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  • [Bioorg Med Chem Lett.] Radiolabeling and preliminary biodistribution study of 99mTc-labeled antibody-mimetic scaffold protein repebody for initial clearance properties

    KAERI, KAIST / SajidMushtaq, 이동은*, 김학성*

  • 출처
    Bioorg Med Chem Lett.
  • 등재일
    2017 Nov 15
  • 저널이슈번호
    27(22):5060-5064.
  • 내용

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    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 (His6)-tag bearing repebody (rEgH9) was labeled with [99mTc]-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.

     

     

    Author information

    Mushtaq S1, Rho JK2, Kang JA2, Lee JJ3, Kim JY4, Nam YR2, Yun SJ2, Lee GH2, Park SH2, Lee DE5, Kim HS6.

    1 Advanced Radiation Technology Institute, Korea Atomic Energy Research Institute (KAERI), Jeongeup, Jeonbuk 580-185, Republic of Korea; Department of Radiation Biotechnology and Applied Radioisotope Science, Korea University of Science and Technology (UST), Daejeon 305-350, Republic of Korea.
    2 Advanced Radiation Technology Institute, Korea Atomic Energy Research Institute (KAERI), Jeongeup, Jeonbuk 580-185, Republic of Korea.
    3 Department of Biological Sciences, Korea Advance Institute of Science and Technology (KAIST), Daejeon 34141, Republic of Korea; Department of Biochemistry, College of Natural Sciences, Kangwon National University, Chuncheon 24341, Republic of Korea.
    4 Department of RI-Convergence Research, Korea Institute of Radiological and Medical Sciences, Seoul, Republic of Korea.
    5 Advanced Radiation Technology Institute, Korea Atomic Energy Research Institute (KAERI), Jeongeup, Jeonbuk 580-185, Republic of Korea. Electronic address: delee@kaeri.re.kr.
    6 Department of Biological Sciences, Korea Advance Institute of Science and Technology (KAIST), Daejeon 34141, Republic of Korea. Electronic address: hskim76@kaist.ac.kr.

  • 키워드
    (99m)Tc labeling; Biodistribution study; Repebody protein; SPECT imaging; Tumor imaging
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