Table 3.
Representative host defense peptides (HDPs) and mimics.
| Compound | Sequence/Structure | Structural Motif | Activity | Reference/Database |
|---|---|---|---|---|
| Hst5 (histatin) |
|
α-helix | Internalized after binding to fungal cell wall. Induces oxidative stress, affects ionic balance and mitochondrial function | Chemspider: 17289075 [33] |
| LL-37 (human cathelicidin) |
|
α-helix | Disrupts fungal membrane and modulates host responses in vitro | PDB: 2K6O [20,37,38,39,40,41,42,43,44,45] |
| Protegrin (porcine cathelicidin) |
|
Cysteine-rich β-sheet, two disulfide bridges | Fungicidal in vitro, cytotoxic and hemolytic to mammalian cells | PDB: 1PG1 [46] |
| Indolicidin (bovine cathelicidin) |
|
Extended chain containing five tryptophans | Antifungal activity, toxic in mammals | PDB:1G89 [47] |
| HNP-1 (α-defensin) |
|
Tri-disulfide stabilized β-sheet dominated monomers that from non-covalent dimers | Fungicidal in vitro, modulates host responses in vivo | PDBE: 3hj2 [48,49,50,51] |
| HBD-2 (β-defensin) |
|
Tri-disulfide stabilized monomers that from non-covalent dimers | Fungicidal in vitro, modulates host responses in vivo | PDB:1FD4 [52,53,54,55] |
| IDR-1018 (bactenecin derivative) |
|
α-helix | Modulates cytokines in bone marrow-derived macrophages stimulated with heat-killed C. albicans | [56,57] |
| hLF1-11 (human lactoferrin cryptide) |
|
First 11 N-terminal amino acids of the human lactoferrin loop peptide | Fungicidal in vitro, inhibits C. albicans filamentation and reduces TNFα and IL-6 in vivo | [58,59] |
| RTD-1 (θ-defensin) |
|
Tri-disulfide β-stranded macrocycle | Permeabilizes fungal cells and induces oxidative stress in vitro, enhances fungal clearance in vivo | PDB: 2LYF [9,60,61,62,63,64,65] |
| AB103; Raltecimod (CD-28 mimetic) |
|
D-Ala1, D-Ala10 CD-28 mimetic | Modulates host responses in vivo | Chemspider: 58828035 [66,67] |
| Zadaxin |
|
α-helix; synthetic version of human peptide thymosin α 1 | Modulates host responses in vivo | PDB: 2L9I [68,69,70] |
| C4; Compound 4 (mPE-derived) |
|
Peptidomimetic derived from the magainin-inspired mPE | Disrupt fungal cell membrane in vitro, fungicidal in oral and systemic candidiasis in vivo | [71,72] |