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. 2010 Jun 25;2(7):1347–1366. doi: 10.3390/v2071347

Table 2.

Characterized mutations within IN conferring resistance to RAL or EVG.

Mutations IN
Virus
Refs
3′-P ST Rce Selection RC
H51Y ++ EVG [76]
H51Y/E92Q/S147G + EVG [76]
H51Y/E92Q/S147G/E157Q ++ EVG [76]

T66A + ++ RAL/EVG ++ [63,77,78]
T66I +++* +++* 51–102X DKA/EVG ++* [29,38,7987]
T66I/E92Q EVG [85,86]

L74M +++ +++ 1X1,2 DKA/EVG [29,80,84,85,88]

E92Q +++* +++* 4–5X1,2 DKA/RAL/EVG ++ [66,76,78,88]
E92Q/S147G + EVG [76]
E92Q/N155H RAL ++* [72,89]

E138K/Q148HRK DKA/RAL ++ [72,87,90]

G140S +++* + 1X1,2 DKA/RAL ++ [61,71,78,8993]
G140A ++ + 2–3X1 RAL [71]
G140S/Q148H ++* +++* >50X1,2 RAL +++ [61,66,72,94]
G140S/Q148K ++ + 10–25X1 DKA/RAL ++ [71,72,90]
G140S/Q148R + >25X1 DKA/RAL ++ [56,72,87]
G140A/Q148H + >25X1 RAL + [71,72]
G140A/Q148K 2–3X1 RAL ++ [71,72]
G140A/Q148R + + >25X1 RAL ++ [71,72,95]
G140S/Q148H/S230N RAL +++ [89]

Y143R + ++ >50X1 RAL + [56,62,93,96]
Y143C + + >50X1 RAL + [62]
Y143R/G163R RAL ++ [89]

S147G + EVG [76]

Q148K +* 50X1* DKA/RAL/EVG + [28,29,71,72,87,90]
Q148R +* + 2–3X1 DKA/RAL/EVG ++ [71,72,78,8587,90,95,97]
Q148H +* 2–3X1,2 RAL ++* [61,71,72,78,89,93]
Q148H/N155H RAL + [89]
Q148K/G163R RAL [87]

N155H +++* +++* 5–10X1,2 DKA/RAL ++ [29,61,66,72,78,86,87,89,9395,97,98]

E157Q ++ RAL/EVG [76,99]

S230R +++ +++ DKA/EVG [80,85]

Rce: resistance expressed as fold change in IC50; RC: replication capacity.

Signs refer to activity compared to WT: − = 0–10%;

+

= 10–40%;

++

= 40–80%;

+++

= 80–100%;

no entry = not tested.

1

RAL,

2

EVG,

*

discordant data in literature (the highest value is presented).