Total synthesis of human beta-lipotropin.
Total synthesis of human beta-lipotropin.
复制标题
人β-促脂激素的全合成。
DOI：
10.1073/pnas.80.6.1556
复制
发表时间：
1983
影响因子：
11.1
通讯作者：
Li,CH
中科院分区：
文献类型：
--
作者：
Blake,J;Li,CH
采用新的水相链段偶联法实现了人β-促脂素的全合成。用固相法合成了Ac-Arg-beta-lipotropin-（61-89）（I）和[GlyS 60]-beta-lipotropin-（1-60）（II）肽。肽I与柠康酸酐反应，然后用胰蛋白酶简单消化以除去乙酰基精氨酸基，得到Ia。肽II与柠康酸酐反应得到柠康酰基肽IIa。Ia和IIa在50%二甲基甲酰胺中通过与银银/N-羟基琥珀酰亚胺反应偶联在一起。在25%乙酸中除去柠康酰基后，可以分离出10%产率的合成β-促脂素。纸电泳、等电聚焦、HPLC、离体兔脂肪细胞中的脂解活性和放射免疫测定显示合成产物与天然人β-促脂素相同。
The total synthesis of human beta-lipotropin has been accomplished by the new segment-coupling method in aqueous solution. The peptides Ac-Arg-beta-lipotropin-(61-89) (I) and [GlyS60]-beta-lipotropin-(1-60) (II) were synthesized by the solid-phase method. Reaction of peptide I with citraconic anhydride followed by brief digestion with trypsin to remove the acetylarginyl group, gave Ia. Reaction of peptide II with citraconic anhydride gave the citraconyl peptide IIa. Ia and IIa were coupled together in 50% dimethylformamide by reaction with silver nitrate/N-hydroxysuccinimide. After removal of the citraconyl groups in 25% acetic acid, a 10% yield of synthetic beta-lipotropin could be isolated. The synthetic product was shown to be identical to native human beta-lipotropin by paper electrophoresis, isoelectric focusing, HPLC, lipolytic activity in isolated rabbit fat cells, and radioimmunoassay.