99mTc-HYNIC-D4 Peptide: A New Small Radiolabeled Peptide for Non Small Cell Lung Tumor Targeting

Author(s): Mona Haddad Zahmatkesh , Seyed Mohammad Abedi , Seyed Jalal Hosseinimehr* .

Journal Name: Anti-Cancer Agents in Medicinal Chemistry

Volume 17 , Issue 5 , 2017

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Abstract:

Objective: The aim of this study was to evaluate the 99mTc-HYNIC-D4 peptide as a new radiotracer for tumor targeting in non small cell lung tumor that overexpresses epidermal growth factor receptor (EGFR).

Method: D4 small peptide (Leu-Ala-Arg-Leu-Leu-Thr) was selected as a candidate for specific targeting on EGFR. It was conjugated with HYNIC on N-terminus and labeled with 99mTc using tricine as a co-ligand. The cellular and animal studies were evaluated for specific binding of this labeled peptide.

Result: Radiochemical purity was determined to be 98% by instant thin layer chromatography and reverse-phase high performance liquid chromatography. Stability of radiolabeled peptide was more than 90% up to 24 h incubation in solution at 37 oC. Specific binding of the radiolabeled peptide to the EGFR showed dissociation constant of 181 ± 41 nM. Animal biodistribution in normal and 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 8.07% at 1 h and 3.82% at 4 h after injection that was blocked by presaturation of EGFR using an excess of cold peptide.

Conclusion: This study showed that 99mTc-HYNIC-D4 is a promising tumor targeting radiotracer on the non small cell lung tumor.

Keywords: Tumor imaging, 99mTc, peptide, lung cancer, small radiolabeled, non small cell.

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Article Details

VOLUME: 17
ISSUE: 5
Year: 2017
Page: [734 - 740]
Pages: 7
DOI: 10.2174/1871520616666160907142130
Price: $58

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