Development of novel ligands for emerging radiometal isotopes

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dc.contributor.authorAshford, MEen_AU
dc.contributor.authorBurgess, Len_AU
dc.contributor.authorCheah, WCen_AU
dc.contributor.authorKrause-Heuer, AMen_AU
dc.contributor.authorFraser, BHen_AU
dc.contributor.authorGreguric, Ien_AU
dc.contributor.authorLengkeek, NAen_AU
dc.date.accessioned2021-08-11T04:52:36Zen_AU
dc.date.available2021-08-11T04:52:36Zen_AU
dc.date.issued2013-04-11en_AU
dc.date.statistics2021-08-10en_AU
dc.descriptionOpen Accessen_AU
dc.description.abstractBackground: The use of radiometals (non-Tc, non-Re) in targeted diagnosis and radiotherapy of different disease states has increased significantly over the last 15 years. ANSTO LifeSciences radiometals program seeks to provide a suite of radiometal tools for use in PET imaging and therapeutic modalities to improve upon the existing technologies which are currently dominated by 99mTc. This will enable researchers and clinicians to study and diagnose diseases with a greater efficacy and efficiency. Method: Many of the ligands currently available for radiometals have numerous drawbacks , including unfavourable in vivo properties such as thermodynamic and kinetic stability and poor lipophilicity. We are developing new ligand systems to have improved radiometal specificity while including design flexibility allowing us to manipulate properties such as biodistribution patterns, excretion rates, pharmacokinetics, thermodynamics and in vivo stability. The synthesis should be straightforward and cost effective and have the potential for bioconjugation in the initial design. Complexation studies are performed in vitro to assess the ligands suitability. Results: We are developing ligand systems for 68Ga, 89Zr, 64Cu, 90Y and 177Lu. We have prepared a novel analogue of the ubiquitous ligand NOTA (Figure 1, b); our system replaces the biologically labile carboxylic acid with a corresponding, biologically inert isotere, a tetrazole. This manipulation should provide additional stability and increased complex lipophilicity. Our studies have shown that a tetrazole analogue of NOTA (Figure 1, b) forms stable cold-metal complexes with potential PET metals of interest such as Ga3+. Conclusion: ANSTO LifeSciences provides a complete synthetic ligand and metal complex program, complementing its broader Radiometals Program. The aim of which is to provide an array of clinically relevant ligands that can be used in multiple applications for specific metal radiopharmaceuticals for improved patient outcomes. © 2013 John Wiley & Sonsen_AU
dc.identifier.citationAshford, M., Burgess, L., Cheah, W. C., Krause-Heuer, A., Fraser, B., Greguric, I., & Lengleek, N. (2015). Development of novel ligands for emerging radiometal isotopes. Poster presented at the 43rd Annual Scientific Meeting of the Australian and New Zealand Society of Nuclear Medicine (ANZSNM), 11-15 April, 2013, Perth Convention and Exhibition Centre, Perth, Australia. In Internal Medicine Journal, 43 (S1), 34. doi:10.1111/imj.12133en_AU
dc.identifier.conferenceenddate15 April 2013en_AU
dc.identifier.conferencename43rd Annual Scientific Meeting of the Australian and New Zealand Society of Nuclear Medicine (ANZSNM), Perth Convention and Exhibition Centre, Perth, Australiaen_AU
dc.identifier.conferenceplacePert, Australiaen_AU
dc.identifier.conferencestartdate11 April 2013en_AU
dc.identifier.issn1445-5994en_AU
dc.identifier.issueSupplement 1en_AU
dc.identifier.journaltitleInternal Medicine Journalen_AU
dc.identifier.pagination34en_AU
dc.identifier.urihttps://doi.org/10.1111/imj.12133en_AU
dc.identifier.urihttps://apo.ansto.gov.au/dspace/handle/10238/11324en_AU
dc.identifier.volume41en_AU
dc.language.isoenen_AU
dc.publisherJohn Wiley & Sons, Inc.en_AU
dc.subjectRadiotherapyen_AU
dc.subjectANSTOen_AU
dc.subjectPositron computed tomographyen_AU
dc.subjectDiseasesen_AU
dc.subjectIn vitroen_AU
dc.subjectLigandsen_AU
dc.subjectThermodynamicsen_AU
dc.subjectKineticsen_AU
dc.titleDevelopment of novel ligands for emerging radiometal isotopesen_AU
dc.typeConference Posteren_AU
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