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

doi:10.1016/j.bmcl.2014.01.031

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

理工学術院総合研究所

研究成果: Article

3 引用（Scopus）

抜粋

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
巻	24
発行部数	5
DOI	https://doi.org/10.1016/j.bmcl.2014.01.031
出版物ステータス	Published - 2014 3 1

ASJC Scopus subject areas

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

文献にアクセス

10.1016/j.bmcl.2014.01.031

フィンガープリント A radiogallium-DOTA-based bivalent peptidic ligand targeting a chemokine receptor, CXCR4, for tumor imaging' の研究トピックを掘り下げます。これらはともに一意のフィンガープリントを構成します。

これを引用

Sano, K., Masuda, R., Hisada, H., Oishi, S., Shimokawa, K., Ono, M., Fujii, N., Saji, H., & Mukai, T. (2014). A radiogallium-DOTA-based bivalent peptidic ligand targeting a chemokine receptor, CXCR4, for tumor imaging. Bioorganic and Medicinal Chemistry Letters, 24(5), 1386-1388. https://doi.org/10.1016/j.bmcl.2014.01.031

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

abstract = "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.",

keywords = "Bivalent effect, CXCR4, DOTA, Radiogallium",

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

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T1 - A radiogallium-DOTA-based bivalent peptidic ligand targeting a chemokine receptor, CXCR4, for tumor imaging

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

PY - 2014/3/1

Y1 - 2014/3/1

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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