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Synthesis and preliminary evaluation of a novel glutamine derivative: (2S,4S)4-[18F]FEBGln
Authors:Yong Huang  Song Liu  Renbo Wu  Lifang Zhang  Yan Zhang  Haiyan Hong  Aili Zhang  Hao Xiao  Yajing Liu  Zehui Wu  Lin Zhu  Hank F. Kung
Affiliation:1. Beijing Institute of Brain Disorders, Capital Medical University, Beijing 100069, China;2. College of Chemistry, Beijing Normal University, Beijing 100875, China;3. Department of Radiology, University of Pennsylvania, Philadelphia 19104, United States
Abstract:
We report the preparation of a novel glutamine derivative, (2S,4S)-2,5-diamino-4-(4-(2-fluoroethoxy)benzyl)-5-oxopentanoic acid, (2S, 4S)4-[18F]FEBGln ([18F]4), through efficient organic and radiosyntheses. In vitro assays of [18F]4 using MCF-7 cells showed that it entered cells via multiple amino acid transporter systems including system L and ASC2 transporters but not through the system A transporter. [18F]4 showed promising properties for tumor imaging and may serve as a lead compound for further optimizing and targeting the system L transporter associated with enhanced glutamine metabolism in cancer cells.
Keywords:Glutamine  Synthesis  Transporter  Radiosynthesis  Amino acid
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