Duffner Jay L, Clemons Paul A, Koehler Angela N
Broad Institute of Harvard and MIT, 7 Cambridge Center, Cambridge, MA 02142, USA.
Curr Opin Chem Biol. 2007 Feb;11(1):74-82. doi: 10.1016/j.cbpa.2006.11.031. Epub 2006 Dec 13.
Uncovering the functions of thousands of gene products, in various states of post-translational modification, is a key challenge in the post-genome era. To identify small-molecule probes for each protein function, high-throughput methods for ligand discovery are needed. In recent years, small-molecule microarrays (SMMs) have emerged as high-throughput and miniaturized screening tools for discovering protein-small-molecule interactions. Microarrays of small molecules from a variety of sources, including FDA-approved drugs, natural products and products of combinatorial chemistry and diversity-oriented synthesis, have been prepared and screened by several laboratories, leading to several newly discovered protein-ligand pairs.
揭示数千种处于各种翻译后修饰状态的基因产物的功能,是后基因组时代的一项关键挑战。为了识别针对每种蛋白质功能的小分子探针,需要高通量的配体发现方法。近年来,小分子微阵列(SMMs)已成为用于发现蛋白质 - 小分子相互作用的高通量和小型化筛选工具。包括美国食品药品监督管理局(FDA)批准的药物、天然产物以及组合化学和多样性导向合成产物在内的各种来源的小分子微阵列,已由多个实验室制备并进行筛选,从而发现了几对新的蛋白质 - 配体对。