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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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Hauptverfasser: Askoxylakis, Vasileios (VerfasserIn) , Marr, Annabell (VerfasserIn) , Altmann, Annette (VerfasserIn) , Markert, Annette (VerfasserIn) , Mier, Walter (VerfasserIn) , Debus, Jürgen (VerfasserIn) , Huber, Peter E. (VerfasserIn) , Haberkorn, Uwe (VerfasserIn)
Dokumenttyp: Article (Journal)
Sprache:Englisch
Veröffentlicht: 2013
In: Molecular imaging & biology
Year: 2012, Jahrgang: 15, Heft: 2, Pages: 212-221
ISSN:1860-2002
DOI:10.1007/s11307-012-0578-7
Online-Zugang:Verlag, Volltext: http://dx.doi.org/10.1007/s11307-012-0578-7
Volltext
Verfasserangaben:Vasileios Askoxylakis, Annabell Marr, Annette Altmann, Annette Markert, Walter Mier, Jürgen Debus, Peter E. Huber, Uwe Haberkorn

MARC

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245 1 0 |a Peptide-based targeting of the platelet-derived growth factor receptor beta  |c Vasileios Askoxylakis, Annabell Marr, Annette Altmann, Annette Markert, Walter Mier, Jürgen Debus, Peter E. Huber, Uwe Haberkorn 
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520 |a 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. 
534 |c 2012 
650 4 |a Amino Acid Sequence 
650 4 |a Animals 
650 4 |a Drug Delivery Systems 
650 4 |a Drug Discovery 
650 4 |a Female 
650 4 |a HEK293 Cells 
650 4 |a Humans 
650 4 |a Immobilized Proteins 
650 4 |a Ligands 
650 4 |a MCF-7 Cells 
650 4 |a Mice 
650 4 |a Mice, Inbred BALB C 
650 4 |a Mice, Nude 
650 4 |a Molecular Sequence Data 
650 4 |a Pancreatic Neoplasms 
650 4 |a Peptide Library 
650 4 |a Peptides 
650 4 |a Receptor, Platelet-Derived Growth Factor beta 
650 4 |a Transfection 
650 4 |a Transplantation, Heterologous 
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