Synthesis of a 2-nitroimidazole glycopeptide radiolabeled with (68)Ga for positron emission tomography (PET) imaging of tumor hypoxia

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dc.contributor.authorNARIO, ARIAN P.pt_BR
dc.contributor.authorPIJIEIRA, MARTHA S.O.pt_BR
dc.contributor.authorSANTOS, SOFIA N. dospt_BR
dc.contributor.authorCAMPOS, VANESSSA L.pt_BR
dc.contributor.authorBERNARDES, EMERSON S.pt_BR
dc.coverageInternacionalpt_BR
dc.creator.eventoINTERNATIONAL NUCLEAR ATLANTIC CONFERENCEpt_BR
dc.date.accessioned2020-01-06T21:18:31Z
dc.date.available2020-01-06T21:18:31Z
dc.date.eventoOctober 21-25, 2019pt_BR
dc.description.abstractHypoxia is a pathological condition characterized by a reduction of oxygen supply to a specific tissue or cell. About 60% of solid tumors in an advanced stage present areas of hypoxia. Tumor-associated hypoxia has been correlated to: 1) tumor aggressiveness; 2) resistance to chemotherapy and radiotherapy; 3) poor prognosis. Thus, the use of non-invasive methods dedicated to assess tumor hypoxic areas are of extremely importance for the treatment of several types of cancers, allowing the use of individualized therapeutic strategies. Here, we developed a new 68Ga-labeled radiopharmaceutical for positron emission tomography (PET) imaging of tumor hypoxia. The 68Ga-labelled 2-nitroimidazole derivative was successfully obtained by linking the 2- nitroimidazole acetic acid derivative with a glycopeptide obtained by solid phase synthesis and further conjugated to DOTA-NHS and its identity was confirmed by mass spectrometry. The radiolabeling procedure of 68Ga-Glycopeptide was optimized regarding the amount of glycopeptide, temperature and time, and was obtained with a high radiochemical purity (96.6± 0.4%). Compared to the standard hypoxic radiopharmaceutical 18 68 F-FAZA, Cancer is a chronic degenerative process that culminates in the loss of mechanisms that regulate cell cycle and death. In addition, it is considered a public health problem worldwide and its incidence has grown by 20% in the last decade. In Brazil, it is the second cause of death due to illness and the National Cancer Institute estimate is approximately 600 thousand Ga-Glycopeptide was obtained in a faster way and high radiochemical purity was achieved after radiolabeling procedures. Our new 68Ga-Glycopeptide may be promising candidate for further evaluation as a potential hypoxia imaging agent. Moreover, the use of 68Ga as an alternative to 18F in the development of new tracers for PET imaging is still an advantage because of the use of radionuclide generators instead of costly cyclotron equipment. Additionally, the use of a glycopeptide may allow the development of a kit-type setup that will ease the preparation of the 68Ga-based agent.pt_BR
dc.event.siglaINACpt_BR
dc.format.extent1687-1701pt_BR
dc.identifier.citationNARIO, ARIAN P.; PIJIEIRA, MARTHA S.O.; SANTOS, SOFIA N. dos; CAMPOS, VANESSSA L.; BERNARDES, EMERSON S. Synthesis of a 2-nitroimidazole glycopeptide radiolabeled with (68)Ga for positron emission tomography (PET) imaging of tumor hypoxia. In: INTERNATIONAL NUCLEAR ATLANTIC CONFERENCE, October 21-25, 2019, Santos, SP. <b>Proceedings...</b> Rio de Janeiro: Associação Brasileira de Energia Nuclear, 2019. p. 1687-1701. Disponível em: http://repositorio.ipen.br/handle/123456789/30577.
dc.identifier.orcid0000-0002-0029-7313pt_BR
dc.identifier.orcidhttps://orcid.org/0000-0002-0029-7313
dc.identifier.urihttp://repositorio.ipen.br/handle/123456789/30577
dc.localRio de Janeiropt_BR
dc.local.eventoSantos, SPpt_BR
dc.publisherAssociação Brasileira de Energia Nuclear
dc.rightsopenAccesspt_BR
dc.subjectanoxia
dc.subjectgallium 68
dc.subjectlabelling
dc.subjectmisonidazole
dc.subjectoxygen
dc.subjectpeptides
dc.subjectpositron computed tomography
dc.subjectradiochemistry
dc.subjectrespiration
dc.titleSynthesis of a 2-nitroimidazole glycopeptide radiolabeled with (68)Ga for positron emission tomography (PET) imaging of tumor hypoxiapt_BR
dc.typeTexto completo de eventopt_BR
dspace.entity.typePublication
ipen.autorMARTHA SAHYLI ORTEGA PIJIEIRA
ipen.autorEMERSON SOARES BERNARDES
ipen.autorSOFIA NASCIMENTO DOS SANTOS
ipen.autorARIAN PEREZ NARIO
ipen.codigoautor14075
ipen.codigoautor12099
ipen.codigoautor14464
ipen.codigoautor14076
ipen.contributor.ipenauthorMARTHA SAHYLI ORTEGA PIJIEIRA
ipen.contributor.ipenauthorEMERSON SOARES BERNARDES
ipen.contributor.ipenauthorSOFIA NASCIMENTO DOS SANTOS
ipen.contributor.ipenauthorARIAN PEREZ NARIO
ipen.date.recebimento20-01
ipen.event.datapadronizada2019pt_BR
ipen.identifier.ipendoc26227pt_BR
ipen.notas.internasProceedingspt_BR
ipen.type.genreArtigo
relation.isAuthorOfPublicationf34ac8ed-8b5e-4916-9492-d6ee6c363ca0
relation.isAuthorOfPublication8115c8bd-822c-4f5a-9f49-3c12570ed40a
relation.isAuthorOfPublicationab78881a-78eb-42be-a463-aaf80e70de3d
relation.isAuthorOfPublication14bd4de9-944c-470d-b7b0-94153395500a
relation.isAuthorOfPublication.latestForDiscovery14bd4de9-944c-470d-b7b0-94153395500a
sigepi.autor.atividadeBERNARDES, EMERSON S.:12099:110:Npt_BR
sigepi.autor.atividadeSANTOS, SOFIA N. dos:14464:110:Npt_BR
sigepi.autor.atividadePIJIEIRA, MARTHA S.O.:14075:110:Npt_BR
sigepi.autor.atividadeNARIO, ARIAN P.:14076:110:Spt_BR
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