Chem. J. Chinese Universities ›› 2023, Vol. 44 ›› Issue (3): 20220438.doi: 10.7503/cjcu20220438

• Review • Previous Articles    

In-solution Selection Methods of DNA-encoded Library

WANG Yingying1, LI Xiaomin1, CAI Yahui1, LI Xiaoyu2,3(), SHI Bingbing1()   

  1. 1.College of Basic Medicine,Jining Medical University,Jining 272067,China
    2.Department of Chemistry,State Key Laboratory of Synthetic Chemistry,The University of Hong Kong,Hong Kong SAR,China
    3.Laboratory for Synthetic Chemistry and Chemical Biology Limited,Health@InnoHK,Innovation and Technology Commission,Hong Kong SAR,China
  • Received:2022-06-21 Online:2023-03-10 Published:2023-03-14
  • Contact: LI Xiaoyu, SHI Bingbing E-mail:xiaoyuli@hku.hk;shibingbing@mail.jnmc.edu.cn
  • Supported by:
    the Shandong Provincial Natural Science Foundation, China(ZR2021QB152);the Faculty Start-up Funds of Jining Medical University, China(600919001);the College Students’ Innovative Entrepreneurial Training Plan Program of Jining Medical University, China(CX2018048)

Abstract:

DNA-encoded library(DEL) has become a nearly indispensable technology platform for the development of new drugs in the pharmaceutical industry. The DEL technology has become matured over the past three decades and the rapid development of DEL-compatible chemistries has tremendously improved the chemical diversity of DELs and promoted its application in drug discovery. DEL technology has been widely adopted by pharmaceutical companies, and numerous clinical candidates have been identified from DEL selection. Usually, the selection of DEL is mainly affinity-based selection on solid-phase. The purified target protein is immobilized on the matrix, and then the binders are separated from non-binders by physical washes. In recent years, a series of in-solution selection methods for DEL have been developed, which has further expanded the target scope suitable for DEL and revealing the potential of DEL as an effective tool to explore fundamental biology. This review mainly introduces the selection methods of DEL in-solution phase and their applications, and finally gives a brief outlook on the application of DEL technology to complex biological targets and functional selection.

Key words: DNA-encoded library, Drug discovery, Drug selection, In-solution selection

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