Key result
Novel radiotracer 18F-MLN-4760 enables specific PET imaging of ACE2 expression with strong uptake correlation.
Why the study?
ACE2 is a key regulatory molecule and therapeutic target in pathological remodeling, necessitating development of efficient imaging agents for ACE2 expression.
18F-MLN-4760 was successfully synthesized and demonstrated potential as a specific probe for ACE2-targeted PET imaging in a preclinical model.
Answers are grounded in this paper and cite their sources.
Advances preclinical ACE2 imaging tools; leaves open human validation and clinical utility.
Angiotensin-converting enzyme-2 (ACE2) acts as a key regulatory molecule and important therapeutic target in the pathological remodeling of numerous organs and diseases. In this study, a rapid, simple, and efficient synthetic route with a catalytic, 18 F-for-Cl ( 18 F/Cl) exchange scheme was designed for the preparation of 18 F-labeled MLN-4760, and its targeting ability was investigated in a humanized ACE2 mouse model. A novel 18 F-labeled MLN-4760 radioligand, abbreviated as 18 F-MLN-4760, was successfully synthesized by the 18 F/Cl exchange-labeling, and was purified by SepPak C18 columns with a radiochemical yield of 30% and a radiochemical purity of 29.89%. Target distribution of 18 F-MLN-4760 in several organs with high ACE2 expression was observed by PET imaging with good stability over 120 min. The biodistribution data showed that the uptake of 18 F-MLN-4760 in ACE2-overexpressing organs and tissues was highly specific, and immunohistochemistry confirmed the same results of ACE2 expression and biodistribution in the major organs (heart, liver, lungs, and kidneys). There was a good correlation between the uptake in the organs with high ACE2 expression and ACE2 expression levels ( r = 0.935). 18 F-MLN-4760 was successfully synthesized via 18 F/Cl exchange under phase transfer catalysis, and served as a potential probe for ACE2-targeted PET imaging.
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Zhou et al. (2024) studied ACE2 expression. 18F-MLN-4760 was evaluated on Correlation between organ uptake and ACE2 expression levels (r = 0.935). 18F-MLN-4760 was successfully synthesized and demonstrated highly specific uptake in ACE2-overexpressing organs, with a strong correlation to ACE2 expression levels (r = 0.935).
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