Comparison of Two Iranian Gastrin Releasing Peptide Analogs as a Malignant Breast and ProstateTumor Imaging Agent

Shirmardi, Seyed Pezhman; Erfani, Mostafa

Volume 4, Issue 15 (9-2014) NCMBJ 2014, 4(15): 67-74 | Back to browse issues page

‎ 20.1001.1.22285458.1393.4.15.7.4

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Shirmardi S P, Erfani M. Comparison of Two Iranian Gastrin Releasing Peptide Analogs as a Malignant Breast and ProstateTumor Imaging Agent. NCMBJ 2014; 4 (15) :67-74
URL: http://ncmbjpiau.ir/article-1-555-en.html

Comparison of Two Iranian Gastrin Releasing Peptide Analogs as a Malignant Breast and ProstateTumor Imaging Agent

Seyed Pezhman Shirmardi

, Mostafa Erfani

2- Nuclear Science Research School, Nuclear Science and Technology Research Institute (NSTRI), Atomic Energy Organization of Iran, Tehran, Iran , mgandomkar@aeoi.org.ir

Abstract: (9056 Views)

Aim and Background: Bombesin is a peptide showing high affinity for the gastrin releasing peptide receptor (GRPr). The prostate, lung, breast and colon tumors express many GRP receptors. The aim of this research was to compare two Iranian radiolabeled BBN analogs based upon the DOTA and Hynic chelators which could be used as a tool for the diagnosis of GRP receptor-positive tumors.

Material and Methods: Two peptides were synthesized using a standard Fmoc strategy which lead to produce DOTA-GABA-Bombesin (7-14) NH2 and HYNIC-GABA-Bombesin (7-14) NH2. Peptide conjugate showed good stability in the presence of human serum (37 degree centigrade). The internalization rates were studied in GRP receptor expressing PC-3 cells. Biodistribution of radiopeptide was studied in nude mice bearing PC-3 tumor.

Results: The results of internalization sowed that [67Ga]-DOTA-GABA-Bombesin (7-14) has a more internalization relative to 99mTc-HYNIC-GABA-Bombesin (7-14) NH2 in three stages. The results of biodistriution showed that the Tumor/Kidney and Tumor/Pancreas ratio after for [67Ga]-DOTA-GABA-Bombesin (7-14) was better than the other one. These data show that two bombesin analogs are specific radioligand for gastrin-releasing peptide receptor positive tumors and is a suitable candidate for clinical studies.

Conclusion: The results of blood clearance and internalization showed that the [67Ga]-DOTA-GABA-Bombesin (7-14) has good conditions as an imaging agent relative to the other one.

Keywords: 67Ga, 99mTc, Peptide Radiolabeling

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Type of Study: Research Article | Subject: Genetics
Received: 2014/09/27 | Accepted: 2014/09/27 | Published: 2014/09/27