Tumor-targeted unimer aggregation |
Temperature-sensitive ELP: (VPGXG)150* X=V5G3A2 and Temperature-insensitive ELP: (VPGXG)160 X=V1G7A8
|
Lysine residue for rhodamine conjugation and visualization of tumor accumulation in vivo
|
[74, 75] |
14C labeling for autoradiography of tumor accumulation in vivo
|
[26] |
Lysine residue for Alexa Fluor 488/Alexa Fluor 546 conjugation and visualization of tumor accumulation by thermal cycling in vivo
|
[76] |
Lysine residue for fluorescein conjugation and quantification of intracellular uptake in vitro
|
[77] |
Penetratin CPP for enhanced intracellular delivery of H1 peptide drug |
[79] |
Bac CPP for enhanced intracellular delivery of H1 (*n=130 for in vitro applications [80]) or p21 peptide drug |
[80, 81, 85, 86] |
TAT CPP for enhanced intracellular delivery of L12 peptide drug |
[82] |
SynB1 CPP for enhanced intracellular delivery of GRG peptide drug |
[83] |
TAT CPP for enhanced intracellular delivery of doxorubicin conjugated to cysteine residue with enzyme-cleavable peptide linker |
[46, 87] |
SynB1 CPP for enhanced intracellular delivery of paclitaxel or doxorubicin conjugated to cysteine residue(s) with acid-cleavable hydrazone linker |
[88–90] |
Tumor-targeted unimer-to-micelle transition |
(VPGXG)96 [X=V1A8G7]-(VPGVG)60
|
NGR at hydrophilic terminus for temperature-triggered multivalent targeting of CD13 receptor |
[47] |
(VPGXG)64 [X=V1A8G7]-(VPGVG)90
|
RGD at hydrophilic terminus for temperature-triggered multivalent targeting of αvβ3 integrin |
[91] |
(VPGXG)96 [X=V1A8G7]-(VPGVG)90
|
Fn3 at hydrophilic terminus for temperature-triggered multivalent targeting of αvβ3 integrin |
[92] |
(VPGVG)40-(VPGXG)60 X=A1G1
|
Arg5 or Arg8 CPP at hydrophilic terminus for temperature-triggered non-specific cellular uptake and controlled delivery of pro-apoptotic BH3 peptide drug |
[93, 94] |
Tumor-targeted micelle aggregation |
(VPGXG)150 or 160 X=AaVb where a:b=1:0, 14:1, 9:1, or 4:1 |
C(GGC)7 for conjugation of doxorubicin with acid-cleavable hydrazone linker |
[95] |