氟代 ΔF508-CFTR 校正剂和增强剂用于 PET 成像。
Fluorinated ΔF508-CFTR correctors and potentiators for PET imaging.
机构信息
Department of Chemistry, University of California, Davis, Davis, CA 95616, United States.
出版信息
Bioorg Med Chem Lett. 2012 Feb 15;22(4):1602-5. doi: 10.1016/j.bmcl.2011.12.128. Epub 2012 Jan 3.
Abstract
(19)F-modified bithiazole correctors and phenylglycine potentiators of the ΔF508-CFTR chloride channel were synthesized and their function assayed in cells expressing human ΔF508-CFTR and a halide-sensitive fluorescent protein. Fluorine was incorporated into each scaffold using prosthetic groups for future biodistribution imaging studies using positron emission tomography (PET). The ΔF508-CFTR corrector and potentiator potencies of the fluorinated analogs were comparable to or better than those of the original compounds.
摘要
（19）F-修饰的双噻唑类 CFTR 氯离子通道校正剂和苯丙氨酸甘氨酸类 CFTR 氯离子通道增强剂被合成，并在表达人 ΔF508-CFTR 和卤化物敏感荧光蛋白的细胞中检测其功能。氟原子通过使用正电子发射断层扫描（PET）进行未来生物分布成像研究的假体基团被引入到每个支架中。氟化类似物的 ΔF508-CFTR 校正剂和增强剂效力与原始化合物相当或优于原始化合物。
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