A NOVEL THIOETHER LINKER - CHEMICAL SYNTHESIS OF A HIV-1 PROTEASE ANALOG BY THIOETHER LIGATION

被引:46
作者
ENGLEBRETSEN, DR [1 ]
GARNHAM, BG [1 ]
BERGMAN, DA [1 ]
ALEWOOD, PF [1 ]
机构
[1] UNIV QUEENSLAND,CTR DRUG DESIGN & DEV,BRISBANE,QLD 4072,AUSTRALIA
关键词
D O I
10.1016/0040-4039(95)01843-7
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
Using the novel thioether linker 4-[N-Boc-2-aminoethylmercapto] methyl phenoxyacetic acid, peptides bearing a C-terminal thiol functionality were synthesised; Reaction of the thiol functionalised peptide with an N-terminal bromoacetylated peptide led to ligation of the two peptides via a thioether bond. The strategy was used to synthesise an enzymatically active analogue of HIV-1 Protease.
引用
收藏
页码:8871 / 8874
页数:4
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