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New Imaging Modality of COVID-19 Pneumonia Developed on the Basis of Alzheimer’s Disease Research.

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cris.lastimport.scopus2024-02-12T19:40:14Z
dc.abstract.enViral pneumonia caused by highly infectious SARS-CoV-2 poses a higher risk to older people and those who have underlying health conditions, including Alzheimer’s disease. In this work we present newly designed tacrine-based radioconjugates with physicochemical and biological properties that are crucial for the potential application as diagnostic radiopharmaceuticals. A set of ten tacrine derivatives was synthesized, labelled with gallium-68 and fully characterized in the context of their physicochemical properties. Based on these results, the final two most promising radioconjugates, [68Ga]Ga-NODAGA-Bn-NH(CH2)9Tac and [68Ga]Ga-THP-NH(CH2)9Tac, were selected for biodistribution studies. The latter compound was proven to be a good inhibitor of cholinesterases with significant affinity toward the lungs, according to the biodistribution studies. On the basis of molecular modelling combined with in vitro studies, we unraveled which structural properties of the developed tacrine derivatives are crucial for high affinity toward acetylcholinesterase, whose increased levels in lung tissues in the course of coronavirus disease indicate the onset of pneumonia. The radiopharmaceutical [68Ga]Ga-THP-NH(CH2)9Tac was ultimately selected due to its increased accuracy and improved sensitivity in PET imaging of lung tissue with high levels of acetylcholinesterase, and it may become a novel potential diagnostic modality for the determination of lung perfusion, including in inflammation after COVID-19.
dc.affiliationUniwersytet Warszawski
dc.contributor.authorGniazdowska, Ewa
dc.contributor.authorSzymański, Paweł
dc.contributor.authorRogulski, Zbigniew
dc.contributor.authorCheda, Łukasz
dc.contributor.authorRogut, Aleksandra
dc.contributor.authorCzarnecka, Kamila
dc.contributor.authorHalik, Paweł K.
dc.contributor.authorWieczorek, Grzegorz
dc.contributor.authorNiedziałek, Dorota
dc.contributor.authorKoźmiński, Przemysław
dc.date.accessioned2024-01-25T13:48:05Z
dc.date.available2024-01-25T13:48:05Z
dc.date.copyright2022-07-29
dc.date.issued2022
dc.description.accesstimeAT_PUBLICATION
dc.description.financePublikacja bezkosztowa
dc.description.number15
dc.description.versionFINAL_PUBLISHED
dc.description.volume23
dc.identifier.doi10.3390/IJMS23158405
dc.identifier.issn1422-0067
dc.identifier.urihttps://repozytorium.uw.edu.pl//handle/item/113584
dc.identifier.weblinkhttps://www.mdpi.com/1422-0067/23/15/8405/pdf
dc.languageeng
dc.pbn.affiliationchemical sciences
dc.relation.ispartofInternational Journal of Molecular Sciences
dc.relation.pages8405 (1-17)
dc.rightsCC-BY
dc.sciencecloudnosend
dc.subject.enTacrine
dc.subject.enCOVID-19
dc.subject.enGallium-68
dc.subject.enRadiopharmaceuticals
dc.subject.enBiodistribution studies
dc.subject.enMolecular docking
dc.titleNew Imaging Modality of COVID-19 Pneumonia Developed on the Basis of Alzheimer’s Disease Research.
dc.typeJournalArticle
dspace.entity.typePublication