Bononi Fernanda C, Luyt Leonard G
Department of Chemistry, The University of Western Ontario, London, ON, Canada.
Methods Mol Biol. 2015;1248:223-37. doi: 10.1007/978-1-4939-2020-4_15.
Combinatorial one-bead-one-compound (OBOC) peptide library screening has proven to be a powerful tool for identification of small molecules, peptides, or peptidomimetics against a variety of specific targets such as cell surface receptors, protein kinases, proteases, and phosphatases. With each bead displaying many copies of a single chemical entity, millions of compounds can be rapidly synthesized and screened with whole-cell binding on-bead functional assays. Here we describe the methodology for the synthesis, screening, and sequence deconvolution of an OBOC peptide library analyzed for affinity to a cancer cell line.
组合单珠单化合物(OBOC)肽库筛选已被证明是一种强大的工具,可用于鉴定针对多种特定靶点的小分子、肽或肽模拟物,这些靶点包括细胞表面受体、蛋白激酶、蛋白酶和磷酸酶。由于每个珠子展示单个化学实体的多个拷贝,因此可以快速合成数百万种化合物,并通过基于珠子的全细胞结合功能测定进行筛选。在此,我们描述了用于合成、筛选和序列反卷积的OBOC肽库的方法,该肽库针对癌细胞系的亲和力进行了分析。