Novel optical contrast agents containing both DFO and multi-RGD peptides

Yunpeng Ye; Sharon Bloch; Samuel Achilefu

doi:10.1117/12.756808

8 January 2008 Novel optical contrast agents containing both DFO and multi-RGD peptides

Yunpeng Ye, Sharon Bloch, Samuel Achilefu

Proceedings Volume 6826, Optics in Health Care and Biomedical Optics III; 68261F (2008) https://doi.org/10.1117/12.756808
Event: Photonics Asia 2007, 2007, Beijing, China

Abstract

A series of novel near-infrared fluorescent compounds containing both desferrioxamine (DFO) and multi-RGD peptides, i.e. DFO-Cypate-(RGD)_n-NH₂ (1), were designed and synthesized based on a dicarboxylic acid-containing near-infrared fluorescent carbocyanine (Cypate) scaffold. The trimeric 1 (n=3) showed the strongest cellular internalization into A549 cells in vitro among the four analogs of 1 (n=1, 2, 3, 4), suggesting that such a linear array of three RGD peptide motifs might be optimal for synergistic effects on cellular internalization. The four analogs showed higher internalization than an integrin α_vβ₃-targeting cyclic RGD peptide analog DFO-cypate-[RGDfK(~)] (2) after 1h of incubation, indicating that the linear arrays of multi-RGD peptides might be different from the cyclic RGD peptide analog in the internalization kinetics and mechanism of receptor targeting. Confocal microscopy showed that 1 (n=4) could localize at least in part to the mitochondria. Noteworthy, the two compounds 1 (n=2, 3) resulted in a 1.5 to 2 fold increase in fluorescence of the calcium indicator fluo4 after 30 min of incubation. These results suggest the possible effects of these compounds on the cellular function by internalization. Such a type of near-infrared fluorescent cypate analogs containing both DFO and multi-RGD peptides could provide a platform for discovering and developing novel multifunctional optical contrast agents for integrin receptor targeting as well as related tumor imaging and therapy.

Citation Download Citation

Yunpeng Ye, Sharon Bloch, and Samuel Achilefu "Novel optical contrast agents containing both DFO and multi-RGD peptides", Proc. SPIE 6826, Optics in Health Care and Biomedical Optics III, 68261F (8 January 2008); https://doi.org/10.1117/12.756808

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