Improved Pharmacokinetics Following PEGylation and Dimerization of a c(RGD-ACH-K) Conjugate Used for Tumor Positron Emission Tomography Imaging
- Authors
- Lee, Ji Woong; Lee, Yong Jin; Shin, Un Chol; Kim, Suhng Wook; Kim, Byung Il; Lee, Kyo Chul; Kim, Jung Young; Park, Ji-Ae
- Issue Date
- 10월-2016
- Publisher
- MARY ANN LIEBERT, INC
- Keywords
- Cu-64; dimerization; PEGlyation; PET; RGD peptides; tumor targeting
- Citation
- CANCER BIOTHERAPY AND RADIOPHARMACEUTICALS, v.31, no.8, pp.295 - 301
- Indexed
- SCIE
SCOPUS
- Journal Title
- CANCER BIOTHERAPY AND RADIOPHARMACEUTICALS
- Volume
- 31
- Number
- 8
- Start Page
- 295
- End Page
- 301
- URI
- https://scholar.korea.ac.kr/handle/2021.sw.korea/87289
- DOI
- 10.1089/cbr.2016.2036
- ISSN
- 1084-9785
- 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 Ga-68 and Cu-64). 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 Cu-64-DOTA-E[c(RGD-ACH-K)](2) (complex 1) and Cu-64-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 Cu-64(NOTA) complex shows better PET imaging than that of the Cu-64(DOTA) complex, which should lead to improved dosimetry and increased suitability for noninvasive monitoring of tumor growth or tumor-targeted radionuclide therapy.
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Collections - College of Health Sciences > School of Health and Environmental Science > 1. Journal Articles
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