1. Radiolabeling and preliminary biodistribution study of 99m Tc-labeled antibody-mimetic scaffold protein repebody for initial clearance properties.
- Author
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Mushtaq S, Rho JK, Kang JA, Lee JJ, Kim JY, Nam YR, Yun SJ, Lee GH, Park SH, Lee DE, and Kim HS
- Subjects
- Administration, Intravenous, Animals, Antibodies chemistry, Antibodies metabolism, Infusions, Parenteral, Isotope Labeling, Kidney diagnostic imaging, Kidney metabolism, Leucine chemistry, Leucine metabolism, Mice, Mice, Inbred BALB C, Proteins metabolism, Radiopharmaceuticals pharmacokinetics, Tissue Distribution, Tomography, Emission-Computed, Single-Photon, Proteins chemistry, Radiopharmaceuticals chemistry, Technetium chemistry
- Abstract
Antibody-mimetic proteins are intensively being developed for biomedical applications including tumor imaging and therapy. Among them, repebody is a new class of protein that consists of highly diverse leucine-rich repeat (LRR) modules. Although all possible biomedical applications with repebody are ongoing, it's in vivo biodistribution and excretion pathway has not yet been explored. In this study, hexahistidine (His
6 )-tag bearing repebody (rEgH9) was labeled with [99m Tc]-tricarbonyl, and biodistribution was performed following intravenous (I.V.) or intraperitoneal (I.P.) injection. Repebody protein was radiolabeled with high radiolabeling efficiency (>90%) and radiolabeled compound was more than 99% pure after purification. Biodistribution data indicates radiotracer has a rapid clearance from blood and excreted through the kidneys for intravenous (I.V.) injection, but comparatively slow clearance for an intraperitoneal (I.P.) injection. SPECT-CT images were found to be in agreement with biodistribution data, high activity was found inside kidneys. The observed result for rapid blood clearance and renal excretion of repebody (rEgH9) provide useful information for the further development of therapeutic strategy., (Copyright © 2017 Elsevier Ltd. All rights reserved.)- Published
- 2017
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