ORCID Profile
0000-0001-7919-8416
Current Organisations
Australian Nuclear Science and Technology Organisation
,
University of New South Wales - Randwick Campus
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Research Topics
In Research Link Australia (RLA), "Research Topics" refer to ANZSRC FOR and SEO codes. These topics are either sourced from ANZSRC FOR and SEO codes listed in researchers' related grants or generated by a large language model (LLM) based on their publications.
Top 5 Research Topics
ANZSRC Field of Research (FoR)
Biologically active molecules | Neurocognitive Patterns and Neural Networks | Characterisation of biological macromolecules | Medicinal and biomolecular chemistry | Biological Psychology (Neuropsychology, Psychopharmacology, Physiological Psychology) | Psychology | Biomedical imaging |
ANZSRC Socio-Economic Objective (SEO)
Expanding Knowledge in the Biological Sciences | Expanding Knowledge in Psychology and Cognitive Sciences |
Related Links
Publications
Purification of 2-[18F]fluoro-2-deoxy-d-glucose by on-chip solid-phase extraction
Publisher: Elsevier BV
Date: 03-2013
DOI: 10.1016/J.CHROMA.2013.01.032
Abstract: Microfluidic devices have shown great potential for the production of positron emission tomography (PET) radiotracers, but most devices have focused only on the synthesis step of the procedure, typically neglecting the other important steps such as [(18)F]fluoride pre-concentration and radiotracer purification that could equally benefit from miniaturisation. Here, we demonstrate the development of microfluidic modules for the purification of PET radiotracers, particularly 2-[(18)F]fluoro-2-deoxy-d-glucose ([(18)F]FDG), via the use of on-chip solid-phase extraction (SPE). In these initial tests, the SPE modules were able to yield [(18)F]FDG with up to 90% radiochemical purity, and methods are proposed for further increasing this value.
Open-field PET: Simultaneous brain functional imaging and behavioural response measurements in freely moving small animals
Publisher: Elsevier BV
Date: 03-2019
DOI: 10.1016/J.NEUROIMAGE.2018.11.051
Abstract: A comprehensive understanding of how the brain responds to a changing environment requires techniques capable of recording functional outputs at the whole-brain level in response to external stimuli. Positron emission tomography (PET) is an exquisitely sensitive technique for imaging brain function but the need for anaesthesia to avoid motion artefacts precludes concurrent behavioural response studies. Here, we report a technique that combines motion-compensated PET with a robotically-controlled animal enclosure to enable simultaneous brain imaging and behavioural recordings in unrestrained small animals. The technique was used to measure in vivo displacement of [
Design, synthesis and preliminary evaluation of 18F-labelled 1,8-naphthyridin- and quinolin-2-one-3-carboxamide derivatives for PET imaging of CB2 cannabinoid receptor
Publisher: Elsevier BV
Date: 06-2015
DOI: 10.1016/J.BMCL.2015.04.055
Abstract: In the present work, we report the synthesis of new aryliodonium salts used as precursors of single-stage nucleophilic (18)F radiofluorination. The corresponding unlabelled fluorinated derivatives showed to be CB2 cannabinoid receptor specific ligands, with Ki values in the low nanomolar range and high CB2/CB1 selectivity. The radiolabelled compound [(18)F]CB91, was successfully formulated for in vivo administration, and its preliminary biodistribution was assessed with microPET/CT. This tracer presented a reasonable in vivo stability and a preferential extraction in the tissues that constitutionally express CB2 cannabinoid receptor. The results obtained indicate [(18)F]CB91 as a possible candidate marker of CB2 cannabinoid receptor distribution. This study would open the way to further validation of this tracer for assessing pathologies for which the expression of this receptor is modified.
Sulfur - fluorine bond in PET radiochemistry
Publisher: Springer Science and Business Media LLC
Date: 17-07-2017
Effect of Rhenium(i) Complexation on Aza-Michael Additions to 5-Amino-1,10-Phenanthroline with [ 18 F]Ethenesulfonyl Fluoride towards PET Optical Tracer Development
Publisher: CSIRO Publishing
Date: 2019
DOI: 10.1071/CH18512
Abstract: Conjugations with the recently developed [18F]ethenesulfonyl fluoride ([18F]ESF) were performed on 5-amino-1,10-phenanthroline, in its free form and coordinated to a rhenium(i) tricarbonyl complex, as a means of radiosynthesizing dual-modal optical and positron emission tomography (PET) tracers. The Michael-donating ability of the aromatic amine was noticeably perturbed on coordination with the rhenium(i) centre, resulting in decreased radiochemical yields from 34%, in the case of the free ligand, to 1%. We attribute the decreased nucleophilicity of the amine to metal deactivation from the electron-withdrawing feature of the rhenium(i) tricarbonyl centre, based on spectroscopic and computational evidence, thus highlighting this effect as a crucial parameter in designing late-stage metal coordination methods employing related aza-Michael additions. Photophysical analyses were also performed on the ESF-conjugated rhenium(i) complex, exhibiting a longer decay lifetime from the triplet metal-to-ligand charge transfer excited state when compared with the non-conjugated analogue.
In vivo [64Cu]CuCl2 PET imaging reveals activity of Dextran-Catechin on tumor copper homeostasis
Publisher: Ivyspring International Publisher
Date: 2018
DOI: 10.7150/THNO.29840
The VMC survey. III. Mass-loss rates and luminosities of LMC AGB stars
Publisher: EDP Sciences
Date: 2012
Optimization of nucleophilic 18F radiofluorinations using a microfluidic reaction approach
Publisher: Springer Science and Business Media LLC
Date: 31-07-2014
Abstract: Microfluidic techniques are increasingly being used to synthesize positron-emitting radiopharmaceuticals. Several reports demonstrate higher incorporation yields, with shorter reaction times and reduced amounts of reagents compared with traditional vessel-based techniques. Microfluidic techniques, therefore, have tremendous potential for allowing rapid and cost-effective optimization of new radiotracers. This protocol describes the implementation of a suitable microfluidic process to optimize classical (18)F radiofluorination reactions by rationalizing the time and reagents used. Reaction optimization varies depending on the systems used, and it typically involves 5-10 experimental days of up to 4 h of s le collection and analysis. In particular, the protocol allows optimization of the key fluidic parameters in the first tier of experiments: reaction temperature, residence time and reagent ratio. Other parameters, such as solvent, activating agent and precursor concentration need to be stated before the experimental runs. Once the optimal set of parameters is found, repeatability and scalability are also tested in the second tier of experiments. This protocol allows the standardization of a microfluidic methodology that could be applied in any radiochemistry laboratory, in order to enable rapid and efficient radiosynthesis of new and existing [(18)F]-radiotracers. Here we show how this method can be applied to the radiofluorination optimization of [(18)F]-MEL050, a melanoma tumor imaging agent. This approach, if integrated into a good manufacturing practice (GMP) framework, could result in the reduction of materials and the time required to bring new radiotracers toward preclinical and clinical applications.
The VMC survey
Publisher: EDP Sciences
Date: 04-02-2011
Optimization of automated large-scale production of [18F]fluoroethylcholine for PET prostate cancer imaging
Publisher: Elsevier BV
Date: 07-2009
DOI: 10.1016/J.NUCMEDBIO.2009.01.004
Abstract: PET tumor imaging is gaining importance in current clinical practice. FDG-PET is the most utilized approach but suffers from inflammation influences and is not utilizable in prostate cancer detection. Recently, (11)C-choline analogues have been employed successfully in this field of imaging, leading to a growing interest in the utilization of (18)F-labeled analogues: [(18)F]fluoroethylcholine (FEC) has been demonstrated to be promising, especially in prostate cancer imaging. In this work we report an automatic radiosynthesis of this tracer with high yields, short synthesis time and ease of performance, potentially utilizable in routine production sites. We used a Modular Lab system to automatically perform the two-step/one-pot synthesis. In the first step, we labeled ethyleneglycolditosylate obtaining [(18)F]fluoroethyltosylate in the second step, we performed the coupling of the latter intermediate with neat dimethylethanolamine. The final mixture was purified by means of solid phase extraction in particular, the product was trapped into a cation-exchange resin and eluted with isotonic saline. The optimized procedure resulted in a non decay corrected yield of 36% and produced a range of 30-45 GBq of product already in injectable form. The product was analyzed for quality control and resulted as pure and sterile in addition, residual solvents were under the required threshold. In this work, we present an automatic FEC radiosynthesis that has been optimized for routine production. This findings should foster the interest for a wider utilization of this radiomolecule for imaging of prostate cancer with PET, a field for which no gold-standard tracer has yet been validated.
Microfluidics in radiopharmaceutical chemistry
Publisher: Elsevier BV
Date: 08-2013
DOI: 10.1016/J.NUCMEDBIO.2013.04.004
Abstract: The increased demand for molecular imaging tracers useful in assessing and monitoring diseases has stimulated research towards more efficient and flexible radiosynthetic routes, including newer technologies. The traditional vessel-based approach suffers from limitations concerning flexibility, reagent mass needed, hardware requirements, large number of connections and valves, repetitive cleaning procedures and overall big footprint to be shielded from radiation. For these reasons, several research groups have started to investigate the application of the fast growing field of microfluidic chemistry to radiosynthetic procedures. After the first report in 2004, many scientific papers have been published and demonstrated the potential for increased process yields, reduced reagent use, improved flexibility and general ease of setup. This review will address definitions occurring in microfluidics as well as analyze the different approaches under two macro-categories: microvessel and microchannel. In this perspective, several works will be collected, involving the use of positron emitting species ((11)C, (18)F, (64)Cu) and the fewer ex les of gamma emitting radionuclides ((99m)Tc, (125/131)I). New directions in microfluidic research applied to PET radiochemistry, future developments and challenges are also discussed.
How Far Are We from Dose On Demand of Short-Lived Radiopharmaceuticals?
Publisher: Springer Japan
Date: 2016
Frontispiece: Fluorine‐18 Radiolabelling and Photophysical Characteristics of Multimodal PET–Fluorescence Molecular Probes
Publisher: Wiley
Date: 13-01-2021
Elemental contamination of an open-pit mining area in the Peruvian Andes
Publisher: Springer Science and Business Media LLC
Date: 21-01-2014
The ACS Nearby Galaxy Survey Treasury. II. Young Stars and their Relation to Hα and UV Emission Timescales in the M81 Outer Disk
Publisher: American Astronomical Society
Date: 07-01-2009
Microfluidic Radiosynthesis of the Muscarinic M2 Imaging Agent [18F]FP-TZTP
Publisher: CSIRO Publishing
Date: 2018
DOI: 10.1071/CH18266
Abstract: 3-(4-(3-[18F]Fluoropropylthio)-1,2,5-thiadiazol-3-yl)-1-methyl-1,2,5,6-tetrahydropyridine ([18F]FP-TZTP) is a selective 18F-radiotracer for the muscarinic acetylcholine receptor subtype M2, which can be used to perform positron emission tomography (PET) scans on patients with neurological disorders such as Alzheimer’s disease. [18F]FP-TZTP was produced using continuous-flow microfluidics, a technique that uses reduced amounts of chemical reagents, shorter reaction times and in general, results in higher radiochemical yields compared to currently used techniques. The optimal 18F-radiolabelling conditions consisted of a total flow rate of 40 µL min−1 and 190°C, which produced [18F]FP-TZTP in 26 ± 10 % radiochemical yield with a molar activity of 182 ± 65 GBq µmol−1 and % radiochemical purity.
Tolerance of Water in Microfluidic Radiofluorinations: A Potential Methodological Shift?
Publisher: Springer Science and Business Media LLC
Date: 07-2014
Dose-on-demand production of diverse 18 F-radiotracers for preclinical applications using a continuous flow microfluidic system
Publisher: Elsevier BV
Date: 09-2017
DOI: 10.1016/J.NUCMEDBIO.2017.05.004
Abstract: The production of [ The complete productions for [ Using the same initial solution of [
Novel Strategy for Non-Aqueous Bioconjugation of Substituted Phenyl-1,2,4-triazole-3,5-dione Analogues
Publisher: MDPI AG
Date: 07-10-2022
DOI: 10.3390/MOLECULES27196667
Abstract: A novel 4-[4-(pentafluoro-λ⁶-sulfanyl)phenyl]-1,2,4-triazole-3,5-dione (5a) was synthesised as a potential [18F]radio-prosthetic group for radiolabelling peptides and proteins via selective bioconjugation with the phenolic side chains of tyrosine residues. Preliminary conjugation tests revealed the rapid hydrolysis of 5a under semi-aqueous conditions these results led to further investigation into the electronic substituent effects of PTAD derivatives and corresponding hydrolytic stabilities. Five derivatives of 5a with para substituents of varying electron donating and withdrawing effects were synthesised for the investigation. The bioconjugation of these derivatives with model tyrosine was monitored in both aqueous and organic media in the presence of a variety of catalysts. From these investigations, we have found HFIP to be an effective catalyst when used in tandem with DCM as a solvent to give PTAD-tyrosine conjugate products (6a–f) in satisfactory to good yields (54–79%), whereas analogous reactions performed in acetonitrile were unsuccessful. The discovery of this system has allowed for the successful conjugation of electron-deficient PTAD derivatives to tyrosine, which would otherwise be unachievable under aqueous reaction conditions. The inclusion of these electron-deficient, fluorinated PTAD derivatives for use in the PTAD-tyrosine conjugation will hopefully broaden their applicability within fields such as 19F-MRI and PET imaging.
Dose-on-demand of diverse 18F-fluorocholine derivatives through a two-step microfluidic approach
Publisher: Elsevier BV
Date: 07-2011
DOI: 10.1016/J.NUCMEDBIO.2011.01.005
Abstract: The validation and confirmation of clinical usefulness of new and known positron emission tomography (PET) tracers require stable production routes and simple and robust radiochemical procedures. Microfluidic technologies are regarded as an approach that could allow an unprecedented flexibility and productivity in PET radiopharmaceutical research. In this work, we will show how a commercially available microfluidic system can be used for a sequential and repeatable radiosynthesis of three different fluorocholine analogues currently under investigation as tumor tracers. Advion microfluidic system was used for performing the synthesis and purification of [(18)F]fluoromethyl, [(18)F]fluoroethyl or [(18)F]fluoropropyl choline employing a two-step approach, starting from the corresponding alkyl-ditosylate and reacting the [(18)F]fluorotosylate obtained in the first step with neat dimethylethanolamine. The purification was obtained using a recyclable SPE cartridge set. The three products, fluoromethylcholine, fluoroethylcholine and fluoropropylcholine, were obtained in good to optimum yields (22%-54% decay corrected) with a 15-min procedure. The production could be restarted several times for producing each one of the tracers without decrease in yields and purities, in accordance with a dose-on-demand (DOD) approach. The final products were formulated in isotonic saline solution. The described approach gives a proof of principle of the enhanced productivity obtainable using a microfluidic approach in particular, the possibility to produce the reported tracers in a DOD fashion following a homogeneous synthetic and purification approach will foster further studies on the clinical evaluation of the best fluorocholine analogue for prostate cancer imaging without biasing for differences in radiochemical approach.
THE ACS NEARBY GALAXY SURVEY TREASURY. I. THE STAR FORMATION HISTORY OF THE M81 OUTER DISK
Publisher: American Astronomical Society
Date: 19-12-2008
Preliminary Investigation of a Novel
Publisher: CSIRO Publishing
Date: 02-2021
DOI: 10.1071/CH20247
Abstract: We successfully radiolabelled a novel prospective cannabinoid type 2 receptor ligand with 18F and tested its biodistribution in animal models by positron emission tomography (PET)/computed tomography (CT) imaging. The radiolabelling process was conducted on an alkyl mesylate fragment of the main naphthyridine core, using highly efficient microfluidic technology. No preliminary protection was needed, and the product was purified by semi-prep HPLC and SPE formulation, allowing the desired diastereomeric mixture to be obtained in 29 % radiochemical yield and 95 % radiochemically pure. SOD1G93A mice were used as model of overexpression of CB2 receptors PET imaging revealed a significant increase of the tracer distribution volume in the brain of symptomatic subjects compared with the asymptomatic ones.
Fabrication of SU-8 microreactors for radiopharmaceutical production
Publisher: Elsevier BV
Date: 08-2011
Positron Emission Tomography Radiosynthesis in Microreactors
Publisher: Springer Science and Business Media LLC
Date: 06-2012
THE ACS NEARBY GALAXY SURVEY TREASURY
Publisher: American Astronomical Society
Date: 19-06-2009
Labeled Rhenium Complexes: Radiofluorination, α-MSH Cyclization, and Deuterium Substitutions
Publisher: American Chemical Society (ACS)
Date: 19-06-2020
Microfluidics in Planar Microchannels: Synthesis of Chemical Compounds On-Chip
Publisher: Springer International Publishing
Date: 14-10-2014
Use of 1,8-bis-(dimethylamino)-naphthalene/H18F complex as new radiofluorinating agent
Publisher: Wiley
Date: 05-2004
DOI: 10.1002/JLCR.823
Microfluidic implementation of Ru-catalyzed methylation of amines using CO2 as carbon source
Publisher: Springer Science and Business Media LLC
Date: 12-2016
Ensemble Asteroseismology of Solar-Type Stars with the NASA Kepler Mission
Publisher: American Association for the Advancement of Science (AAAS)
Date: 08-04-2011
Abstract: Measurements of 500 Sun-like stars show that their properties differ from those predicted by stellar population models.
Fluorine-18 Radiolabelling and Photophysical Characteristics of Multimodal PET–Fluorescence Molecular Probes
Publisher: Wiley
Date: 09-11-2021
Hardware and software modifications on the Advion NanoTek microfluidic platform to extend flexibility for radiochemical synthesis
Publisher: Elsevier BV
Date: 02-2014
DOI: 10.1016/J.APRADISO.2013.10.020
Abstract: Microfluidic systems are currently receiving a lot of attention in the PET radiochemistry field, due to their demonstrated ability to obtain higher incorporation yields with reduced total processing time and using a decreased amount of precursors. The Advion NanoTek LF was the first commercial microfluidic system available for radiochemistry that allows basic parameter optimization to be performed. In this paper we report hardware and software modifications that would allow better performing procedures, higher product throughput and flexibility to utilize the system. In particular, HPLC purification and SPE formulation have been fully integrated.
Perspectives on the Use of Liquid Extraction for Radioisotope Purification
Publisher: MDPI AG
Date: 18-01-2019
DOI: 10.3390/MOLECULES24020334
Abstract: The reliable and efficient production of radioisotopes for diagnosis and therapy is becoming an increasingly important capability, due to their demonstrated utility in Nuclear Medicine applications. Starting from the first processes involving the separation of 99mTc from irradiated materials, several methods and concepts have been developed to selectively extract the radioisotopes of interest. Even though the initial methods were based on liquid-liquid extraction (LLE) approaches, the perceived difficulty in automating such processes has slowly moved the focus towards resin separation methods, whose basic chemical principles are often similar to the LLE ones in terms of chelators and phases. However, the emerging field of flow chemistry allows LLE to be easily automated and operated in a continuous manner, resulting in an even improved efficiency and reliability. In this contribution, we will outline the fundamentals of LLE processes and their translation into flow-based apparatuses in addition, we will provide ex les of radioisotope separations that have been achieved using LLE methods. This article is intended to offer insights about the future potential of LLE to purify medically relevant radioisotopes.
Development of an automated modular system for the synthesis of [11C]acetate
Publisher: Ovid Technologies (Wolters Kluwer Health)
Date: 12-2010
On-chip pre-concentration and complexation of [18F]fluoride ions via regenerable anion exchange particles for radiochemical synthesis of Positron Emission Tomography tracers
Publisher: Elsevier BV
Date: 07-2011
DOI: 10.1016/J.CHROMA.2011.05.062
Abstract: Microfluidic approaches have demonstrated a relevant impact on radiochemical reactions involving Positron Emission Tomography (PET) nuclides, due to shorter reaction times and smaller precursor quantities. However, little attention has been given to the integration of the initial pre-concentration and drying of radioactive [(18)F]fluoride ions, required for the labeling of radiotracer compounds. In this work we report the design, fabrication and implementation of a glass microfluidic device filled with recyclable anion exchange particles for the repeated recovery of [(18)F] and [(19)F]fluoride ions. The device was first tested with non radioactive [(19)F]fluoride ions and it was shown to repeatedly trap and elute >95% fluoride over 40 successive experimental runs with no decrease in efficiency. The same device was then tested for the trapping and release of [(18)F]fluoride ions over 20 experiments with no measurable decrease in performance. Finally, the [(18)F]fluoride ions were eluted as a K(18)F/K2.2.2 complex, dried by repeated dissolution in acetonitrile and evaporation of residual water, and reacted with ethyl ditosylate (EtDT) leading to the desired product ([(18)F]fluoroethyltosylate) with 96 ± 3% yield (RCY). The overall time needed for conditioning, trapping, elution and regeneration was less than 6 min. This approach will be of great benefit towards an integrated platform able to perform faster and safer radiochemical synthesis on the micro-scale.
Radioactivity resistance evaluation of polymeric materials for application in radiopharmaceutical production at microscale
Publisher: Springer Science and Business Media LLC
Date: 03-02-2011
[18F]Ethenesulfonyl Fluoride as a Practical Radiofluoride Relay Reagent
Publisher: Wiley
Date: 09-05-2019
Abstract: Fluorine-18 is the most utilized radioisotope in positron emission tomography (PET), but the wide application of fluorine-18 radiopharmaceuticals is hindered by its challenging labelling conditions. As such, many potentially important radiotracers remain underutilized. Herein, we describe the use of [
Synthesis, bioconjugation and stability studies of [18F]ethenesulfonyl fluoride
Publisher: Wiley
Date: 12-07-2018
DOI: 10.1002/JLCR.3667
Abstract: Fluorine-18 labelled prosthetic groups (PGs) are often necessary for radiolabelling sensitive biological molecules such as peptides and proteins. Several shortcomings, however, often diminish the final yield of radiotracer. In an attempt to provide higher yielding and operationally efficient tools for radiolabelling biological molecules, we describe herein the first radiochemical synthesis of [
Telescoping the Synthesis of the [18F]CABS13 Alzheimer's Disease Radiopharmaceutical via Flow Microfluidic Rhenium(I) Complexations
Publisher: Wiley
Date: 24-09-2020
Microfluidic approach for fast labeling optimization and dose-on-demand implementation
Publisher: Elsevier BV
Date: 07-2010
DOI: 10.1016/J.NUCMEDBIO.2010.03.006
Abstract: The diffusion of PET as a pivotal molecular imaging modality has emphasized the need for new positron-emitting radiotracers to be used in diagnostic applications and research. Microfluidic represents an innovative approach, owing to its potential to increase radiochemical productivity in terms of yields, time reduction, precursor consumption and flexible experimental planning. We focused on fluorine-18 labeling and used a microfluidic platform to perform sequential reactions, by using the same batch of (18)F-labeling solution on one or more substrates, during the same experimental session. A solid-phase extraction (SPE) workup procedure was also implemented in the system to provide a repeatable purification step. We were able to quickly optimize the conditions for labeling of ethyl and propyl ditosylate and of a new cannabinoid type 2 (CB2) receptor agonist, CB41. In all substrates, we obtained good incorporation yields (60% to 85%) in short (<90 s) reaction times. Single dosages of the CB2 ligand were sequentially prepared, upon request, in satisfactory quantities and purity for small animal PET scanning. This work demonstrates the usefulness of a microfluidic-based system for a rapid optimization of temperature, flow rate of reactants and their relative ratio in the labeling of different precursors by using the same (18)F-fluoride batch. This approach was used to obtain in sequence several injectable doses of a novel CB2 ligand, thus providing the proof of principle that microfluidic systems permit a dose-on-demand production of new radiotracers.
A Fluorine-18 Radiolabeling Method Enabled by Rhenium(I) Complexation Circumvents the Requirement of Anhydrous Conditions
Publisher: Wiley
Date: 11-04-2017
Abstract: Azeotropic distillation is typically required to achieve fluorine-18 radiolabeling during the production of positron emission tomography (PET) imaging agents. However, this time-consuming process also limits fluorine-18 incorporation, due to radioactive decay of the isotope and its adsorption to the drying vessel. In addressing these limitations, the fluorine-18 radiolabeling of one model rhenium(I) complex is reported here, which is significantly improved under conditions that do not require azeotropic drying. This work could open a route towards the investigation of a simplified metal-mediated late-stage radiofluorination method, which would expand upon the accessibility of new PET and PET-optical probes.
Rhenium(i ) complexation–dissociation strategy for synthesising fluorine-18 labelled pyridine bidentate radiotracers
Publisher: Royal Society of Chemistry (RSC)
Date: 2020
DOI: 10.1039/D0RA00318B
Abstract: A novel fluorine-18 radiolabelling method employing rhenium( i ) mediation is described herein. In less than 1 minute, fluorine-18 labelled complexes and ligands were synthesised in greater than 80% and 60% radiochemical yields (RCY), respectively.
A micro-PET/CT approach using O-(2-[18F]fluoroethyl)-l-tyrosine in an experimental animal model of F98 glioma for BNCT
Publisher: Elsevier BV
Date: 12-2011
DOI: 10.1016/J.APRADISO.2011.02.037
Abstract: The present study focuses on a micro-PET/CT application to be used for experimental Boron Neutron Capture Therapy (BNCT), which integrates, in the same frame, micro-CT derived anatomy and PET radiotracer distribution. Preliminary results have demonstrated that (18)F-fluoroethyl-tyrosine (FET)/PET allows the identification of the extent of cerebral lesions in F98 tumor bearing rat. Neutron autoradiography and α-spectrometry on axial tissues slices confirmed the tumor localization and extraction, after the administration of fructose-boronophenylalanine (BPA). Therefore, FET-PET approach can be used to assess the transport, the net influx, and the accumulation of FET, as an aromatic amino acid analog of BPA, in experimental animal model. Coregistered micro-CT images allowed the accurate morphological localization of the radiotracer distribution and its potential use for experimental BNCT.
[18F]Fluorination Optimisation and the Fully Automated Production of [18F]MEL050 Using a Microfluidic System
Publisher: CSIRO Publishing
Date: 2015
DOI: 10.1071/CH14130
Abstract: The [18F]radiolabelling of the melanin-targeting positron-emission tomography radiotracer [18F]MEL050 was rapidly optimised using a commercial continuous-flow microfluidic system. The optimal [18F]fluorination incorporation conditions were then translated to production-scale experiments (35–150 GBq) suitable for preclinical imaging, complete with automated HPLC–solid phase extraction purification and formulation. [18F]MEL050 was obtained in 43 ± 10 % radiochemical yield in ~50 min.
The Magellanic Clouds as a Template for the Study of Stellar Populations and Galaxy Interactions
Publisher: Cambridge University Press (CUP)
Date: 2008
DOI: 10.1071/AS07046
Abstract: The Magellanic System represents one of the best places to study the formation and evolution of galaxies. Photometric surveys of various depths, areas and wavelengths have had a significant impact on our understanding of the system however, a complete picture is still lacking. VMC (the VISTA near-infrared YJK s survey of the Magellanic System) will provide new data to derive the spatially resolved star formation history and to construct a three-dimensional map of the system. These data combined with those from other ongoing and planned surveys will give us an absolutely unique view of the system opening up the doors to truly new science!
Identification of chemical byproducts in the radiofluorination of structurally complex aryliodonium salts
Publisher: Springer Science and Business Media LLC
Date: 24-08-2014
Evaluation of Substituted N-Aryl Maleimide and Acrylamides for Bioconjugation
Publisher: MDPI AG
Date: 15-05-2023
DOI: 10.3390/APPLIEDCHEM3020016
Abstract: Novel SF5-bearing maleimide and acrylamide derivatives were synthesised as potential [18F]radio-prosthetic groups for radiolabelling peptides and proteins. The efficacy of selected prosthetic groups was first assessed through bioconjugation with protected model amino acid derivatives. These reactions were investigated on an analytical scale via LC-MS across a pH range to quantitatively evaluate this prosthetic group’s reactivity and stability. Model bioconjugate reactions were then replicated using analogous para-substituted derivatives to determine the influence of the electronic effects of -SF5. Finally, the SF5-bearing prosthetic groups were utilised for bioconjugation with cancer-targeting c-RGD peptides. N-aryl maleimides reacted extremely efficiently with the model amino acid N-acetyl-L-cysteine. The subsequent conjugates were obtained as regio-isomeric mixtures of the corresponding thio-succinamic acids in yields of 80–96%. Monitoring the bioconjugate reaction by LC-MS revealed that ring hydrolysis of the intermediate SF5–thio-succinimide conjugate occurred instantaneously, an advantageous quality in minimising undesirable thiol exchange reactions with non-targeted cysteine residues. In contrast, N-aryl acrylamides demonstrated poor solubility in semi-aqueous media ( mM). In turn, synthetic-scale model bioconjugations with Nα-acetyl-L-lysine were performed in methanol, affording the corresponding acrylamide conjugates in modest to high yield (58–89%). Including electron-deficient, fluorinated prosthetic groups for bioconjugation will broaden their applicability within the fields of 19F-MRI and PET imaging.
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Australian Nuclear Science And Technology Organisation
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