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3 results on '"Zientek, Simon H."'

1. Potential of miRNA as Imaging Targets for PET.

Author

Zientek, Simon H., Thompson, Stephen, Aigbirhio, Franklin I., and Sephton, Selena Milicevic

Subjects
*POSITRON emission tomography, *SMALL molecules, *DRUG target, *BONE remodeling, *DIAGNOSTIC imaging
Abstract

Positron Emission Tomography (PET) is an important part of the medical imaging field which is continually exploring novel biological targets as exemplified by PET imaging of neuroinflammation. Due to limitations stemming from either sub‐optimal biological targets or a lack of available selective radiotracers, alternative biomarkers and PET imaging agent candidates are considered. One such possible target is microRNA (miRNA) and herein, we discuss the potential of miRNA for PET imaging. With the aim of addressing key strategies for imaging miRNA with PET, we identify three distinct approaches as follows: small molecules directly targeting miRNA, small molecules indirectly targeting Argonaute 2 (AGO2)‐protein complexes, and direct chemical modification of antisense oligonucleotides. The radiosynthetic approaches are based on the methods of direct radiolabelling of respective antisense oligonucleotides and several examples are described herein, showcasing the potential of miRNA in PET imaging. Whilst these approaches offer different radiolabelling strategies, application of these radiolabelled molecules towards PET imaging of miRNA are scarce with only one, limited example applied to bone remodeling reported in the literature. [ABSTRACT FROM AUTHOR]

Published
2024
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3. The Inverse Electron Demand Diels Alder Cycloaddition with Carbon-11 and Fluorine-18 - A Gateway to Pretargeted Imaging across the Blood-Brain Barrier

Author

Zientek, Simon H, Thompson, Stephen, Sephton, Selena Milicevic, Aigbirhio, Franklin I, Thompson, Stephen [0000-0003-3596-7812], Sephton, Selena Milicevic [0000-0002-1105-6726], and Apollo - University of Cambridge Repository

Subjects
34 Chemical Sciences, 3406 Physical Chemistry, Neurosciences, Biomedical Imaging
Abstract

There is increased focus on developing tools to image large biomolecules, such as antibodies, within the brain using positron emission tomography (PET). The inverse electron demand Diels-Alder cycloaddition (IEDDA) reaction has offered the greatest prospect of achieving such a feat and has gained much interest over the past decade. The fast reaction kinetics of the IEDDA reaction opens up the possibility of utilising a pretargeted approach whereby the patient is pretreated with a biomolecule that has high specificity for its target. A radiolabelled second component is then administered to the patient enabling the biomolecule to be visualised by PET. However, for this to become common practice, there is a need for the development of either radiolabelled trans-cyclooctenes (TCOs) or tetrazines that can cross the blood-brain barrier (BBB). This review highlights the advancements in the development of both radiolabelled TCOs and tetrazines which have been radiolabelled with either carbon-11 or fluorine-18 and show promise or have been evaluated for use in pretargeted PET imaging across the BBB.

Published
2023

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