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Table 1 Resistance of Purified RTs to DNA and RNA Aptamers. Assays were performed as described previously [34]. Data represent mean ± SEM of three independent experiments.

From: HIV-1 reverse transcriptase mutations that confer decreased in vitro susceptibility to anti-RT DNA aptamer RT1t49 confer cross resistance to other anti-RT aptamers but not to standard RT inhibitors

 

WT

N255D

N265D

Dbl

aTRTI

bIC50, nM

cRatio

IC50, nM

Ratio

IC50, nM

Ratio

IC50, nM

Ratio

RT1t49d

RT26f

1.6

4.0 ± 0.05

1

1

7.9

7.6 ± 0.1

4.9

1.9

17.4

11.2 ± 0.1

10.9

2.8

245

24 ± 0.1

153

6

RT4f

38 ± 1.2

1

80 ± 3.7

2.1

1015 ± 16

27

> 1000

> 27e

RT6f

19.6 ± 0.1

1

26 ± 0.7

1.3

87 ± 2.2

4.4

142 ± 3.4

7.2

RT8f

19.5 ± 0.3

1

2.0 ± 0.02

0.1

17.2 ± 0.2

0.9

3.0 ± 0.02

0.1

RT10f

82 ± 2.5

1

57 ± 1.4

0.7

923 ± 8.9

11

509 ± 4.2

6

Rknot 1.1f

1.4 ± 0.02

1

0.8 ± 0.01

0.8

2.5 ± 0.04

2

4.5 ± 0.08

4

  1. aDescribed in references 23 and 25.
  2. bConcentration of aptamer at which 50% of the activity was inhibited.
  3. cFold increase or decrease over the IC50 for the wild type (WT) RT.
  4. dReproduced from Fisher et al. [25] eAt the highest concentration of aptamer tested (1000 nM), the Dbl mutant retained 70% of its activity, thus the actual IC50 would be much higher.
  5. fAptamer sequences: RT1t49: 5' ATCCGCCTGATTAGCGATACTCAGAAGGATAAACTGTCCAGAACTTGGA3'
  6. RT26: 5'ATCCGCCTGATTAGCGATACTTACGTGAGCGTGCTGTCCCCTAAAGGTGATACGTCACTTGAGCAAAATC ACCTGCAGGGG3'
  7. RT4:5'ATCCGCCTGATTAGCGATACTTTAGCAAAGTTGAAGCCGGACTAACAAGCTCTACGACTTGAGCAAAATCA CCTGCAGGGG3'
  8. RT6: 5'ATCCGCCTGATTAGCGATACTCAGGCGTTAGGGAAGGGCGTCGAAAGCAGGGTGGGACTTGAGCAAAATCA CCTGAGGGG3'
  9. RT8:5'ATCCGCCTGATTAGCGATACTAGCCAGTCAAGTTAATGGGTGCCATGCAGAAGCAACTTGAGCAAAATCA CCTGCAGGGG3'
  10. RT10:5'ATCCGCCTGATTAGCGATACTTATTTGCCCCTGCAGGCCGCAGGAGTGCAGCAGTACTTGAGCAAAATCA CCTGCAGGGG3'
  11. Rknot 1.1: 5'GGGAGAUUCCGUUUUCAGUCGGGAAAAACUGAA3'