Metal ion-dependent biological properties of a chelator-derivatised somatostatin analogue for tumour targeting
Autor(a) principal: | |
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Data de Publicação: | 2008 |
Outros Autores: | , , , , , , |
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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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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1799132616940584960 |