Table 4.
Antimicrobial Activity of Antisense Conjugates
| |
|
MIC (μM)*Pseudomonas aeruginosa |
||
|---|---|---|---|---|
| PA01 | PA14 | LESB58 | ||
| Anti-acpP peptide-PNA | ||||
| 3969 | H-(R-Ahx)6-(βala)-ctc ata cct tg-NH2 | 2 | 2 | 2 |
| 3984 | H-(R-Ahx-R)4-Ahx-(βala)-ctc ata cct tg-NH2 | 2 | 2 | 2 |
| Mismatch peptide-PNA | ||||
| 3993 | H-(R-Ahx)6-(βala)-ctc cta cat tg-NH2 | 20 | >10 | 10 |
| 3985 | H-(R-Ahx-R)4-Ahx-(βala)-ctc cta cat tg-NH2 | 5 | >4 | >2 |
| Anti-ftsZ peptide-PNA | ||||
| 4071 | H-(R-Ahx)6-(βala)-cca gtt caa a-NH2 | 2 | 2 | 1.5 |
| 4073 | H-(R-Ahx-R)4-Ahx-(βala)-cca gtt caa a-NH2 | 1 | 2 | .6 |
| Mismatch peptide-PNA | ||||
| 4070 | H-(R-Ahx)6-(βala)-cta gtc caa a-NH2 | 12 | >10 | >1.5 |
| 4072 | H-(R-Ahx-R)4-Ahx-(βala)-cta gtc caa a-NH2 | 5 | >4 | .6 |
| Antibiotic Controls | ||||
| Gentamicin | .3 | .3 | 1 | |
| Ciprofloxacin | .3 | .3 | 2 | |
| Ofloxacin | 2 | 2 | >6 | |
| Ceftazidime | 2 | 3 | >10 | |
MIC values are reported as the concentration resulting in an OD value <0.15 after 20 hours incubation at 37°C (PA14 growth inhibition data are shown in Figure S1).
Ahx, 6-aminohexanoic acid; βala, β-alanine.