Table 1 Selective inhibition of influenza A group-1 sialidase by locking open the 150-loop.

From: Novel sialic acid derivatives lock open the 150-loop of an influenza A virus group-1 sialidase

Sialidase type

K i (μM) *

 

5

6

4

1

N1 (A/HongKong/156/97 (H5N1))

222±17

7.3±0.8

0.97±0.15

0.17±0.08×10−3

N1 (A/Paris/2590/2009 (H1N1 pandemic))

153±18

1.7±0.2

0.67±0.08

0.13±0.01×10−3

N2 (A/Paris/908/97 (H3N2))

3629±2130

219±30

1.24±0.23

0.56±0.16×10−3

N1 (A/HongKong/156/97 (H5N1) H274Y)

459±92

11±0.9

1.43±0.17

0.38±0.14×10−3

N1 (A/Paris/2590/2009 (H1N1 pandemic) H274Y)

232±15

2.9±0.1

0.91±0.05

0.23±0.04×10−3

N1 (A/HongKong/156/97 (H5N1) N294S)

980±50

25±3.1

3.90±0.5

0.71±0.04×10−3

N1 (A/HongKong/156/97 (H5N1) Q136K)

16.8±2.5

2.6±0.4

1.37±0.15

13.6±1.3×10−3

  1. Inhibition of wild-type N1, H274Y, N294S and Q136 K mutant N1 sialidases, and an N2 sialidase by 5 and 6 compared with parent template 4 and zanamivir (1).
  2. *Results are given as means ± s.d. (see Methods—Inhibition Assays for details).
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