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. 2021 Mar 22;26(6):1792. doi: 10.3390/molecules26061792

Table 2.

List of c(RGD) multimeric radioligands αvβ3-integrin cell and tumor models tested.

# Name Cell & Tumor Model Ref. Figure
1 [18F]FBOA-Dpr-HEG-c(RGDfE) M21 Human melanoma
U87MG human glioblastoma
[22,33] Figure 2
2 [18F]FBOA-Dpr-K(HEG-c(RGDfE))2
3 [18F]FBOA-Dpr-K{K[HEG-(c(RGDfE)]2}2
4 [18F]FB-E[c(RGDyK)]2 HBCECs human brain capillary endothelial cells, U87MG [34,35] Figure 3
5 [18F]FP-E[c(RGDyK)]2
18F-FP-RGD2
U87MG
6 [18F]AlF-NOTA-E[c(RGDyK)]2
[18F]AlF-NOTA-RGD2
U87MG [35,46]
7 [18F]FB-PEG3-E[c(RGDyK)]2
[18F]FB-PRGD2
U87MG [36,37]
8 [18F]FP-PEG3-E[c(RGDyK)]2
[18F]FP-PRGD2
HCT116 human colon cancer, U87MG [27,39,72,73,74]
9 [68Ga]Ga-NOTA-PEG3-E[c(RGDyK)]2 U87MG [38,39]
10 [18F]AlF-NOTA-PEG3-E[c(RGDyK)]2
[18F]Alfatide I
U87MG, A549 adenocarcinomic human alveolar basal epithelial cells, PC-3 prostate cancer, LLC Lewis Lung Carcinoma [38,39,40,41,76,77]
11 [18F]FP-PEG4-E[c(RGDfK)]2
[18F]FP-PRGD2
U87MG, MDA-MB-435 [45] Figure 4
12 [68Ga]Ga-NOTA-PEG4-E[c(RGDfK)]2 U87MG [78]
13 [18F]AlF-NOTA-PEG4-E[c(RGDfK)]2 U87MG [46]
14 [18F]AlF-NOTA-E[PEG4-c(RGDfK)]2,
[18F]Alfatide II
U87MG, MDA-MB-435 human breast cancer [43,44,46,52,53,54]
15 [68Ga]Ga-NOTA-E[PEG4-c(RGDfK)]2
[68Ga]Ga-NOTA-PRGD2,
- [51,79]
16 [18F]FP-PEG4-E[PEG4-c(RGDfK)]2
[18F]FP-PPRGD2
U87MG, MDA-MB-435 [45]
17 [18F]FP-PEG2-β-E[c(RGDyK)]2 A549, PC-3 [47] Figure 5
18 [18F]FP-SAA-E[c(RGDyK)2 U87MG [48] Figure 6
19 [18F]FB-SAA-E[c(RGDyK)2
20 NOTA-E[c(RGDyK)]2 - [49] Figure 7
21 [68Ga]Ga-NOTA-E[c(RGDyK)]2
22 [68Ga]Ga-NOTA-Y-c(RGDyK)]
(Y =2-(4-anilinyl-methyl)-4-(3-oxopropyl)thiazol-5(4H)-one)
23 [64Cu]Cu-DOTA-E[c(RGDfK)]2 U87MG, MDA-MB-435 [55,56] Figure 8
24 [68Ga]Ga-DOTA-E[c(RGDfK)]2 B16-F10-luc melanoma tumors, SK-RC-52, FaDu [61,70]
25 [64Cu]Cu-DOTA-E[c(RGDyK)]2 MDA-MB-435 [55]
26 [64Cu]Cu-DOTA-E{E[c(RGDfK)]2}2 U87MG [56,58]
27 [64Cu]Cu-DOTA-E{E[c(RGDyK)]2}2 U87MG, c-neu onco-mice [30]
28 [64Cu]Cu-DOTA-E(E{E[c(RGDfK)]2}2)2 U87MG, c-neu onco-mice [30]
29 [64Cu]Cu-NOTA-PEG4-E[(PEG2-Tz-c(RGDfK)]2 HUVEC human umbilical vein endothelial cells [57] Figure 9
30 FITC-PEG4-E[PEG2-Tz-c(RGDfK)]2
31 [64Cu]Cu-DOTA-PEG4-E[PEG4-c(RGDfK)]2 U87MG [58]
32 [64Cu]Cu-DOTA-G3-E[G3-c(RGDfK)]2
33 [64Cu]Cu-AmBaSar-E[c(RGDyK)]2 U87MG [59,60] Figure 10
34 [64Cu]Cu-AmBaBaSar-c(RGDyK)2
35 [68Ga]Ga-NOTA-E[PEG4-c(RGDfK)]2 U87MG: MDA-MB-435 [62] Figure 11
36 [68Ga]Ga-NOTA-E[G3-c(RGDfK)]2 U87MG, MDA-MB-435, HT1080 fibrosarcoma [62,64]
37 [68Ga]Ga-NOTA-E[G3-c(CNGRC)]2 HT1080 fibrosarcoma [64]
38 [68Ga]Ga-NOTA-E[c(RGDyK)]2 U87MG [66]
39 [68Ga]Ga-NOTA-E{E[c(RGDyK)]2}2
40 [68Ga]Ga-NODAGA-E[c(RGDyK)]2 U87MG, H727 human neuroendocrine [67]
41 [64Cu]Cu-NODAGA-E[c(RGDyK)]2
42 [68Ga]Ga-FSC-[E-c(RGDfK)]3 M21 human melanoma, SK-RC-52 (human renal cell carcinoma), FaDu (human squamous cell carcinoma) [68,70] Figure 12
43 [68Ga]Ga-FSC-(CH2)-Tz-c(RGDfK) U87MG, M21 human melanoma [23]
44 [68Ga]Ga-FSC-[(CH2)-Tz-c(RGDfK)]2
45 [68Ga]Ga-FSC-[(CH2)-Tz-c(RGDfK)]3
46 [68Ga]Ga-TRAP-PEG4-c(RGDfK)3 M21 human melanoma,
SK-RC-52, FaDu
[69,70] Figure 13
47 [68Ga]Ga-THP-c(RGDfK)3 SK-RC-52, FaDu [70]