title: Radioiodination of protein using 2,3,5,6-tetrafluorophenyl 3-(nido-carboranyl) propionate (TCP) as a potential bi-functional linker: Synthesis and biodistribution in mice.
abstract: 2,3,5,6-Tetrafluorophenyl 3-(nido-carboranyl) propionate (TCP), as a new potential bi-functional linker for radiohalogenation of proteins or peptides, was synthesized. With this bi-functional linker, the first attempt to conjugate bovine serum albumin (BSA) with (125)I was made and the biodistribution of the conjugated BSA ((125)I-TCP-BSA) was investigated in NIH strain mice. By the use of TCP as the linker, BSA was conjugated with (125)I in a labeling yield of 58-75% and with radiochemical purity of 99.8% after purification by Sephadex(TM) G-50. Even after being kept at room temperature for 72h, the radiochemical purity of (125)I-TCP-BSA was still more than 98%, much higher than that of the directly (125)I-labeled BSA ((125)I-BSA). Meanwhile, biodistribution experiments in mice indicated that the uptake of (125)I with (125)I-TCP-BSA into thyroid was obviously less than that with (125)I-BSA post-injection. All the results implied that the (125)I-conjugated BSA ((125)I-TCP-BSA) was considerably stable in vivo as well as in vitro, and TCP was regarded as a promising bi-functional linker for radiohalogenation of proteins.
authors.affiliation: Key Laboratory of Radiation Physics and Technology, Ministry of Education, Institute of Nuclear Science and Technology, Sichuan University, Chengdu 610064, PR China.
authors.forename: Rushan
authors.initials: R
authors.lastname: Lin
authors.forename: Ning
authors.initials: N
authors.lastname: Liu
authors.forename: Yuanyou
authors.initials: Y
authors.lastname: Yang
authors.forename: Bing
authors.initials: B
authors.lastname: Li
authors.forename: Jiali
authors.initials: J
authors.lastname: Liao
authors.forename: Jiannan
authors.initials: J
authors.lastname: Jin