TABLE 1.
Drug | Jurkat cells |
MT-4 cells |
MDM cells |
CD4+ T cells |
||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|
EC50 (μM) |
FC | EC50 (μM) |
FC | EC50 (μM) |
FC | EC50 (μM) |
FC | |||||
−Vpx | +Vpx | −Vpx | +Vpx | −Vpx | +Vpx | −Vpx | +Vpx | |||||
AZT | 0.023 | 0.034 | 1 | 0.017 | 0.082 | 5 | 0.015 | 0.389 | 26 | 0.068 | 4.607 | 67 |
d4T | 5.000 | 4.300 | 1 | 0.962 | 2.376 | 2 | 0.300 | 2.009 | 7 | 1.245 | 1/>5b | 1/>4b |
3TC | 0.164 | 0.156 | 1 | 0.816 | 0.758 | 1 | 0.081 | 0.022 | 1 | 0.524 | 0.372 | 1 |
ddC | 0.052 | 0.059 | 1 | 0.292 | 0.308 | 1 | 0.113 | 0.042 | 1 | 0.115 | 0.081 | 1 |
ABC | 0.053 | 0.059 | 1 | 0.001 | 0.001 | 1 | 0.003 | 0.003 | 1 | 0.015 | 0.009 | 1 |
TFV | 11.598 | 10.858 | 1 | 2.877 | 2.162 | 1 | 6.114 | 5.599 | 1 | 1.949 | 6.822 | 3 |
ddI | 2.045 | 2.572 | 1 | 1.470 | 2.692 | 2 | 1.805 | 2.251 | 1 | 0.402 | 0.481 | 1 |
NVP | 0.090 | 0.095 | 1 | 0.237 | 0.295 | 1 | 0.274 | 0.361 | 1 | 1.017 | 1.256 | 1 |
EFV | 0.038 | 0.072 | 2 | 0.047 | 0.055 | 1 | 0.071 | 0.071 | 1 | 0.068 | 0.091 | 1 |
RAL | 0.003 | 0.007 | 3 | 0.005 | 0.004 | 1 | 0.022 | 0.031 | 1 | 0.017 | 0.015 | 1 |
NRTI are AZT, d4T, 3TC, ddC, TFV, ddI, and ABC; NNRTI are NVP and EFV; the integrase inhibitor is RAL. EC50 values were calculated in T cell lines negative or expressing low levels of SAMHD1 (Jurkat and MT4) and primary cells MDM and CD4+ T cells. EC50, effective concentration required to block HIV-1 replication by 50%; FC, fold change or ratio of the EC50 with Vpx (+) and the EC50 without Vpx (−). Results are the means from at least two independent experiments done in triplicates.
EC50 > 5 μM in 2/5 donors, which resulted in a fold change of <4.