synthesis and evaluation of a new radiolabeled bombesin analogue for diagnosis of grp receptor expressing tumors
نویسندگان
چکیده
introduction: bombesin (bn), a 14-amino acid neuropeptide, shows high affinity for the human grp (gastrin releasing peptide) receptors, which are overexpressed by a variety of cancers, including prostate, breast, pancreas, gastrointestinal, and small cell lung cancer. aim was to prepare [6-hydrazinopyridine-3-carboxylic acid (hynic0), d-tyr6, d-trp8] - bn [6-14] nh2 that could be easily labeled with 99mtc and evaluation of its potential as an imaging agent. methods: synthesis of the peptide amide was carried out onto rink amide mbha (4-methylbenzhydrylamine) resin. a bifunctional chelating agent (bfca) was attached to the n terminal peptide in solid-phase. 99mtc labeling was performed by addition of sodium pertechnetate to solution that include [hynic0, d-tyr6, d-trp8] bombesin [6-14] nh2, tricine, ethylenediamine-n,n′-diacetic acid (edda) and sncl2. radiochemical evaluation was carried out by reverse phase high-performance liquid chromatography (hplc) and instant thin layer chromatography (itlc). in-vitro internalization was tested using human prostate cancer cells (pc-3) with blocked and non-blocked receptors. biodistribution was determined in rats. results:[99mtc/tricine/edda-hynic0, d-tyr6, d-trp8] bombesin [6-14] nh2 was obtained with radiochemical purities >98%. results of in-vitro studies demonstrated a high stability in serum and suitable internalization. biodistribution data showed a rapid blood clearance, with renal excretion and specific binding towards grp receptor-positive tissues such as pancreas. conclusion: in this study, labeling of this novel conjugate with 99mtc easily was performed using coligand. the prepared 99mtc-hynic-bn conjugate has promising characteristics for the diagnosis of malignant tumors.
منابع مشابه
Synthesis and evaluation of a new radiolabeled bombesin analogue for diagnosis of GRP receptor expressing tumors
Introduction: Bombesin (BN), a 14-amino acid neuropeptide, shows high affinity for the human GRP (gastrin releasing peptide) receptors, which are overexpressed by a variety of cancers, including prostate, breast, pancreas, gastrointestinal, and small cell lung cancer. Aim was to prepare [6-hydrazinopyridine-3-carboxylic acid (HYNIC0), D-Tyr6, D...
متن کاملSynthesis and Evaluation of a New Radiolabeled Bombesin Analogue for Diagnosis of GRP Receptor Expressing Tumors
Introduction: Bombesin (BN), a 14-amino acid neuropeptide, shows high affinity for the human GRP (gastrin releasing peptide) receptors, which are overexpressed by a variety of cancers, including prostate, breast, pancreas, gastrointestinal, and small cell lung cancer. Aim was to prepare [6-hydrazinopyridine-3-carboxylic acid (HYNIC), D-Tyr, D-Trp] BN [6-14] NH2 that could be easily labeled with...
متن کاملNew freeze-dried kit for diagnosis of Bombesin receptor expressing tumors
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-hydrazinopyr...
متن کاملSynthesis, labeling and quality control of a new Neuropeptide Y analogue for diagnosis of breast tumors
Introduction: Over expression of selected peptide receptors in human tumors has been shown to represent clinically relevant targets for cancer diagnosis and therapy. The aim of this work was to investigate Neuropeptide Y (NPY) as a new radiopharmaceutical for diagnosis of breast cancer. Methods: A neuropeptide Y analogues with Y1 receptor preference and agonistic p...
متن کاملnew freeze-dried kit for diagnosis of bombesin receptor expressing tumors
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 (hyni...
متن کاملsynthesis, labeling and quality control of a new neuropeptide y analogue for diagnosis of breast tumors
introduction: over expression of selected peptide receptors in human tumors has been shown to represent clinically relevant targets for cancer diagnosis and therapy. the aim of this work was to investigate neuropeptide y (npy) as a new radiopharmaceutical for diagnosis of breast cancer. methods: a neuropeptide y analogues with y1 receptor preference and agonistic properties was synthesized by s...
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عنوان ژورنال:
iranian journal of nuclear medicineناشر: tehran university of medical sciences
ISSN 1681-2824
دوره 17
شماره 1 2009
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