| 镜像配基筛选:克服“酶屏障”的多肽、寡核苷酸药物研发技术 |
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| 引用本文： | 李翀,沈洁,陆伟跃,陆五元.镜像配基筛选:克服“酶屏障”的多肽、寡核苷酸药物研发技术[J].中国科学:化学,2011(7):1112-1120. |
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| 作者姓名： | 李翀 沈洁 陆伟跃 陆五元 |
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| 作者单位： | 西南大学药学院;复旦大学药学院;School;Medicine;University;Maryland; |
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| 基金项目： | 国家重点基础研究发展计划(973计划)(2007CB935800和2010CB934000); 西南大学博士基金(SWU110028),西南大学基本科研业务费专项资金项目(XDJK2009C077)资助 |
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| 摘 要： | 生物体内存在的酶屏障是功能性多肽和寡核苷酸成药的重要瓶颈.以镜像噬菌体展示技术(mirror-image phage display)和镜像适配体筛选技术(Spiegelmer technology)为代表的镜像配基筛选技术能有效地克服这一屏障,获得对靶点具有特异识别能力且在生理条件下高度稳定的D型多肽和L型寡核苷酸配基,有望成为多肽或寡核苷酸类特异性药物研发的有利工具.本文主要综述镜像配基筛选技术的原理及其在药学领域的研究进展.
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| 关 键 词： | 镜像噬菌体展示技术 镜像适配体筛选技术 D型多肽 L型寡核苷酸 |
Mirror-image isomers screening:Overcoming the enzyme barriers for the development of peptide and oligonucleotide therapeutics |
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| LI Chong ,SHEN Jie ,LU WeiYue & LU WuYuan College of Pharmaceutical Sciences,Southwest University,Chongqing ,China School of Pharmacy,Fudan University,Shanghai ,China School of Medicine,University of Maryl,Baltimore,MD ,USA.Mirror-image isomers screening:Overcoming the enzyme barriers for the development of peptide and oligonucleotide therapeutics[J].Scientia Sinica Chimica,2011(7):1112-1120. |
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| Authors: | LI Chong SHEN Jie LU WeiYue & LU WuYuan College of Pharmaceutical Sciences Southwest University Chongqing China School of Pharmacy Fudan University Shanghai China School of Medicine University of Maryl Baltimore MD USA |
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| Institution: | LI Chong 1,SHEN Jie 2,LU WeiYue 2 & LU WuYuan 3 1 College of Pharmaceutical Sciences,Southwest University,Chongqing 400715,China 2 School of Pharmacy,Fudan University,Shanghai 201203,China 3 School of Medicine,University of Maryland,Baltimore,MD 21201,USA |
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| Abstract: | The enzyme barriers in vivo greatly limited the development of peptide and oligonucleotide therapeutics.The mirror-image isomers screening including mirror-image phage display and Spiegelmer technology can obtain biostable D-peptides and L-oligonuclotides with high specificity to their targets,thus will be a promising technology for the development of novel peptide and oligonucleotide drugs.This review will focus on the principle of mirror-image isomers screening and highlight recent developments of this te... |
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| Keywords: | mirror-image phage display Spiegelmer technology D-peptide L-oligonucleotide |
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