Development and evaluation of a 99m Tc(V)-nitrido complex derived from estradiol for breast cancer imaging
Estrogen receptors are overexpressed in 70% of breast cancer and identification of their presence is important to select the appropriate treatment. This work proposes the preparation and evaluation of an estradiol derived as potential ER imaging agent. Ethinylestradiol was derivatized to introduce a...
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| Veröffentlicht in: | Applied radiation and isotopes 2019-12, Vol.154, p.108854 |
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| container_title | Applied radiation and isotopes |
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| creator | Tejería, Emilia Giglio, Javier Fernández, Leticia Rey, Ana |
| description | Estrogen receptors are overexpressed in 70% of breast cancer and identification of their presence is important to select the appropriate treatment. This work proposes the preparation and evaluation of an estradiol derived as potential ER imaging agent. Ethinylestradiol was derivatized to introduce a dithiocarbamate function for Tc coordination. Labeling was achieved through the formation of a symmetric Tc(V)-nitrido complex with a radiochemical purity (RCP) > 95%. Physicochemical evaluation, cell uptake, biodistribution in normal animals and in nude mice bearing induced ER + breast tumors showed promising results. |
| doi_str_mv | 10.1016/j.apradiso.2019.108854 |
| format | Article |
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This work proposes the preparation and evaluation of an estradiol derived as potential ER imaging agent. Ethinylestradiol was derivatized to introduce a dithiocarbamate function for Tc coordination. Labeling was achieved through the formation of a symmetric Tc(V)-nitrido complex with a radiochemical purity (RCP) > 95%. Physicochemical evaluation, cell uptake, biodistribution in normal animals and in nude mice bearing induced ER + breast tumors showed promising results.</description><identifier>EISSN: 1872-9800</identifier><identifier>DOI: 10.1016/j.apradiso.2019.108854</identifier><identifier>PMID: 31442798</identifier><language>eng</language><publisher>England</publisher><subject>Animals ; Breast Neoplasms - diagnostic imaging ; Breast Neoplasms - metabolism ; Drug Stability ; Estradiol - analogs & derivatives ; Estradiol - chemical synthesis ; Estradiol - chemistry ; Female ; Humans ; MCF-7 Cells ; Mice ; Mice, Nude ; Neoplasm Transplantation ; Organotechnetium Compounds - chemical synthesis ; Organotechnetium Compounds - chemistry ; Organotechnetium Compounds - pharmacokinetics ; Protein Binding ; Radiopharmaceuticals - chemical synthesis ; Radiopharmaceuticals - chemistry ; Radiopharmaceuticals - pharmacokinetics ; Rats ; Rats, Wistar ; Receptors, Estrogen - metabolism ; Tissue Distribution</subject><ispartof>Applied radiation and isotopes, 2019-12, Vol.154, p.108854</ispartof><rights>Copyright © 2019. 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This work proposes the preparation and evaluation of an estradiol derived as potential ER imaging agent. Ethinylestradiol was derivatized to introduce a dithiocarbamate function for Tc coordination. Labeling was achieved through the formation of a symmetric Tc(V)-nitrido complex with a radiochemical purity (RCP) > 95%. Physicochemical evaluation, cell uptake, biodistribution in normal animals and in nude mice bearing induced ER + breast tumors showed promising results.</description><subject>Animals</subject><subject>Breast Neoplasms - diagnostic imaging</subject><subject>Breast Neoplasms - metabolism</subject><subject>Drug Stability</subject><subject>Estradiol - analogs & derivatives</subject><subject>Estradiol - chemical synthesis</subject><subject>Estradiol - chemistry</subject><subject>Female</subject><subject>Humans</subject><subject>MCF-7 Cells</subject><subject>Mice</subject><subject>Mice, Nude</subject><subject>Neoplasm Transplantation</subject><subject>Organotechnetium Compounds - chemical synthesis</subject><subject>Organotechnetium Compounds - chemistry</subject><subject>Organotechnetium Compounds - pharmacokinetics</subject><subject>Protein Binding</subject><subject>Radiopharmaceuticals - chemical synthesis</subject><subject>Radiopharmaceuticals - chemistry</subject><subject>Radiopharmaceuticals - pharmacokinetics</subject><subject>Rats</subject><subject>Rats, Wistar</subject><subject>Receptors, Estrogen - metabolism</subject><subject>Tissue Distribution</subject><issn>1872-9800</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2019</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFjstKAzEUQIMgtj5-odylLmZMpqNN1j7oBxS35XZyp2RIckOSDvr3VtC1qwOHszhCrJRslVTPj1OLKaN1hdtOKnOWWj_1F2Kp9KZrjJZyIa5LmaSUvTbdlVisVd93G6OXYnqlmTynQLECRgs0oz9hdRyBR0AwJsBuuP94aKKr2VmGgUPy9AmWspvJwpg5AJX6s8AeRs5wyISlwoBxoAwu4NHF4624HNEXuvvljVi9v-1etk06HQLZfcrnMH_t_-bW_wbfM29NVA</recordid><startdate>201912</startdate><enddate>201912</enddate><creator>Tejería, Emilia</creator><creator>Giglio, Javier</creator><creator>Fernández, Leticia</creator><creator>Rey, Ana</creator><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope></search><sort><creationdate>201912</creationdate><title>Development and evaluation of a 99m Tc(V)-nitrido complex derived from estradiol for breast cancer imaging</title><author>Tejería, Emilia ; Giglio, Javier ; Fernández, Leticia ; Rey, Ana</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-pubmed_primary_314427983</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2019</creationdate><topic>Animals</topic><topic>Breast Neoplasms - diagnostic imaging</topic><topic>Breast Neoplasms - metabolism</topic><topic>Drug Stability</topic><topic>Estradiol - analogs & derivatives</topic><topic>Estradiol - chemical synthesis</topic><topic>Estradiol - chemistry</topic><topic>Female</topic><topic>Humans</topic><topic>MCF-7 Cells</topic><topic>Mice</topic><topic>Mice, Nude</topic><topic>Neoplasm Transplantation</topic><topic>Organotechnetium Compounds - chemical synthesis</topic><topic>Organotechnetium Compounds - chemistry</topic><topic>Organotechnetium Compounds - pharmacokinetics</topic><topic>Protein Binding</topic><topic>Radiopharmaceuticals - chemical synthesis</topic><topic>Radiopharmaceuticals - chemistry</topic><topic>Radiopharmaceuticals - pharmacokinetics</topic><topic>Rats</topic><topic>Rats, Wistar</topic><topic>Receptors, Estrogen - metabolism</topic><topic>Tissue Distribution</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Tejería, Emilia</creatorcontrib><creatorcontrib>Giglio, Javier</creatorcontrib><creatorcontrib>Fernández, Leticia</creatorcontrib><creatorcontrib>Rey, Ana</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><jtitle>Applied radiation and isotopes</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Tejería, Emilia</au><au>Giglio, Javier</au><au>Fernández, Leticia</au><au>Rey, Ana</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Development and evaluation of a 99m Tc(V)-nitrido complex derived from estradiol for breast cancer imaging</atitle><jtitle>Applied radiation and isotopes</jtitle><addtitle>Appl Radiat Isot</addtitle><date>2019-12</date><risdate>2019</risdate><volume>154</volume><spage>108854</spage><pages>108854-</pages><eissn>1872-9800</eissn><abstract>Estrogen receptors are overexpressed in 70% of breast cancer and identification of their presence is important to select the appropriate treatment. 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| identifier | EISSN: 1872-9800 |
| ispartof | Applied radiation and isotopes, 2019-12, Vol.154, p.108854 |
| issn | 1872-9800 |
| language | eng |
| recordid | cdi_pubmed_primary_31442798 |
| source | MEDLINE; ScienceDirect Journals (5 years ago - present) |
| subjects | Animals Breast Neoplasms - diagnostic imaging Breast Neoplasms - metabolism Drug Stability Estradiol - analogs & derivatives Estradiol - chemical synthesis Estradiol - chemistry Female Humans MCF-7 Cells Mice Mice, Nude Neoplasm Transplantation Organotechnetium Compounds - chemical synthesis Organotechnetium Compounds - chemistry Organotechnetium Compounds - pharmacokinetics Protein Binding Radiopharmaceuticals - chemical synthesis Radiopharmaceuticals - chemistry Radiopharmaceuticals - pharmacokinetics Rats Rats, Wistar Receptors, Estrogen - metabolism Tissue Distribution |
| title | Development and evaluation of a 99m Tc(V)-nitrido complex derived from estradiol for breast cancer imaging |
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