18 F-Radiolabeling and Evaluation of an AMD3465 Derivative for PET Imaging of CXCR4 in a Mouse Breast Tumor Model
The exploration of pharmaceutically active agents and positron emission tomography (PET) tracers targeting CXCR4 has been a focal point in cancer research given its pivotal role in the development and progression of various cancers. While significant strides have been made in PET imaging with radiom...
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| Veröffentlicht in: | Bioconjugate chemistry 2024-05, Vol.35 (5), p.567-574 |
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| container_title | Bioconjugate chemistry |
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| creator | Li, Huiqiang Li, Xiaochen Sun, Lingyi He, Yanjie Wang, Li Gao, Yongju Zeng, Dexing Pang, Xinchang Xu, Junling |
| description | The exploration of pharmaceutically active agents and positron emission tomography (PET) tracers targeting CXCR4 has been a focal point in cancer research given its pivotal role in the development and progression of various cancers. While significant strides have been made in PET imaging with radiometal-labeled tracers, the landscape of
F-labeled small molecule tracers remains relatively limited. Herein, we introduce a novel and promising derivative, [
F]SFB-AMD3465, as a targeted PET tracer for CXCR4. The compound was synthesized by modifying the pyridine ring of AMD3465, which was subsequently labeled with
F using [
F]SFB. The study provides comprehensive insights into the design, synthesis, and biological evaluation of [
F]SFB-AMD3465.
and
assessments demonstrated the CXCR4-dependent, specific, and sensitive uptake of [
F]SFB-AMD3465 in the CXCR4-overexpressing 4T1 cell line and the corresponding xenograft-bearing mouse model. These findings contribute to bridging the gap in
F-labeled PET tracers for CXCR4 and underscore the potential of [
F]SFB-AMD3465 as a PET radiotracer for
CXCR4 imaging. |
| doi_str_mv | 10.1021/acs.bioconjchem.4c00167 |
| format | Article |
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F-labeled small molecule tracers remains relatively limited. Herein, we introduce a novel and promising derivative, [
F]SFB-AMD3465, as a targeted PET tracer for CXCR4. The compound was synthesized by modifying the pyridine ring of AMD3465, which was subsequently labeled with
F using [
F]SFB. The study provides comprehensive insights into the design, synthesis, and biological evaluation of [
F]SFB-AMD3465.
and
assessments demonstrated the CXCR4-dependent, specific, and sensitive uptake of [
F]SFB-AMD3465 in the CXCR4-overexpressing 4T1 cell line and the corresponding xenograft-bearing mouse model. These findings contribute to bridging the gap in
F-labeled PET tracers for CXCR4 and underscore the potential of [
F]SFB-AMD3465 as a PET radiotracer for
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F-labeled small molecule tracers remains relatively limited. Herein, we introduce a novel and promising derivative, [
F]SFB-AMD3465, as a targeted PET tracer for CXCR4. The compound was synthesized by modifying the pyridine ring of AMD3465, which was subsequently labeled with
F using [
F]SFB. The study provides comprehensive insights into the design, synthesis, and biological evaluation of [
F]SFB-AMD3465.
and
assessments demonstrated the CXCR4-dependent, specific, and sensitive uptake of [
F]SFB-AMD3465 in the CXCR4-overexpressing 4T1 cell line and the corresponding xenograft-bearing mouse model. These findings contribute to bridging the gap in
F-labeled PET tracers for CXCR4 and underscore the potential of [
F]SFB-AMD3465 as a PET radiotracer for
CXCR4 imaging.</description><issn>1043-1802</issn><issn>1520-4812</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2024</creationdate><recordtype>article</recordtype><recordid>eNpNkMtOwzAQRS0EolD4BfAPpPiVOF6WPqBSK1CVBbvIsSclVRKXuKnE3-OqBbGa0Z17ZnEQeqRkRAmjT9r4UVE549qt-YRmJAwhNJEX6IbGjEQipewy7ETwiKaEDdCt91tCiKIpu0YDniZcxDS5QV80xfNorW3lal1AXbUbrFuLZwdd93pfuRa7MiR4vJpykcR4Cl11CIcD4NJ1-H2W4UWjN0cuFCcfk7XAVYs1XrneA37uQPs9zvomlFfOQn2Hrkpde7g_zyHK5rNs8hot314Wk_EyMpImkbRKAOhYSllSbWyplQmJYpBKAQxMqZQhsrQKgHEKUrGU2oIZllrNDedDJE9vTee876DMd13V6O47pyQ_OsyDw_yfw_zsMJAPJ3LXFw3YP-5XGv8BkC5w5A</recordid><startdate>20240515</startdate><enddate>20240515</enddate><creator>Li, Huiqiang</creator><creator>Li, Xiaochen</creator><creator>Sun, Lingyi</creator><creator>He, Yanjie</creator><creator>Wang, Li</creator><creator>Gao, Yongju</creator><creator>Zeng, Dexing</creator><creator>Pang, Xinchang</creator><creator>Xu, Junling</creator><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><orcidid>https://orcid.org/0000-0003-1375-9908</orcidid><orcidid>https://orcid.org/0000-0002-7954-5817</orcidid><orcidid>https://orcid.org/0000-0002-3878-9161</orcidid></search><sort><creationdate>20240515</creationdate><title>18 F-Radiolabeling and Evaluation of an AMD3465 Derivative for PET Imaging of CXCR4 in a Mouse Breast Tumor Model</title><author>Li, Huiqiang ; Li, Xiaochen ; Sun, Lingyi ; He, Yanjie ; Wang, Li ; Gao, Yongju ; Zeng, Dexing ; Pang, Xinchang ; Xu, Junling</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c716-7d94eea5777f1acdfa9c94e92e874e2ecf99c07fd9ee231e79281db2c28da3c33</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2024</creationdate><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Li, Huiqiang</creatorcontrib><creatorcontrib>Li, Xiaochen</creatorcontrib><creatorcontrib>Sun, Lingyi</creatorcontrib><creatorcontrib>He, Yanjie</creatorcontrib><creatorcontrib>Wang, Li</creatorcontrib><creatorcontrib>Gao, Yongju</creatorcontrib><creatorcontrib>Zeng, Dexing</creatorcontrib><creatorcontrib>Pang, Xinchang</creatorcontrib><creatorcontrib>Xu, Junling</creatorcontrib><collection>PubMed</collection><collection>CrossRef</collection><jtitle>Bioconjugate chemistry</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Li, Huiqiang</au><au>Li, Xiaochen</au><au>Sun, Lingyi</au><au>He, Yanjie</au><au>Wang, Li</au><au>Gao, Yongju</au><au>Zeng, Dexing</au><au>Pang, Xinchang</au><au>Xu, Junling</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>18 F-Radiolabeling and Evaluation of an AMD3465 Derivative for PET Imaging of CXCR4 in a Mouse Breast Tumor Model</atitle><jtitle>Bioconjugate chemistry</jtitle><addtitle>Bioconjug Chem</addtitle><date>2024-05-15</date><risdate>2024</risdate><volume>35</volume><issue>5</issue><spage>567</spage><epage>574</epage><pages>567-574</pages><issn>1043-1802</issn><eissn>1520-4812</eissn><abstract>The exploration of pharmaceutically active agents and positron emission tomography (PET) tracers targeting CXCR4 has been a focal point in cancer research given its pivotal role in the development and progression of various cancers. While significant strides have been made in PET imaging with radiometal-labeled tracers, the landscape of
F-labeled small molecule tracers remains relatively limited. Herein, we introduce a novel and promising derivative, [
F]SFB-AMD3465, as a targeted PET tracer for CXCR4. The compound was synthesized by modifying the pyridine ring of AMD3465, which was subsequently labeled with
F using [
F]SFB. The study provides comprehensive insights into the design, synthesis, and biological evaluation of [
F]SFB-AMD3465.
and
assessments demonstrated the CXCR4-dependent, specific, and sensitive uptake of [
F]SFB-AMD3465 in the CXCR4-overexpressing 4T1 cell line and the corresponding xenograft-bearing mouse model. These findings contribute to bridging the gap in
F-labeled PET tracers for CXCR4 and underscore the potential of [
F]SFB-AMD3465 as a PET radiotracer for
CXCR4 imaging.</abstract><cop>United States</cop><pmid>38634516</pmid><doi>10.1021/acs.bioconjchem.4c00167</doi><tpages>8</tpages><orcidid>https://orcid.org/0000-0003-1375-9908</orcidid><orcidid>https://orcid.org/0000-0002-7954-5817</orcidid><orcidid>https://orcid.org/0000-0002-3878-9161</orcidid></addata></record> |
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| ispartof | Bioconjugate chemistry, 2024-05, Vol.35 (5), p.567-574 |
| issn | 1043-1802 1520-4812 |
| language | eng |
| recordid | cdi_crossref_primary_10_1021_acs_bioconjchem_4c00167 |
| source | American Chemical Society Journals |
| title | 18 F-Radiolabeling and Evaluation of an AMD3465 Derivative for PET Imaging of CXCR4 in a Mouse Breast Tumor Model |
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