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

  • Mushtaq, Sajid
  • Rho, Jong Kook
  • Kang, Jung Ae
  • Lee, Joong-Jae
  • Kim, Jung Young
  • 외 6명
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초록

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.

키워드

Tc-99m labelingRepebody proteinSPECT imagingBiodistribution studyTumor imagingIN-VIVO EVALUATIONAFFIBODY MOLECULESTC(I)-CARBONYL COMPLEXANTI-HER2 AFFIBODYHER2 EXPRESSIONCANCERTUMORSVISUALIZATIONINTERLEUKIN-6ACCUMULATION
제목
Radiolabeling and preliminary biodistribution study of <SUP>99m</SUP>Tc-labeled antibody-mimetic scaffold protein repebody for initial clearance properties
저자
Mushtaq, SajidRho, Jong KookKang, Jung AeLee, Joong-JaeKim, Jung YoungNam, You ReeYun, Seong-JaeLee, Gyeong HeePark, Sang HyunLee, Dong-EunKim, Hak-Sung
DOI
10.1016/j.bmcl.2017.09.047
발행일
2017-11-15
유형
Article
저널명
Bioorganic & Medicinal Chemistry Letters
27
22
페이지
5060 ~ 5064