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Information Journal Paper

Title

NEW FREEZE-DRIED KIT FOR DIAGNOSIS OF BOMBESIN RECEPTOR EXPRESSING TUMORS

Pages

  9-19

Abstract

 Introduction: It has been shown that some primary human TUMORs and their metastases, including prostate and breast TUMORs, over-express gastrin-releasing peptide (GRP) receptors. BOMBESIN is a neuropeptide with a high affinity for these GRP RECEPTORS. The purpose of this study was to prepare and evaluate the characteristics of a new FREEZE-DRIED KIT, [6-hydrazinopyridine-3-carboxylic acid (HYNIC)]-GABA-BOMBESIN [7-14] NH2  designed for the labeling with 99mTc using tricine and EDDA as coligand.Methods: Synthesis was performed on a solid phase using a standard Fmoc strategy and HYNIC precursor coupled at the N-terminus. Purified peptide conjugate was labeled with 99mTc at 100°C for 10 min. Radiochemical analysis involved ITLC and high-performance liquid chromatography methods. Peptide conjugate stability and affinity to human serum was challenged for 24 hours. The internalization rate was studied in GRP receptor expressing PC-3 cells. Biodistribution of radiopeptide was studied in rats.Results: Radiolabeling was performed at high specific activities, and radiochemical purity was >98%. The stability of radiolabeled peptide in human serum was excellent. In vitro studies showed >14% of activity was specific internalized into PC-3 cells up to 4 h. After injection into rat biodistribution data showed a rapid blood clearance, with renal excretion and specific binding towards GRP receptor-positive tissues such as pancreas (1.15±0.19% ID/g after 4 h).Conclusion: [99mTc-HYNIC]-GABA-BOMBESIN [7-14] NH2 showed favorable radiochemical and biological characteristics which make our new designed labeled peptide conjugate as a very suitable agent for diagnostic purposes in malignant TUMORs.

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    APA: Copy

    ERFANI, MOSTAFA, SHIRMARDI, SEYED PEZHMAN, GHANNADI MARAGHEH, MOHAMMAD, SHAFIEI, MOHAMMAD, GOUDARZI, MOSTAFA, & FARAHANI, MASOUD. (2010). NEW FREEZE-DRIED KIT FOR DIAGNOSIS OF BOMBESIN RECEPTOR EXPRESSING TUMORS. IRANIAN JOURNAL OF NUCLEAR MEDICINE, 18(2 (SERIAL NUMBER 34)), 9-19. SID. https://sid.ir/paper/585377/en

    Vancouver: Copy

    ERFANI MOSTAFA, SHIRMARDI SEYED PEZHMAN, GHANNADI MARAGHEH MOHAMMAD, SHAFIEI MOHAMMAD, GOUDARZI MOSTAFA, FARAHANI MASOUD. NEW FREEZE-DRIED KIT FOR DIAGNOSIS OF BOMBESIN RECEPTOR EXPRESSING TUMORS. IRANIAN JOURNAL OF NUCLEAR MEDICINE[Internet]. 2010;18(2 (SERIAL NUMBER 34)):9-19. Available from: https://sid.ir/paper/585377/en

    IEEE: Copy

    MOSTAFA ERFANI, SEYED PEZHMAN SHIRMARDI, MOHAMMAD GHANNADI MARAGHEH, MOHAMMAD SHAFIEI, MOSTAFA GOUDARZI, and MASOUD FARAHANI, “NEW FREEZE-DRIED KIT FOR DIAGNOSIS OF BOMBESIN RECEPTOR EXPRESSING TUMORS,” IRANIAN JOURNAL OF NUCLEAR MEDICINE, vol. 18, no. 2 (SERIAL NUMBER 34), pp. 9–19, 2010, [Online]. Available: https://sid.ir/paper/585377/en

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