Chiral DOTA chelators as an improved platform for biomedical imaging and therapy applications

Lixiong Dai, Chloe M. Jones, Wesley Ting Kwok Chan, Tiffany A. Pham, Xiaoxi Ling, Eric M. Gale, Nicholas J. Rotile, William Chi-Shing Tai, Carolyn J. Anderson (), Peter Caravan () and Ga-Lai Law ()
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Lixiong Dai: The Hong Kong Polytechnic University
Chloe M. Jones: Massachusetts General Hospital and Harvard Medical School
Wesley Ting Kwok Chan: The Hong Kong Polytechnic University
Tiffany A. Pham: University of Pittsburgh
Xiaoxi Ling: University of Pittsburgh
Eric M. Gale: Massachusetts General Hospital and Harvard Medical School
Nicholas J. Rotile: Massachusetts General Hospital and Harvard Medical School
William Chi-Shing Tai: The Hong Kong Polytechnic University
Carolyn J. Anderson: University of Pittsburgh
Peter Caravan: Massachusetts General Hospital and Harvard Medical School
Ga-Lai Law: The Hong Kong Polytechnic University

Nature Communications, 2018, vol. 9, issue 1, 1-10

Abstract: Abstract Despite established clinical utilisation, there is an increasing need for safer, more inert gadolinium-based contrast agents, and for chelators that react rapidly with radiometals. Here we report the syntheses of a series of chiral DOTA chelators and their corresponding metal complexes and reveal properties that transcend the parent DOTA compound. We incorporated symmetrical chiral substituents around the tetraaza ring, imparting enhanced rigidity to the DOTA cavity, enabling control over the range of stereoisomers of the lanthanide complexes. The Gd chiral DOTA complexes are shown to be orders of magnitude more inert to Gd release than [GdDOTA]−. These compounds also exhibit very-fast water exchange rates in an optimal range for high field imaging. Radiolabeling studies with (Cu-64/Lu-177) also demonstrate faster labelling properties. These chiral DOTA chelators are alternative general platforms for the development of stable, high relaxivity contrast agents, and for radiometal complexes used for imaging and/or therapy.

Date: 2018
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DOI: 10.1038/s41467-018-03315-8

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