Selection of DNA-encoded small molecule libraries against unmodified and non-immobilized protein targets

Peng Zhao; Zitian Chen; Yizhou Li; Dawei Sun; Yuan Gao; Yanyi Huang; Xiaoyu Li

doi:10.1002/anie.201404830

Selection of DNA-encoded small molecule libraries against unmodified and non-immobilized protein targets

Angew Chem Int Ed Engl. 2014 Sep 15;53(38):10056-9. doi: 10.1002/anie.201404830. Epub 2014 Jul 7.

Authors

Peng Zhao¹, Zitian Chen, Yizhou Li, Dawei Sun, Yuan Gao, Yanyi Huang, Xiaoyu Li

Affiliation

¹ College of Chemistry and Molecular Engineering, Peking University, Beijing, 100871 (China).

PMID: 25044298
DOI: 10.1002/anie.201404830

Abstract

The selection of DNA-encoded libraries against biological targets has become an important discovery method in chemical biology and drug discovery, but the requirement of modified and immobilized targets remains a significant disadvantage. With a terminal protection strategy and ligand-induced photo-crosslinking, we show that iterated selections of DNA-encoded libraries can be realized with unmodified and non-immobilized protein targets.

Keywords: DNA; DNA-encoded library; DNA-templated chemistry; drug discovery; selection.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

DNA / chemistry*
DNA / metabolism
Ligands
Molecular Structure
Proteins / antagonists & inhibitors*
Small Molecule Libraries / chemical synthesis
Small Molecule Libraries / chemistry*
Small Molecule Libraries / pharmacology*

Substances

Ligands
Proteins
Small Molecule Libraries
DNA