The N-acetyltransferase 10 inhibitor [¹¹C]remodelin: synthesis and preliminary positron emission tomography study in mice.

ABSTRACT:

Background

4-(4-Cyanophenyl)-2-(2-cyclopentylidenehydrazinyl)thiazole (remodelin) is a potent N-acetyltransferase 10 (NAT10) inhibitor. This compound inhibits tumors and weakens tumor resistance to antitumor drugs. Moreover, remodelin has been found to enhance healthspan in an animal model of the human accelerated ageing syndrome. In this study, we synthesized C-11-labelled remodelin ([¹¹C]remodelin) for the first time as a positron emission tomography (PET) probe and assessed its biodistribution in mice using PET.

Results

[¹¹C]Remodelin was synthesized by the reaction of a boron ester precursor (1) with hydrogen [¹¹C]cyanide, which was prepared from the cyclotron-produced [¹¹C]carbon dioxide via [¹¹C]methane. The decay-

SUBMITTER: Luo R 

PROVIDER: S-EPMC11785860 | biostudies-literature | 2025 Jan

REPOSITORIES: biostudies-literature