Identification of a novel small-molecule inhibitor of the HIV-1 reverse transcriptase activity with a non-nucleoside mode of action

Table 2 Antiviral effect of BPPT on clinically derived multi-drug resistant variants

Virus^a	Major NNRTI RAMs	Major NRTI RAMs	EC₅₀ (μM)^b (Fold change, FC)^c
Virus^a	Major NNRTI RAMs	Major NRTI RAMs	BPPT	EFV	NVP	AZT
WT			0.06 ± 0.01 (1.00)	0.001 ± 0.00 (1.00)	0.08 ± 0.02 (1.00)	0.29 ± 0.06 (1.00)
7396		41L/67N/69N/70R/215F	0.09 ± 0.01 (1.34)	0.001 ± 0.00 (1.00)	0.35 ± 0.07 (4.38)	3.83 ± 1.21 (13.21)
7406	190C	41L/69S*/74 V/184 V/210W/215Y	0.35 ± 0.04 (5.41)	1.09 ± 0.24 (1,090.00)	> 50 (> 625)	15.13 ± 2.16 (52.17)
7407	103N	70R/115F	19.69 ± 1.6 (328.16)	0.35 ± 0.03 (350.00)	> 50 (> 625)	> 50 (> 172)
12,227	101P/103N	41L/215Y	> 50 (> 833)	1.94 ± 0.23 (1,940.00)	> 50 (> 625)	1.00 ± 0.13 (3.48)
12,231	103N/179F/181C	41L/215F	> 50 (> 833)	0.18 ± 0.22 (180.00)	> 50 (> 625)	0.63 ± 0.19 (2.17)
12,241	101E/138G/190S		4.57 ± 2.3 (71. 41)	2.16 ± 0.51 (2,160.00)	> 50 (> 625)	0.08 ± 0.03 (0.28)
12,243	100I/179D/230L	41L/67G/74I	> 50 (> 833)	10.82 ± 0.37 (10,820.00)	21.45 ± 2.21 (268.13)	0.29 ± 0.01 (1.00)

^aCatalog number provided by the NIH HIV Reagent Program
^bThe half maximal effective concentration
^cThe fold-change (FC) values were calculated by dividing the drug-resistant mutant HIV-1 EC₅₀ by the wild type EC₅₀
^*Indicates the insertion mutation

ISSN: 1743-422X