Activatable cell-penetrating peptides (ACPPs) based on linkage of an inhibitory domain. Amino acids are indicated via the single letter code, in which d-amino acids are noted in lower case. Cy5 = cyanine5 red dye; PpIX = protoporphyrin IX; Dox = doxorubicin; PLK-1 = polo-like kinase 1; PSA = protease specific antigen; NE = neutrophil elastase; FITC = fluorescein; NA = not available; CPT = camptothecin; EGFR = epidermal growth factor; QDs = quantum dots.
CPP | Trigger | Ref. | ||||
---|---|---|---|---|---|---|
Enzyme sensitive linkers | ||||||
1 | PLGLAG | r9 | e6,8 | Cy5 | MMP-2 and -9 | 19 and 21 |
R9 | E8 | PpIX | 23 | |||
R9 | E9 | Dox | 24 | |||
Poly(M-block-K) | PEG | Dox | 25 | |||
2 | PVGLIG | R9 | (EGG)3 | CsA-LMNC | MMP-9 | 26 |
3 | PGFK | Tat | E6 | Dox | Cathepsin B | 28 |
4 | HSSKYQ | R8 | (DGG)4 | PLK-1 siRNA | PSA | 29 |
5 | RLQLK(Ac)L | r9 | e9 | Cy5 | NE | 32 |
6 | DPRSFL | r9 | e8 | Cy5 Rhodamine | Thrombin | 33 |
pH sensitive linkers | ||||||
7 | R8 | (ehG)4 | PLK-1 siRNA | pH < 6.8 | 37 | |
ROS sensitive linkers | ||||||
8 | R9 | E9 | FITC Cy5 | H2O2 | 43 | |
Light sensitive linkers | ||||||
9 | Tat | PEG | Liposomes loaded with Atto655 | λ = 254 nm, 2 min | 47 | |
10 | R7 | E7 | FITC CPT | λ = 365 nm, 10 min | 48 | |
11 | Penetratin | E4R4 | EGFR siRNA | λ = 740 nm, 30 min and pH < 6.4 | 53 | |
12 | R7 | E7 | QDs | Two-photon, λ = 740 nm, 3 h | 48 |