Table 1:
Properties of cargoes that have previously been delivered by pHLIP
| Cargo | LogP/LogD | Molecular Weight |
Reference |
|---|---|---|---|
| Cytotoxic Agents | |||
| Amanitin (SPDP linker) | −0.2 | 1007.1 | Moshnikova et al., 2013 (Ref 17) |
| Amanitin (Lc-SMPT linker) | 0.2 | 1196.36 | Moshnikova et al., 2013 (Ref 17) |
| Phalloidin, TAMRA (via separate linkers) | −1.5, 1.58* | 1305.49 | An et al., 2010 (Ref 16) |
| Phalloidin-TRITC | −0.05 | 1305.57 | Reshetnyak et al., 2006 (Ref 24) |
| Monomethyl Auristatin E | 2.2 | 692.96 | Burns et al., 2015 (Ref 21) |
| Monomethyl Auristatin F | 0.7 | 806.07 | Burns et al., 2017 (Ref 20) |
| Peptide Nucleic Acids | |||
| TAMRA-oo-CATAGTATAAGT-o-Cys | 4055.08 | Reshetnyak et al., 2006 (Ref 24) | |
| ooo-TCTGTAACTC-ooo-Cys-Cy3 (Anti-HOTAIR PNA) | 3635.24 | Özeş et al., 2017 (Ref 23) | |
| TAMRA-ooo-ACCCCTATCACAATTA GCATTAA-ooo-Cys (Anti-miR-155 PNA) | 7036.94 | Cheng et al., 2015 (Ref 22) | |
| Fluorophores | |||
| Dansyl | −1.43* | 354.44 | Reshetnyak et al., 2006 (Ref 24) |
| TAMRA | 1.58* | 489.59 | Karabadzhak et al., 2014 (Ref 15) |
| 2x TAMRA (via separate linkers) | 1.58*, 1.58* | 979.18 | Karabadzhak et al., 2014 (Ref 15) |
| TAMRA, QSY-9 (via separate linkers) | 1.58*, 0.98* | 1367.63 | Karabadzhak et al., 2014 (Ref 15) |
| Nitrobenzoxadiazole (NBD) | −0.83 | 293.3 | Thevenin et al., 2009 (Ref 26) |
| Cyclic Peptides | |||
| NBD-cyclic(Ser)4 | −2.68 | 742.7 | Thevenin et al., 2009 (Ref 26) |
| NBD-cyclic(Asp)4 | −2.87 | 854.8 | Thevenin et al., 2009 (Ref 26) |
*
LogD7.4 values calculated from Chemicalize chemical properties calculator (ChemAxon)
**
Antimicrobial peptides (Ref 19) are excluded from this table since measurements of lactate dehydrogenase release from cells treated with the antimicrobial peptides suggested that the antimicrobial peptides can disrupt the cell membrane at low pH. Therefore, the mechanism of pHLIP delivery was likely different for these peptides.