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Synthesis and biological properties of radiohalogenated α , α ‐disubstituted amino acids for PET and SPECT imaging of amino acid transporters (AATs)
Author(s) -
Goodman Mark M.,
Yu Weiping,
Jarkas Nashwa
Publication year - 2018
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.3584
Subject(s) - chemistry , amino acid , amino acid transporter , iodine 123 , positron emission tomography , carboxylic acid , organic anion transporter 1 , transporter , biochemistry , combinatorial chemistry , nuclear medicine , medicine , gene
Fluorine‐18 and iodine‐123 labeled nonnatural alicyclic and methyl branched disubstituted α , α ‐amino acids are a diverse and useful class of tumor imaging agents suitable for positron emission tomography and single photon emission computed tomography. These tracers target the increased expression of the cell membrane amino acid transporter systems L, ASC, and A exhibited by many human tumor cells. The most established clinical use for these radiolabeled amino acids is imaging primary and recurrent gliomas and primary, recurrent, and metastatic prostate cancer. This review focuses on the synthesis, radiolabeling, and amino acid transport mechanism of a series of nonnatural fluorine‐18 and iodine‐123 labeled analogs of 1‐aminocyclobutane‐1‐carboxylic acid, 1‐aminocyclopentane‐1‐carboxylic acid, α ‐aminoisobutyric acid, and α ‐methylaminoisobutyric acid.