Shreder Kevin R, Wong Melissa S, Nomanbhoy Tyzoon, Leventhal Phillip S, Fuller Stacy R
ActivX Biosciences, Inc., 11025 North Torrey Pines Road, La Jolla, California 92037, USA.
Org Lett. 2004 Oct 14;6(21):3715-8. doi: 10.1021/ol048656a.
[structure: see text] The synthesis of a photoaffinity probe for EGFR is described. O-Alkylation of 4-(meta-azidoanilino)-6-methoxy-7-hydroxy-quinazoline with a protected tetraethyleneglycol linker followed by the attachment of tetramethylrhodamine yielded the fluorescent probe AX7593. Photoaffinity labeling of EGFR by AX7593 (K(b) = 280 nM) was shown to have an efficiency of 34% and to be competitive with the EGFR inhibitors PP2 and AG1478.
[结构：见正文] 本文描述了一种用于表皮生长因子受体（EGFR）的光亲和探针的合成。4-（间位叠氮基苯胺基）-6-甲氧基-7-羟基喹唑啉与受保护的四甘醇连接基进行O-烷基化反应，随后连接四甲基罗丹明，得到荧光探针AX7593。AX7593（解离常数K(b)=280 nM）对EGFR的光亲和标记显示其效率为34%，并且与EGFR抑制剂PP2和AG1478具有竞争性。
