Cationic polyamines inhibit anthrax lethal factor protease

BMC Pharmacology

Table 1 Endogenous polyamine and aminoglycoside-mediated inhibition of anthrax lethal factor activity-comparison with other proteases-(Mean ± SEM $K_{i}^{a p p}$ or IC₅₀ values)

	LF	Bot	MMP-9	Furin
Name	$K_{i}^{a p p}$ μM	IC₅₀ μM	$K_{i}^{a p p}$ μM	$K_{i}^{a p p}$ 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