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Exploring the Potential of 99mTc(CO)3-Labeled Triazolyl Peptides for Tumor Diagnosis

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Title Exploring the Potential of 99mTc(CO)3-Labeled Triazolyl Peptides for Tumor Diagnosis
 
Creator Gaonkar, Raghuvir H
Ganguly, Soumya
Baishya, Rinku
Dewanjee, Saikat
Sinha, Samarendu
Gupta, Amit
Ganguly, Shantanu
Chatterjee Debnath, Mita
 
Subject Infectious Diseases and Immunology
 
Description In recent years the authors have reported on 99mTc(CO)3-labeled peptides that serve as carriers for biomolecules
or radiopharmaceuticals to the tumors. In continuation of that work they report the synthesis of a pentapeptide
(Met-Phe-Phe-Gly-His; pep-1), a hexapeptide (Met-Phe-Phe-Asp-Gly-His; pep-2), and a tetrapeptide (Asp-Gly-
Arg-His; pep-3) and the attachment of 3-amino-1,2,4-triazole to the b carboxylic function of the aspartic acid
unit of pep-2 and pep-3. The pharmacophores were radiolabeled in high yields with [99mTc(CO)3(H2O)3]+ metal
aqua ion, characterized for their stability in serum and saline, as well as in His solution, and found to be
substantially stable. B16F10 cell line binding studies showed favorable uptake and internalization. In vivo
behavior of the radiolabeled triazolyl peptides was assessed in mice bearing induced tumor. The 99mTc(CO)3-
triazolyl pep-3 demonstrated rapid urinary clearance and comparatively better tumor uptake. Imaging studies
showed visualization of the tumor using 99mTc(CO)3-triazolyl pep-3, but due to high abdominal background,
low delineation occurred. Based on the results further experiments will be carried out for targeting tumor with
triazolyl peptides
 
Publisher Mary Ann Liebert
 
Date 2016
 
Type Article
PeerReviewed
 
Format application/pdf
 
Identifier http://www.eprints.iicb.res.in/2516/1/cbr.2015.1915.pdf
Gaonkar, Raghuvir H and Ganguly, Soumya and Baishya, Rinku and Dewanjee, Saikat and Sinha, Samarendu and Gupta, Amit and Ganguly, Shantanu and Chatterjee Debnath, Mita (2016) Exploring the Potential of 99mTc(CO)3-Labeled Triazolyl Peptides for Tumor Diagnosis. Cancer Biotherapy and Radiopharmaceuticals, 31 (3). pp. 110-117.
 
Relation http://dx.doi.org/10.1089/cbr.2015.1915
http://www.eprints.iicb.res.in/2516/