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 |
| 巻 | 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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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
}
TY - JOUR
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
UR - http://www.scopus.com/inward/record.url?scp=84894591288&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=84894591288&partnerID=8YFLogxK
U2 - 10.1016/j.bmcl.2014.01.031
DO - 10.1016/j.bmcl.2014.01.031
M3 - Article
C2 - 24491461
AN - SCOPUS:84894591288
VL - 24
SP - 1386
EP - 1388
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
SN - 0960-894X
IS - 5
ER -