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. 2020 Aug 26;1(4):192–203. doi: 10.1039/d0cb00114g

Overview of activatable cell-penetrating peptides (ACPPs) triggered through conformational changes. Amino acids are indicated via the single letter code. PEG = poly(ethylene) glycol; CPT = camptothecin; PTX = paclitaxel; probe = IR-probe; SC= side chain; LK = leucine and lysine rich CPP; trans-Ab = trans-azobenzene; Tamra = Tamra red dye; RhoB = rhodamineB dye; yAhx = O-aminohexylated d-tyrosine; FITC = fluorescein.

Premise CPP Inhibiting factor Cargo Trigger Ref.
pH sensitive conformational changes
1 graphic file with name d0cb00114g-u19.jpg Tat PEG DOX loaded micelle pH drop 63
2 graphic file with name d0cb00114g-u20.jpg TH H side chain charge CPT pH drop 64
LH CPT 66
TH PTX probe 65
3 graphic file with name d0cb00114g-u21.jpg K97 SC modi-fications with imi-dazole or carboxylic acids pH drop to 6.0 67
Light sensitive conformational changes
4 graphic file with name d0cb00114g-u22.jpg LK trans-Ab Tamra 365 nm, 5 min, 8 mW cm−2 68
5 graphic file with name d0cb00114g-u23.jpg R9 E9 RhoB λ = 488, 1–1.5 μW, ∼60 ms μm−2 69
6 graphic file with name d0cb00114g-u24.jpg RRF-yAhxP-FRR Circular structure FITC λ = 590 nm 70