Kunys Andrew R, Lian Wenlong, Pei Dehua
Department of Chemistry and Biochemistry, The Ohio State University, Columbus, Ohio.
Curr Protoc Chem Biol. 2012 Dec 1;4(4):331-55. doi: 10.1002/9780470559277.ch120125.
One-bead-one-compound (OBOC) libraries consist of structurally related compounds (e.g., peptides) covalently attached to a solid support, with each resin bead carrying a unique compound. OBOC libraries of high structural diversity can be rapidly synthesized and screened without the need for any special equipment, and therefore can be employed in any chemical or biochemical laboratory. OBOC peptide libraries have been widely used to map the ligand specificity of proteins, to determine the substrate specificity of enzymes, and to develop inhibitors against macromolecular targets. They have proven particularly useful in profiling the binding specificity of protein modular domains (e.g., SH2 domains, BIR domains, and PDZ domains); subsequently, the specificity information can be used to predict the protein targets of these domains. The protocols outlined in this article describe the methodologies for synthesizing and screening OBOC peptide libraries against SH2 and PDZ domains, and the related data analysis. Curr. Protoc. Chem. Biol. 4:331-355 © 2012 by John Wiley & Sons, Inc.
单珠单化合物（OBOC）文库由共价连接到固体支持物上的结构相关化合物（如肽）组成，每个树脂珠携带一种独特的化合物。具有高结构多样性的OBOC文库无需任何特殊设备即可快速合成和筛选，因此可在任何化学或生化实验室中使用。OBOC肽文库已广泛用于绘制蛋白质的配体特异性、确定酶的底物特异性以及开发针对大分子靶标的抑制剂。事实证明，它们在分析蛋白质模块化结构域（如SH2结构域、BIR结构域和PDZ结构域）的结合特异性方面特别有用；随后，特异性信息可用于预测这些结构域的蛋白质靶标。本文概述的方案描述了针对SH2和PDZ结构域合成和筛选OBOC肽文库的方法以及相关的数据分析。《化学与生物学实验指南》第4卷：331 - 355页 2012年约翰威立国际出版公司版权所有
