摘要
本文用固相多肽合成法以逐步和片段缩合并用的方武首次合成了人胰酶抑制剂,其中采用了TMSOT_t-硫代茴香醚/TFA糸统切断载体-肽的连接键及脱除全部侧链保护基,合成产物经脱氢胰酶亲合层析与HPLC精制,总产率6.3％.合成品对牛胰酶有很强的抑制能力,其活性约为天然产物的97％。
This paper describes synthesis of the human trypsin inhibitor (HTI) by the solid phase method in which both stepwise and segment condensation are involved. TMSOT1-thioanisol/TFA have been used as the agent which cleaves HTI from the resin and removes all of the side chain protecting groups simultaneously. Crude HTI was purified by affinity chromatography on anhydro- trypsinr sepharose and reverse phase HPLC, the total yield is 6. 3%. The resulting product shows powerful trypsin inhibitory activity that near 97% of the activity of natural HTI.
出处
《高等学校化学学报》
SCIE
EI
CAS
CSCD
北大核心
1990年第8期837-842,共6页
Chemical Journal of Chinese Universities
基金
国家自然科学基金
关键词
人胰酶抑制剂
固相合成
Human trypsin inhibitor, Solid phase peptide synthesis, Trimethylsilyl trifluoromethane-sulf onate (TMSOT1)
