Targeted alpha therapy using astatine (²¹¹At)-labeled phenylalanine: A preclinical study in glioma bearing mice.

ABSTRACT: Phenylalanine derivatives, which target tumors especially through L-type amino acid transporter-1 (LAT1), have elicited considerable attention. In this study, we evaluated the treatment effect of phenylalanine labeled with the alpha emitter astatine (²¹¹At-PA) in tumor bearing mice. The C6 glioma, U-87MG, and GL261 cell lines were subjected to a cellular ²¹¹At-PA uptake analysis that included an evaluation of the uptake inhibition by the system L amino acid transporter inhibitor 2-aminobicyclo-(2,2,1)-heptane-2-carboxylic acid (BCH). BCH significantly inhibited para-²¹¹At-PA uptake in C6 glioma (12.2 ± 0.8%), U-87MG (27.6 ± 1.1%), and GL261 (12.6 ± 2.0%) cells compared to baseline, suggesting an uptake contribution by system L amino acid transporters. Subse

SUBMITTER: Watabe T 

PROVIDER: S-EPMC7170498 | biostudies-literature | 2020 Apr

REPOSITORIES: biostudies-literature