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基于改进固相多肽合成技术的前列腺靶向膜抗原的合成

于瀚淼 徐聪靓 曹嘉懿 徐文琪 张宸瑞 罗东

中国医学工程2025,Vol.33Issue(4):25-30,6.
中国医学工程2025,Vol.33Issue(4):25-30,6.DOI:10.19338/j.issn.1672-2019.2025.04.006

基于改进固相多肽合成技术的前列腺靶向膜抗原的合成

Synthesis of prostate targeted membrane antigen based on improved solid phase peptide synthesis technology

于瀚淼 1徐聪靓 1曹嘉懿 1徐文琪 1张宸瑞 1罗东1

作者信息

  • 1. 华南理工大学生物医学科学与工程学院 广州国际校区,广东 广州 511442
  • 折叠

摘要

Abstract

[Objective]To optimize the solid-phase peptide synthesis(SPPS)technique in order to solve the problems of decreased synthesis efficiency,increased by-products,and purification difficulties caused by the growth of peptide chains,and to enhance the synthetic efficacy of prostate-targeted membrane antigen C(Trt)Y-PSMA-1.[Methods]Using Fmoc chemical protection strategy,combined with microwave-assisted solid-phase synthesizer and manual synthesis techniques,a peptide chain with sequence Cys-Tyr-(Lys)-Glu-Glu-Glu-Ahx-Amc-Glu'-CO-Glu(n=1,2,4)was constructed step by step using 4-methoxybenzylamino(MBHA)resin as a solid-phase carrier;the peptide chain was cut by acidic conditions to cleave the peptide-resin complexes,and purification and freeze-drying were utilized to obtain the final products by high performance liquid chromatography(HPLC).[Results]The improved method increased the coupling efficiency by 60%and solved the terminal cyclization problem common in the synthesis of long-chain peptides by manual complementary synthesis strategy.[Conclusion]The SPPS technology,which combines microwave-assisted and Fmoc protection,significantly improves the efficiency of long-chain peptide synthesis,and provides a reproducible technological solution for the large-scale preparation of biomaterials for prostate cancer targeting,and the related optimization strategy can be extended to the synthesis of other functional peptides.

关键词

固相多肽合成/9-芴甲氧羰基保护基/微波固相多肽合成仪/前列腺靶向膜抗原

Key words

solid-phase peptide synthesis/Fmoc chemistry/microwave solid-phase peptide synthesizer/prostate targeted membrane antigen

分类

药学

引用本文复制引用

于瀚淼,徐聪靓,曹嘉懿,徐文琪,张宸瑞,罗东..基于改进固相多肽合成技术的前列腺靶向膜抗原的合成[J].中国医学工程,2025,33(4):25-30,6.

中国医学工程

1672-2019

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