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Medical application of radiohalogenated peptides; Synthesis and ${it in vitro}$ evaluation of F(${it p}$-$$^{131}$$I)KCCYSL for targeting HER2

放射性ハロゲン標識ペプチドの医学的応用; HER2を標的としたF(${it p}$-$$^{131}$$I)KCCYSLの合成と${it in vitro}$評価

佐々木 一郎; 渡辺 茂樹; 大島 康宏; 須郷 由美; 山田 圭一*; 花岡 宏史*; 石岡 典子

Sasaki, Ichiro; Watanabe, Shigeki; Ohshima, Yasuhiro; Sugo, Yumi; Yamada, Keiichi*; Hanaoka, Hirofumi*; Ishioka, Noriko

Radioisotope labeled peptides with high affinity to receptors overexpressing on the surface of tumor cells are promising for applications in nuclear medicine such as diagnostic radiography and radiotherapy. Radiohalogens such as $$^{131}$$I and $$^{211}$$At are useful for clinical imaging and therapeutic applications, and it can be introduced at the ${it para}$ position of phenylalanine residue via electrophilic destannylation. KCCYSL (Lys$$^{1}$$-Cys$$^{2}$$-Cys$$^{3}$$-Tyr$$^{4}$$-Ser$$^{5}$$-Leu$$^{6}$$) is a hexapeptide containing disulfide bond. Previous study revealed that KCCYSL has potential as tumor imaging and therapeutic agent targeting tumor cells overexpressing the human epidermal growth factor receptor type 2 (HER2). In this study, we report synthesis and ${it in vitro}$ evaluation of radiohalogenated KCCYSL derivatives. Precursor peptides, Boc-F(${it p}$-SnBu$$_{3}$$)K(Boc)C(Trt)C(Trt)Y($$^{t}$$Bu)S($$^{t}$$Bu)L-OH and Boc-F(${it p}$-SnBu$$_{3}$$)GS($$^{t}$$Bu)GK(Boc)C(Trt)C(Trt)Y($$^{t}$$Bu)S($$^{t}$$Bu)L-OH, were synthesized by the Fmoc solid phase peptide synthesis. Then, precursor peptides were radioiodinated via electrophilic destannylation, and they were deprotected to obtain F(${it p}$-$$^{131}$$I)KCCYSL and F(${it p}$-$$^{131}$$I)GSGKCCYSL in radiochemical yield 15% and 17%, respectively. ${it In vitro}$ assays of the radioiodinated peptides for HER2 and stability in serum are being undertaken.

使用言語

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English

掲載資料名

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Peptide Science 2015

巻

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号

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ページ数

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p.243 - 246

発行年月

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2016/03

発表会議名

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第52回ペプチド討論会

開催年月

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2015/11

開催都市

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平塚

開催国

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日本

キーワード

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nuclear medicine; radiohalogen; peptide; HER2; synthesis; electrophilic destannylation; in vitro evaluation

特許データ

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PDF

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論文URL

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この論文を読む・探す

研究データの公開先DOI

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使用施設

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TIARA(イオン照射研究施設)

広報プレスリリース

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論文解説記事
(成果普及情報誌)

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受委託・共同研究相手機関

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群馬大学

Access

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- Accesses

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