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dc.contributor.authorLiang, SH-
dc.contributor.authorSouthon, AG-
dc.contributor.authorFraser, BH-
dc.contributor.authorKrause-Heuer, AM-
dc.contributor.authorZhang, B-
dc.contributor.authorShoup, TM-
dc.contributor.authorLewis, R-
dc.contributor.authorVolitakis, I-
dc.contributor.authorHan, Y-
dc.contributor.authorGreguric, I-
dc.contributor.authorBush, AI-
dc.contributor.authorVasdev, Y-
dc.identifier.citationLiang, S. H., Southon, A. G., Fraser, B. H., Krause-Heuer, A. M., Zhang, B., Shoup, T. M., Lewis, R., Volitakis, I., Han, Y., Greguric, I., Bush, A. I., &. Vasdev, N. (2015). Novel fluorinated 8-hydroxyquinoline based metal ionophores for exploring the metal hypothesis of Alzheimer’s disease. ACS Medicinal Chemistry Letters, 6(9), 1025-1029. doi:10.1021/acsmedchemlett.5b00281en_AU
dc.description.abstractZinc, copper, and iron ions are involved in amyloid-beta (Aβ) deposition and stabilization in Alzheimer’s disease (AD). Consequently, metal binding agents that prevent metal-Aβ interaction and lead to the dissolution of Aβ deposits have become well sought therapeutic and diagnostic targets. However, direct intervention between diseases and metal abnormalities has been challenging and is partially attributed to the lack of a suitable agent to determine and modify metal concentration and distribution in vivo. In the search of metal ionophores, we have identified several promising chemical entities by strategic fluorination of 8-hydroxyquinoline drugs, clioquinol, and PBT2. Compounds 15–17 and 28–30 showed exceptional metal ionophore ability (6–40-fold increase of copper uptake and >2-fold increase of zinc uptake) and inhibition of zinc induced Aβ oligomerization (EC50s < ∼5 μM). These compounds are suitable for further development as drug candidates and/or positron emission tomography (PET) biomarkers if radiolabeled with 18F. © 2015 American Chemical Societyen_AU
dc.publisherAmerican Chemical Societyen_AU
dc.subjectReaction product transport systemsen_AU
dc.subjectCentral nervous systemen_AU
dc.subjectEmission computed tomographyen_AU
dc.titleNovel fluorinated 8-hydroxyquinoline based metal Ionophores for exploring the metal hypothesis of alzheimer’s diseaseen_AU
dc.typeJournal Articleen_AU
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