Franzini Raphael M, Randolph Cassie
Department of Medicinal Chemistry, College of Pharmacy, University of Utah , 30 S 2000 E, Salt Lake City, Utah 84112, United States.
J Med Chem. 2016 Jul 28;59(14):6629-44. doi: 10.1021/acs.jmedchem.5b01874. Epub 2016 Feb 25.
In recent years, DNA-encoded chemical libraries (DECLs) have attracted considerable attention as a potential discovery tool in drug development. Screening encoded libraries may offer advantages over conventional hit discovery approaches and has the potential to complement such methods in pharmaceutical research. As a result of the increased application of encoded libraries in drug discovery, a growing number of hit compounds are emerging in scientific literature. In this review we evaluate reported encoded library-derived structures and identify general trends of these compounds in relation to library design parameters. We in particular emphasize the combinatorial nature of these libraries. Generally, the reported molecules demonstrate the ability of this technology to afford hits suitable for further lead development, and on the basis of them, we derive guidelines for DECL design.
近年来，DNA编码化学文库（DECLs）作为药物开发中一种潜在的发现工具，已引起了广泛关注。筛选编码文库可能比传统的命中发现方法具有优势，并且有潜力在药物研究中补充此类方法。由于编码文库在药物发现中的应用不断增加，科学文献中出现了越来越多的命中化合物。在本综述中，我们评估了报道的源自编码文库的结构，并确定了这些化合物与文库设计参数相关的一般趋势。我们特别强调这些文库的组合性质。一般来说，报道的分子证明了该技术能够提供适合进一步先导物开发的命中物，基于这些命中物，我们得出了DECL设计的指导原则。
