글로벌 연구동향
분자영상 및 방사화학
- 2016년 11월호
[Cancer Biother Radiopharm.] Improved Pharmacokinetics Following PEGylation and Dimerization of a c(RGD-ACH-K) Conjugate Used for Tumor Positron Emission Tomography Imaging.KIRAMS/ 이지웅, 박지애*
- 출처
- Cancer Biother Radiopharm.
- 등재일
- 2016 Oct
- 저널이슈번호
- 31(8):295-301.
- 내용
Abstract
Improving the in vivo pharmacokinetics (PK) of positron emission tomography (PET) radiotracers is of critical importance to tumor diagnosis and therapy. In the case of peptide-based radiotracers, the modification and addition of a linker or spacer functional group often offer faster in vivo pharmacokinetic behavior. In this study, the authors introduced two new PEGlyated dimeric c(RGD-ACH-K) conjugates, in which an aminocyclohexane carboxylic acid (ACH) is inserted into the ring chain of the cyclic RGD peptides, with a common bifunctional chelator (DOTA or NOTA) used for labeling with radiometals (including 68Ga and 64Cu). The addition of polyethylene glycol (PEG) and dimerization of c(RGD-ACH-K) affected the PK of the renal system and the tumor-targeting ability, relative to unmodified molecule. As a result, both 64Cu-DOTA-E[c(RGD-ACH-K)]2 (complex 1) and 64Cu-NOTA-E[c(RGD-ACH-K)]2 (complex 2) exhibited specific tumor-targeting properties relative to tumor-blocking control group, most likely resulting from improved in vivo tumor imaging. The in vivo tumor-to-blood ratio of the 64Cu(NOTA) complex shows better PET imaging than that of the 64Cu(DOTA) complex, which should lead to improved dosimetry and increased suitability for noninvasive monitoring of tumor growth or tumor-targeted radionuclide therapy.
Author information
Lee JW1,2, Lee YJ1, Shin UC1, Kim SW2, Kim BI3, Lee KC1, Kim JY1, Park JA1.
11 Molecular Imaging Research Center, Korea Institute of Radiological & Medical Sciences , Seoul, Republic of Korea.
22 Department of Integrated Biomedical and Life Science, Korea University , Seoul, Republic of Korea.
33 Department of Nuclear Medicine, Korea Cancer Center Hospital , Seoul, Republic of Korea.
- 키워드
- 64Cu; PEGlyation; PET; RGD peptides; dimerization; tumor targeting
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