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dc.contributor.authorSneddon, Deborah
dc.contributor.authorNiemans, Raymon
dc.contributor.authorBauwens, Matthias
dc.contributor.authorYaromina, Ala
dc.contributor.authorvan Kuijk, Simon JA
dc.contributor.authorLieuwes, Natasja G
dc.contributor.authorBiemans, Rianne
dc.contributor.authorPooters, Ivo
dc.contributor.authorPellegrini, Paul A
dc.contributor.authorLengkeek, Nigel A
dc.contributor.authorGreguric, Ivan
dc.contributor.authorTonissen, Kathryn F
dc.contributor.authorSupuran, Claudiu T
dc.contributor.authorLambin, Philippe
dc.contributor.authorDubois, Ludwig
dc.contributor.authorPoulsen, Sally-Ann
dc.date.accessioned2018-01-23T01:00:27Z
dc.date.available2018-01-23T01:00:27Z
dc.date.issued2016
dc.identifier.issn0022-2623
dc.identifier.doi10.1021/acs.jmedchem.6b00623
dc.identifier.urihttp://hdl.handle.net/10072/100269
dc.description.abstractTumor hypoxia contributes resistance to chemo- and radiotherapy, while oxygenated tumors are sensitive to these treatments. The indirect detection of hypoxic tumors is possible by targeting carbonic anhydrase IX (CA IX), an enzyme overexpressed in hypoxic tumors, with sulfonamide-based imaging agents. In this study, we present the design and synthesis of novel gallium-radiolabeled small-molecule sulfonamides targeting CA IX. The compounds display favorable in vivo pharmacokinetics and stability. We demonstrate that our lead compound, [68Ga]-2, discriminates CA IX-expressing tumors in vivo in a mouse xenograft model using positron emission tomography (PET). This compound shows specific tumor accumulation and low uptake in blood and clears intact to the urine. These findings were reproduced in a second study using PET/computed tomography. Small molecules investigated to date utilizing 68Ga for preclinical CA IX imaging are scarce, and this is one of the first effective 68Ga compounds reported for PET imaging of CA IX.
dc.description.peerreviewedYes
dc.description.sponsorshipCancer Council Qld
dc.languageEnglish
dc.language.isoeng
dc.publisherAmerican Chemical Society
dc.relation.ispartofpagefrom6431
dc.relation.ispartofpageto6443
dc.relation.ispartofissue13
dc.relation.ispartofjournalJournal of Medicinal Chemistry
dc.relation.ispartofvolume59
dc.subject.fieldofresearchMedicinal and biomolecular chemistry
dc.subject.fieldofresearchMedicinal and biomolecular chemistry not elsewhere classified
dc.subject.fieldofresearchOrganic chemistry
dc.subject.fieldofresearchPharmacology and pharmaceutical sciences
dc.subject.fieldofresearchcode3404
dc.subject.fieldofresearchcode340499
dc.subject.fieldofresearchcode3405
dc.subject.fieldofresearchcode3214
dc.titleSynthesis and in Vivo Biological Evaluation of 68Ga-Labeled Carbonic Anhydrase IX Targeting Small Molecules for Positron Emission Tomography
dc.typeJournal article
dc.type.descriptionC1 - Articles
dc.type.codeC - Journal Articles
gro.facultyGriffith Sciences, School of Natural Sciences
gro.hasfulltextNo Full Text
gro.griffith.authorPoulsen, Sally-Ann
gro.griffith.authorTonissen, Kathryn F.


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