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Peptide-based targeting of the platelet-derived growth factor receptor beta

PURPOSE: The aim of this work is to identify new ligands targeting the platelet-derived growth factor receptor beta (PDGFRβ). PROCEDURES: Biopanning was carried out with a 12-amino-acid phage display library against the recombinant extracellular domain of PDGFRβ. The identified peptide PDGFR-P1 was...

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Main Authors: Askoxylakis, Vasileios (Author) , Marr, Annabell (Author) , Altmann, Annette (Author) , Markert, Annette (Author) , Mier, Walter (Author) , Debus, Jürgen (Author) , Huber, Peter E. (Author) , Haberkorn, Uwe (Author)
Format: Article (Journal)
Language:English
Published: 2013
In: Molecular imaging & biology
Year: 2012, Volume: 15, Issue: 2, Pages: 212-221
ISSN:1860-2002
DOI:10.1007/s11307-012-0578-7
Online Access:Verlag, Volltext: http://dx.doi.org/10.1007/s11307-012-0578-7
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Author Notes:Vasileios Askoxylakis, Annabell Marr, Annette Altmann, Annette Markert, Walter Mier, Jürgen Debus, Peter E. Huber, Uwe Haberkorn
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Summary:PURPOSE: The aim of this work is to identify new ligands targeting the platelet-derived growth factor receptor beta (PDGFRβ). PROCEDURES: Biopanning was carried out with a 12-amino-acid phage display library against the recombinant extracellular domain of PDGFRβ. The identified peptide PDGFR-P1 was chemically synthesized and labeled with (125)I or (131)I. In vitro studies were performed on the PDGFRβ-expressing cell lines BxPC3 and MCF7 and on PDGFRβ-transfected HEK cells in comparison to negative control wtHEK293 and CaIX-transfected HEK cells. Biodistribution experiments were performed in Balb/c nude mice, carrying subcutaneously BxPC3 tumors. RESULTS: In vitro studies demonstrated a higher binding to BxPC3, MCF7, and PDGFRβ-tr-HEK cells in comparison to negative control cell lines. Binding was inhibited up to 90% by the unlabeled PDGFR-P1 peptide. Organ distribution studies revealed a higher accumulation in BxPC3 tumors than in most organs. CONCLUSIONS: PDGFR-P1 is a promising candidate for targeting human PDGFRβ.
Item Description:Published online: 13 July 2012
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Physical Description:Online Resource
ISSN:1860-2002
DOI:10.1007/s11307-012-0578-7

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