FIGURE SUMMARY
Title

Synthesis and Anti-Angiogenic Activity of Novel c(RGDyK) Peptide-Based JH-VII-139-1 Conjugates

Authors
Leonidis, G., Koukiali, A., Sigala, I., Tsimaratou, K., Beis, D., Giannakouros, T., Nikolakaki, E., Sarli, V.
Source
Full text @ Pharmaceutics
Fig. 1

General structures of alectinib, JH-VII-139-1 and c(RGDyK) peptide conjugates that carry an SRPK1 inhibitor.
Fig. 2

Chemostability of JH-VII-139-1.
Fig. 3

Chemostability of conjugate geo75.
Fig. 4

Chemostability of geo77.
Fig. 5

Chemostability of conjugate geo85.
Fig. 6

Chemostability of conjugate geo107.
Fig. 7

Confocal microscopy images of MCF7 and MDA-MB-231 cells after incubation with 5 μM of geo106 for 2, 24 and 48 h, respectively. Cells were fixed with 4% paraformaldehyde. DNA was stained with DAPI (pseudo color red). Cells were visualized with a Zeiss LSM 780 confocal microscope using the Zen 2011 software.
Fig. 8

Confocal microscopy images of MDA-MB-231 cells after incubation with 5 μM of geo106 for 2 h. Cells were preincubated, prior to addition of geo106, with okadaic acid (100 nM) for 30 min. Cells were fixed with 4% paraformaldehyde. DNA was stained with DAPI. Cells were visualized with a Zeiss LSM 780 confocal microscope using the Zen 2011 software.
Fig. 9

In vivo screening unravels inhibitors of angiogenesis. (A–G) Fluorescence microscopy images of representative Tg(kdrl:gfp) embryos treated with the specified compounds from 24 hpf, and DMSO-treated control at 72 hpf. White arrows show sections of ISVs with decreased width. Scale bar, 100 μm. (H) Estimated and presented total width of 8 ISVs per embryo. Width was measured and averaged at three different points (top, middle and bottom point) of each ISV. Compounds JII-VII-139-1 (10 μM), geo75 (1.3 μM), geo77 (1.3 μM), geo85 (1.3 μM) and geo107 (1.3 μM), show statistically significant inhibition on the total width of ISVs, while compound c(RGDyK) (10 μM) shows a non-significant trend at the tested concentration. Data are expressed as mean ± SD (n = 4–7/group). ** p < 0.05.
Fig. 10

geo77 also affects the length of ISVs. (A–G) Fluorescence microscopy images of representative Tg(kdrl:gfp) embryos treated from 24 hpf, and DMSO-treated control at 72 hpf. Yellow arrows indicate sections of ISVs with decreased length angiogenesis. Scale bar, 100 μm. (H) Estimated and presented total lengths of 8 ISVs per embryo. Compound geo77 (1.3 μM) shows statistically significant inhibition on the total length of ISVs, while the other tested compounds show a non-significant trend at the tested concentrations. Data are expressed as mean ± SD (n = 4–7/group). ** p < 0.05.
Acknowledgments
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