Exploring the Potential of (99m)Tc(CO)3-Labeled Triazolyl Peptides for Tumor Diagnosis.
In recent years the authors have reported on (99m)Tc(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 β carboxylic function of the aspartic acid unit of pep-2 and pep-3. The pharmacophores were radiolabeled in high yields with [(99m)Tc(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 (99m)Tc(CO)3-triazolyl pep-3 demonstrated rapid urinary clearance and comparatively better tumor uptake. Imaging studies showed visualization of the tumor using (99m)Tc(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.
1 Infectious Diseases and Immunology Division, CSIR-Indian Institute of Chemical Biology , Kolkata, India .
Raghuvir H
RH
Gaonkar
1 Infectious Diseases and Immunology Division, CSIR-Indian Institute of Chemical Biology , Kolkata, India .
Soumya
S
Ganguly
1 Infectious Diseases and Immunology Division, CSIR-Indian Institute of Chemical Biology , Kolkata, India .
Rinku
R
Baishya
2 Department of Pharmaceutical Technology, Jadavpur University , Kolkata, India .
Saikat
S
Dewanjee
3 Regional Radiation Medicine Center, Thakurpukur Cancer Center and Welfare Home Campus , Kolkata, India .
Samarendu
S
Sinha
3 Regional Radiation Medicine Center, Thakurpukur Cancer Center and Welfare Home Campus , Kolkata, India .
Amit
A
Gupta
3 Regional Radiation Medicine Center, Thakurpukur Cancer Center and Welfare Home Campus , Kolkata, India .
Shantanu
S
Ganguly
1 Infectious Diseases and Immunology Division, CSIR-Indian Institute of Chemical Biology , Kolkata, India .
Mita C
MC
Debnath
D000818:Animals; D002286:Carcinoma, Ehrlich Tumor / Q000175:diagnosis* / Q000378:metabolism; D039302:Integrin alphaVbeta3 / Q000378:metabolism*; D008546:Melanoma, Experimental / Q000175:diagnosis* / Q000378:metabolism; D051379:Mice; D008807:Mice, Inbred BALB C; D009842:Oligopeptides / Q000737:chemistry / Q000493:pharmacokinetics*; D015609:Organotechnetium Compounds / Q000737:chemistry / Q000493:pharmacokinetics*; D019275:Radiopharmaceuticals / Q000737:chemistry / Q000493:pharmacokinetics*; D051381:Rats; D014018:Tissue Distribution; D014230:Triazoles / Q000737:chemistry*; D014407:Tumor Cells, Cultured
D039302:Integrin alphaVbeta3; D009842:Oligopeptides; D015609:Organotechnetium Compounds; D019275:Radiopharmaceuticals; D014230:Triazoles
fac-[99mTc(CO)3(H2O)3]+ core; internalization; triazolyl peptide synthesis; tumor imaging