Synthesis of fluorescent probes directed to the active site gorge of acetylcholinesterase.
Synthesis of fluorescent probes directed to the active site gorge of acetylcholinesterase.
复制标题
合成针对乙酰胆碱酯酶活性位点峡谷的荧光探针。
DOI：
10.1016/s0960-894x(00)00275-4
复制
发表时间：
2000
影响因子：
2.7
通讯作者：
Thompson,CM
中科院分区：
文献类型：
--
作者：
Saltmarsh,JR;Boyd,AE;Rodriguez,OP;Radić,Z;Taylor,P;Thompson,CM
Six organophosphorus compounds linked to fluorophore groups were prepared in an effort to selectively modify the active site of acetylcholinesterase and deliver probes to the gorge region. Two compounds that vary by the length of a methylene (CH2) group, pyrene-SO2NH(CH2)nNHC(O)CH2CH2P(O)(OEt)(F) (where n=2 or 3) were found to be potent, irreversible inhibitors of recombinant mouse AChE (Ki≅105M−1min−1). Size exclusion chromatography afforded a fluorescently-labeled cholinesterase conjugate.
