Development of a 68Ga-labelled PET tracer for carbonic anhydrase IX-overexpressed tumors using the artificial sweetener saccharin

Un chul Shin; Jeong Su Choi; Yeon Jae Beak; Min woo Lee; Hyung Soo Kim; DalWoong Choi; Dong Gil Kim; Suhng Wook Kim

doi:10.1002/jlcr.3893

Development of a ⁶⁸Ga-labelled PET tracer for carbonic anhydrase IX-overexpressed tumors using the artificial sweetener saccharin

Un chul Shin, Jeong Su Choi, Yeon Jae Beak, Min woo Lee, Hyung Soo Kim, DalWoong Choi, Dong Gil Kim, Suhng Wook Kim^*

^*Corresponding author for this work

Research output: Contribution to journal › Article › peer-review

2 Citations (Scopus)

Abstract

In this study, we developed a saccharin (SAC)-based radiopharmaceutical (⁶⁸Ga-NOTA-SAC) and evaluated the possibility of its application as a PET tracer in the diagnosis of carbonic anhydrase IX (CA IX)-overexpressed tumors. We did a water-soluble tetrazolium assay and flow cytometry analysis to identify the cell viability decrease by SAC. The radiochemical purity and stability of ⁶⁸Ga- NOTA-SAC in human and mouse serum was greater than 98%. The small animal PET image-based radioactivity distribution of all organs decreased over time.⁶⁸Ga-NOTA-SAC presented the highest tumor-to-muscle ratio at 90 min post injection (p.i). The growth rates of tumor-to-muscle ratios of ⁶⁸Ga-NOTA-SAC were 88% at 60 min and 220% at 90 min, compared to 30 min p.i. The potential of ⁶⁸Ga-NOTA-SAC as a PET tracer is expected to contribute to the diagnostic research on CA IX-overexpressed tumors with the advantages of a relatively simple synthesis method.

Original language	English
Pages (from-to)	129-139
Number of pages	11
Journal	Journal of Labelled Compounds and Radiopharmaceuticals
Volume	64
Issue number	3
DOIs	https://doi.org/10.1002/jlcr.3893
Publication status	Published - 2021 Mar

Bibliographical note

Funding Information:
This work was supported by Kyung‐In Synthetic Corporation (KISCO) and a Korea University Grant.

Publisher Copyright:
© 2020 The Authors. Journal of Labelled Compounds and Radiopharmaceuticals published by John Wiley & Sons Ltd

Keywords

Carbonic anhydrase IX
Ga-NOTA-SAC
PET tracer
Saccharin
U87MG

ASJC Scopus subject areas

Analytical Chemistry
Biochemistry
Radiology Nuclear Medicine and imaging
Drug Discovery
Spectroscopy
Organic Chemistry

Access to Document

10.1002/jlcr.3893

Cite this

@article{005a6d0d11e44279bf7f62cc025a2481,

title = "Development of a 68Ga-labelled PET tracer for carbonic anhydrase IX-overexpressed tumors using the artificial sweetener saccharin",

abstract = "In this study, we developed a saccharin (SAC)-based radiopharmaceutical (68Ga-NOTA-SAC) and evaluated the possibility of its application as a PET tracer in the diagnosis of carbonic anhydrase IX (CA IX)-overexpressed tumors. We did a water-soluble tetrazolium assay and flow cytometry analysis to identify the cell viability decrease by SAC. The radiochemical purity and stability of 68Ga- NOTA-SAC in human and mouse serum was greater than 98\%. The small animal PET image-based radioactivity distribution of all organs decreased over time.68Ga-NOTA-SAC presented the highest tumor-to-muscle ratio at 90 min post injection (p.i). The growth rates of tumor-to-muscle ratios of 68Ga-NOTA-SAC were 88\% at 60 min and 220\% at 90 min, compared to 30 min p.i. The potential of 68Ga-NOTA-SAC as a PET tracer is expected to contribute to the diagnostic research on CA IX-overexpressed tumors with the advantages of a relatively simple synthesis method.",

keywords = "Carbonic anhydrase IX, Ga-NOTA-SAC, PET tracer, Saccharin, U87MG",

author = "Shin, \{Un chul\} and Choi, \{Jeong Su\} and Beak, \{Yeon Jae\} and Lee, \{Min woo\} and Kim, \{Hyung Soo\} and DalWoong Choi and Kim, \{Dong Gil\} and Kim, \{Suhng Wook\}",

note = "Funding Information: This work was supported by Kyung‐In Synthetic Corporation (KISCO) and a Korea University Grant. Publisher Copyright: {\textcopyright} 2020 The Authors. Journal of Labelled Compounds and Radiopharmaceuticals published by John Wiley \& Sons Ltd",

year = "2021",

month = mar,

doi = "10.1002/jlcr.3893",

language = "English",

volume = "64",

pages = "129--139",

journal = "Journal of Labelled Compounds and Radiopharmaceuticals",

issn = "0362-4803",

publisher = "John Wiley and Sons Ltd",

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T1 - Development of a 68Ga-labelled PET tracer for carbonic anhydrase IX-overexpressed tumors using the artificial sweetener saccharin

AU - Shin, Un chul

AU - Choi, Jeong Su

AU - Beak, Yeon Jae

AU - Lee, Min woo

AU - Kim, Hyung Soo

AU - Choi, DalWoong

AU - Kim, Dong Gil

AU - Kim, Suhng Wook

N1 - Funding Information: This work was supported by Kyung‐In Synthetic Corporation (KISCO) and a Korea University Grant. Publisher Copyright: © 2020 The Authors. Journal of Labelled Compounds and Radiopharmaceuticals published by John Wiley & Sons Ltd

PY - 2021/3

Y1 - 2021/3

N2 - In this study, we developed a saccharin (SAC)-based radiopharmaceutical (68Ga-NOTA-SAC) and evaluated the possibility of its application as a PET tracer in the diagnosis of carbonic anhydrase IX (CA IX)-overexpressed tumors. We did a water-soluble tetrazolium assay and flow cytometry analysis to identify the cell viability decrease by SAC. The radiochemical purity and stability of 68Ga- NOTA-SAC in human and mouse serum was greater than 98%. The small animal PET image-based radioactivity distribution of all organs decreased over time.68Ga-NOTA-SAC presented the highest tumor-to-muscle ratio at 90 min post injection (p.i). The growth rates of tumor-to-muscle ratios of 68Ga-NOTA-SAC were 88% at 60 min and 220% at 90 min, compared to 30 min p.i. The potential of 68Ga-NOTA-SAC as a PET tracer is expected to contribute to the diagnostic research on CA IX-overexpressed tumors with the advantages of a relatively simple synthesis method.

AB - In this study, we developed a saccharin (SAC)-based radiopharmaceutical (68Ga-NOTA-SAC) and evaluated the possibility of its application as a PET tracer in the diagnosis of carbonic anhydrase IX (CA IX)-overexpressed tumors. We did a water-soluble tetrazolium assay and flow cytometry analysis to identify the cell viability decrease by SAC. The radiochemical purity and stability of 68Ga- NOTA-SAC in human and mouse serum was greater than 98%. The small animal PET image-based radioactivity distribution of all organs decreased over time.68Ga-NOTA-SAC presented the highest tumor-to-muscle ratio at 90 min post injection (p.i). The growth rates of tumor-to-muscle ratios of 68Ga-NOTA-SAC were 88% at 60 min and 220% at 90 min, compared to 30 min p.i. The potential of 68Ga-NOTA-SAC as a PET tracer is expected to contribute to the diagnostic research on CA IX-overexpressed tumors with the advantages of a relatively simple synthesis method.

KW - Carbonic anhydrase IX

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KW - PET tracer

KW - Saccharin

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