Comparison of efficiency of WT pol γ and RT incorporation of nucleoside analogs, FDA-approved NRTIs, and NRTIs under development
Discrimination (efficiencydNTP/efficiencyanalog) is shown, rather than incorporation efficiency, to minimize the rate constant variations associated with different primer/template substrates.
| dNTP Analog | Discrimination | Reference | |
|---|---|---|---|
| WT pol γ | RT | ||
| ddC-TP | 2.9 | 10 | Feng and Anderson, 1999; Feng et al., 2001; Ray et al., 2003 |
| ddA-TP | 4.0 | 5 | Johnson et al., 2001 |
| d4T-TP | 7.4 | 0.56 | Vaccaro et al., 2000; Johnson et al., 2001 |
| KP1212-TP | 26 | 14 | Murakami et al., 2005 |
| FLT-TP | 35 | 4.2 | Current study |
| (−)-3TC-TP | 2900 | 40 | Feng and Anderson, 1999; Feng et al., 2001; Ray et al., 2003 |
| EFdA-TP | 4300 | N.D.a | Sohl et al., 2012 |
| Ed4T-TP | 6200 | 0.51 | Current study |
| PMPApp | 11,400 | 6.1 | Johnson et al., 2001 |
| AZT-TP | 37,000 | 2.7 | Vaccaro and Anderson, 1998; Johnson et al., 2001 |
| (−)-FTC-TP | 290,000 | 16 | Feng et al., 2004 |
| CBV-TP | 900,000 | 34 | Johnson et al., 2001 |
N.D., no data; KP1212, 5-aza-5,6-dihydro-2'-deoxycytidine; 3TC, lamivudine; PMPApp, tenofovir diphosphate; FTC, emtricitabine; CBV, carbovir.
↵a Steady-state studies indicated an efficiency of 0.5 (Michailidis et al., 2009).