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Updated: Nov 4, 2025

Preparation and Evaluation of 99mTc-labeled Tridentate Chelates for Pre-targeting Using Bioorthogonal Chemistry
Published on: February 4, 2017
Emerging chelators for nuclear imaging
Deborah Sneddon1, Bart Cornelissen1
1MRC Oxford Institute for Radiation Oncology, Department of Oncology, University of Oxford, OX3 7LE, United Kingdom.
Abstract:
Chelators are necessary in nuclear medicine imaging to direct an inorganic radionuclide, a radiometal, to a desired target; unfortunately, there is no 'one-size-fits-all' chelator. As the toolbox of radiometals is expanding, new chelators are required to prevent off-target side effects. 1,4,7,10-Tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) is the current gold standard chelator for several radiometals, but typically, chelation requires harsh conditions, making it unsuitable to label biological vectors. The ideal chelator would allow labelling under mild conditions (near-neutral pH and low temperatures [∼37 °C]) and be both thermodynamically and kinetically stable. Over the past 2-3 years, several exciting chelators have been developed that have superior properties to make them worth investigating for future clinical applications.
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