Metal ion-dependent biological properties of a chelator-derivatised somatostatin analogue for tumour targeting

Detalhes bibliográficos
Autor(a) principal: Heppeler, Axel
Data de Publicação: 2008
Outros Autores: André, João P., Buschmann, Ingeborg, Wang, Xuejuan, Reubi, Jean-Claude, Hennig, Michael, Kaden, Thomas A., Maecke, Helmut R.
Tipo de documento: Artigo
Idioma: eng
Título da fonte: Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)
Texto Completo: http://hdl.handle.net/1822/14426
Resumo: A publicar na Revista Chemistry a European Journal
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spelling Metal ion-dependent biological properties of a chelator-derivatised somatostatin analogue for tumour targetingAntitumour agentsRadiocobaltSomatostatinPETRadiopharmaceuticalsantitumor agentscobaltpositron emission tomographyScience & TechnologyA publicar na Revista Chemistry a European JournalSomatostatin-based radioligands were shown to have sensitive imaging properties for neuroendocrine tumours and their metastases. The potential of [55Co]DOTATOC (DOTATOC = 4,7, 10-tricarboxymethyl-1,4,7,10- tetraazacyclododecane-1-yl-acetyl-DPhe- Lys-Tyr-D-Trp-Lys-Thr-Lys-1- threoninol (disulfide bond) as a new radiopharmaceutical agent for PET was evaluated. 57Co was used as a surrogate of the positron emitter 55Co and the pharmacokinetics of [57Co]DOTATOC was investigated using two nude mouse models. The somatostatin receptor subtype (sst1-5) affinity profile of [natCo]DOTA-TOC was assessed using autoradiographic methods on membranes transfected with human somatostatin receptor subtypes. These studies revealed that [57Co]DOTATOC is an sst2-specific radiopeptide presenting the highest affinity ever found for the sst2 receptor subtype. The rate of internalisation into the AR4-2J cell line also was the highest found for any somatostatin-based radiopeptide. Biodistribution studies, performed in nude mice bearing the AR4-2J tumour or a transfected HEK-sst2 cell-based tumour, showed high and specific uptake in the tumour and in other sst receptor-expressing tissues reflecting the high receptor binding affinity and the high rate of internalisation. The pharmacologic differences between [57Co]DOTATOC and [67Ga]DOTATOC were discussed in terms of the structural parameters found for the chelate models CoII(DOTA)2- and GaIII(DOTA)-, whose X-ray structures were determined. Both chelates show sixfold coordination in pseudooctahedral arrangements.Wiley-BlackwellUniversidade do MinhoHeppeler, AxelAndré, João P.Buschmann, IngeborgWang, XuejuanReubi, Jean-ClaudeHennig, MichaelKaden, Thomas A.Maecke, Helmut R.20082008-01-01T00:00:00Zinfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articleapplication/pdfhttp://hdl.handle.net/1822/14426eng0947-653910.1002/chem.20070126418246556info:eu-repo/semantics/openAccessreponame:Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)instname:Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informaçãoinstacron:RCAAP2023-07-21T12:23:03Zoai:repositorium.sdum.uminho.pt:1822/14426Portal AgregadorONGhttps://www.rcaap.pt/oai/openaireopendoar:71602024-03-19T19:16:40.213515Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) - Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informaçãofalse
dc.title.none.fl_str_mv Metal ion-dependent biological properties of a chelator-derivatised somatostatin analogue for tumour targeting
title Metal ion-dependent biological properties of a chelator-derivatised somatostatin analogue for tumour targeting
spellingShingle Metal ion-dependent biological properties of a chelator-derivatised somatostatin analogue for tumour targeting
Heppeler, Axel
Antitumour agents
Radiocobalt
Somatostatin
PET
Radiopharmaceuticals
antitumor agents
cobalt
positron emission tomography
Science & Technology
title_short Metal ion-dependent biological properties of a chelator-derivatised somatostatin analogue for tumour targeting
title_full Metal ion-dependent biological properties of a chelator-derivatised somatostatin analogue for tumour targeting
title_fullStr Metal ion-dependent biological properties of a chelator-derivatised somatostatin analogue for tumour targeting
title_full_unstemmed Metal ion-dependent biological properties of a chelator-derivatised somatostatin analogue for tumour targeting
title_sort Metal ion-dependent biological properties of a chelator-derivatised somatostatin analogue for tumour targeting
author Heppeler, Axel
author_facet Heppeler, Axel
André, João P.
Buschmann, Ingeborg
Wang, Xuejuan
Reubi, Jean-Claude
Hennig, Michael
Kaden, Thomas A.
Maecke, Helmut R.
author_role author
author2 André, João P.
Buschmann, Ingeborg
Wang, Xuejuan
Reubi, Jean-Claude
Hennig, Michael
Kaden, Thomas A.
Maecke, Helmut R.
author2_role author
author
author
author
author
author
author
dc.contributor.none.fl_str_mv Universidade do Minho
dc.contributor.author.fl_str_mv Heppeler, Axel
André, João P.
Buschmann, Ingeborg
Wang, Xuejuan
Reubi, Jean-Claude
Hennig, Michael
Kaden, Thomas A.
Maecke, Helmut R.
dc.subject.por.fl_str_mv Antitumour agents
Radiocobalt
Somatostatin
PET
Radiopharmaceuticals
antitumor agents
cobalt
positron emission tomography
Science & Technology
topic Antitumour agents
Radiocobalt
Somatostatin
PET
Radiopharmaceuticals
antitumor agents
cobalt
positron emission tomography
Science & Technology
description A publicar na Revista Chemistry a European Journal
publishDate 2008
dc.date.none.fl_str_mv 2008
2008-01-01T00:00:00Z
dc.type.status.fl_str_mv info:eu-repo/semantics/publishedVersion
dc.type.driver.fl_str_mv info:eu-repo/semantics/article
format article
status_str publishedVersion
dc.identifier.uri.fl_str_mv http://hdl.handle.net/1822/14426
url http://hdl.handle.net/1822/14426
dc.language.iso.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv 0947-6539
10.1002/chem.200701264
18246556
dc.rights.driver.fl_str_mv info:eu-repo/semantics/openAccess
eu_rights_str_mv openAccess
dc.format.none.fl_str_mv application/pdf
dc.publisher.none.fl_str_mv Wiley-Blackwell
publisher.none.fl_str_mv Wiley-Blackwell
dc.source.none.fl_str_mv reponame:Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)
instname:Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação
instacron:RCAAP
instname_str Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação
instacron_str RCAAP
institution RCAAP
reponame_str Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)
collection Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)
repository.name.fl_str_mv Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) - Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação
repository.mail.fl_str_mv
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