2018 Fiscal Year Annual Research Report
Stabilized peptide targeting programmed death-ligand 1 for Positron Emission Tomography imaging and cancer immunotherapy
| Project/Area Number |
18H06217
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| Research Institution | National Institutes for Quantum and Radiological Science and Technology |
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Principal Investigator |
胡 寛 国立研究開発法人量子科学技術研究開発機構, 放射線医学総合研究所 標識薬剤開発部, 博士研究員(任常) (00827678)
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| Project Period (FY) |
2018-08-24 – 2020-03-31
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| Keywords | stabilized peptide / PD-L1 / PET imaging |
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| Outline of Annual Research Achievements |
I developed a native peptide-based PET tracer for imaging tumor PD-L1 for the first time. I labeled the peptide with 18F and 64Cu. Moreover, the peptide was pegylated to form PEG-peptide conjugates via an optimum ‘one-pot’ strategy. The as-made radiotracers were evaluated for stability and specificity in vitro and imaged in normal mice and in a tumor model. As consequence, the 64Cu labeled compounds showed preferable imaging potential in vivo. Furthermore, the pegylation was demonstrated to change the pharmacokinetics and biodistribution of the tracers. Our studies suggested that native peptide-based tracers are capable of PD-L1 imaging, further improvement of the performance via rational design and exactly under current investigation.These results were published in Chem Commun.
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| Research Progress Status |
平成30年度が最終年度であるため、記入しない。
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| Strategy for Future Research Activity |
平成30年度が最終年度であるため、記入しない。
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[Journal Article] Design, Synthesis, and Evaluation of Reversible and Irreversible Monoacylglycerol Lipase Positron Emission Tomography (PET) Tracers Using a “Tail Switching” Strategy on a Piperazinyl Azetidine Skeleton2019
Author(s)
Z.Chen, W.Mori, X.Deng, R.Cheng, K.Dahl, H.Fu, A.Hatori, T.Shao, Y. Zhang, T. Yamasaki, X. Zhang, J. Rong, Q. Yu, K. Hu, M. Fujinaga, L.Xie, K.Kumata, Y.Gou, J.Chen, S.Gu, L. Bao, L.Wang, T. L.Collier, N. Vasdev, Y. Shao, J.-A.Ma, B.F.Cravatt, C.Fowler, L.Josephson, M.-R.Zhang, S.H.Liang
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Journal Title
Jounal of Medicinal Chemistry
Volume: 62
Pages: 3336-3353
DOI
Peer Reviewed / Int'l Joint Research
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