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Selective tyrosine conjugation with a newly synthesized PCB -TE2A-luminol bifunctional chelator
수브라므니 라즈쿠말,박현,Abhinav Bhise,조성환,김정영,이교철,유정수 대한방사성의약품학회 2021 Journal of radiopharmaceuticals and molecular prob Vol.7 No.2
Selective amino acid conjugation of bulky antibodies is a valuable asset for real-time diagnosis and therapy. However, selective conjugation incorporating a chelate-bearing radioactive atom into an antibody without affecting its immunoreactivity is a challenging task. A bifunctional chelator (BFC), a selective amino acid-targeting probe, and a linker have been developed to overcome this problem. Here, we report the synthesis of a novel propylene cross-bridged chelator (PCB)‒1,8-N,N′-bis-(carboxymethyl)-1,4,8,11-tetraazacyclotetradecane (TE2A)‒luminol BFC via a click reaction and radiolabel it with a 64Cu ion for tyrosine-selective conjugation of trastuzumab. In the initial optimization study, we tried different oxidative addition conditions such as electro-oxidation, hemin, horseradish peroxidase, iodogen tube, chloramine-T, and iodo beads. In this study, up to 82% of 64Cu-PCB-TE2A-luminol was conjugated with the antibody in an iodo bead-catalyzed oxidative addition reaction with an isolated yield of 24.4%.
Recent progress in selective bioconjugation
수브라므니 라즈쿠말,Abhinav Bhise,BOBBA KONDAPA NAIDU,유정수 대한방사성의약품학회 2020 Journal of radiopharmaceuticals and molecular prob Vol.6 No.2
Selective installation of proteins using chemical reagents is important for the development of potential biomaterials for the treatment of human diseases. However, modification in a chemo- and regioselective manner under physiological conditions is a great challenge due to the presence of multiple reactive centers in the protein. Currently, the majority of conjugations are limited to lysine (Lys)- and cysteine (Cys)-selective reagents. Thus, they have been extensively studied. Apart from Lys and Cys, widespread site selectivity has been recently achieved through most of the 20 naturally occurring amino acid-bearing reactive functional groups. Consequently, this review focused on several recent achievements in site-selective modification of the rarest amino acid backbones (e.g., methionine, serine, glutamic acid, and tyrosine).
Role of polyethylene glycol (PEG) linkers: trends in antibody conjugation and their pharmacokinetics
BOBBA KONDAPA NAIDU,Abhinav Bhise,수브라므니 라즈쿠말,이웅희,유정수 대한방사성의약품학회 2020 Journal of radiopharmaceuticals and molecular prob Vol.6 No.2
Polyethylene glycol (PEG) has been the most commonly used polymer for the past few decades in the field of biomedical applications due to its gold standard stealth effect. PEGylation of antibody–drug conjugates, liposomes, peptides, nanoparticles, and proteins is done to improve their pharmaceutical efficacy and pharmacokinetic properties. PEGylation of antibodies with various PEG linkers improves targeting ability by increasing the blood circulation time and thus enhances the biodistribution profiles. It also assists in minimizing the immediate capture by the reticuloendothelial system. In this review, we summarize the effect of PEG linkers in an antibody conjugation and their pharmacokinetics in the field of biomedical imaging.
Synthesis of a PEGylated tracer for radioiodination and evaluation of potential in tumor targeting
Abhinav Bhise,Sushil K. Dwivedi,이기웅,임정은,수브라므니 라즈쿠말,이웅희,조성환,유정수 대한방사성의약품학회 2021 Journal of radiopharmaceuticals and molecular prob Vol.7 No.2
Radiopharmaceuticals are important for tumor diagnosis and therapy. To deliver a radio-tracer at the desired target excluding non-targeted tissues is difficult. The development of a targeted tracer that has a good clearance profile while maintaining high biostability and biocompatibility is key to optimizing its biodistribution and transport across biological barriers. Improving the hydrophilicity of radiotracers by PEGylation can reduce serum binding, allowing the tracer to circulate without retention and reducing its affinity for non-targeted tissues. In this study, we synthesized a new benzamido tracer (SnBz-PEG36) with the introduction of a low molecular weight polyethylene glycol unit (PEG36, ~2100 Da). The tumor-targeting efficiency and biodistribution of [131I]-Bz-PEG36 or radiotracer-loaded liposomes were evaluated after their administration to normal mice or mouse tumor models including CT26 (xenograft) and 4T1 (xenograft and orthotopic). Most of the radiotracer was cleared out rapidly (1-24 h post-administration) through the kidney and there was little tumor uptake.