Radiolabeling and preliminary biodistribution study of Tc-99m-labeled antibody-mimetic scaffold protein repebody for initial clearance properties

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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 [Tc-99m]-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. (C) 2017 Elsevier Ltd. All rights reserved.
Publisher
PERGAMON-ELSEVIER SCIENCE LTD
Issue Date
2017-11
Language
English
Article Type
Article
Keywords

IN-VIVO EVALUATION; AFFIBODY MOLECULES; TC(I)-CARBONYL COMPLEX; ANTI-HER2 AFFIBODY; HER2 EXPRESSION; CANCER; TUMORS; VISUALIZATION; INTERLEUKIN-6; ACCUMULATION

Citation

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.27, no.22, pp.5060 - 5064

ISSN
0960-894X
DOI
10.1016/j.bmcl.2017.09.047
URI
http://hdl.handle.net/10203/227198
Appears in Collection
BS-Journal Papers(저널논문)
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