Synthesis and Cell-Based Screening of One-Bead-One-Compound Peptide Libraries

Synthesis and Cell-Based Screening of One-Bead-One-Compound Peptide Libraries
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DOI:
10.1007/978-1-4939-2020-4_15
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发表时间:
2015-01-01
期刊:
PEPTIDE LIBRARIES: METHODS AND PROTOCOLS
影响因子:
--
通讯作者:
Luyt, Leonard G.
Luyt, Leonard G.
中科院分区:
其他
文献类型:
--
作者:
Bononi, Fernanda C.;Luyt, Leonard G.

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组合单头一化合物(OBOC)肽库筛选已被证明是一种强大的工具,用于鉴定小分子、肽或肽拟物,以对抗各种特定靶标,如细胞表面受体、蛋白激酶、蛋白酶和磷酸酶。由于每个头显示单一化学实体的许多副本,数百万种化合物可以快速合成并通过全细胞结合头功能测定进行筛选。在这里,我们描述了OBOC肽库的合成、筛选和序列反卷积的方法,以分析其对癌细胞系的亲和力。
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.