Raltegravir, elvitegravir, and metoogravir: the birth of

Retrovirology

Table 1 Effect of single mutations on IN sensitivity to clinically tested inhibitors.

Mutation	S-1360	L870, 810	MK-0518	GS-9137	GSK-364735
T66I	++	+	++	+++	+
L68V			+	+
L68I			+	+
V72I		+		++
L74M	++++	+	+	++
E92Q	++	+	++	+++	++
Q95K		++		++
F121Y	+++	++	++	+++	+++
T124A	+				+
T125K		+	+	+
E138K	+	+	+	+
G140S	++		+	++
P145S	++				+
Q146R	++	+		+++	+
S147G		++	+	++
Q148H	+++		+++	++
Q148R	++++		+++	+++++	++++
Q148K	++++		+++	++++	+++++
V15II		+++	+	++
S153Y	++		+	++	+
N155H	++		+++	+++
N155S	+++	++	++		+++
E157Q				++
R263K				++
E92Q/N155H			++++	++++
F121Y/T125K			++	++++
G140S/Q148H			+++++	+++++
V72I/F121Y/T125K/V151I		+++++		+++++

Fold change in potency compared to wild type: + <2, ++ 2–10, +++ 11–50, ++++ 51–100, +++++ >100

ISSN: 1742-4690