doi: 10.1002/jlcr.2965.
Epub 2012 Sep 5.
(111)In- and (203)Pb-Labeled Cyclic RGD Peptide Conjugate as an α(v)β(3) Integrin-Binding Radiotracer
Affiliations
- PMID: 23162207
- PMCID: PMC3496268
- DOI: 10.1002/jlcr.2965
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(111)In- and (203)Pb-Labeled Cyclic RGD Peptide Conjugate as an α(v)β(3) Integrin-Binding Radiotracer
J Labelled Comp Radiopharm.
.
Abstract
Methodology for site-specific modification and chelate conjugation of a cyclic RGD (cRGD) peptide for the preparation of a radiotracer molecular imaging agent suitable for detecting α(v)β(3) integrin is described. The method involves functionalizing the peptide with an aldehyde moiety and conjugation to a 1,4,7,10-tetraazacyclododecane-N,N',N″,N‴-tetraacetic acid (DOTA) derivative that possesses an aldehyde reactive aminooxy group. The binding assay of the (111)In-labeled peptide conjugate with α(v)β(3) integrin showed 60% bound when four equivalents of the integrin was added, a reasonable binding affinity for a mono-valent modified RGD peptide.
Figures
Reaction scheme for preparation of the peptide conjugate.
Radio-HPLC profiles of 111In-4 (top) and 203Pb-4 (bottom)
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References
-
- Bello L, Francolini M, Marthyn P, Zhang J, Carroll R, Nikas DC, Strasser JF, Villani R, Cheresh DA, Black P. Neurosurgery. 2001;1:380. - PubMed
-
- Gasparini G, Brooks PC, Biganzoli E, Vermeulen PB, Bonoldi E, Dirix LY, Ranieri G, Miceli R, Cheresh DA. Clin. Cancer Res. 1998;4:2625. - PubMed
-
- Albelda SM, Damjanovich L, Herlyn M, Buck CA. Cancer Res. 1990;50:6757. - PubMed
-
- Zitzmann S, Ehemann V, Schwab M. Cancer Res. 2002;62:5139. - PubMed
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