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Influence of the position and composition of radiometals and radioiodine labels on imaging of epcam expression in prostate cancer model using the darpin ec1

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dc.contributor.authorXu, T.
dc.contributor.authorLiu, Y.
dc.contributor.authorSchulga, A.
dc.contributor.authorKonovalova, E.
dc.contributor.authorDeyev, S. M.
dc.contributor.authorДеев, Сергей Михайлович
dc.date.accessioned2024-11-29T17:30:53Z
dc.date.available2024-11-29T17:30:53Z
dc.date.issued2021
dc.description.abstract© 2021 by the authors. Licensee MDPI, Basel, Switzerland.The epithelial cell adhesion molecule (EpCAM) is intensively overexpressed in 40–60% of prostate cancer (PCa) cases and can be used as a target for the delivery of drugs and toxins. The designed ankyrin repeat protein (DARPin) Ec1 has a high affinity to EpCAM (68 pM) and a small size (18 kDa). Radiolabeled Ec1 might be used as a companion diagnostic for the selection of PCa patients for therapy. The study aimed to investigate the influence of radiolabel position (N-or C-terminal) and composition on the targeting and imaging properties of Ec1. Two variants, having an N-or C-terminal cysteine, were produced, site-specifically conjugated to a DOTA chelator and labeled with cobalt-57, gallium-68 or indium-111. Site-specific radioiodination was performed using ((4-hydroxyphenyl)-ethyl)maleimide (HPEM). Biodistribution of eight radiolabeled Ec1-probes was measured in nude mice bearing PCa DU145 xenografts. In all cases, positioning of a label at the C-terminus provided the best tumor-to-organ ratios. The non-residualizing [125 I]I-HPEM label provided the highest tumor-to-muscle and tumor-to-bone ratios and is more suitable for EpCAM imaging in early-stage PCa. Among the radiometals, indium-111 provided the highest tumor-to-blood, tumor-to-lung and tumor-to-liver ratios and could be used at late-stage PCa. In conclusion, label position and composition are important for the DARPin Ec1.
dc.identifier.citationInfluence of the position and composition of radiometals and radioiodine labels on imaging of epcam expression in prostate cancer model using the darpin ec1 / Xu, T. [et al.] // Cancers. - 2021. - 13. - № 14. - 10.3390/cancers13143589
dc.identifier.doi10.3390/cancers13143589
dc.identifier.urihttps://www.doi.org/10.3390/cancers13143589
dc.identifier.urihttps://www.scopus.com/record/display.uri?eid=2-s2.0-85110215519&origin=resultslist
dc.identifier.urihttp://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=Alerting&SrcApp=Alerting&DestApp=WOS_CPL&DestLinkType=FullRecord&UT=WOS:000676200900001
dc.identifier.urihttps://openrepository.mephi.ru/handle/123456789/24355
dc.relation.ispartofCancers
dc.titleInfluence of the position and composition of radiometals and radioiodine labels on imaging of epcam expression in prostate cancer model using the darpin ec1
dc.typeArticle
dspace.entity.typePublication
oaire.citation.issue14
oaire.citation.volume13
relation.isAuthorOfPublication66f50b35-0e92-49e0-ad1a-0ac386d858b7
relation.isAuthorOfPublication.latestForDiscovery66f50b35-0e92-49e0-ad1a-0ac386d858b7
relation.isOrgUnitOfPublicationc8407a6f-7272-450d-8d99-032352c76b55
relation.isOrgUnitOfPublication.latestForDiscoveryc8407a6f-7272-450d-8d99-032352c76b55
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