Development of a New Thiol Site-Specific Prosthetic Group and Its Conjugation with [Cys(40)]-exendin-4 for in Vivo Targeting of Insulinomas
作者： Xuyi Yue , Dale O. Kiesewetter , Jinxia Guo , Zhongchan Sun , Xiaoxiang Zhang
DOI: 10.1021/BC400084U
关键词:
摘要: A new tracer, N-5-[18F]fluoropentylmaleimide ([18F]FPenM), for site-specific labeling of free thiol group in proteins and peptides was developed. The tracer synthesized three steps (18F displacement the aliphatic tosylate, di-Boc removal by TFA to expose amine, incorporation amine into a maleimide). radiosynthesis completed 110 min with 11–17% radiochemical yield (uncorrected), specific activity 20–49 GBq/μmol. [18F]FPenM showed comparable efficiency N-[2-(4-[18F]fluorobenzamido)ethyl]maleimide ([18F]FBEM). Its application demonstrated conjugation glucagon-like peptide type 1 (GLP-1) analogue [cys40]-exendin-4. cell uptake, binding affinity, imaging properties, biodistribution, metabolic stability radiolabeled [18F]FPenM-[cys40]-exendin-4 were studied using INS-1 tumor cells xenograft model. Positron emission tomography (PET) results that thiol-specific [18F]FPenM-[cys40]-exendin-4, h...
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