Abstract
Purpose: We aimed to develop a gallium-68 (Ga-68)-labeled single-chain variable fragment (scFv) targeting the human epidermal growth factor receptor 2 (HER2) to rapidly and noninvasively evaluate the status of HER2 expression.Procedures: Anti-HER2 scFv was labeled with Ga-68 by using deferoxamine (Df) as a bifunctional chelate. Biodistribution of [68Ga]Df-anti-HER2 scFv was examined with tumor-bearing mice and positron emission tomography (PET) imaging was performed. The changes in HER2 expression after anti-HER2 therapy were monitored by PET imaging.Results: [68Ga]Df-anti-HER2 scFv was obtained with high radiochemical yield after only a 5-min reaction at room temperature. The probe showed high accumulation in HER2-positive xenografts and the intratumoral distribution of radioactivity coincided with HER2-positive regions. Furthermore, [68Ga]Df-anti-HER2 scFv helped visualize HER2-positive xenografts and monitor the changes in HER2 expression after anti-HER2 therapy.Conclusion: [68Ga]Df-anti-HER2 scFv could be a promising probe to evaluate HER2 status by in vivo PET imaging, unless trastuzumab is prescribed as part of the therapy.
| Original language | English |
|---|---|
| Pages (from-to) | 102-110 |
| Number of pages | 9 |
| Journal | Molecular Imaging and Biology |
| Volume | 17 |
| Issue number | 1 |
| DOIs | |
| Publication status | Published - 2014 |
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Keywords
- 17-DMAG
- Gallium-68
- Human epidermal growth factor receptor 2(HER2)
- Positron emission tomography (PET)
- Single-chain Fv Fragment (scFv)
- Therapy
ASJC Scopus subject areas
- Cancer Research
- Oncology
- Radiology Nuclear Medicine and imaging
- Medicine(all)
Cite this
Gallium-68-Labeled Anti-HER2 Single-Chain Fv Fragment : Development and In Vivo Monitoring of HER2 Expression. / Ueda, Masashi; Hisada, Hayato; Temma, Takashi; Shimizu, Yoichi; Kimura, Hiroyuki; Ono, Masahiro; Nakamoto, Yuji; Togashi, Kaori; Saji, Hideo.
In: Molecular Imaging and Biology, Vol. 17, No. 1, 2014, p. 102-110.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - Gallium-68-Labeled Anti-HER2 Single-Chain Fv Fragment
T2 - Development and In Vivo Monitoring of HER2 Expression
AU - Ueda, Masashi
AU - Hisada, Hayato
AU - Temma, Takashi
AU - Shimizu, Yoichi
AU - Kimura, Hiroyuki
AU - Ono, Masahiro
AU - Nakamoto, Yuji
AU - Togashi, Kaori
AU - Saji, Hideo
PY - 2014
Y1 - 2014
N2 - Purpose: We aimed to develop a gallium-68 (Ga-68)-labeled single-chain variable fragment (scFv) targeting the human epidermal growth factor receptor 2 (HER2) to rapidly and noninvasively evaluate the status of HER2 expression.Procedures: Anti-HER2 scFv was labeled with Ga-68 by using deferoxamine (Df) as a bifunctional chelate. Biodistribution of [68Ga]Df-anti-HER2 scFv was examined with tumor-bearing mice and positron emission tomography (PET) imaging was performed. The changes in HER2 expression after anti-HER2 therapy were monitored by PET imaging.Results: [68Ga]Df-anti-HER2 scFv was obtained with high radiochemical yield after only a 5-min reaction at room temperature. The probe showed high accumulation in HER2-positive xenografts and the intratumoral distribution of radioactivity coincided with HER2-positive regions. Furthermore, [68Ga]Df-anti-HER2 scFv helped visualize HER2-positive xenografts and monitor the changes in HER2 expression after anti-HER2 therapy.Conclusion: [68Ga]Df-anti-HER2 scFv could be a promising probe to evaluate HER2 status by in vivo PET imaging, unless trastuzumab is prescribed as part of the therapy.
AB - Purpose: We aimed to develop a gallium-68 (Ga-68)-labeled single-chain variable fragment (scFv) targeting the human epidermal growth factor receptor 2 (HER2) to rapidly and noninvasively evaluate the status of HER2 expression.Procedures: Anti-HER2 scFv was labeled with Ga-68 by using deferoxamine (Df) as a bifunctional chelate. Biodistribution of [68Ga]Df-anti-HER2 scFv was examined with tumor-bearing mice and positron emission tomography (PET) imaging was performed. The changes in HER2 expression after anti-HER2 therapy were monitored by PET imaging.Results: [68Ga]Df-anti-HER2 scFv was obtained with high radiochemical yield after only a 5-min reaction at room temperature. The probe showed high accumulation in HER2-positive xenografts and the intratumoral distribution of radioactivity coincided with HER2-positive regions. Furthermore, [68Ga]Df-anti-HER2 scFv helped visualize HER2-positive xenografts and monitor the changes in HER2 expression after anti-HER2 therapy.Conclusion: [68Ga]Df-anti-HER2 scFv could be a promising probe to evaluate HER2 status by in vivo PET imaging, unless trastuzumab is prescribed as part of the therapy.
KW - 17-DMAG
KW - Gallium-68
KW - Human epidermal growth factor receptor 2(HER2)
KW - Positron emission tomography (PET)
KW - Single-chain Fv Fragment (scFv)
KW - Therapy
UR - http://www.scopus.com/inward/record.url?scp=84938591134&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=84938591134&partnerID=8YFLogxK
U2 - 10.1007/s11307-014-0769-5
DO - 10.1007/s11307-014-0769-5
M3 - Article
C2 - 25049073
AN - SCOPUS:84938591134
VL - 17
SP - 102
EP - 110
JO - Molecular Imaging and Biology
JF - Molecular Imaging and Biology
SN - 1536-1632
IS - 1
ER -