In Vivo Albumin-Binding of a C-Functionalized Cyclam Platform for 64 Cu-PET/CT Imaging in Breast Cancer Model
An improved glucose-chelator-albumin bioconjugate (GluCAB) derivative, GluCAB-2 , has been synthesized and studied for in vivo Cu-PET/CT imaging in breast cancer mice models together with its first-generation analogue GluCAB-1 . The radioligand works on the principle of tumor targeting through the e...
Gespeichert in:
| Veröffentlicht in: | ChemMedChem 2021-03, Vol.16 (5), p.809-821 |
|---|---|
| Hauptverfasser: | , , , , , |
| Format: | Artikel |
| Sprache: | eng |
| Schlagworte: | |
| Online-Zugang: | Volltext |
| Tags: |
Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
|
| container_end_page | 821 |
|---|---|
| container_issue | 5 |
| container_start_page | 809 |
| container_title | ChemMedChem |
| container_volume | 16 |
| creator | Le Bihan, Thomas Driver, Cathryn H S Ebenhan, Thomas Le Bris, Nathalie Zeevaart, Jan Rijn Tripier, Raphaël |
| description | An improved glucose-chelator-albumin bioconjugate (GluCAB) derivative, GluCAB-2
, has been synthesized and studied for in vivo
Cu-PET/CT imaging in breast cancer mice models together with its first-generation analogue GluCAB-1
. The radioligand works on the principle of tumor targeting through the enhanced permeability and retention (EPR) effect with a supportive role played by glucose metabolism. [
Cu]Cu-GluCAB-2
(99 % RCP) exhibited high serum stability with immediate binding to serum proteins. In vivo experiments for comparison between tumor targeting of [
Cu]Cu-GluCAB-2
and previous-generation [
Cu]Cu-GluCAB-1
encompassed microPET/CT imaging and biodistribution analysis in an allograft E0771 breast cancer mouse model. Tumor uptake of [
Cu]Cu-GluCAB-2
was clearly evident with twice as much accumulation as compared to its predecessor and a tumor/muscle ratio of up to 5 after 24 h. Further comparison indicated a decrease in liver accumulation for [
Cu]Cu-Glu-CAB-2
. |
| doi_str_mv | 10.1002/cmdc.202000800 |
| format | Article |
| fullrecord | <record><control><sourceid>proquest_hal_p</sourceid><recordid>TN_cdi_hal_primary_oai_HAL_hal_03079054v1</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><sourcerecordid>2461003552</sourcerecordid><originalsourceid>FETCH-LOGICAL-c1747-d2dbf8f1e316d26bda571887a75af70dcfce03c632b5385b39d3ac8e6945f44b3</originalsourceid><addsrcrecordid>eNo9kctv1DAQxi1ERUvhyhH5CIdsx4_EznEbtXSlRfSwcLUcP4qRHyXeVGr_erLaspeZ0eg3nzTfh9AnAisCQK9MsmZFgQKABHiDLojsoBFEirenWfTn6H2tfwA4l0S-Q-eMkZ50VFygtMn4V3gqeB3HOYXcXIdsQ37AxWONh-Z2zmYfStYxvDiLh2cTdcL3Ue99mRJeCu44Hubm_mZ3NezwJumHw3nI-Hpyuu7xoLNxE_5erIsf0JnXsbqPr_0S_by92Q13zfbHt82w3jaGCC4aS-3opSeOkc7SbrS6XT6SQotWewHWeOOAmY7RsWWyHVlvmTbSdT1vPecju0Rfj7q_dVSPU0h6elZFB3W33qrDDhiIHlr-RBb2y5F9nMrf2dW9SqEaF6POrsxVUd4tTrO2pQu6OqJmKrVOzp-0CahDHOoQhzrFsRx8ftWex-TsCf_vP_sHOV6DDw</addsrcrecordid><sourcetype>Open Access Repository</sourcetype><iscdi>true</iscdi><recordtype>article</recordtype><pqid>2461003552</pqid></control><display><type>article</type><title>In Vivo Albumin-Binding of a C-Functionalized Cyclam Platform for 64 Cu-PET/CT Imaging in Breast Cancer Model</title><source>Wiley Online Library Journals Frontfile Complete</source><creator>Le Bihan, Thomas ; Driver, Cathryn H S ; Ebenhan, Thomas ; Le Bris, Nathalie ; Zeevaart, Jan Rijn ; Tripier, Raphaël</creator><creatorcontrib>Le Bihan, Thomas ; Driver, Cathryn H S ; Ebenhan, Thomas ; Le Bris, Nathalie ; Zeevaart, Jan Rijn ; Tripier, Raphaël</creatorcontrib><description>An improved glucose-chelator-albumin bioconjugate (GluCAB) derivative, GluCAB-2
, has been synthesized and studied for in vivo
Cu-PET/CT imaging in breast cancer mice models together with its first-generation analogue GluCAB-1
. The radioligand works on the principle of tumor targeting through the enhanced permeability and retention (EPR) effect with a supportive role played by glucose metabolism. [
Cu]Cu-GluCAB-2
(99 % RCP) exhibited high serum stability with immediate binding to serum proteins. In vivo experiments for comparison between tumor targeting of [
Cu]Cu-GluCAB-2
and previous-generation [
Cu]Cu-GluCAB-1
encompassed microPET/CT imaging and biodistribution analysis in an allograft E0771 breast cancer mouse model. Tumor uptake of [
Cu]Cu-GluCAB-2
was clearly evident with twice as much accumulation as compared to its predecessor and a tumor/muscle ratio of up to 5 after 24 h. Further comparison indicated a decrease in liver accumulation for [
Cu]Cu-Glu-CAB-2
.</description><identifier>ISSN: 1860-7179</identifier><identifier>EISSN: 1860-7187</identifier><identifier>DOI: 10.1002/cmdc.202000800</identifier><identifier>PMID: 33191627</identifier><language>eng</language><publisher>Germany: Wiley-VCH Verlag</publisher><subject>Chemical Sciences ; Medicinal Chemistry</subject><ispartof>ChemMedChem, 2021-03, Vol.16 (5), p.809-821</ispartof><rights>2020 Wiley-VCH GmbH.</rights><rights>Distributed under a Creative Commons Attribution 4.0 International License</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c1747-d2dbf8f1e316d26bda571887a75af70dcfce03c632b5385b39d3ac8e6945f44b3</citedby><cites>FETCH-LOGICAL-c1747-d2dbf8f1e316d26bda571887a75af70dcfce03c632b5385b39d3ac8e6945f44b3</cites><orcidid>0000-0001-9364-788X ; 0000-0002-6792-457X ; 0000-0002-6936-3876</orcidid></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>230,314,776,780,881,27901,27902</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/33191627$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink><backlink>$$Uhttps://hal.univ-brest.fr/hal-03079054$$DView record in HAL$$Hfree_for_read</backlink></links><search><creatorcontrib>Le Bihan, Thomas</creatorcontrib><creatorcontrib>Driver, Cathryn H S</creatorcontrib><creatorcontrib>Ebenhan, Thomas</creatorcontrib><creatorcontrib>Le Bris, Nathalie</creatorcontrib><creatorcontrib>Zeevaart, Jan Rijn</creatorcontrib><creatorcontrib>Tripier, Raphaël</creatorcontrib><title>In Vivo Albumin-Binding of a C-Functionalized Cyclam Platform for 64 Cu-PET/CT Imaging in Breast Cancer Model</title><title>ChemMedChem</title><addtitle>ChemMedChem</addtitle><description>An improved glucose-chelator-albumin bioconjugate (GluCAB) derivative, GluCAB-2
, has been synthesized and studied for in vivo
Cu-PET/CT imaging in breast cancer mice models together with its first-generation analogue GluCAB-1
. The radioligand works on the principle of tumor targeting through the enhanced permeability and retention (EPR) effect with a supportive role played by glucose metabolism. [
Cu]Cu-GluCAB-2
(99 % RCP) exhibited high serum stability with immediate binding to serum proteins. In vivo experiments for comparison between tumor targeting of [
Cu]Cu-GluCAB-2
and previous-generation [
Cu]Cu-GluCAB-1
encompassed microPET/CT imaging and biodistribution analysis in an allograft E0771 breast cancer mouse model. Tumor uptake of [
Cu]Cu-GluCAB-2
was clearly evident with twice as much accumulation as compared to its predecessor and a tumor/muscle ratio of up to 5 after 24 h. Further comparison indicated a decrease in liver accumulation for [
Cu]Cu-Glu-CAB-2
.</description><subject>Chemical Sciences</subject><subject>Medicinal Chemistry</subject><issn>1860-7179</issn><issn>1860-7187</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2021</creationdate><recordtype>article</recordtype><recordid>eNo9kctv1DAQxi1ERUvhyhH5CIdsx4_EznEbtXSlRfSwcLUcP4qRHyXeVGr_erLaspeZ0eg3nzTfh9AnAisCQK9MsmZFgQKABHiDLojsoBFEirenWfTn6H2tfwA4l0S-Q-eMkZ50VFygtMn4V3gqeB3HOYXcXIdsQ37AxWONh-Z2zmYfStYxvDiLh2cTdcL3Ue99mRJeCu44Hubm_mZ3NezwJumHw3nI-Hpyuu7xoLNxE_5erIsf0JnXsbqPr_0S_by92Q13zfbHt82w3jaGCC4aS-3opSeOkc7SbrS6XT6SQotWewHWeOOAmY7RsWWyHVlvmTbSdT1vPecju0Rfj7q_dVSPU0h6elZFB3W33qrDDhiIHlr-RBb2y5F9nMrf2dW9SqEaF6POrsxVUd4tTrO2pQu6OqJmKrVOzp-0CahDHOoQhzrFsRx8ftWex-TsCf_vP_sHOV6DDw</recordid><startdate>20210303</startdate><enddate>20210303</enddate><creator>Le Bihan, Thomas</creator><creator>Driver, Cathryn H S</creator><creator>Ebenhan, Thomas</creator><creator>Le Bris, Nathalie</creator><creator>Zeevaart, Jan Rijn</creator><creator>Tripier, Raphaël</creator><general>Wiley-VCH Verlag</general><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7X8</scope><scope>1XC</scope><scope>VOOES</scope><orcidid>https://orcid.org/0000-0001-9364-788X</orcidid><orcidid>https://orcid.org/0000-0002-6792-457X</orcidid><orcidid>https://orcid.org/0000-0002-6936-3876</orcidid></search><sort><creationdate>20210303</creationdate><title>In Vivo Albumin-Binding of a C-Functionalized Cyclam Platform for 64 Cu-PET/CT Imaging in Breast Cancer Model</title><author>Le Bihan, Thomas ; Driver, Cathryn H S ; Ebenhan, Thomas ; Le Bris, Nathalie ; Zeevaart, Jan Rijn ; Tripier, Raphaël</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c1747-d2dbf8f1e316d26bda571887a75af70dcfce03c632b5385b39d3ac8e6945f44b3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2021</creationdate><topic>Chemical Sciences</topic><topic>Medicinal Chemistry</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Le Bihan, Thomas</creatorcontrib><creatorcontrib>Driver, Cathryn H S</creatorcontrib><creatorcontrib>Ebenhan, Thomas</creatorcontrib><creatorcontrib>Le Bris, Nathalie</creatorcontrib><creatorcontrib>Zeevaart, Jan Rijn</creatorcontrib><creatorcontrib>Tripier, Raphaël</creatorcontrib><collection>PubMed</collection><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><collection>Hyper Article en Ligne (HAL)</collection><collection>Hyper Article en Ligne (HAL) (Open Access)</collection><jtitle>ChemMedChem</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Le Bihan, Thomas</au><au>Driver, Cathryn H S</au><au>Ebenhan, Thomas</au><au>Le Bris, Nathalie</au><au>Zeevaart, Jan Rijn</au><au>Tripier, Raphaël</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>In Vivo Albumin-Binding of a C-Functionalized Cyclam Platform for 64 Cu-PET/CT Imaging in Breast Cancer Model</atitle><jtitle>ChemMedChem</jtitle><addtitle>ChemMedChem</addtitle><date>2021-03-03</date><risdate>2021</risdate><volume>16</volume><issue>5</issue><spage>809</spage><epage>821</epage><pages>809-821</pages><issn>1860-7179</issn><eissn>1860-7187</eissn><abstract>An improved glucose-chelator-albumin bioconjugate (GluCAB) derivative, GluCAB-2
, has been synthesized and studied for in vivo
Cu-PET/CT imaging in breast cancer mice models together with its first-generation analogue GluCAB-1
. The radioligand works on the principle of tumor targeting through the enhanced permeability and retention (EPR) effect with a supportive role played by glucose metabolism. [
Cu]Cu-GluCAB-2
(99 % RCP) exhibited high serum stability with immediate binding to serum proteins. In vivo experiments for comparison between tumor targeting of [
Cu]Cu-GluCAB-2
and previous-generation [
Cu]Cu-GluCAB-1
encompassed microPET/CT imaging and biodistribution analysis in an allograft E0771 breast cancer mouse model. Tumor uptake of [
Cu]Cu-GluCAB-2
was clearly evident with twice as much accumulation as compared to its predecessor and a tumor/muscle ratio of up to 5 after 24 h. Further comparison indicated a decrease in liver accumulation for [
Cu]Cu-Glu-CAB-2
.</abstract><cop>Germany</cop><pub>Wiley-VCH Verlag</pub><pmid>33191627</pmid><doi>10.1002/cmdc.202000800</doi><tpages>13</tpages><orcidid>https://orcid.org/0000-0001-9364-788X</orcidid><orcidid>https://orcid.org/0000-0002-6792-457X</orcidid><orcidid>https://orcid.org/0000-0002-6936-3876</orcidid><oa>free_for_read</oa></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 1860-7179 |
| ispartof | ChemMedChem, 2021-03, Vol.16 (5), p.809-821 |
| issn | 1860-7179 1860-7187 |
| language | eng |
| recordid | cdi_hal_primary_oai_HAL_hal_03079054v1 |
| source | Wiley Online Library Journals Frontfile Complete |
| subjects | Chemical Sciences Medicinal Chemistry |
| title | In Vivo Albumin-Binding of a C-Functionalized Cyclam Platform for 64 Cu-PET/CT Imaging in Breast Cancer Model |
| url | https://sfx.bib-bvb.de/sfx_tum?ctx_ver=Z39.88-2004&ctx_enc=info:ofi/enc:UTF-8&ctx_tim=2025-02-15T14%3A15%3A14IST&url_ver=Z39.88-2004&url_ctx_fmt=infofi/fmt:kev:mtx:ctx&rfr_id=info:sid/primo.exlibrisgroup.com:primo3-Article-proquest_hal_p&rft_val_fmt=info:ofi/fmt:kev:mtx:journal&rft.genre=article&rft.atitle=In%20Vivo%20Albumin-Binding%20of%20a%20C-Functionalized%20Cyclam%20Platform%20for%2064%20Cu-PET/CT%20Imaging%20in%20Breast%20Cancer%20Model&rft.jtitle=ChemMedChem&rft.au=Le%20Bihan,%20Thomas&rft.date=2021-03-03&rft.volume=16&rft.issue=5&rft.spage=809&rft.epage=821&rft.pages=809-821&rft.issn=1860-7179&rft.eissn=1860-7187&rft_id=info:doi/10.1002/cmdc.202000800&rft_dat=%3Cproquest_hal_p%3E2461003552%3C/proquest_hal_p%3E%3Curl%3E%3C/url%3E&disable_directlink=true&sfx.directlink=off&sfx.report_link=0&rft_id=info:oai/&rft_pqid=2461003552&rft_id=info:pmid/33191627&rfr_iscdi=true |