Multimeric cyclic RGD peptides as potential tools for tumor targeting: solid-phase peptide synthesis and chemoselective oxime ligation.

Georgette Thumshirn; Ulrich Hersel; Simon L Goodman; Horst Kessler

doi:10.1002/chem.200204304

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Multimeric cyclic RGD peptides as potential tools for tumor targeting: solid-phase peptide synthesis and chemoselective oxime ligation.

Georgette Thumshirn·Ulrich Hersel·Simon L Goodman·Horst Kessler

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Abstract

The alpha v beta 3 integrin receptor plays an important role in human metastasis and tumor-induced angiogenesis. Targeting this receptor may provide information about the receptor status of the tumor and enable specific therapeutic planning. Solid-phase peptide synthesis of multimeric cyclo(-RGDfE-)-peptides is described, which offer the possibility of enhanced integrin targeting due to polyvalency effects. These peptides contain an aminooxy group for versatile chemoselective oxime ligation. Conjugation with para-trimethylstannylbenzaldehyde results in a precursor for radioiododestannylation, which would allow them to be used as potential tools for targeting and imaging alpha v beta 3-expressing tumor cells. The conjugates were obtained in good yield without the need of a protection strategy and under mild conditions.

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Animals Integrin alphaVbeta3 Mice Mice, Nude Neoplasms, Experimental Oligopeptides Oximes Peptides, Cyclic Vitronectin Journal Article Research Support, Non-U.S. Gov't

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Georgette Thumshirn, Ulrich Hersel, Simon L Goodman, Horst Kessler. 2003-06-16. Multimeric cyclic RGD peptides as potential tools for tumor targeting: solid-phase peptide synthesis and chemoselective oxime ligation.. https://doi.org/10.1002/chem.200204304

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