111In-labeled cystine-knot peptides based on the Agouti-related protein for targeting tumor angiogenesis.

Journal of Biomedicine & Biotechnology
Lei JiangZhen Cheng

Abstract

Agouti-related protein (AgRP) is a 4-kDa cystine-knot peptide of human origin with four disulfide bonds and four solvent-exposed loops. The cell adhesion receptor integrin α(v)β(3) is an important tumor angiogenesis factor that determines the invasiveness and metastatic ability of many malignant tumors. AgRP mutants have been engineered to bind to integrin α(v)β(3) with high affinity and specificity using directed evolution. Here, AgRP mutants 7C and 6E were radiolabeled with (111)In and evaluated for in vivo targeting of tumor integrin α(v)β(3) receptors. AgRP peptides were conjugated to the metal chelator 1, 4, 7, 10-tetra-azacyclododecane- N, N', N″, N'''-tetraacetic acid (DOTA) and radiolabeled with (111)In. The stability of the radiopeptides (111)In-DOTA-AgRP-7C and (111)In-DOTA-AgRP-6E was tested in phosphate-buffered saline (PBS) and mouse serum, respectively. Cell uptake assays of the radiolabeled peptides were performed in U87MG cell lines. Biodistribution studies were performed to evaluate the in vivo performance of the two resulting probes using mice bearing integrin-expressing U87MG xenograft tumors. Both AgRP peptides were easily labeled with (111)In in high yield and radiochemical purity (>99%). The two probes exh...Continue Reading

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Citations

Oct 26, 2012·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Michael ReinwarthOlga Avrutina
Mar 19, 2016·British Journal of Clinical Pharmacology·Barbara MolesiniTiziana Pandolfini
Mar 17, 2018·Journal of Nuclear Medicine : Official Publication, Society of Nuclear Medicine·Ahmet KrasniqiVladimir Tolmachev
Apr 25, 2015·Journal of Nuclear Medicine : Official Publication, Society of Nuclear Medicine·Lei JiangZhen Cheng

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Methods Mentioned

BETA
xenograft
xenografts

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