|
Endogenous polyamine and aminoglycoside-mediated inhibition of anthrax lethal factor activity-comparison with other proteases-(Mean ± SEM or IC50 values) |
|
LF
|
Bot
|
MMP-9
|
Furin
|
|
Name
|
μM
|
IC50 μM
|
μM
|
μM
|
Neomycin B tris-sulfate
|
0.71 ± 0.04
|
92.5
|
>300
|
N/T
|
Sisomicin Sulfate
|
1.8
|
>300
|
>300
|
N/T
|
Spermine, diphosphate salt
|
0.9 ± 0.09
|
57
|
>300
|
N/T
|
Amikacin
|
23.3
|
>300
|
>300
|
N/T
|
Neamine (free base)
|
31.1 ± 5.6
|
175
|
>300
|
N/T
|
Spermidine
|
>100
|
76
|
N/T
|
N/T
|
Apramycin
|
111
|
>300
|
>300
|
N/T
|
Putrescine (1,4-diaminobutane)
|
>300
|
>300
|
>300
|
N/T
|
Ac-CRATKML-N
|
>300
|
3.5
|
N/T
|
N/T
|
GM 6001
|
7.2 ± 1.76
|
>300
|
0.002 ± 0.001
|
N/T
|
H-RRRRRR-OH
|
0.24
|
N/T*
|
N/T
|
0.06
|
Ac-RRRRRR-OH
|
0.29 ± 0.04
|
N/T
|
N/T
|
0.05
|
Ac-RRRRRR-NH2
|
0.12
|
N/T
|
N/T
|
N/T
|
H-(D-Arg)-(D-Arg)-(D-Arg)-(D-Arg)-(D-Arg)-(D-Arg)-NH2
|
0.04 ± 0.02
|
N/T
|
N/T
|
0.06
|
H-R(NO2)R(NO2)
|
>300
|
N/T
|
N/T
|
N/T
|
Neomycin B hexaguanyl hexatrifluoroacetate salt
|
0.03
|
14
|
>170
|
1.5
|
Tetraguanyl neamine, free base
|
0.3
|
N/T
|
N/T
|
N/T
|
|
|
*N/T = not tested |
Goldman et al. BMC Pharmacology 2006 6:8 doi:10.1186/1471-2210-6-8
|