Gloriam David E
Drug Discov Today Technol. 2013 Summer;10(2):e307-13. doi: 10.1016/j.ddtec.2012.07.010.
Chemogenomic techniques connect the chemical and biological domains to establish ligand and target relationships not evident from the individual disciplines. Chemogenomics has been applied in lead generation, target classification, focused library design as well as selectivity and polypharmacology profiling. This review describes recent developments structured into ligand-, target- and combined chemogenomic techniques and applications to allosteric GPCR ligands. It also outlines relative strengths and limitations of these techniques and the impact of the increasing crystallographic data.
化学基因组学技术将化学和生物学领域联系起来,以建立从单个学科中不明显的配体与靶点之间的关系。化学基因组学已应用于先导化合物发现、靶点分类、聚焦文库设计以及选择性和多药理学分析。本综述描述了最近的进展,这些进展分为配体、靶点和联合化学基因组学技术以及对变构GPCR配体的应用。它还概述了这些技术的相对优势和局限性以及不断增加的晶体学数据的影响。