Synthesis, Characterization and Radiolabeling of Bortezomib with 99mTC
European Journal of Biophysics
Volume 3, Issue 3-1, June 2015, Pages: 11-14
Received: Apr. 30, 2015;
Accepted: May 1, 2015;
Published: Jul. 14, 2015
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Ravi Ranjan Kumar, Department of Biophysics, Post Graduate Institute of Medical Education and Research (PGIMER), Chandigarh, India; Centre for Nuclear Medicine, Panjab University, Chandigarh, India
Devinder Kumar Dhawan, Centre for Nuclear Medicine, Panjab University, Chandigarh, India
Anshoo Malhotra, Department of Biophysics, Post Graduate Institute of Medical Education and Research (PGIMER), Chandigarh, India
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The development of new specific diagnostic radiopharmaceutical is the need of the hour for the timely management of cancer patients. At present, available radiopharmaceuticals are not much specific for tumor imaging. The present study was conducted to radiolabel bortezomib with technetium-99m ([99m]Tc). Labelling was performed by both direct as well as indirect methods and the developed radiotracer was subjected to quality control tests. The labelling efficiency of [99m]Tc-bortezomib was estimated to be more than 39%. with direct method. On the other hand, indirect method using protein albumin as ligand resulted in net binding of 41 %. The present study resulted in successfully labelling of target specific anticancer drug Bortezomib by both direct as well as indirect methods. This newly developed radiotracer has promising avenues for early detection of deadly disease of cancer. The radiotracer, however, needs further validation through animal experimentation and clinical studies.
Bortezomib, Albumin, Direct Labelling, Indirect Labelling, 99mTC
To cite this article
Ravi Ranjan Kumar,
Devinder Kumar Dhawan,
Synthesis, Characterization and Radiolabeling of Bortezomib with 99mTC, European Journal of Biophysics. Special Issue: Recent Perspectives in Biophysics.
Vol. 3, No. 3-1,
2015, pp. 11-14.
Gerber DE. Targeted Therapies. American Family Physician 2008 77(3): 311-319.
Bonvini P, Zorzi E, Basso G, Rosolen A. Bortezomib-mediated 26S proteasome inhibition causes cell-cycle arrest and induces apoptosis in CD-30+ anaplastic large cell lymphoma. Leukemia 2007; 21 (4): 838–42.
Feng-Ting Liu, Samir G, Agrawal I Zanyar Movasaghi et al. Dietary flavonoids inhibit the anticancer effects of the proteasome inhibitor bortezomib. Blood 2008;112(9): 3835-3846.
Montagut C, Rovira A, Albanell J. The proteasome: a novel target for anticancer therapy. Clinical Translational Oncology 2006; 8(5):313-7.
Rajkumar SV, Richardson P, Hideshima T. Proteasome inhibition as a novel therapeutic target in human cancer. Journal of Clinical Oncology 2005; 23:630-9.
Mujtaba T, Dou QP.Advances in the understanding of mechanisms and therapeutic use of bortezomib. Discov Med. 2011 Dec;12(67):471-80.
Cvek B. Proteasome inhibitors. Prog Mol Biol Transl Sci. 2012;109:161-226.
Costa DL. Albuquerque AC, Camacho ACLF, Costa FCH. Studying Of The Biological Effects Of Stannous Chloride On The Cell Membrane. New York Science Journal 2010;3(7).
Carter and Ho, Structure of serum albumin. Adv Protein Chem 45 (1994) 153-203.
Gradishar WJ, Tjulandin S, Davidson N, Shaw H, Desai N, Bhar P, et al. Phase III trial of nanoparticle albumin-bound paclitaxel compared with polyethylated castor oil-based paclitaxel in women with breast cancer. J Clin Oncol. 2005;23:7794–7803.
Desai N, Trieu V, Yao Z, Louie L, Ci S, Yang A, et al. Increased antitumor activity, intratumor paclitaxel concentrations, and endothelial cell transport of cremophor-free, albumin-bound paclitaxel, ABI-007, compared with cremophor-based paclitaxel. Clin Cancer Res. 2006;12:1317–1324.
KumarP, Singh B, Sharma S, Mittal BR. Evaluation of [99m]Tc-Labeled Doxorubicin as a Potential Scintigraphic Probe for Tumor Imaging. Cancer Bio and radiophar 2012;27(3): 221-26.