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Table 3 Steady-state kinetic parameters of nucleotide incorporation catalyzed by wild-type and mutant RTs, and inhibition constants for AZTTP and tenofovir-DP

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

RTs

Nucleotide

kcat(min-1)

Km(nM)

kcat/Km(μM-1 min-1)

Ki(AZTTP) (μM)

Ki(Tenofovir-DP) (μM)

WT

dTTP

3.14 ± 0.55

108.3 ± 12.9

30.9 ± 4.7

2.10 ± 0.38

 
 

dATP

3.87 ± 0.99

25.8 ± 6.7

172.0 ± 27.7

 

3.59 ± 0.26

M41L/L210W/T215Y

dTTP

3.53 ± 0.09

117.4 ± 21.9

30.8 ± 6.0

2.18 ± 0.17

 
 

dATP

5.70 ± 0.87

32.1 ± 9.6

243.9 ± 51.1

 

2.63 ± 0.64

M41L/L210W/T215Y/R284K

dTTP

5.66 ± 0.23

184.5 ± 6.1

30.7 ± 2.3

2.32 ± 0.74

 
 

dATP

10.09 ± 1.47

15.9 ± 2.5

639.6 ± 101.2

 

2.54 ± 0.55

  1. D38/25PGA and D38T/25PGA were used as substrates for dTTP and dATP incorporation, respectively. Reported values are the averages ± standard deviations, obtained from at least three independent experiments.
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Retrovirology

ISSN: 1742-4690

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