Stratingh Institute for Chemistry, University of Groningen, Nijenborgh 7, 9747 AG Groningen, The Netherlands.
Chem Soc Rev. 2015 Apr 21;44(8):2455-88. doi: 10.1039/c4cs00493k.
Dynamic combinatorial chemistry (DCC) has emerged as a powerful strategy to identify ligands for biological targets given that it enables the target to direct the synthesis and amplification of its strongest binder(s) from the library of interconverting compounds. Since the first report of DCC applied to the discovery of binders for a protein, this elegant tool has been employed on a range of protein targets at various stages of medicinal-chemistry projects. A series of suitable, reversible reactions that are biocompatible have been established and the portfolio of analytical techniques is growing. Despite progress, in most cases, the libraries employed remain of moderate size. We present here the most recent advances in the field of DCC applied to protein targets, paying particular attention to the experimental conditions and analytical methods chosen.
动态组合化学（DCC）已成为一种强大的策略，可用于鉴定生物靶标配体，因为它使靶标能够从相互转化的化合物库中指导其最强结合物（多个）的合成和扩增。自从首次报道将 DCC 应用于发现蛋白质结合物以来，该优雅的工具已在药物化学项目的各个阶段用于各种蛋白质靶标。已经建立了一系列合适的、生物相容的可逆反应，并且分析技术的组合正在不断增加。尽管取得了进展，但在大多数情况下，所使用的文库仍然规模适中。我们在此介绍了 DCC 在蛋白质靶标应用方面的最新进展，特别关注所选择的实验条件和分析方法。
