[99mTc] HYNIC-hEGF, a potential agent for imaging of EGF receptors in vivo: Preparation and pre-clinical evaluation

Mohammad Hussein Babaei, Ylva Almqvist, Anna Orlova, Mohammad Shafii, Kalevi Kairemo, Vladimir Tolmachev

Research output: Contribution to journalArticlepeer-review

17 Citations (Scopus)

Abstract

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 99mTc-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 99mTc- EDDA-HYNIC-EGF in normal mice demonstrated fast blood clearance of conjugate, and its ability to bind EGFR in vivo. 99mTc-EDDA-HYNIC-EGF is a promising candidate for visualization of EGFR expression in vivo.

Original languageEnglish
Pages (from-to)1169-1175
Number of pages7
JournalOncology Reports
Volume13
Issue number6
DOIs
Publication statusPublished - Jun 2005
Externally publishedYes

Keywords

  • A431 cells
  • Epithelial growth factor
  • Ethylenediamine-N,N′-diacetic acid
  • Hydrazinopyridine-3-carboxylic acid
  • Tricine

ASJC Scopus subject areas

  • Oncology
  • Cancer Research

Fingerprint Dive into the research topics of '[<sup>99m</sup>Tc] HYNIC-hEGF, a potential agent for imaging of EGF receptors in vivo: Preparation and pre-clinical evaluation'. Together they form a unique fingerprint.

Cite this