In this section
@article{Zhu:2026:10.1021/jacsau.5c00946,
author = {Zhu, Y and Cheng, Z and Zhang, J and Feng, L and Mishra, A and de, Rosales RTM and Brown, RK and Long, N and Law, G-L},
doi = {10.1021/jacsau.5c00946},
journal = {JACS Au},
pages = {113--123},
title = {Influences of Ring Sizes and Chiral Substituents on Macrocyclic Chelators for Improving 68Ga Radiolabeling.},
url = {http://dx.doi.org/10.1021/jacsau.5c00946},
volume = {6},
year = {2026}
}
TY - JOUR
AB - 68Ga-labeled macrocyclic ligands have been extensively studied and used for positron emission tomography (PET) imaging. Compared with 12-membered DOTA derivatives, NOTA-based chelators with 9-membered macrocyclic rings exhibit more advantageous coordination stability for Ga3+ ions. However, studies of the 10-membered DETA macrocycle are still quite limited. Here, we present the synthesis of four different-sized chiral macrocyclic ligands L1-L4, followed by radiolabeling and stability studies to reveal the influence of ring size and chiral substituents on Ga3+ chelation. In the 68Ga radiolabeling experiments, chiral NOTA L1 exhibits the highest radiochemical yield of 99% at 25 °C. While for the chiral DETA L2/L3 and the chiral DOTA L4, their radiolabeling efficiencies are inferior at room temperature, but remarkable improvements were observed at higher temperatures. L1-L4 all exhibit superior Ga3+ coordination stability than their achiral counterparts, while the chiral DETA L2 with an α-methyl group shows a slightly better performance than its β-analogue L3. Serum stability tests and kinetic studies under acid and alkaline conditions were conducted, highlighting the favorable kinetic inertness of these chiral ligands for potential 68Ga-labeled PET imaging applications.
AU - Zhu,Y
AU - Cheng,Z
AU - Zhang,J
AU - Feng,L
AU - Mishra,A
AU - de,Rosales RTM
AU - Brown,RK
AU - Long,N
AU - Law,G-L
DO - 10.1021/jacsau.5c00946
EP - 123
PY - 2026///
SP - 113
TI - Influences of Ring Sizes and Chiral Substituents on Macrocyclic Chelators for Improving 68Ga Radiolabeling.
T2 - JACS Au
UR - http://dx.doi.org/10.1021/jacsau.5c00946
UR - https://www.ncbi.nlm.nih.gov/pubmed/41614168
VL - 6
ER -
Professor Nick Long
Email: n.long@imperial.ac.uk
Telephone: +44 (0)20 7594 5781
501J
Molecular Sciences Research Hub
White City Campus
