Mehta V D, Kulkarni P V, Mason R P, Constantinescu A, Antich P P
Department of Radiology, University of Texas Southwestern Medical Center, Dallas 75235.
Bioconjug Chem. 1994 May-Jun;5(3):257-61. doi: 10.1021/bc00027a011.
Fluorinated proteins have been synthesized and characterized as potential in vivo 19F magnetic resonance imaging (MRI) and spectroscopy (MRS) agents. Proteins labeled with fluorine include bovine serum albumin, gamma-globulin, and purified immunoglobulin (IgG). The amino groups in proteins were selectively trifluoroacetylated using S-ethyl trifluorothioacetate to synthesize fluorinated proteins (TFA-protein; 1-3). In another approach, trifluoroacetamidosuccinic anhydride has been used to prepare corresponding fluorinated derivatives of proteins (TFASA-protein; 4-6). The fluorinated proteins have been purified by exhaustive dialysis and isolated in good yields (55-76%). The fluorinated proteins exhibit useful NMR characteristics and the biocompatibility for in vivo studies. The initial investigations demonstrate the potential of these new fluorinated proteins as in vivo MRI/MRS probes.
含氟蛋白质已被合成并表征为潜在的体内19F磁共振成像（MRI）和光谱学（MRS）造影剂。用氟标记的蛋白质包括牛血清白蛋白、γ-球蛋白和纯化的免疫球蛋白（IgG）。使用S-乙基三氟硫代乙酸酯对蛋白质中的氨基进行选择性三氟乙酰化，以合成含氟蛋白质（TFA-蛋白质；1-3）。在另一种方法中，三氟乙酰胺琥珀酸酐已被用于制备蛋白质的相应含氟衍生物（TFASA-蛋白质；4-6）。含氟蛋白质已通过彻底透析纯化，并以良好的产率（55-76%）分离出来。含氟蛋白质表现出有用的核磁共振特性和用于体内研究的生物相容性。初步研究证明了这些新型含氟蛋白质作为体内MRI/MRS探针的潜力。
