Ziba Kazemi, Mona Haddad Zahmatkesh , Seyed Mohammad Abedi and Seyed Jalal Hosseinimehr Pages 123 - 130 ( 8 )
Background: D4 small peptide (Leu-Ala-Arg-Leu-Leu-Thr) was selected as an appropriate agent for specific targeting of epidermal growth factor receptor (EGFR).Objective: The aim of study was to investigate the 99mTc-labeled D4 peptide for non-small cell lung tumor targeting. Method: HYNIC-(Ser)3-D4 peptide was labeled with 99mTc using mixture of tricine and ethylenediamine diacetic acid (EDDA) as co-ligands. The in vitro cellular uptake of radiolabeled peptide was evaluated by blocking test on human non-small cell lung cancer (A-549) cell line and its biodistribution was evaluated in A-549 xenografted nude mice. Results: This conjugated peptide was labeled with 99mTc in high radiochemical purity and it was highly stable in buffer and serum. The un-blocked to blocked cellular radioactivity ratio was 4- fold that showed a specific binding of this radiolabeled peptide on A-549 cell. Animal biodistribution in A-549 xenografted nude mice showed rapid clearance from blood and other non-target organs. Tumor uptake values as %ID/g (percentage of injection dose per gram of tissue) were 2.47% and 1.30% at 1 and 4 h after injection. Conclusion: This study showed the 99mTc-EDDA/tricine-HYNIC-(Ser)3-D4 peptide had tumor targeting on the non-small cell lung tumor.
Tumor targeting, 99mTc, peptide, EDDA/tricine, lung cancer, EGFR.
Department of Radiopharmacy, Faculty of Pharmacy, Phramaceutical Sciences Research Center, Mazandaran University of Medical Sciences, Sari, Department of Medicinal Chemistry, Faculty of Pharmacy, Guilan University of Medical Sciences, Rasht, Department of Radiology, Faculty of Medicine, Mazandaran University of Medical Sciences, Sari, Department of Radiopharmacy, Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari