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Table 2 Susceptibility of HIV-1 constructs to nucleoside RT inhibitors

From: Clinical, virological and biochemical evidence supporting the association of HIV-1 reverse transcriptase polymorphism R284K and thymidine analogue resistance mutations M41L, L210W and T215Y in patients failing tenofovir/emtricitabine therapy

 

IC50(nM)

RTs

AZT

d4T

Tenofovira

Emtricitabine

WT

2.3 ± 1.5

276.0 ± 90.5

6.7 ± 2.2

144.3 ± 69.9

R284K

1.7 ± 1.1 (0.7)

130.0 ± 24.8 (0.5)

12.1 ± 5.3 (1.8)

104.2 ± 81.5 (0.7)

M41L/L210W/T215Y

11.7 ± 1.1 (5.1)

217.0 ± 75.5 (0.8)

11.0 ± 4.6 (1.6)

226.9 ± 113.2 (1.6)

M41L/L210W/T215Y/R284K

13.3 ± 1.5 (5.8)

287.3 ± 84.5 (1.0)

18.1 ± 4.4 (2.7)

294.7 ± 93.7 (2.0)

  1. The IC50 values represent averages ± standard deviations of at least three tests, with each one performed six times. The fold increase in IC50 relative to the wild-type HXB2 virus control carrying the RT sequence of BH10 is shown between parentheses.
  2. a Experiments were carried out with the water soluble diester prodrug tenofovir disoproxil fumarate.