title: Boramino acid as a marker for amino acid transporters.
abstract: Amino acid transporters (AATs) are a series of integral channels for uphill cellular uptake of nutrients and neurotransmitters. Abnormal expression of AATs is often associated with cancer, addiction, and multiple mental diseases. Although methods to evaluate in vivo expression of AATs would be highly useful, efforts to develop them have been hampered by a lack of appropriate tracers. We describe a new class of AA mimics-boramino acids (BAAs)-that can serve as general imaging probes for AATs. The structure of a BAA is identical to that of the corresponding natural AA, except for an exotic replacement of the carboxylate with -BF3 (-). Cellular studies demonstrate strong AAT-mediated cell uptake, and animal studies show high tumor-specific accumulation, suggesting that BAAs hold great promise for the development of new imaging probes and smart AAT-targeting drugs.
authors.affiliation: Laboratory of Molecular Imaging and Nanomedicine, National Institute of Biomedical Imaging and Bioengineering, National Institutes of Health (NIH), Bethesda, MD 20892, USA.
authors.forename: Zhibo
authors.initials: Z
authors.lastname: Liu
authors.affiliation: Laboratory of Molecular Imaging and Nanomedicine, National Institute of Biomedical Imaging and Bioengineering, National Institutes of Health (NIH), Bethesda, MD 20892, USA. ; Department of nuclear medicine, Xiamen Cancer Center, First Affiliated Hospital of Xiamen University, Xiamen 361003, China.
authors.forename: Haojun
authors.initials: H
authors.lastname: Chen
authors.affiliation: Department of Radiology, Keck School of Medicine, University of Southern California, Los Angeles, CA 90089, USA.
authors.forename: Kai
authors.initials: K
authors.lastname: Chen
authors.affiliation: Laboratory of Computational Biology, National Heart Lung and Blood Institute, NIH, Bethesda, MD 20892, USA.
authors.forename: Yihan
authors.initials: Y
authors.lastname: Shao
authors.affiliation: Laboratory of Molecular Imaging and Nanomedicine, National Institute of Biomedical Imaging and Bioengineering, National Institutes of Health (NIH), Bethesda, MD 20892, USA.
authors.forename: Dale O
authors.initials: DO
authors.lastname: Kiesewetter
authors.affiliation: Laboratory of Molecular Imaging and Nanomedicine, National Institute of Biomedical Imaging and Bioengineering, National Institutes of Health (NIH), Bethesda, MD 20892, USA.
authors.forename: Gang
authors.initials: G
authors.lastname: Niu
authors.affiliation: Laboratory of Molecular Imaging and Nanomedicine, National Institute of Biomedical Imaging and Bioengineering, National Institutes of Health (NIH), Bethesda, MD 20892, USA.
authors.forename: Xiaoyuan
authors.initials: X
authors.lastname: Chen
keywords: Biology; amino acids