7.2 ± 0.2

12

D36S/V38M

202.6 ± 12.6

3.9

11.7 ± 0.7

6.5

1.2 ± 0.0

2

I37T/N43K

>2250

>43

>250

>138.9

21.2 ± 4.4

35.3

V38A/N42T

>2250

>43

37.7 ± 6.4

20.9

0.6 ± 0.0

1

  1. aThe data were derived from the results of three independent experiments and expressed as means ± SD. bn-fold values are relative to the IC50 of the wild-type (WT) virus.