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2020 年度 実績報告書

New strategy of diagnostic imaging probes prior to administrating molecular target drugs

研究課題

研究課題/領域番号 20K16722
研究機関金沢大学

研究代表者

Effendi Nurmaya  金沢大学, 新学術創成研究機構, 特任助教 (60842911)

研究期間 (年度) 2020-04-01 – 2021-03-31
キーワードimaging / PDGFRb / EGFR / Osimertinib / Peptide
研究実績の概要

Tyrosine kinase receptors (TKRs) are transmembrane proteins consisting of the extracellular domain for ligand binding and the intracellular part for signaling. This study aims to develop radiolabeled probes targeting TKRs for imaging and therapy.
1. Seven radiotracers, 67Ga-DOTA-linker-IPLPPPRRPFFK peptides with different lengths and types of linkers, were designed, synthesized, and evaluated as platelet-derived growth factor receptor beta (PDGFRb) imaging agents. Two radiotracers were chosen based on the result of in vitro studies and continued in vivo studies. [67Ga]Ga-DOTA-EG2-IPLPPPRRPFFK and [67Ga]Ga-DOTA-EG4-IPLPPPRRPFFK showed the tumor-to-blood ratios were 2.61±0.75 and 2.05±0.77, respectively at 1h post-injection. Co-injection of [67Ga]Ga-DOTA-EG2-IPLPPPRRPFFK and an excess amount of IPLPPPRRPFFK peptide as a blocking agent can significantly decrease this ratio. However, tumor accumulation was not considered sufficient. Therefore, further probe modification is required to assess tumor accumulation for in vivo imaging.
2. The aim of this study is developing radiohalogenated-Osimertinib conjugated with a recombinant human IgG1 mAb Necitumumab and/or its fragment Necitumumab-derived Fab, which possess high binding affinity and specificity toward EGFR. In the first year, Osimertinib, Br-Osimertinib, I-Osimertinib, and three enzyme-cleavable linkers (Mc-Val-Cit-PABOH, Mc-Val-Ala-PABOH, and Mc-Phe-Ala-PABOH) were prepared.

  • 研究成果

    (1件)

すべて 2020

すべて 雑誌論文 (1件) (うち国際共著 1件、 オープンアクセス 1件)

  • [雑誌論文] Development of Radiogallium-Labeled Peptides for Platelet-Derived Growth Factor Receptor β (PDGFRβ) Imaging: Influence of Different Linkers2020

    • 著者名/発表者名
      Effendi Nurmaya、Mishiro Kenji、Shiba Kazuhiro、Kinuya Seigo、Ogawa Kazuma
    • 雑誌名

      Molecules

      巻: 26 ページ: 1~13

    • DOI

      10.3390/molecules26010041

    • オープンアクセス / 国際共著

URL: 

公開日: 2021-12-27  

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