{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2022,3,31]],"date-time":"2022-03-31T19:55:54Z","timestamp":1648756554318},"reference-count":0,"publisher":"Walter de Gruyter GmbH","issue":"11","content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":[],"published-print":{"date-parts":[[2015,11,28]]},"abstract":"<jats:title>Abstract<\/jats:title>\n               <jats:p>The oestrogen receptor (ER) is an important tumour target for molecular imaging and radionuclide therapy due to its overexpression in\nmany malignant cells as compared to normal cells. Aiming to find new functional molecular imaging\/therapeutic agents for ER positive\ntumours, we have synthesized a new estradiol derivative substituted at the 16-<jats:italic>\u03b1<\/jats:italic> position with a diethylene triamine tetraacetic\nacid (DTTA)-like chelating ligand through a four-carbon spacer. The new bioconjugate (H<jats:sub>4<\/jats:sub>L), was used to synthesize\nthe corresponding indium complexes (InL\/[<jats:sup>111<\/jats:sup>In]L). The radioactive complex\n[<jats:sup>111<\/jats:sup>In]L was prepared in high yield (&gt;98%) at final concentrations of 1\u2009\u00b7\u200910<jats:sup>\n                     <jats:italic>\u2013<\/jats:italic>4<\/jats:sup>\u2009M and its chemical\nidentity was ascertained by comparing its HPLC gamma-chromatogram to the HPLC UV-vis-chromatogram of the InL\nanalogue. [<jats:sup>111<\/jats:sup>In]L is hydrophilic and kinetically stable in the presence of an excess of apo-transferrin and in\nhuman blood serum. Cellular studies in breast cancer cells (MCF-7 and MDA-MB-431) suggest that [<jats:sup>111<\/jats:sup>In]L uptake may\nbe mediated by an ER dependent mechanism. Biodistribution studies were performed in mice indicating a rapid clearance from most organs\nand a slow total excretion that occurs mainly by hepatobiliar pathway. High <jats:italic>in vivo<\/jats:italic>\nstability of [<jats:sup>111<\/jats:sup>In]L\nwas confirmed by HPLC analysis of urine and blood samples. Nevertheless, the hydrophilicity, the low ER affinity and the\nbiodistribution of [<jats:sup>111<\/jats:sup>In]L indicate that structural modifications are required to improve its behaviour for ER\ntargeting <jats:italic>in vivo<\/jats:italic>.<\/jats:p>","DOI":"10.1515\/ract-2014-2355","type":"journal-article","created":{"date-parts":[[2015,10,9]],"date-time":"2015-10-09T17:01:31Z","timestamp":1444410091000},"page":"765-776","source":"Crossref","is-referenced-by-count":0,"title":["New estradiol based <sup>111<\/sup>In complex towards the estrogen receptor"],"prefix":"10.1515","volume":"103","author":[{"given":"Filipe","family":"Vultos","sequence":"first","affiliation":[{"name":"Centro de Ci\u00eancias e Tecnologias Nucleares C TN, Instituto Superior T\u00e9cnico, Universidade de Lisboa, Estrada Nacional 10 (km 139,7), 2695-066 Bobadela LRS, Portugal"}]},{"given":"Susana","family":"Cunha","sequence":"additional","affiliation":[{"name":"Centro de Ci\u00eancias e Tecnologias Nucleares C TN, Instituto Superior T\u00e9cnico, Universidade de Lisboa, Estrada Nacional 10 (km 139,7), 2695-066 Bobadela LRS, Portugal"}]},{"given":"C\u00e9lia","family":"Fernandes","sequence":"additional","affiliation":[{"name":"Centro de Ci\u00eancias e Tecnologias Nucleares C TN, Instituto Superior T\u00e9cnico, Universidade de Lisboa, Estrada Nacional 10 (km 139,7), 2695-066 Bobadela LRS, Portugal"}]},{"given":"Maria Cristina","family":"Oliveira","sequence":"additional","affiliation":[{"name":"Centro de Ci\u00eancias e Tecnologias Nucleares C TN, Instituto Superior T\u00e9cnico, Universidade de Lisboa, Estrada Nacional 10 (km 139,7), 2695-066 Bobadela LRS, Portugal"}]},{"given":"Fernanda","family":"Marques","sequence":"additional","affiliation":[{"name":"Centro de Ci\u00eancias e Tecnologias Nucleares C TN, Instituto Superior T\u00e9cnico, Universidade de Lisboa, Estrada Nacional 10 (km 139,7), 2695-066 Bobadela LRS, Portugal"}]},{"given":"Maria Filomena","family":"Botelho","sequence":"additional","affiliation":[{"name":"Instituto de Biof\u00edsica\/Biomatem\u00e1tica, IBILI, CIMAGO, Faculdade de Medicina, Universidade de Coimbra, Coimbra, Portugal"}]},{"given":"Isabel","family":"Santos","sequence":"additional","affiliation":[{"name":"Centro de Ci\u00eancias e Tecnologias Nucleares C TN, Instituto Superior T\u00e9cnico, Universidade de Lisboa, Estrada Nacional 10 (km 139,7), 2695-066 Bobadela LRS, Portugal"}]},{"given":"Lurdes","family":"Gano","sequence":"additional","affiliation":[{"name":"Centro de Ci\u00eancias e Tecnologias Nucleares C TN, Instituto Superior T\u00e9cnico, Universidade de Lisboa, Estrada Nacional 10 (km 139,7), 2695-066 Bobadela LRS, Portugal"}]}],"member":"374","published-online":{"date-parts":[[2015,10,9]]},"container-title":["Radiochimica Acta"],"original-title":[],"language":"en","link":[{"URL":"https:\/\/www.degruyter.com\/document\/doi\/10.1515\/ract-2014-2355\/xml","content-type":"application\/xml","content-version":"vor","intended-application":"text-mining"},{"URL":"https:\/\/www.degruyter.com\/document\/doi\/10.1515\/ract-2014-2355\/pdf","content-type":"unspecified","content-version":"vor","intended-application":"similarity-checking"}],"deposited":{"date-parts":[[2021,6,22]],"date-time":"2021-06-22T00:56:25Z","timestamp":1624323385000},"score":1,"resource":{"primary":{"URL":"https:\/\/www.degruyter.com\/document\/doi\/10.1515\/ract-2014-2355\/html"}},"subtitle":[],"short-title":[],"issued":{"date-parts":[[2015,10,9]]},"references-count":0,"journal-issue":{"issue":"11","published-online":{"date-parts":[[2015,9,14]]},"published-print":{"date-parts":[[2015,11,28]]}},"alternative-id":["10.1515\/ract-2014-2355"],"URL":"https:\/\/doi.org\/10.1515\/ract-2014-2355","relation":{},"ISSN":["0033-8230","2193-3405"],"issn-type":[{"value":"0033-8230","type":"print"},{"value":"2193-3405","type":"electronic"}],"subject":[],"published":{"date-parts":[[2015,10,9]]}}}