Studies on heterobifunctional cross-linking reagents, 6-maleimidohexanoic acid active esters
Studies on heterobifunctional cross-linking reagents, 6-maleimidohexanoic acid active esters
复制标题
DOI：
10.1248/cpb.55.685
复制
发表时间：
2007-04-01
影响因子：
1.7
通讯作者：
Kawasaki, Koichi
中科院分区：
文献类型：
--
作者：
Kida, Shinya;Maeda, Mitsuko;Kawasaki, Koichi
6-马来酰亚胺己酸N-羟基琥珀酰亚胺酯作为一种独特的异双功能交联剂，广泛应用于酶免疫偶联物的制备。其异双官能反应性良好，但其酯部分在水存在下容易水解。制备了几种6-马来酰亚胺基己酸活性酯（6-马来酰亚胺基己酸4-硝基苯酯、6-马来酰亚胺基己酸N-羟基-5-己烯-内-2，3-二甲酰亚胺酯和6-马来酰亚胺基己酸五氟苯基酯），并测试了它们在水介质中的反应性和稳定性。在合成的酯中，五氟苯基酯在水介质中表现出最高的反应性和稳定性。
6-Maleimidohexanoic acid N-hydroxysuccinimide ester has been used widely for preparation of enzyme immunoconjugates as a unique heterobifunctional cross-linking reagent. Its heterobifunctional reactivity is good, but its ester portion hydrolyzes easily in the presence of water. Several 6-maleimidohexanoic acid active esters (6-maleimidohexanoic acid 4-nitrophenyl ester, 6-maleimidohexanoic acid N-hydroxy-5-norbornene-endo-2,3-dicarboximide ester, and 6-maleimidohexanoic acid pentafluorophenyl ester) were prepared and their reactivity and stability in an aqueous media were tested. Of the synthetic esters, the pentafluorophenyl ester exhibited the highest reactivity and stability in aqueous media.