A radiogallium-DOTA-based bivalent peptidic ligand targeting a chemokine receptor, CXCR4, for tumor imaging

Kohei Sano, Ryo Masuda, Hayato Hisada, Shinya Oishi, Kenta Shimokawa, Masahiro Ono, Nobutaka Fujii, Hideo Saji, Takahiro Mukai

研究成果: Article

3 引用 (Scopus)

抄録

We have developed a novel radiogallium (Ga)-DOTA-based bivalent peptidic ligand targeting a chemokine receptor, CXCR4, for tumor imaging. A CXCR4 imaging probe with two CXCR4 antagonists (Ac-TZ14011) on Ga-DOTA core, Ga-DOTA-TZ2, was synthesized, and the affinity and binding to CXCR4 was evaluated in CXCR4 expressing cells in vitro. The affinity of Ga-DOTA-TZ2 for CXCR4 was 20-fold greater than the corresponding monovalent probe, Ga-DOTA-TZ1. 67Ga-DOTA-TZ2 showed the significantly higher accumulation in CXCR4-expressing tumor cells compared with 67Ga-DOTA-TZ1, suggesting the bivalent effect enhances its binding to CXCR4. The incorporation of two CXCR4 antagonists to Ga-DOTA could be effective in detecting CXCR4-expressing tumors.

元の言語English
ページ(範囲)1386-1388
ページ数3
ジャーナルBioorganic and Medicinal Chemistry Letters
24
発行部数5
DOI
出版物ステータスPublished - 2014 3 1
外部発表Yes

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Chemokine Receptors
Tumors
Ligands
Imaging techniques
Neoplasms
Cells

ASJC Scopus subject areas

  • Pharmaceutical Science
  • Drug Discovery
  • Organic Chemistry
  • Molecular Medicine
  • Molecular Biology
  • Clinical Biochemistry
  • Biochemistry

これを引用

A radiogallium-DOTA-based bivalent peptidic ligand targeting a chemokine receptor, CXCR4, for tumor imaging. / Sano, Kohei; Masuda, Ryo; Hisada, Hayato; Oishi, Shinya; Shimokawa, Kenta; Ono, Masahiro; Fujii, Nobutaka; Saji, Hideo; Mukai, Takahiro.

:: Bioorganic and Medicinal Chemistry Letters, 巻 24, 番号 5, 01.03.2014, p. 1386-1388.

研究成果: Article

Sano, Kohei ; Masuda, Ryo ; Hisada, Hayato ; Oishi, Shinya ; Shimokawa, Kenta ; Ono, Masahiro ; Fujii, Nobutaka ; Saji, Hideo ; Mukai, Takahiro. / A radiogallium-DOTA-based bivalent peptidic ligand targeting a chemokine receptor, CXCR4, for tumor imaging. :: Bioorganic and Medicinal Chemistry Letters. 2014 ; 巻 24, 番号 5. pp. 1386-1388.
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AU - Sano, Kohei

AU - Masuda, Ryo

AU - Hisada, Hayato

AU - Oishi, Shinya

AU - Shimokawa, Kenta

AU - Ono, Masahiro

AU - Fujii, Nobutaka

AU - Saji, Hideo

AU - Mukai, Takahiro

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N2 - We have developed a novel radiogallium (Ga)-DOTA-based bivalent peptidic ligand targeting a chemokine receptor, CXCR4, for tumor imaging. A CXCR4 imaging probe with two CXCR4 antagonists (Ac-TZ14011) on Ga-DOTA core, Ga-DOTA-TZ2, was synthesized, and the affinity and binding to CXCR4 was evaluated in CXCR4 expressing cells in vitro. The affinity of Ga-DOTA-TZ2 for CXCR4 was 20-fold greater than the corresponding monovalent probe, Ga-DOTA-TZ1. 67Ga-DOTA-TZ2 showed the significantly higher accumulation in CXCR4-expressing tumor cells compared with 67Ga-DOTA-TZ1, suggesting the bivalent effect enhances its binding to CXCR4. The incorporation of two CXCR4 antagonists to Ga-DOTA could be effective in detecting CXCR4-expressing tumors.

AB - We have developed a novel radiogallium (Ga)-DOTA-based bivalent peptidic ligand targeting a chemokine receptor, CXCR4, for tumor imaging. A CXCR4 imaging probe with two CXCR4 antagonists (Ac-TZ14011) on Ga-DOTA core, Ga-DOTA-TZ2, was synthesized, and the affinity and binding to CXCR4 was evaluated in CXCR4 expressing cells in vitro. The affinity of Ga-DOTA-TZ2 for CXCR4 was 20-fold greater than the corresponding monovalent probe, Ga-DOTA-TZ1. 67Ga-DOTA-TZ2 showed the significantly higher accumulation in CXCR4-expressing tumor cells compared with 67Ga-DOTA-TZ1, suggesting the bivalent effect enhances its binding to CXCR4. The incorporation of two CXCR4 antagonists to Ga-DOTA could be effective in detecting CXCR4-expressing tumors.

KW - Bivalent effect

KW - CXCR4

KW - DOTA

KW - Radiogallium

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