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Novel indium-111 labeled gastrin peptide analogues (MG-CL1-4): synthesis and quality control.

Identifieur interne : 000509 ( Main/Exploration ); précédent : 000508; suivant : 000510

Novel indium-111 labeled gastrin peptide analogues (MG-CL1-4): synthesis and quality control.

Auteurs : RBID : pubmed:23455200

English descriptors

Abstract

Radiolabeled neuropeptides are widely investigated to diagnose and therapy of tumors. These peptides get internalization after binding with particular receptors at the surface of cells and finally move to lysosome. Internalization into tumor cells helps in mapping the infected site. Minigastrin peptide analogues (MG-CL1-4) were synthesised and labeled with 111-In radioisotope under different sets of conditions for imaging CCk-2 receptor bearing tumors. Different parameters such as temperature (80-100°C), pH (4-12), incubation time (5-30 minutes) and dilution effect were investigated to get the maximum labeling yield and stability. The results indicated that MG-CL1-4 is successfully labeled with indium-111 at pH 4.5 with heating at 98°C for 15 minute. At these conditions i.e. heating, pH and incubation minimum oxidized and maximum labeling yield, more than 94 %, was obtained. The labeling stability was studied by incubating the radiolabeled complex for predefined time points in PBSA and blood serum. Results show that more than 90% radiolabeled MG-CL1-4 remained intact.

PubMed: 23455200

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Le document en format XML

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<title xml:lang="en">Novel indium-111 labeled gastrin peptide analogues (MG-CL1-4): synthesis and quality control.</title>
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<name sortKey="Naqvi, Syed Ali Raza" uniqKey="Naqvi S">Syed Ali-Raza Naqvi</name>
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<nlm:affiliation>Department of Chemistry, Government College University, Faisalabad, Pakistan.</nlm:affiliation>
<country xml:lang="fr">Pakistan</country>
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<name sortKey="Khan, Zulfiqar Ali" uniqKey="Khan Z">Zulfiqar Ali Khan</name>
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<name sortKey="Nagra, Saeed Ahmad" uniqKey="Nagra S">Saeed Ahmad Nagra</name>
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<name sortKey="Yar, Muhammad" uniqKey="Yar M">Muhammad Yar</name>
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<name sortKey="Sherazi, Tauqir A" uniqKey="Sherazi T">Tauqir A Sherazi</name>
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<name sortKey="Shahzad, Sohail Shahzad" uniqKey="Shahzad S">Sohail Shahzad Shahzad</name>
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<name sortKey="Shah, Syed Qaiser" uniqKey="Shah S">Syed Qaiser Shah</name>
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<name sortKey="Mahmood, Nasir" uniqKey="Mahmood N">Nasir Mahmood</name>
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<name sortKey="Ishfaq, Malik Muhammad" uniqKey="Ishfaq M">Malik Muhammad Ishfaq</name>
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<name sortKey="Mather, Stephen John" uniqKey="Mather S">Stephen John Mather</name>
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<term>Hydrogen-Ion Concentration</term>
<term>Indium Radioisotopes</term>
<term>Isotope Labeling (standards)</term>
<term>Oxidation-Reduction</term>
<term>Protein Stability</term>
<term>Quality Control</term>
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<term>Gastrins</term>
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<div type="abstract" xml:lang="en">Radiolabeled neuropeptides are widely investigated to diagnose and therapy of tumors. These peptides get internalization after binding with particular receptors at the surface of cells and finally move to lysosome. Internalization into tumor cells helps in mapping the infected site. Minigastrin peptide analogues (MG-CL1-4) were synthesised and labeled with 111-In radioisotope under different sets of conditions for imaging CCk-2 receptor bearing tumors. Different parameters such as temperature (80-100°C), pH (4-12), incubation time (5-30 minutes) and dilution effect were investigated to get the maximum labeling yield and stability. The results indicated that MG-CL1-4 is successfully labeled with indium-111 at pH 4.5 with heating at 98°C for 15 minute. At these conditions i.e. heating, pH and incubation minimum oxidized and maximum labeling yield, more than 94 %, was obtained. The labeling stability was studied by incubating the radiolabeled complex for predefined time points in PBSA and blood serum. Results show that more than 90% radiolabeled MG-CL1-4 remained intact.</div>
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<Title>Pakistan journal of pharmaceutical sciences</Title>
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<AbstractText>Radiolabeled neuropeptides are widely investigated to diagnose and therapy of tumors. These peptides get internalization after binding with particular receptors at the surface of cells and finally move to lysosome. Internalization into tumor cells helps in mapping the infected site. Minigastrin peptide analogues (MG-CL1-4) were synthesised and labeled with 111-In radioisotope under different sets of conditions for imaging CCk-2 receptor bearing tumors. Different parameters such as temperature (80-100°C), pH (4-12), incubation time (5-30 minutes) and dilution effect were investigated to get the maximum labeling yield and stability. The results indicated that MG-CL1-4 is successfully labeled with indium-111 at pH 4.5 with heating at 98°C for 15 minute. At these conditions i.e. heating, pH and incubation minimum oxidized and maximum labeling yield, more than 94 %, was obtained. The labeling stability was studied by incubating the radiolabeled complex for predefined time points in PBSA and blood serum. Results show that more than 90% radiolabeled MG-CL1-4 remained intact.</AbstractText>
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