Table 1.
Select antimicrobial peptides with potent activity against MDR pathogens
| Peptide | Sequence | Development phase | Description |
|---|---|---|---|
| Human LL-37 | LLGDFFRKSKEKIGKEFKRIVQRIKDFLRNLVPRTES | From human leucocytes, kills bacteria through pore formation and possesses immunomodulation activities. | |
| SAAP-148 (de Breij et al., 2018) | LKRVWKRVFKLLKRYWRQLKKPVR | Preclinical | LL-37 derivative, shows potent bactericidal activity through membrane permeabilization and wound healing activity. |
| Cathelicidin-BF (Wang et al., 2008) | KFFRKLKKSVKKRAKEFFKKPRVIGVSIPF | Lysine-phenylalanine-rich peptide from snake venom. Shows potent efficacy against fungal and bacterial strains including MDR pathogens. Low hemolytic activity. | |
| D-OH-CATH30 (Zhao et al., 2018) | KFFKKLKNSVKKRAKKFFKKPRVIGVSIPF | Preclinical | Cathelicidin from snake venom, rapidly kills MDR gram-positive and gram-negative pathogens, with low hemolytic activity and in vivo toxicity. |
| Indolicidin (Falla et al., 1996) | ILPWKWPWWPWRR | III | Isolated from bovine leucocytes, shows potent bactericidal activity through pore formation. |
| Omiganan (Melo & Castanho, 2007) | ILRWPWWPWRRK-NH2 | III | Indolicidin derivative, broad-spectrum antimicrobial activity, therapeutic agent against acne and catheter related infections. |
| Ci-MAM-A24 (Fedders et al., 2010) | WRSLGRTLLRLSHALKPLARRSGW-NH2 | Preclinical | Isolated from Ciona intestinalis, shows potent bactericidal activity against MRSA, VRE, and MDR P. aeruginosa through pore formation. |
| Pexiganan (Ge et al., 1999) | GIGKFLKKAKKFGKAFVKILKK-NH2 | III | Magainin analog, phase III clinical trials for treatment of bacterial infections and diabetic foot ulcers. Potent antimicrobial activity. |
| S-thanatin (Wu et al., 2011) | GSKKPVPIIYCNRRSGKCQRM | Preclinical | Thanatin derivative, shows improved antimicrobial activity with reduced hemolytic activity. Potently inhibits gram-negative growth in vitro and in vivo and alleviates sepsis in mice. |
| AA139 (van der Weide et al., 2019) | GFCWYVCARRNGARVCYRRCN | Preclinical | Analog of arenicin-3 with β-hairpin structure, exhibits potent microbicidal activity against MDR gram-negative pathogens, and excellent candidate for in vivo application. |
| SET-M33 (Van De Weide et al., 2019) | KKIRVRLSA)4K2KβΑ-ΟΗ | Preclinical | Synthetic tetra-branched peptide with potent microbicidal activity against MDR bacteria and in vivo therapeutic potential. Currently under development for treatment of sepsis and lung infections (Brunetti et al., 2016a). |
| EC-hepcidin3 | APAKCTPYCYPTHDGVFCGVRCDFQ | Preclinical | Cysteine-rich peptide cloned from marine fish. Potent microbicidal activity against S. aureus and Pseudomonas spp. |
| Tachyplesin-1 (Ohta et al., 1992) | KWCFRVCYRG ICYRRCR | II | Cationic β-hairpin peptide from horseshoe crab. Potent microbicidal activity against gram-negative and gram-positive bacteria. Use limited by high cytotoxicity. |