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Table 9.1 Enzyme-activated NIR-dye-labeled macromolecular imaging probes and their use for optical imaging in vivo
Fluorophore,
mol/mol carrier
macromolecule Animal model
Macromolecule,
type
Target/background
ratio a
Imaging
method
Specificity
Reference
PGC b
PE c
Cathepsin
B/H/L/S
Cy5.5, 11
Murine breast
adenocarcinoma
12
67
PGC
Cathepsin
B/H/L/S
Cy5.5, 11
Murine breast tumor
9.4 (250 pM dye) and
27.5 (2.5 nM dye)
FMT
68
PGC
Cathepsin D Cy5.5, 22
Murine hCaD-
expressing tumors
22
PE
69
PGC
MMP2
Cy5.5, 12
Murine fibrosarcoma
3
FRI
70
PGC
Cathepsin
B/H/L/S
Cy5.5
Murine atherosclerosis
(NO and ApoE
knockouts)
71
PGC
Cathepsin
B/H/L/S
Cy5.5
Murine breast tumor
5
FMT
72
PGC
Thrombin
Cy5.5
Murine thrombosis
2
FRI
73
PGC
Cathepsin
B/H/L/S
Cy5.5
Murine dysplastic
intestinal adenomas
2-4.5
FRI
74
PGC
Cathepsin
B/H/L/S
Cy5.5
Murine breast cancer
1.5 times higher signal
in invasive versus
noninvasive tumors
FRI
75
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