Synthesis and activity of generated peptides.
| cpda | Sequenceb | P. aeruginosa c (μg mL−1) | A. baumannii c (μg mL−1) | MRSAc (μg mL−1) | MHCd (μg mL−1) | E. coli c (μg mL−1) |
|---|---|---|---|---|---|---|
| Gram-neg. active, non-hemolytic: | ||||||
| GN1 | AKRIRKLIKKIFKKI | 4 | 4 | 16 | >2000 | 8 |
| GN2 | RRWKWRRKIKKWL | 8 | 8 | 4 | 1000 | 16 |
| GN3 | IDKWKAAFKKIKNLF | 8–16 | 2 | 8 | 500 | 8–16 |
| GN4 | LNALKKVFQKIRQGL | 32 | 16 | >64 | >2000 | 4 |
| GN5 | KFFRKLKKLVKK | 16 | >64 | 64 | >2000 | 64 |
| GN6 | RLRKKWRKLKKLL | 32 | 16–32 | 64 | 2000 | 16–32 |
| Gram-neg. active, hemolytic: | ||||||
| GN7 | KRIRKWVRRILKKL | 4 | 4 | 4 | 250 | 16 |
| GN8 | LRKFWKKIRKFLKKI | 8 | 4 | 4 | 62.5 | 16 |
| GN9 | KRLWKRIYRLLKK | 8 | 8 | 8 | 250 | 4–8 |
| Gram-neg. inactive: | ||||||
| GN10 | IRRIRKKIKKIFKKI | 32 | 32 | 64 | >2000 | 16 |
| GN11 | LRKARRLLKKLRARL | >64 | 32 | 32 | >2000 | 32 |
| GN12 | GNWRKIVHKIKKAG | 32 | >64 | >64 | >2000 | 16 |
| GN13 | AGRLQKVFKVIAK | 64 | >64 | >64 | >2000 | 32 |
| GN14 | IHKLAKLAKNVL | >64 | >64 | >64 | >2000 | 32 |
| Gram-pos. active, non-hemolytic: | ||||||
| GP1 | FLKAVKKLIPSLF | 16 | 8–16 | 16 | 2000 | 8 |
| GP2 | RWRWPILGRILR | 8 | 16 | 16 | 500 | 16 |
| Gram-pos. active, hemolytic: | ||||||
| GP3 | FLHSIGKAIGRLLR | 16 | 16 | 8 | 250 | 8 |
| Gram-pos. inactive: | ||||||
| GP4 | GIGAVLNVAKKLL | 64 | 32 | 32 | >2000 | 16 |
| GP5 | KVARFLKKFFR | 64 | 32–64 | 32 | >2000 | 4 |
| GP6 | LKKLWKRIIKVGR | 32 | 16–32 | 64 | >2000 | 8 |
| GP7 | ARKWRKFLKKI | >64 | 64 | 64 | >2000 | 32–64 |
| GP8 | GRIKRIRKIIHKY | 8 | 32 | >64 | >2000 | 32 |
| GP9 | ARKKWRKRLKKLKI | 32–64 | >64 | >64 | >2000 | 32–64 |
| GP10 | AKKVVKKIYKRFQK | >64 | 64 | >64 | >2000 | 64 |
| GP11 | ARKFRRLVKKLR | >64 | >64 | >64 | >2000 | 64 |
| GP12 | LRKARRLVKKLA | >64 | >64 | >64 | >2000 | >64 |
| GP13 | KRLWKIRQRIAK | >64 | >64 | >64 | >2000 | 32 |
| GP14 | LNALKKVFQKIH | >64 | >64 | >64 | >2000 | >64 |
Compounds labeled as GN were obtained from the P. aeruginosa/A. baumannii model, compounds labeled as GP were obtained from the S. aureus model; in both sets, compounds were ordered according to their activity and hemolysis profile; GN2, 6, 9, 10 and GP2, 6, 9, 11 were obtained using the second selection strategy.
One-letter code for amino acids. All peptides are carboxamides (–CONH2) at the C terminus.
MIC was determined after incubation for 16–20 h at 37 °C.
MHC was measured on human red blood cells in 10 mM phosphate buffer saline, pH 7.4, 25 °C. 0.1% Triton X-100 was used as a positive control. Cells in italic denote MIC <32 μg mL−1 towards the bacterial strains used for the design (P. aeruginosa/A. baumannii for GN and S. aureus for GP) and MHC ≥500 μg mL−1.