Selecting chemicals: the emerging utility of DNA-encoded libraries

被引:66
作者
Clark, Matthew A. [1 ]
机构
[1] GlaxoSmithKline Inc, Mol Discovery Res, Waltham, MA 02451 USA
关键词
IN-VITRO SELECTION; TEMPLATED SYNTHESIS; SMALL MOLECULES; CHEMISTRY; DESIGN;
D O I
10.1016/j.cbpa.2010.02.017
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
Over the past 10 years, a handful of academic and industrial research groups have developed strategies for the synthesis and interrogation of DNA-encoded small-molecule libraries. These strategies can be divided into those in which DNA directs small-molecule synthesis and those in which it records the synthesis. These libraries have started to yield novel modulators of biological targets, including: SH3-domain-binding peptoids, macrocyclic peptide-based BcI-X(L)/BH3 interaction disruptors, ligands for TNF, albumin, streptavidin and others, and 'small-molecule kinase inhibitors. The DNA-encoded library field holds the potential to address the general problem of biological ligand discovery, including pharmaceutical lead generation.
引用
收藏
页码:396 / 403
页数:8
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