J Pharmacol Exp Ther 2020 12 27;375(3):451-462. Epub 2020 Sep 27.
Department of Bio-system Pharmacology, Graduate School of Medicine (C.J., L.W., R.O., M.X., S.O., H.O., Ya.K., Yo.K.) and Integrated Frontier Research for Medical Science Division, Institute for Open and Transdisciplinary Research Initiative (OTRI) (Yo.K.), Osaka University, Osaka, Japan; Department of Oncology Clinical Development, Gunma University Graduate School of Medicine, Maebashi, Gunma, Japan (H.T.); School of Traditional Chinese Medicine, Guangdong Pharmaceutical University, Guangzhou, Guangdong, China (L.W., X.H.); and Department of Collaborative Research for Bio-Molecular Dynamics, Nara Medical University, Nara, Japan (S.N.)
Halogenated tyrosine/phenylalanine derivatives have been developed for use in tumor imaging and targeted alpha therapy. 3-Fluoro--methyl-l-tyrosine (FAMT), targeting amino acid transporter LAT1 (SLC7A5), is a cancer-specific positron emission tomography probe that exhibits high renal accumulation, which is supposed to be mediated by organic anion transporter OAT1 (SLC22A6). In the present study, we investigated the structural requirements of FAMT essential for interaction with OAT1. Read More