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Synthesis, radiolabeling, and preclinical evaluation of a new octreotide analog for somatostatin receptor-positive tumor scintigraphy

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Title Synthesis, radiolabeling, and preclinical evaluation of a new octreotide analog for somatostatin receptor-positive tumor scintigraphy
 
Creator De, Kakali
Bhowmik, Arijit
Behera, Ashok
Banerjee, Indranil
Ghosh, Mrinal Kanti
Misra, Mridula
 
Subject Cancer Biology and Inflammatory Disorder Division
Infectious Diseases and Immunology
 
Description Radiolabeled somatostatin analogs have become powerful tools in the diagnosis and staging of neuroendocrine tumors, which express somatostatin receptors. The aim of this study was to evaluate a new somatostatin analog, 6-hydrazinopyridine-3-carboxylic acid-Ser3-octreotate (HYNIC-SATE) radiolabeled with 99mTc, using ethylenediamine-N,N0-diacetic acid and tricine as coligands, to be used as a radiopharmaceutical for the in vivo imaging of somatostatin receptor subtype 2 (SSTR2)-positive tumor. Synthesis of the peptide was carried out on a solid phase using a standard Fmoc strategy. Peptide conjugate affinities for SSTR2 were determined by receptor binding affinity on rat brain cortex and C6 cell membranes. Internalization rate of 99mTc-HYNIC-SATEwas studied in SSTR2-expressing C6 cells thatwere used for intracranial tumor studies in rat brain. A reproducible in vivo C6 glioma model was developed in Sprague–Dawley rat and confirmed by histopathology and immunohistochemical
analysis. Biodistribution and imaging properties of this new radiopeptide were also studied in C6 tumor-bearing rats.
Radiolabeling was performed at high specific activities, with a radiochemical purity of >96%. Peptide conjugate showed high affinity binding for SSTR2 (HYNIC-SATE IC50 = 1.60�0.05 nM) and specific internalization into rat C6 cells. After administration of 99mTc-HYNIC-SATE in C6 glioma-bearing rats, a receptor specific uptake of radioactivity was observed in SSTR-positive rgans and in the implanted intracranial tumor and rapid excretion from nontarget tissues via kidneys.
 
Publisher John Wiley & Sons
 
Date 2012
 
Type Article
PeerReviewed
 
Format application/pdf
 
Identifier http://www.eprints.iicb.res.in/2269/1/JOURNAL_OF_PEPTIDE_SCIENCE__V._18__(12)___Pages_720%2D730;2013.pdf
De, Kakali and Bhowmik, Arijit and Behera, Ashok and Banerjee, Indranil and Ghosh, Mrinal Kanti and Misra, Mridula (2012) Synthesis, radiolabeling, and preclinical evaluation of a new octreotide analog for somatostatin receptor-positive tumor scintigraphy. Journal of Peptide Science, 18 (12). pp. 720-730. ISSN 1075-2617
 
Relation http://dx.doi.org/10.1002/psc.2458
http://www.eprints.iicb.res.in/2269/