Radiosynthesis and evaluation of tumor cell-penetrating oligopeptides containing short-lived positron-emitt ing radionuclides
Project/Area Number |
26861031
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Research Category |
Grant-in-Aid for Young Scientists (B)
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Allocation Type | Multi-year Fund |
Research Field |
Radiation science
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Research Institution | National Institutes for Quantum and Radiological Science and Technology |
Principal Investigator |
Hanyu Masayuki 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, 研究員(任常) (80435552)
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Project Period (FY) |
2014-04-01 – 2017-03-31
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Project Status |
Completed (Fiscal Year 2016)
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Budget Amount *help |
¥3,770,000 (Direct Cost: ¥2,900,000、Indirect Cost: ¥870,000)
Fiscal Year 2015: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
Fiscal Year 2014: ¥2,210,000 (Direct Cost: ¥1,700,000、Indirect Cost: ¥510,000)
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Keywords | PETイメージング / オリゴペプチド / ピクテスペングラー反応 / PET / 標識反応 / 標識合成 |
Outline of Final Research Achievements |
A procedure for the synthesis of a carbon-11 labeled oligopeptide containing [1-11C]1,2,3,4-tetrahydro-beta-carboline-3-carboxylic acid ([1-11C]Tpi) from the corresponding Trp・HCl-containing peptides has been developed involving a Pictet-Spengler reaction with [11C]formaldehyde. The radiolabeling of a Trp・HCl-containing iRGD peptide using the Pictet-Spengler reaction was successful. Furthermore, the remote-controlled synthesis of a [1-11C]Tpi-containing iRGD (1) peptide was attempted using an automatic production system to generate [11C]CH3I. The radiochemical yield of the compound 1 at the end of synthesis was 4.2 ± 3.2 % (n=3), for a total synthesis time of about 35 min. The usefulness of our synthesis was demonstrated PET studies using the compound 1 for the mouse bearing MIAPaca-2 and BxPC-3, a small cell pancreatic cancer cell line. The BxPC-3 cell-to-muscle and MIAPaca-2 cell-to-muscle of 1 at 22 min were not retained.
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Report
(4 results)
Research Products
(15 results)
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[Journal Article] High-contrast PET imaging of vasopressin V1B receptors with a novel radioligand, 11C-TASP6992017
Author(s)
Kazumi Koga, Yugi Nagai, Masayuki Hanyu, Mitsukane Yoshinaga, Shigeyuki Chaki, Norikazu Ohtake, Satoshi Ozaki, Ming-Rong Zhang, Tetsuya Suhara, Makoto HIguchi
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Journal Title
Journal of Nuclear Medicine
Volume: -
Issue: 10
Pages: 1652-1658
DOI
Related Report
Peer Reviewed
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[Journal Article] Synthesis and Evaluation of [64Cu]PSMA-617 Targeted for Prostate-Specific Membrane Antigen in Prostate Cancer2017
Author(s)
Can Cui, Masayuki Hanyu, Akiko Hatori, Yiding Zhang, Lin Xie, Tomoyuki Ohya, Masami Fukada, Hisashi Suzuki, Kotaro Nagatsu, Cuiping Jiang, Rui Luo, Guoqiang Shao, Ming-Rong Zhang, Feng Wang
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Journal Title
American Journal of Nuclear Medicine and Molecular Imaging
Volume: 7
Pages: 40-52
Related Report
Peer Reviewed / Int'l Joint Research
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[Journal Article] Radiosynthesis and quality control of [11C]TASP457 as a clinically useful PET ligand for imaging of histamine H3 receptors in human brain2016
Author(s)
Masayuki Hanyu, Kazunori Kawamura, Makoto Takei, Kenji Furutsuka, Satoshi Shiomi, Tomoya Fujishiro, Masanao Ogawa, Nobuki Nengaki, Hiroki Hashimoto, Toshimitsu Fukumura, Ming-Rong Zhang
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Journal Title
Nuclear Medicine and Biology
Volume: 43
Issue: 11
Pages: 679-684
DOI
Related Report
Peer Reviewed
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[Journal Article] Development of TASP0410457 (TASP457), a novel dihydroquinolinone derivative as a PET radioligand for central histamine H3 receptors2016
Author(s)
Kazumi Koga, Jun Maeda, Masaki Tokunaga, Masayuki Hanyu, Kazunori Kawamura, Mari Ohmichi, Toshio Nakamura, Yuji Nagai, Chie Seki, Yasuyuki Kimura, Takafumi Minamimoto, Ming-Rong Zhang, Toshimitsu Fukumura, Tetsuya Suhara, Makoto Higuchi
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Journal Title
EJNMMI Research
Volume: 6
Issue: 1
Pages: 1-14
DOI
Related Report
Peer Reviewed / Open Access
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