Woolley P V, Dion R L, Kohn K W, Bono V H
Cancer Res. 1976 Apr;36(4):1470-4.
The binding of 1-(2-chloroethyl)-3-(cyclohexyl)-1-nitrosourea (CCNU) to the proteins of the L1210 cell nucleus has been studied using both [cyclohexyl-14C]CCNU and [chloroethyl-14C]CCNU. Most of the bound [cyclohexyl-14C] moiety of CCNU was found to exist in a form that was stable in acid solution but labile and dialyzable in alkaline solution. A small amount of the cyclohexyl moiety was bound to histones in a stable, nondialyzable form. The drug/protein ratio for the H1 histone was about 0.01 to 0.02 mole/mole. No binding of the cyclohexyl group to acidic proteins or of the chloroethyl group to either histones or acidic proteins was observed. Thus, the interaction of CCNU with the proteins of the cell nucleus can be defined in terms of the modification of histones by the cyclohexyl moiety.
使用[环己基-¹⁴C]洛莫司汀（CCNU）和[氯乙基-¹⁴C]CCNU研究了1-(2-氯乙基)-3-(环己基)-1-亚硝基脲（CCNU）与L1210细胞核蛋白质的结合。发现CCNU大部分结合的[环己基-¹⁴C]部分以在酸性溶液中稳定但在碱性溶液中不稳定且可透析的形式存在。少量环己基部分以稳定的、不可透析的形式与组蛋白结合。H1组蛋白的药物/蛋白质比率约为0.01至0.02摩尔/摩尔。未观察到环己基与酸性蛋白质结合，也未观察到氯乙基与组蛋白或酸性蛋白质结合。因此，CCNU与细胞核蛋白质的相互作用可以通过环己基部分对组蛋白的修饰来定义。
