作者:Hongli Chen、Rong Huang、Zhihong Li、Wei Zhu、Jiakang Chen、Yuexiong Zhan、Biao Jiang
DOI:10.1039/c7ob01866e
日期:——
vinylsulfonamides were synthesized and screened for site-selective modification of the ε-amino group of lysine-bearing free α-amine residues. N-methyl-N-phenylethenesulfonamide has emerged as an applicable reagent and has been developed for efficient and highly selective modification of the lysine residue of native peptides in the presence of a free N-terminus via aza-Michael addition. We demonstrated that functional
合成并筛选了一系列乙烯基磺酰胺,以对带有赖氨酸的游离α-胺残基的ε-氨基进行位点选择性修饰。N-甲基-N-苯基乙磺酰胺已成为一种适用的试剂,并已开发出来,可在存在游离N端的情况下通过氮杂-迈克尔加成反应对天然肽的赖氨酸残基进行高效,高度选择性的修饰。我们证明具有荧光部分或药物的功能性N-苯基乙烯基磺酰胺衍生物也可以高特异性结合到奥曲肽和胰岛素的赖氨酸残基上,而无需修饰N末端。我们的方法为具有游离N末端的天然肽中的位点选择性赖氨酸功能化提供了一种有希望的策略。