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[99mTc] HYNIC-hEGF, a potential agent for imaging of EGF receptors in vivo: preparation and pre-clinical evaluation
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Medicine, Department of Oncology, Radiology and Clinical Immunology.
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Medicine, Department of Oncology, Radiology and Clinical Immunology.ORCID iD: 0000-0001-6120-2683
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2005 (English)In: Oncology Reports, ISSN 1021-335X, E-ISSN 1791-2431, Vol. 13, no 6, 1169-75 p.Article in journal (Refereed) Published
Abstract [en]

Expression of epidermal growth factor receptors (EGFR) has prognostic and predictive value in many kinds of tumors. Imaging of expression of EGFR in vivo may give valuable diagnostic information. The epidermal growth factor (EGF), a natural ligand, is a possible candidate for the targeting of EGFR. The present study describes a method for preparation of (99m)Tc-EGF via the hydrazinopyridine-3-carboxylic acid (HYNIC) conjugation using tricine and ethylenediamine-N,N'-diacetic acid (EDDA) as co-ligands. Both conjugates bound EGFR expressing cells with nanomolar affinity, and demonstrated good intracellular retention. The complex with EDDA demonstrated much higher stability in blood serum and during cysteine challenge. Biodistribution of (99m)Tc-EDDA-HYNIC-EGF in normal mice demonstrated fast blood clearance of conjugate, and its ability to bind EGFR in vivo. (99m)Tc-EDDA-HYNIC-EGF is a promising candidate for visualization of EGFR expression in vivo.

Place, publisher, year, edition, pages
2005. Vol. 13, no 6, 1169-75 p.
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Medical and Health Sciences
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URN: urn:nbn:se:uu:diva-72815PubMedID: 15870939OAI: oai:DiVA.org:uu-72815DiVA: diva2:100726
Available from: 2005-05-30 Created: 2005-05-30 Last updated: 2017-12-14Bibliographically approved

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Almqvist, YlvaOrlova, AnnaTolmachev, Vladimir

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